US Pat. No. 11,066,487

MODIFIED CONJUGATED DIENE-BASED POLYMER AND METHOD OF PREPARING THE SAME

LG Chem, Ltd.


1. A modified conjugated diene-based polymer, comprising a repeating unit derived from a conjugated diene-based monomer and a functional group derived from a modifier comprising a compound represented by the following Formula 1 at one terminal:



in Formula 1,
Z1 and Z2 are each independently hydrogen, a monovalent hydrocarbon group of 1 to 30 carbon atoms, or a substituent represented by the following Formula 2, where one or more of Z1 and Z2 are required to be substituents represented by the following Formula 2:




in Formula 2,
X1 is a S atom or a N atom, where if X1 is the S atom, n is 1, and if X1 is the N atom, n is 2, A1 is a divalent hydrocarbon group of 1 to 30 carbon atoms, R1 to R3 are each independently halogen, a monovalent hydrocarbon group of 1 to 30 carbon atoms, or an alkoxy group of 1 to 30 carbon atoms, where one or more of R1 to R3 are required to be halogen groups, or alkoxy groups of 1 to 30 carbon atoms.

US Pat. No. 11,066,486

POLYMERS FUNCTIONALIZED WITH IMINE COMPOUNDS CONTAINING A CYANO GROUP

Bridgestone Corporation, ...


1. A method for preparing a functionalized polymer, the method comprising the steps of:(i) polymerizing monomer to form a reactive polymer, and
(ii) reacting the reactive polymer with an imine compound containing a cyano group wherein the imine compound containing a cyano group is defined by formula II:





where R4 and R5 are each independently a hydrogen atom or a monovalent organic group, and R2 is a bond or a divalent organic group, or where R4 and R5 join to form a divalent organic group.

US Pat. No. 11,066,465

ANTIBODIES AND CONJUGATES THEREOF

KODIAK SCIENCES INC., Pa...


1. An antibody conjugate comprising:(1) an anti-VEGF-A antibody; and
(2) a phosphorylcholine containing polymer, wherein the polymer is covalently bonded to the anti-VEGF-A antibody at a cysteine outside a variable region of the anti-VEGF-A antibody, and wherein said cysteine replaces a non-cysteine amino acid that occurs in a same position in a sequence, wherein the anti-VEGF-A antibody comprises a light chain and heavy chain, said heavy chain comprising an Fc region, wherein the cysteine is in the Fc region of the heavy chain, and wherein the anti-VEGF-A antibody heavy chain comprises CDRH1: GYDFTHYGMN, CDRH2: WINTYTGEPTYAADFKR, and CDRH3: YPYYYGTSHWYFDV, and position 231 is T (via sequential counting as in SEQ ID NO: 1), and the anti-VEGF-A antibody light chain comprises CDRL1: SASQDISNYLN (SEQ ID NO: 12), CDRL2: FTSSLHS (SEQ ID NO: 13), and CDRL3: QQYSTVPWT (SEQ ID NO: 14), and Kabat position 4 is L,
wherein the antibody conjugate has the following structure:




wherein X=a) OR where R?H, Methyl, ethyl, propyl, isopropyl, b) H, or c) a halide;
wherein:
each heavy chain of the anti-VEGF-A antibody is denoted by the letter H, and each light chain of the anti-VEGF-A antibody is denoted by the letter L;
the polymer is bonded to the anti-VEGF-A antibody through the sulfhydryl of a cysteine at position 449, as numbered in SEQ ID NO: 1, which bond is depicted on one of the heavy chains;
PC is





where the curvy line indicates the point of attachment to the rest of the polymer; andn1, n2, n3, n4, n5, n6, n7, n8 and n9 are the same or different such that the sum of n1, n2, n3, n4, n5, n6, n6, n7, n8 and n9 is 2500 to 3000 plus or minus 15%.

US Pat. No. 11,066,461

METHOD FOR PREVENTING OR TREATING NOSOCOMIAL PNEUMONIA

MEDIMMUNE LIMITED, Cambr...


1. A method of treating a Pseudomonas aeruginosa infection in a susceptible human subject comprising administering to the subject 1500 mg or 3000 mg of a bispecific antibody that specifically binds Pseudomonas aeruginosa Psl and PcrV,wherein the bispecific antibody comprises a binding domain which specifically binds to P. aeruginosa Psl comprising a set of complementarity determining regions (CDRs): HCDR1-Psl, HCDR2-Psl, HCDR3-Psl, LCDR1-Psl, LCDR2-Psl, and LCDR3-Psl, wherein HCDR1-Psl has the amino acid sequence of SEQ ID NO: 10, HCDR2-Psl has the amino acid sequence of SEQ ID NO: 11, HCDR3-Psl has the amino acid sequence of SEQ ID NO: 12, LCDR1-Psl has the amino acid sequence of SEQ ID NO: 13, LCDR2-Psl has the amino acid sequence of SEQ ID NO: 14, and LCDR3-Psl has the amino acid sequence of SEQ ID NO: 15; and a binding domain which specifically binds to P. aeruginosa PcrV comprising a set of CDRs: HCDR1-PcrV, HCDR2-PcrV, HCDR3-PcrV, LCDR1-PcrV, LCDR2-PcrV, and LCDR3-PcrV, wherein HCDR1-PcrV has the amino acid sequence of SEQ ID NO: 2, HCDR2-PcrV has the amino acid sequence of SEQ ID NO: 3, HCDR3-PcrV has the amino acid sequence of SEQ ID NO: 4, LCDR1-PcrV has the amino acid sequence of SEQ ID NO: 6, LCDR2-PcrV has the amino acid sequence of SEQ ID NO: 7, and LCDR3-PcrV has the amino acid sequence of SEQ ID NO: 8, and
wherein the subject maintains a serum concentration of the bispecific antibody of at least 1.7 ?g/mL through 7 days following administration of the bispecific antibody.

US Pat. No. 11,066,459

HYBRID IMMUNOGLOBULIN CONTAINING NON-PEPTIDYL LINKAGE

BIOMOLECULAR HOLDINGS LLC...


1. A compound having the structure:A-B - - - Z
wherein A is a biologically active structure of the compound;
wherein Z is a protein component of the compound, which protein component comprises one or more polypeptides, wherein at least one of the one or more polypeptides comprises consecutive amino acids which (i) are identical to a stretch of consecutive amino acids present in a chain of an Fc domain of an antibody; (ii) bind to an Fc receptor; and (iii) have at their N-terminus a cysteine or a selenocysteine;
wherein B is (a) an organic acid residue or (b) a stretch of consecutive amino acid residues which is, or is present in any of the following sequences: EPKSCDKTHTCPPCP (SEQ ID NO: 213), ERKCCVECPPCP (SEQ ID NO: 214), ELKTPLGDTTHTCPRCP(EPKSCDTPPPCPRCP)3 (SEQ ID NO: 215), or ESKYGPPCPSC (SEQ ID NO: 216);
wherein the dashed line between B and Z represents a peptidyl linkage between the N-terminal cysteine or selenocysteine of Z and an amino acid residue or an organic acid residue of B; and
wherein the solid line between A and B represents a nonpeptidyl linkage comprising the structure:




wherein Xa is a chemical structure containing a cyclooctane fused to a dihydropyridazine; and
wherein Ra represents an organic structure which connects to A and Rb represents an organic structure which comprises





and connects to B, wherein X1 is CH or N, and X2 is CH2 or a carbonyl group.

US Pat. No. 11,066,448

ZIKA AS A CELL PENETRATING PEPTIDE FOR DELIVERY TO THE BRAIN

Buck Institute for Resear...


1. A construct comprising a cell penetrating peptide attached to an effector that is to be delivered into a cell, wherein:said cell penetrating peptide comprises a Zika cell penetrating peptide (Zika CPP) where the amino acid sequence of said cell penetrating peptide comprises the sequence ENLEYRIMLSVHGSQHSGMIVNDTG HETDENRAKVEITPNSPR (SEQ ID NO:1), or a fragment thereof that retains the ability to penetrate into a target cell, and said cell penetrating peptide ranges in length up to 50 amino acids; and
said effector is selected from the group consisting of a protein that is not a Zika protein, a nucleic acid, an organic compound, a viral particle, and a nanoparticle.

US Pat. No. 11,066,447

AUREOBASIDIUM DERIVATIVES AND METHODS OF SYNTHESIS

AueroGen Biosciences, Inc...


1. A compound of Formula I-P2:



or a pharmaceutically acceptable salt thereof, whereineach of R1 and RP1 is independently selected from hydrogen, phenyl, naphthyl, a 5 to 6 membered monocyclic heteroaryl with 1 to 3 nitrogen atoms, or a 9-12 membered bicyclic heteroaryl having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, wherein the phenyl, naphthyl, 5 to 6 membered monocyclic heteroaryl, and 9-12 membered bicyclic heteroaryl are each independently substituted with x instances of R3;
x is independently 1, 2, or 3;
each R3 is independently






each R5 is independently selected from the group consisting of —H, C1-4 alkyl, —N(CH3)2, —C(O)—CH3, —C(O)—CH2—CH3, and —C(O)—O—C(CH3)3;
R2 is independently selected from hydrogen, phenyl, naphthyl, a 5 to 6 membered monocyclic heteroaryl with 1 to 3 nitrogen atoms, or a 9-12 membered bicyclic heteroaryl having 1-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur, wherein R2 is optionally substituted with x instances of R3;
provided that
at least one of R1, R2, and RP1 is not hydrogen.


US Pat. No. 11,066,446

CYCLIC PEPTIDE, AFFINITY CHROMATOGRAPHY SUPPORT, LABELED ANTIBODY, ANTIBODY DRUG CONJUGATE, AND PHARMACEUTICAL PREPARATION

FUJIFILM Corporation, To...


1. A cyclic peptide represented by Formula (I),RN—Xg—[Xi—Xa—Xm—X1—X2—X3—Xn—Xb—Xj]k—Xh—RC??(I)

in Formula (I),RN represents an N-terminal group;
RC represents a C-terminal group;
X1 represents an L-leucine residue, an L-isoleucine residue, an L-methionine residue, an L-lysine residue, or an L-arginine residue;
X2 represents an L-valine residue or an L-isoleucine residue;
X3 represents an L-tryptophan residue or an L-phenylalanine residue;
one of Xa and Xb represents an amino acid residue derived from an amino acid having an azide group on a side chain and the other represents an amino acid residue derived from an amino acid having an alkynyl group on a side chain, and Xa and Xb are bonded to each other through a triazole bond;
wherein the triazole bond is represented by the following formula,





wherein in the formula, * represents a point of binding to an adjacent amino acid residue, x is an integer of 1 to 4, and y is an integer of 1 to 3,

Xg, Xh, Xi, Xj, Xm and Xn each represent g consecutive X's, h consecutive X's, i consecutive X's, j consecutive X's, m consecutive X's, and n consecutive X's;
X represents an amino acid residue, and in a case where there is a plurality of X's, the plurality of X's may be the same as or different from each other;
g, h, i, and j each independently represent an integer equal to or greater than 0;
m and n are integers satisfying 0?m?9, 0?n?9, and 3?m+n 9 simultaneously; and
k is an integer equal to or greater than 1, and in a case where k?2, X1, X2, X3, Xa, Xb, Xi, Xj, Xm, and Xn in a repeating unit [Xi—Xa—Xm—X1—X2—X3—Xa—Xn—Xb—Xj] each may be the same or different between the repeating units.

US Pat. No. 11,066,445

IMMUNOMODULATORS ACTING AS ANTAGONISTS OF PD-1

Bristol-Myers Squibb Comp...


1. A compound of formula (I)




or a pharmaceutically acceptable salt thereof, wherein:A is selected from





wherein: denotes the point of attachment to the carbonyl group and denotes the point of attachment to the nitrogen atom;
n is 0 or 1;
m is 1 or 2;
m? is 0 or 1;
w is 0, 1, or 2;
RX is selected from hydrogen, amino, hydroxy, and methyl;
R14 and R15 are independently selected from hydrogen and methyl;
R16a is selected from hydrogen and C1-C6 alkyl;
R16 is selected from
—(C(R17a)2)2—X—R30,
—C(R17a)2C(O)N(R16a)C(R17a)2—X?—R31,
—C(R17a)2[C(O)N(R16a)C(R17a)2]w?—X—R31,
—(C(R17a)(R17)C(O)NR16a)n?—H; and
—(C(R17a)(R17)C(O)NR16a)m?—C(R17a)(R17)—CO2H;

wherein:w? is 2 or 3;
n? is 1-6;
m? is 0-5;
X is a chain of between 1 and 172 atoms wherein the atoms are selected from carbon and oxygen and wherein the chain may contain one, two, three, or four groups selected from —NHC(O)NH—, and —C(O)NH— embedded therein; and wherein the chain is optionally substituted with one to six groups independently selected from —CO2H, —C(O)NH2, —CH2C(O)NH2, and —(CH2)CO2H;
X? is a chain of between 1 and 172 atoms wherein the atoms are selected from carbon and oxygen and wherein the chain may contain one, two, three, or four groups selected from —NHC(O)NH—, and —C(O)NH— embedded therein; and wherein the chain is optionally substituted with one to six groups independently selected from —CO2H, —C(O)NH2, and —CH2CO2H, provided that X? is other than unsubstituted PEG;
R30 is selected from —CO2H, —C(O)NRWRX, and —CH3 wherein RW and RX are independently selected from hydrogen and C1-C6alkyl, provided that when X is all carbon, R30 is other than —CH3;
R31 is —CO2H, —C(O)NRWRX, —CH3, alexa-5-SDP, and biotin;
each R17a is independently selected from hydrogen, C1-C6alkyl, —CH2OH, —CH2CO2H, —(CH2)2CO2H,
each R17 is independently selected from hydrogen, —CH3, (CH2)zN3, —(CH2)zNH2, —X—R31, —(CH2)zCO2H, —CH2OH, CH2C?CH, and —(CH2)z-triazolyl-X—R35, wherein z is 1-6 and R35 is selected from —CO2H, —C(O)NRWRX, CH3, biotin, -2-fluropyridine, —C(O)—(CH2)2—C(O)O-vitamin E, —C(O)O-vitamin E; and





provided at least one R17 is other than hydrogen, —CH3, or —CH2OH;Rc, Rf, Rh, Ri, Rm, and Rn are hydrogen;
Ra and Rj are each independently selected from hydrogen and methyl;
R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, R12, and R13 are independently selected from a natural amino acid side chain and an unnatural amino acid side chain or form a ring with the corresponding vicinal R group as described below;
R10 is indolylC1-C3alkyl, wherein the indolyl part is optionally substituted with one group selected from C1-C6alkoxy, C1-C6alkoxycarbonyl, C1-C6alkoxycarbonylC1-C3alkyl, (C1-C6alkyl)S(O)2NHC(O)C1-C3alkyl, arylS(O)2NHC(O)C1-C3alkyl, arylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, cyano, haloC1-C3alkoxy, haloC1-C3alkyl, heteroarylS(O)2NHC(O)C1-C3alkyl, heteroarylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, —NRpRq, (NRpRq)C1-C3alkyl, and tetrazolylC1-C3alkyl, or with two groups selected from C1-C6alkoxy, C1-C6alkoxycarbonyl, C1-C6alkoxycarbonylC1-C3alkyl, C1-C3alkyl, (C1-C6alkyl)S(O)2NHC(O)C1-C3alkyl, arylS(O)2NHC(O)C1-C3alkyl, arylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, carboxy, carboxyC1-C3alkyl, cyano, C3-C6cycloalkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, halo, haloC1-C3alkoxy, haloC1-C3alkyl, heteroarylS(O)2NHC(O)C1-C3alkyl, heteroarylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, hydroxy, —NRpRq, (NRpRq)C1-C3alkyl, tetrazolyl, tetrazolylC1-C3alkyl, and phenyl, wherein the phenyl is further optionally substituted by one, two, or three groups independently selected from C1-C3alkoxy, C1-C3alkyl, and halo; or
R10 is azaindolylC1-C3alkyl wherein the azaindolyl part of the azaindolylC1-C3alkyl is substituted with one or two other groups independently selected from C1-C6alkoxy, C1-C6alkoxycarbonyl, C1-C6alkoxycarbonylC1-C3alkyl, C1-C3alkyl, (C1-C6alkyl)S(O)2NHC(O)C1-C3alkyl, arylS(O)2NHC(O)C1-C3alkyl, arylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, carboxy, carboxyC1-C3alkyl, cyano, C3-C6cycloalkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, halo, haloC1-C3alkoxy, haloC1-C3alkyl, heteroarylS(O)2NHC(O)C1-C3alkyl, heteroarylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, hydroxy, —NRpRq, (NRpRq)C1-C3alkyl, tetrazolyl, tetrazolylC1-C3alkyl, and phenyl, wherein the phenyl is further optionally substituted by one, two, or three groups independently selected from C1-C3alkoxy, C1-C3alkyl, and halo; or
R10 is —(CH2)nQ?, wherein n is 1-3 and Q? is a five, six-fused saturated or unsaturated ring system containing one, two, three, or four nitrogen atoms, wherein said ring system is optionally substituted with one, two, or three groups selected from C1-C6alkoxy, C1-C6alkoxycarbonyl, C1-C6alkoxycarbonylC1-C3alkyl, C1-C3alkyl, (C1-C6alkyl)S(O)2NHC(O)C1-C3alkyl, arylS(O)2NHC(O)C1-C3alkyl, arylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, carboxy, carboxyC1-C3alkyl, cyano, C3-C6cycloalkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, halo, haloC1-C3alkoxy, haloC1-C3alkyl, heteroarylS(O)2NHC(O)C1-C3alkyl, heteroarylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, hydroxy, —NRpRq, (NRpRq)C1-C3alkyl, tetrazolyl, tetrazolylC1-C3alkyl, and phenyl, wherein the phenyl is further optionally substituted by one, two, or three groups independently selected from C1-C3alkoxy, C1-C3alkyl, and halo; provided Q? is other than azaindolyl or indolyl; or
R10 is —(CH2)nZ?, wherein n is 1-3 and Z? is a six, six-fused saturated or unsaturated ring system containing one, two, three or four nitrogen atoms, wherein said ring system is optionally substituted with one, two, or three groups selected from C1-C6alkoxy, C1-C6alkoxycarbonyl, C1-C6alkoxycarbonylC1-C3alkyl, C1-C3alkyl, (C1-C6alkyl)S(O)2NHC(O)C1-C3alkyl, arylS(O)2NHC(O)C1-C3alkyl, arylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, carboxy, carboxyC1-C3alkyl, cyano, C3-C6cycloalkylS(O)2NHC(O)C1-C3alkyl, C3-C6cycloalkylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, halo, haloC1-C3alkoxy, haloC1-C3alkyl, heteroarylS(O)2NHC(O)C1-C3alkyl, heteroarylC1-C3alkylS(O)2NHC(O)C1-C3alkyl, hydroxy, —NRpRq, (NRpRq)C1-C3alkyl, tetrazolyl, tetrazolylC1-C3alkyl, and phenyl, wherein the phenyl is further optionally substituted by one, two, or three groups independently selected from C1-C3alkoxy, C1-C3alkyl, and halo;
Rb is methyl or, Rb and R2, together with the atoms to which they are attached, form a ring selected from azetidine, pyrollidine, morpholine, piperidine, piperazine, and tetrahydrothiazole; wherein each ring is optionally substituted with one to four groups independently selected from amino, cyano, methyl, halo, and hydroxy;
Rd is hydrogen or methyl, or, Rd and R4, together with the atoms to which they are attached, can form a ring selected from azetidine, pyrollidine, morpholine, piperidine, piperazine, and tetrahydrothiazole; wherein each ring is optionally substituted with one to four groups independently selected from amino, cyano, methyl, halo, hydroxy, and phenyl;
Re is hydrogen or methyl, or Re and R5, together with the atoms to which they are attached, can form a ring selected from azetidine, pyrollidine, morpholine, piperidine, piperazine, and tetrahydrothiazole; wherein each ring is optionally substituted with one to four groups independently selected from amino, cyano, methyl, halo, and hydroxy;
Rg is hydrogen or methyl, or Rg and R7, together with the atoms to which they are attached, can form a ring selected from azetidine, pyrollidine, morpholine, piperidine, piperazine, and tetrahydrothiazole; wherein each ring is optionally substituted with one to four groups independently selected from amino, benzyl optionally substituted with a halo group, benzyloxy, cyano, cyclohexyl, methyl, halo, hydroxy, isoquinolinyloxy optionally substituted with a methoxy group, quinolinyloxy optionally substituted with a halo group, and tetrazolyl; and wherein the pyrrolidine and the piperidine ring are optionally fused to a cyclohexyl, phenyl, or indole group;
Rk is hydrogen or methyl, or Rk and R11, together with the atoms to which they are attached, can form a ring selected from azetidine, pyrollidine, morpholine, piperidine, piperazine, and tetrahydrothiazole; wherein each ring is optionally substituted with one to four groups independently selected from amino, cyano, methyl, halo, and hydroxy; and
R1 is methyl or, R1 and R12, together with the atoms to which they are attached, form a ring selected from azetidine and pyrollidine, wherein each ring is optionally substituted with one to four independently selected from amino, cyano, methyl, halo, and hydroxy.

US Pat. No. 11,066,443

ANTI-BACTERIAL PEPTIDE MACROCYCLES AND USE THEREOF

Hoffmann-La Roche Inc., ...


1. A method for the treatment of infections and resulting diseases caused by Pseudomonas aeruginosa, comprising the step of administering to a human being or animal in need thereof a compound of formula (I):



wherein:
X1 is C—R11;
X2 is C—R12;
X3 is C—R13;
X4 is N;
X5 is C—R15;
X6 is C—R16;
X7 is C—R17;
X8 is C—R18;
R1 is —(CH2)m-heteroaryl optionally substituted with one or more halo or C1-7-alkyl;
R2, R4 and R6 are each individually selected from hydrogen or C1-7-alkyl;
R3 and R5 are each independently selected from hydrogen, —C1-7-alkyl, hydroxy-C1-7-alkyl, —(CH2)m—NR20R21, —(CH2)m—C(O)NR20R21, —(CH2)m—CF2—(CH2)m—NR20R21, —(CH2)m—NH—C(O)—(CH2)m—NR20R21 or —(CH2)m—O—(CH2)n—NR20R21, —(CH2)m—NH—C(NH)—NR20R21, —(CH2)m—NH—C(O)—OR21, —(CH2)o—C3-7-cycloalkyl, —(CH2)o-heterocycloalkyl, —(CH2)o-heteroaryl, —(CH2)o-aryl, wherein cycloalkyl, heterocycloalkyl, heteroaryl and aryl are optionally substituted by halo, cyano, C1-7-alkyl, C1-7-haloalkyl, C1-7-hydroxyalkyl, C1-7-alkoxy or aryl;
R5? is hydrogen or C1-7-alkyl;
R7, R7? and R8, R8? are each individually selected from hydrogen or C1-7-alkyl;
R11, R12, R13, R14, R15, R16, R17 and R18 are each individually selected from hydrogen, halogen, C1-7-alkyl, C1-7-haloalkyl, hydroxy, C1-7-hydroxyalkyl, C1-7-alkoxy, C1-7-haloalkoxy, —NR24R25, C1-7-alkyl-NR24R25, aryl-C1-7-alkyl-O—C1-7-alkinyl-, aryl and heteroaryl, wherein aryl and heteroaryl are optionally substituted with one, two or three substituents selected from the list of halogen, cyano, C1-7-alkyl C1-7-haloalkyl, hydroxy, C1-7-alkoxy, —NR24R25, C1-7-alkyl-NR24R25, —CO—NH—(CH2)n—NR24R25, —CO—NH—(CH2)r—OH, —CO—NH—(CH2)o-heterocycloalkyl, —CO—OH, —O—C1-7-hydroxyalkyl, —O—(CH2)o—CO—OH, —SO2—C1-7-alkyl, —SO2—NR24R25, heterocycloalkyl, —O—heterocycloalkyl and heterocycloalkyl substituted with C1-7-alkyl or oxo;
R20 and R22 are each individually selected from hydrogen, C1-7-alkyl and benzyl;
R21 and R23 are each individually selected from hydrogen and C1-7-alkyl;
R24 and R25 are each individually selected from hydrogen, C1-7-alkyl, C1-7-haloalkyl, C1-7-hydroxyalkyl, and C3-7-cycloalkyl;
m is 1, 2, 3, 4, 5 or 6;
n is 2, 3, 4, 5 or 6; and
o is 0, 1, 2, 3, 4, 5, 6, 7 or 8;
or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,442

DEUTERATED COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATING CANCERS ASSOCIATED WITH ETBR ACTIVATION

ENB Therapeutics, Inc., ...


1. A method of treating a tumor in a subject in need thereof, comprising administering to the subject a deuterated endothelin B-receptor (ETBR) antagonist according to Formula:




a stereoisomer, or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,441

METHOD FOR SEPARATING AND PURIFYING ?2-MACROGLOBULIN FROM COHN FRACTION IV PRECIPITATION

ACADEMY OF MILITARY MEDIC...


1. A method for separating and purifying ?2-macroglobulin from a Cohn Fraction IV precipitation, the method comprising subjecting the Cohn Fraction IV precipitation to the following sequential steps:(a) ammonium sulfate precipitation;
(b) zinc ion affinity chromatography;
(c) gel filtration; and
(d) ultrafiltration and concentration;
thereby obtaining ?2-macroglobulin, wherein the ultrafiltration step utilizes an ultrafiltration membrane having a molecular weight cutoff within a range of 30-500 kD, and
wherein, in the ammonium sulfate precipitation, the saturation of the ammonium sulfate is 40-60%, and the ammonium sulfate precipitation consists of a single precipitation.

US Pat. No. 11,066,440

PROCESSES FOR INCREASING PLANT PROTEIN YIELD FROM BIOMASS

Cavitation Technologies, ...


1. A process for extracting proteins from plant biomass, comprising the steps of:preparing plant biomass for extraction of protein to remove contaminants and reduce particle size;
storing the prepared plant biomass in a storage hopper;
combining the stored plant biomass from the storage hopper with a solvent in an agitation tank forming a biomass slurry;
subjecting the biomass slurry to a hydrodynamic cavitation treatment to extract plant protein from the biomass slurry;
separating the biomass slurry into a protein extract and biomass waste;
adjusting a pH value of the protein extract to an isoelectric point for proteins in the plant biomass;
precipitating plant proteins from the protein extract at the isoelectric point; and
separating the plant proteins from the protein extract.

US Pat. No. 11,066,437

METHODS AND INTERMEDIATES FOR THE PREPARATION OF BILE ACID DERIVATIVES

Intercept Pharmaceuticals...


1. A method of preparing a compound of formula I




or a pharmaceutically acceptable salt, hydrate, solvate, or amino acid, sulfate or glucuronide conjugate, or prodrug thereof,
wherein:R1 is OH, alkoxy, or oxo;
R2 is OH, OSO3H, OCOCH3, OPO3H2, halogen, or alkyl optionally substituted with one or more halogen;
R3 is H; or R2 and R3 taken together with the carbon atom to which they are attached form a carbonyl;
R5 is OH, OR11, OSO3H, OCOCH3, OPO3H2, halogen, or alkyl optionally substituted with one or more halogen;
R6 is H; or R5 and R6 taken together with the carbon atom to which they are attached form a carbonyl;
R4 is alkyl optionally substituted with one or more halogen or OH, alkenyl, or alkynyl;
R7 is OH, OSO3H, SO3H, OSO2NH2, SO2NH2, OPO3H2, PO3H2, CO2H, C(O)NHOH, NH(CH2)2SO3H, NHCH2CO2H or optionally substituted tetrazolyl, oxadiazolyl, thiadiazolyl, 5-oxo-1,2,4-oxadiazolyl, 5-oxo-1,2,4-thiadiazolyl, oxazolidine-dionyl, thiazolidine-dionyl, 3-hydroxyisoxazolyl, 3-hydroxyisothiazolyl, pyrimidine, 3,5-difluoro-4-hydroxyphenyl, or 2,4-difluoro-3-hydroxyphenyl;
R8, R9, and R10 are each independently H, OH, halogen, or alkyl optionally substituted with one or more halogen or OH, or R8 and R9 taken together with the carbon atoms to which they are attached form a 3- to 6-membered carbocyclic or heterocyclic ring comprising 1 or 2 heteroatoms selected from N, O, and S, or R9 and R10 taken together with the carbon atoms to which they are attached form a 3- to 6-membered carbocyclic or heterocyclic ring comprising 1 or 2 heteroatoms selected from N, O, and S;
m is 0, 1, or 2;
n is 0 or 1; and
p is 0 or 1;

the method comprising the step of reacting a compound of formula I-4 with a halogenating reagent to provide a compound of formula I-5a




wherein X is —(CHR8)m(CHR9)n(CHR10)p—R7, and R7, R8, R9, and R10 may be protected by R11 selected from acetyl, benzoyl, C(O)C1-C4 alkyl, C1-C6 alkoxycarbonyl, optionally substituted aryloxycarbonyl, benzyl, pivaloyl, tetrahydropyranyl ether, tetrahydrofuranyl, 2-methoxyethoxymethyl ether, methoxymethyl ether, ethoxyethyl ether, p-methoxybenzyl ether, methylthiomethyl ether, triphenylmethyl, dimethoxytrityl, methoxytrityl, and silyl ether.

US Pat. No. 11,066,436

5?-PHOSPHOROTHIOLATE MRNA 5?-END (CAP) ANALOGS, MRNA COMPRISING THE SAME, METHOD OF OBTAINING AND USES THEREOF

UNIWERSYTET WARSZAWSKI, ...


1. A 5?-phosphorothiolate cap analog according to formula 1



wherein
L1 and L2 are independently selected from O or S, wherein at least one of L1 and L2 is not O;
n=0, 1, or 2;
X1, X2, and X3 are independently selected from O or S;
R1 is selected from CH3, C2H5, CH2Ph, alkyl, or substituted alkyl;
R2 and R3 are independently selected from H, OH, OCH3, OC2H5, —COOH, N3, alkyl, alkenyl or alkynyl;
R4 and R5 are independently selected from H, OH, OCH3, OC2H5, —COOH, CH2COOH, N3, CH2N3, alkyl, alkenyl, or alkynyl;
Y1 and Y2 are independently selected from CH2, CHCl, CCl2, CF2, CHF, NH, or O;
and B is a group according to formula 3, 4, 5, 6 or 7





US Pat. No. 11,066,434

METAL COMPLEXES COMPRISING ANILINE TYPE LIGANDS


1. An olefin metathesis catalyst comprising cyclic alkyl amino carbenes, represented by the structure of Formula (A16B4CDII)



wherein:
Y3 is C or N;
m is 0, 1 or 2;
b is 0, 1, 2 or 3;
c is 0, 1, 2 or 3;
d is 0 when Y3 is N; d is 1 when Y3 is C;
W is optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, halogen, optionally substituted C5-C24 aryl, optionally substituted C6-C24 aralkyl, optionally substituted C1-C20 heteroalkyl, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR27, or together with an adjacent W can form optionally substituted unsaturated polycyclic ring;
Z is optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, halogen, optionally substituted C5-C24 aryl, optionally substituted C6-C24 aralkyl, optionally substituted C1-C20 heteroalkyl, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR27, or together with an adjacent Z can form optionally substituted unsaturated polycyclic ring;
x is 1 or 2;
X1 and X2 are independently anionic ligands;
R1 and R2 are independently selected from hydrogen, optionally substituted hydrocarbyl, optionally substituted heteroatom-containing hydrocarbyl; or any two or more of X1, X2, R1, and R2 are taken together to form one or more cyclic groups;
Y1 is —NR1cR2c—;
R1c is H or optionally substituted C1-24 alkyl;
R2c is H or optionally substituted C1-24 alkyl;
Y2 is —NR1dR2d—;
R1d is H or optionally substituted C1-24 alkyl;
R2d is H or optionally substituted C1-24 alkyl;
the Ar groups can be identical or different;
Ar is




R5a is H, optionally substituted C1-24 alkyl, halogen, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR26, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl, optionally substituted C3-8 cycloalkenyl, or together with R6a can form an optionally substituted polycyclic ring;
R6a is H, optionally substituted C1-24 alkyl, halogen, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR26, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl, optionally substituted C3-8 cycloalkenyl or together with R5a or together with R7a can form an optionally substituted polycyclic ring;
R7a is H, optionally substituted C1-24 alkyl, halogen, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR26, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl, optionally substituted C3-8 cycloalkenyl, or together with R6a or together with R8a can form an optionally substituted polycyclic ring;
R8a is H, optionally substituted C1-24 alkyl, halogen, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR26, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl, optionally substituted C3-8 cycloalkenyl, or together with R7a or together with R9a can form an optionally substituted polycyclic ring;
R9a is H, optionally substituted C1-24 alkyl, halogen, —C(O)R21, —OR22, —CN, —NR23R24, NO2, —CF3, —S(O)xR25, —P(O)(OH)2, —OP(O)(OH)2, —SR26, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl, optionally substituted C3-8 cycloalkenyl, or together with R8a can form a polycyclic ring;
R21 is OH, OR26, NR23R24, optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R22 is H, optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R23 is H, optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R24 is H, optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R25 is H, optionally substituted C1-24 alkyl, OR22, —NR23R24, optionally substituted heterocycle, optionally substituted C3-8 cycloalkyl, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R26 is optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl;
R27 is H, optionally substituted C1-24 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted heterocycle, optionally substituted C5-24 aryl or optionally substituted C3-8 cycloalkenyl; and
R11a, R12a, R13a and R14a are independently hydrogen, unsubstituted C1-C12 alkyl, substituted C1-C12 alkyl, unsubstituted C1-C12 heteroalkyl, substituted C1-C12 heteroalkyl, unsubstituted C5-C14 aryl, or substituted C5-C14 aryl; or any two of R11a, R12a, R13a, and R14a, are optionally linked together to form a substituted or unsubstituted, saturated or unsaturated ring structure.

US Pat. No. 11,066,433

PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY

GALERA LABS, LLC, Creve ...


1. A method of lessening the severity of tissue damage resulting from a cancer treatment in a mammal afflicted with cancer, comprising orally administering a therapeutically effective dose of a pentaaza macrocyclic ring complex to the mammal,wherein the pentaaza macrocyclic ring complex comprises the following formula:





US Pat. No. 11,066,430

METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END

SHIN-ETSU CHEMICAL CO., L...


1. An alcohol compound having silyl-protected amino group of formula (I-2-A):



wherein R1 are each independently a linear monovalent hydrocarbon group having 1 to 6 carbon atoms, or a branched or cyclic monovalent hydrocarbon group having 3 to 6 carbon atoms; and
RA2 is a saturated linear divalent hydrocarbon group having 3 to 6 carbon atoms, or a branched or cyclic divalent hydrocarbon group having 3 to 6 carbon atoms.

US Pat. No. 11,066,428

BIS-PHENYL-PHENOXY POLYOLEFIN CATALYSTS HAVING A METHYLENETRIALKYLSILICON LIGAND ON THE METAL FOR IMPROVED SOLUBILITY

Dow Global Technologies L...


1. A catalyst system comprising a metal-ligand complex according to formula (I):




where:M is a metal chosen from titanium, zirconium, or hafnium, the metal being in a formal oxidation state of +2, +3, or +4;
X is selected from the group consisting of —(CH2)SiRX3, where each RX is independently a (C1-C30)hydrocarbyl or a (C1-C30)heterohydrocarbyl and at least one of RX is a (C2-C30)hydrocarbyl, where any two RX or all three RX are optionally covalently linked;
each Z is independently chosen from —O—, —S—, —N(RN)—, or —P(RP)—;
each of R1 and R16 is independently selected from the group consisting of —H, (C1-C40)hydrocarbyl, (C1-C40)heterohydrocarbyl, —Si(RC)3, —Ge(RC)3, —P(RP)2, —N(RN)2, —ORC, —SRC, —NO2, —CN, —CF3, RCS(O)—, RCS(O)2—, (RC)2C?N—, RCC(O)O—, RCOC(O)—, RCC(O)N(R)—, (RC)2NC(O)—, halogen, radicals having formula (II), radicals having formula (III), and radicals having formula (IV):




?where each of R31-R35, R41—R48, and R51—R59 is independently chosen from —H, (C1-C40)hydrocarbyl, (C1-C40)heterohydrocarbyl, —Si(RC)3, —Ge(RC)3, —P(RP)2, —N(RN)2, —ORC, —SRC, —NO2, —CN, —CF3, RCS(O)—, RCS(O)2—, (RC)2C?N—, RCC(O)O—, RCOC(O)—, RCC(O)N(RN)—, (RC)2NC(O)—, or halogen,provided that at least one of R1 or R16 is a radical having formula (II), a radical having formula (III), or a radical having formula (IV);

each of R2-R4, R5-R8, R9-R12, and R13-R15 is independently selected from —H, (C1-C40)hydrocarbyl, (C1-C40)heterohydrocarbyl, —Si(RC)3, —Ge(RC)3, —P(RP)2, —N(RN)2, —ORC, —SRC, —NO2, —CN, —CF3, RCS(O)—, RCS(O)2—, (RC)2C?N—, RCC(O)O—, RCOC(O)—, RCC(O)N(R)—, (RC)2NC(O)—, and halogen;
L is (C2-C40)hydrocarbylene or (C2-C40)heterohydrocarbylene; and
each RC, RP, and RN in formula (I) is independently a (C1-C30)hydrocarbyl, (C1-C30)heterohydrocarbyl, or —H.

US Pat. No. 11,066,427

ORGANOSILANE COMPOUNDS HAVING BULKY SUBSTITUENT AND PREPARATION THEREOF

SHIN-ETSU CHEMICAL CO., L...


1. An organosilane compound having a bulky substituent group, represented by the general formula (1):



wherein R1 is a C4-C10 tertiary hydrocarbon group, R2 is a C1-C10 straight alkyl group, and LG is halogen or trifluoromethanesulfonyloxy.

US Pat. No. 11,066,426

METHODS OF MAKING POROUS MOLECULAR STRUCTURES

GEORGIA TECH RESEARCH COR...


1. A method comprising:masking a metal-containing material with a nonreactive mask having a predetermined pattern;
mixing the masked metal-containing material, a ligand-providing material, and a solvent in which the metal-containing material and the mask are insoluble, forming a mixture; and
reacting, in the mixture, the masked metal-containing material with the ligand-providing material, forming a porous molecular structure.

US Pat. No. 11,066,425

OXO-SUBSTITUTED COMPOUND

SUMITOMO DAINIPPON PHARMA...


1. A pharmaceutical composition comprising at least one compound selected from the group of compounds consisting of:a) 7-[(1-{[4-(2-aminoethyl)-1H-imidazol-1-yl]acetyl}azetidin-3-yl)oxy]-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




b) 8-[(1-{[4-(2-aminoethyl)-1H-imidazol-1-yl]acetyl}azetidin-3-yl)oxy]-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




c) 7-({1-[(2R)-2-amino-2-(1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




d) 8-({1-[(2R)-2-amino-2-(1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




e) 7-({1-[(2S)-2-amino-2-(1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




f) 8-({1-[(2S)-2-amino-2-(1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




g) 7-({1-[amino(1-methyl-1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




h) 8-({1-[amino(1-methyl-1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




i) 7-({1-[2-amino-2-(1H-imidazol-4-yl)(2H)ethanoyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




j) 8-({1-[2-amino-2-(1H-imidazol-4-yl)(2H)ethanoyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




k) 7-({1-[2-amino-2-(1H-imidazol-4-yl)propanoyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




l) 8-({1-[2-amino-2-(1H-imidazol-4-yl)propanoyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




m) 7-({1-[amino(2-methyl-1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




n) 8-({1-[amino(2-methyl-1H-imidazol-4-yl)acetyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




o) 2-hydroxy-7-({1-[(1H-1,2,3-triazol-1-yl)acetyl]azetidin-3-yl}oxy)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




p) 4,4-dihydroxy-8-({1-[(H-1,2,3-triazol-1-yl)acetyl]azetidin-3-yl}oxy)-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




q) 2-hydroxy-7-[(1-D-serylazetidin-3-yl)oxy]-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




r) 4,4-dihydroxy-8-[(1-D-serylazetidin-3-yl)oxy]-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




s) 2-hydroxy-7-{[1-(4-hydroxyprolyl)azetidin-3-yl]oxy}-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




t) 4,4-dihydroxy-8-{[1-(4-hydroxyprolyl)azetidin-3-yl]oxy}-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




u) 2-hydroxy-7-({1-[(pyrrolidin-3-yl)acetyl]azetidin-3-yl}oxy)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




v) 4,4-dihydroxy-8-({1-[(pyrrolidin-3-yl)acetyl]azetidin-3-yl}oxy)-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




w) 2-hydroxy-7-({1-[(morpholin-2-yl)acetyl]azetidin-3-yl}oxy)-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




x) 4,4-dihydroxy-8-({1-[(morpholin-2-yl)acetyl]azetidin-3-yl}oxy)-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




y) 7-{[1-(L-?-asparaginyl)azetidin-3-yl]oxy}-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid




z) 8-{[1-(L-?-asparaginyl)azetidin-3-yl]oxy}-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




aa) 7-({1-[amino(1H-imidazol-5-yl)acetyl]azetidin-3-yl}oxy)-2-hydroxy-3,4-dihydro-2H-1,2-benzoxaborinine-8-carboxylic acid





andab) 8-({1-[amino(1H-imidazol-5-yl)acetyl]azetidin-3-yl}oxy)-4,4-dihydroxy-5-oxa-4-boranuidabicyclo[4.4.0]deca-l(6),7,9-triene-7-carboxylic acid




or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,424

SOLID FORMS OF SUBSTITUTED BENZOXABOROLE AND COMPOSITIONS THEREOF

Boragen, Inc., Durham, N...


1. A crystalline form of a compound of formula I:




5-chlorobenzo[c][1,2]oxaboral-1(3H)-ol, wherein the crystalline form is Crystalline Form A characterized by an X-ray powder diffraction pattern (XRPD) comprising one or more 2? angle values selected from: about 16°±1.0, about 23°±1.0, about 25°±1.0, and about 27°±1.0.

US Pat. No. 11,066,423

MONOMERIC BIMETAL HYDROXYCITRIC ACID COMPOUNDS AND METHODS OF MAKING AND USING THE SAME

GLYKON TECHNOLOGIES GROUP...


1. A covalent monomeric hydroxycitric acid (HCA) compound of formula (I):



wherein:
X is a divalent metal selected from Group IIA metals, Group IIB metals or a divalent metal selected from Mn, Tc and Re; and
Y is a monovalent metal;
or a hydrate thereof,
wherein X—O and Y—O comprise covalent bonds.

US Pat. No. 11,066,422

METHOD OF PRODUCING CYCLOALKYL(TRIFLUOROMETHYL)BENZENE

Toray Fine Chemicals Co.,...


1. A method of producing cycloalkyl(trifluoromethyl)benzene comprising:reacting a halogen-substituted trifluoromethyl benzene as represented by general formula (1) with magnesium metal to produce a Grignard reagent,
treating 1) an iron salt selected from the group consisting of ferrous chloride, ferric chloride, iron acetate, and iron acetylacetonate or 2) a cobalt salt selected from the group consisting of cobalt chloride and cobalt acetylacetonate with a reducing agent selected from the group consisting of lithium aluminum hydride, sodium boron hydride, sulfites, hydrazine, diisobutylaluminum hydride, oxalic acid, formic acid, and Grignard reagents having 1 to 4 carbon atoms, and
cross-coupling the Grignard reagent with a cycloalkyl halide in the presence of the iron salt or the cobalt salt at a reaction temperature of 60° C. to 80° C. to produce a cycloalkyl(trifluoromethyl)benzene as represented by general formula (2):





wherein X is Cl or Br, and n is 1 or 2, and




wherein R is one selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl, and n is 1 or 2.

US Pat. No. 11,066,421

SYNTHETIC CINCHONA ALKALOIDS AGAINST CANCER

Ares Pharmaceuticals, LLC...


1. A compound having the structure of Formula I or II, or a pharmaceutically acceptable salt of Formula I or Formula II, the compound of Formula I comprising three alkaloid moieties substituted with R and R? and bound to pyrimidine as a linker, and the compound of Formula II comprising three alkaloid moieties substituted with R and R? and bound to L:







wherein each R is, independent of R?, independently selected from the group consisting of H, Me, Et, Pr, Bu, tBu, Ph, PhCH2, OH, OMe, OEt, OPr, OBu, OtBu, OPh, OCH2Ph; each R? is, independent of R, independently selected from the group consisting of CH?CH2, Me, Et, Pr, Bu, tBu, Ph, PhCH2, OH, OMe, OEt, OPr, OBu, OtBu, OPh, or OCH2Ph; and L represents a linker moiety selected from pyrazine, pyridazine, pyrimidine, and phthalazine.

US Pat. No. 11,066,420

INHIBITORS OF LOW MOLECULAR WEIGHT PROTEIN TYROSINE PHOSPHATASE (LMPTP) AND USES THEREOF

SANFORD BURNHAM PREBYS ME...


1. A compound of Formula (I), or a pharmaceutically acceptable salt, or solvate thereof:



wherein,
R1 is





and R2 is —Z1-L4-R4; is an aryl;each R1 is independently H, halogen, —CN, —OH, —OR13, —SR13, —S(?O)R13, —S(?O)2R13, —N(R12)S(?O)2R13, —S(?O)2NR12R13, —C(?O)R13, —OC(?O)R13, —CO2R12, —OCOO2R13, —NR12R12, —NR12R13, —C(?O)NR12R12, —C(?O)NR12R13, —OC(?O)NR12R12, —OC(?O)NR12R13, —NR12C(?O)NR12R12, —NR12C(?O)NR12R13, —NR12C(?O)R13, —NR12C(?O)OR13, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, or substituted or unsubstituted C1-C6heteroalkyl;
each Rb is independently H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, or substituted or unsubstituted C1-C6heteroalkyl;
m is 0, 1, or 2; n is 0, 1, or 2;

L2 is -L7-Y1—;L7 is absent, substituted or unsubstituted C1-C4alkylene, —CH?CH—, substituted or unsubstituted C3-C6cycloalkylene, —Y2-L8-, or -L8-Y2-L8-;
Y1 is —C(?O)NRc—, —C(?O)—, —SO2NRc—, —C(?O)O—, —C(?NRc)—, —C(?N—ORc)—, —C(?NRc)NRc—, or —C(?N—ORc)—NRc—;
each L8 is independently substituted or unsubstituted C1-C4alkylene or substituted or unsubstituted C3-C6cycloalkylene;

Y2 is —O—, —S—, —S(?O)—, —SO2—, —NRc—, —C(?O)NRc—, —C(?O)—, —NRcC(?O)—, —SO2NRc—, —NRcSO2—, —OC(?O)—, —C(?O)O—, —OC(?O)O—, —OC(?O)NRc—, —NRcC(?O)O—, or —NRcC(?O)NRc—;each Rc is independently H or substituted or unsubstituted C1-C6alkyl;

R3 is H or -L3-R5;L3 is absent, substituted or unsubstituted C1-C6alkylene, or substituted or unsubstituted C1-C6heteroalkylene;
R5 is H, substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

or R3 and Rc are taken together with the N atom to which they are attached to form a substituted or unsubstituted N-containing heterocycle;
Z1 is —NRd—, —S—, —SO2—, —SO2NRd—, —OC(?O)—, —OC(?O)O—, —OC(?O)NRd—, —NRdC(?O)O—, or —NRdC(?O)NRd—;each Rd is independently H or substituted or unsubstituted C1-C6alkyl;

L4 is absent or -L5-L6-;L5 is substituted or unsubstituted C1-C6alkylene, substituted or unsubstituted C1-C6heteroalkylene, substituted or unsubstituted arylene or substituted or unsubstituted heteroarylene;
L6 is absent, substituted or unsubstituted C1-C6alkylene, substituted or unsubstituted C1-C6heteroalkylene, —NR6—, —C(?O)NR6—, —NR6C(?O)—, or —NR6C(?O)NR6—;

R4 is substituted or unsubstituted C3-C10cycloalkyl, substituted or unsubstituted C2-C10heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
or R4 and R6 are taken together with the N atom to which they are attached to form a substituted or unsubstituted N-containing heterocycle;
X1 is CR7;
X2 is CR8;
X3 is N;
X4 is CR10;
X5 is CR11;
R7, R8, R9, R10, and R11 are independently selected from H, halogen, —CN, —OH, —OR13, —SR13, —S(?O)R13, —S(?O)2R13, —N(R12)S(?O)2R13, —S(?O)2NR12R12, —S(?O)2NR12R13, —C(?O)R13, —OC(?O)R13, —CO2R12, —OCO2R13, —NR12R12, —NR12R13, —C(?O)NR12R12, —C(?O)NR12R13, —OC(?O)NR12R12, —OC(?O)NR12R13, —NR12C(?O)NR12R12, —NR12C(?O)NR12R13, —NR12C(?O)R13, —NR12C(?O)OR13, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6fluoroalkyl, substituted or unsubstituted C1-C6heteroalkyl, a substituted or unsubstituted C3-C6cycloalkyl, a substituted or unsubstituted C2-C6heterocycloalkyl, a substituted or unsubstituted aryl, and a substituted or unsubstituted heteroaryl;
each R12 is independently selected from the group consisting of H, C1-C6alkyl, C1-C6fluoroalkyl, and C1-C6heteroalkyl;
each R13 is independently selected from the group consisting of C1-C6alkyl, C1-C6fluoroalkyl, C1-C6heteroalkyl, a substituted or unsubstituted C3-C6cycloalkyl, a substituted or unsubstituted C2-C6heterocycloalkyl, a substituted or unsubstituted aryl, a substituted or unsubstituted heteroaryl, a substituted or unsubstituted —C1-C4alkylene-C3-C10cycloalkyl, a substituted or unsubstituted —C1-C4alkylene-C2-C10heterocycloalkyl, a substituted or unsubstituted —C1-C4alkylene-aryl, and a substituted or unsubstituted —C1-C4alkylene-heteroaryl;
or when R12 and R13 are attached to the same N atom then R12 and R13 are taken together with the N atom to which they are attached to form a substituted or unsubstituted C2-C10heterocycle.

US Pat. No. 11,066,419

1H-PYRROLE-2,5-DIONE COMPOUNDS AND METHODS OF USING SAME

Frequency Therapeutics, I...


1. A compound of Formula (I):




or a pharmaceutically acceptable salt or tautomer thereof, wherein:Q1 is CH or N;
Q2 is C or N;
Q3 is C or N;wherein at least one of Q1, Q2, and Q3 is N;

R1 is selected from the group consisting of hydrogen, halo, C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, —CN, —OH, —O—C1-C4alkyl, —NH2, —NHC(O)R1a, and —S(O)2NH2; wherein the alkyl is optionally substituted with one to 3 substituents independently selected from the group consisting of halo and OH; and wherein R1a is C1-C4alkyl;
R2 is selected from the group consisting of fluoro, C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, —CN, —OH, —O—C1-C4alkyl, —NH2, —NH(C1-C4alkyl), —N(C1-C4alkyl)2, —NHC(O)R2a, and —S(O)2NH2; wherein the alkyl is substituted with one to 3 substituents independently selected from the group consisting of halo and OH; and wherein R2a is C1-C4alkyl;
R3 is selected from the group consisting of hydrogen, halo, C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, —CN, —OH, —O—C1-C4alkyl, —NH2, —NHC(O)R3a, and —S(O)2NH2; wherein the alkyl is optionally substituted with one to 3 substituents independently selected from the group consisting of halo and —OH; and wherein R3a is C1-C4alkyl;
Ar is selected from the group consisting of




—Z—W—X—Y— is —C(RZ)2—C(RW)2—N(RX)—C(RY)2—, —C(RZ)2—C(RW)2—CH(RX)—C(RY)2—, or —C(RW)2—CH(RX)—C(RY)2—;
each RZ is independently selected from the group consisting of hydrogen, deuterium, halo, and C1-C4alkyl, or both RZ groups together form C3-C6cycloalkyl or oxo;
each RW is independently selected from the group consisting of hydrogen, deuterium, halo, and C1-C4alkyl, or both RW groups together form C3-C6cycloalkyl or oxo;
or RZ and RW together with the carbons to which they are attached form a C3-C6cycloalkyl;
RX is selected from the group consisting of —CORX1, —SO2RX1, heteroaryl, and —(C1-C4alkylene)-(C3-C8cycloalkyl), and wherein the —(C1-C4alkylene)-(C3-C8cycloalkyl) is optionally substituted with one to four halo on the C1-C4alkylene;
wherein RX1 is heterocyclyl, wherein the heterocyclyl is optionally substituted with one to twelve substituents independently selected from the group consisting of deuterium, halo, —[C(RX1a)2]p—CN, —CF3, C1-C4alkyl, —(CH2)p—OH, —[C(RX1a)2]p—OH, —[C(RX1a)2]p—O—C1-C4alkyl, —NHCOC1-C4alkyl, —CONHC1-C4alkyl, —COH, —CO2H, —[C(RX1a)2]p—COO—C1-C4alkyl, —(CH2)p—NH2, —[C(RX1a)2]p—NH2, —[C(RX1a)2]p—NH—C1-C4alkyl, —[C(RX1a)2]p—N—(C1-C4alkyl)2; wherein p is 0, 1, 2, or 3; wherein each RX1a is independently selected from the group consisting of hydrogen, deuterium, halo, —CF3, and C1-C4alkyl, or both RX1a groups together form C3-C6cycloalkyl;
or RX1 is N(RX2)2 wherein R? is independently selected from hydrogen, alkyl, substituted alkyl, wherein the alkyl substitution can be halo, heterocyclyl, and substituted heterocyclyl;
each RY is independently selected from the group consisting of hydrogen, deuterium, halo, and C1-C4alkyl, or both RY groups together form C3-C6cycloalkyl or oxo; and
m is 0, 1, or 2;
provided that the compound is not





US Pat. No. 11,066,418

COMPOUND AND THIN FILM TRANSISTOR AND ELECTRONIC DEVICE

Samsung Electronics Co., ...


1. A compound represented by Chemical Formula 1A or 1B:



wherein, in Chemical Formulae 1A and 1B,
X1 is O, S, Se, or Te,
R1 to R4 are each independently hydrogen, a substituted or unsubstituted C1 to C30 alkyl group, a substituted or unsubstituted C2 to C30 alkenyl group, a substituted or unsubstituted C2 to C30 alkynyl group, a substituted or unsubstituted C1 to C30 alkoxy group, a substituted or unsubstituted C6 to C30 aryl group, a substituted or unsubstituted C6 to C30 aryloxy group, a substituted or unsubstituted C3 to C30 heteroaryl group, a halogen, a cyano group, or a combination thereof, and
n1 is 1,
Ar1 is one of substituted or unsubstituted rings listed in Group 1-1:




wherein, in Group 1-1,
Y1 and Y2 are each independently one of O, S, Se, and Te, and
* is a linking point with Chemical Formula 1A or 1B.

US Pat. No. 11,066,417

MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR, PHARMACEUTICAL COMPOSITIONS, METHODS OF TREATMENT, AND PROCESS FOR MAKING THE MODULATORS

Vertex Pharmaceuticals In...


1. A compound of Formula (I):




a pharmaceutically acceptable salt thereof, or a deuterated derivative of any of the foregoing,
wherein:Ring A is a phenyl, a 5-membered heteroaryl ring, or a 6-membered heteroaryl ring;
Ring B is a pyridinyl ring;
Ring D is a phenyl ring, a 5-membered heterocyclyl ring, a 6-membered heterocyclyl ring, a 5-membered heteroaryl ring, or a 6-membered heteroaryl ring;
X is O, NH, or an N(C1-C4 alkyl);
each R1 is independently chosen from C1-C2 alkyl groups, C1-C2 alkoxyl groups, C1-C2 haloalkyl groups, C1-C2 haloalkoxyl groups, halogens, a cyano group, and a hydroxyl group;
m is 0, 1, 2, 3, or 4;
each R2 is independently chosen from C1-C2 alkyl groups, C1-C2 alkoxyl groups, C1-C2 haloalkyl groups, C1-C2 haloalkoxyl groups, halogens, a cyano group, and a hydroxyl group;
n is 0, 1, or 2;
each R3 is methyl;
each R4 is independently chosen from halogens, an oxo group, a hydroxyl group, a cyano group, and —(Y)k—R7 groups, or optionally two R4, together with the atom(s) they are attached to, form a 5-6 membered cycloalkyl or heterocyclyl ring that is optionally and independently substituted with one or more groups chosen from halogens, C1-C2 alkyl groups, haloalkyl groups, a hydroxyl group, C1-C2 alkoxyl groups, and C1-C2 haloalkoxyl groups; wherein:k is 0, 1, 2, 3, 4, 5, or 6;
each Y is independently chosen from C(R5)(R6) groups, —O—, and —NRa— groups, wherein a heteroatom in —(Y)k—R7 is not bonded to another heteroatom in —(Y)k—R7, wherein:each R5 and R6 is independently chosen from hydrogen, halogens, a hydroxyl group, C1-C4 alkyl groups, and C3-5 cycloalkyl groups, or R5 and R6 on the same carbon together form a C3-5 cycloalkyl group or oxo;each of R5 and R6 is optionally independently substituted with one or more groups chosen from C1-C2 alkyl groups, C1-C2 haloalkyl groups, halogens, a hydroxyl group, C1-C2 alkoxyl groups, and C1-C2 haloalkoxyl groups; and

each Ra is independently chosen from hydrogen and C1-C2 alkyl groups; and

R7 is chosen from hydrogen, halogens, a cyano group, and C3-C10 cycloalkyl groups optionally substituted with one or more groups chosen from C1-C2 alkyl groups, C1-C2 haloalkyl groups, and halogens;

q is 1, 2, 3 or 4; and
Z is a divalent linker of formula (L)r, wherein:r is 1, 2, 3, 4, 5, or 6;
each L is independently chosen from C(R8)(R9) groups, —O—, and —NRb— groups, wherein a heteroatom in Z is not bonded to another heteroatom in Z, wherein:each R8 and R9 is independently chosen from hydrogen, halogens, C1-C2 haloalkyl groups, C1-C2 alkyl groups, a hydroxyl group, C1-C2 alkoxyl groups, and C1-C2 haloalkoxyl groups; and
each Rb is independently chosen from hydrogen and C1-C2 alkyl groups.



US Pat. No. 11,066,416

RAPAFUCIN DERIVATIVE COMPOUNDS AND METHODS OF USE THEREOF

The Johns Hopkins Univers...


1. A macrocyclic compound according to Formula (XII):



or a pharmaceutically acceptable salt or stereoisomer thereof
wherein
Ring A is a 5-10 membered aryl substituted with 1-17 substituents independently selected from the group consisting of halo, alkyl, alkoxy, cyano, haloalkyl, haloalkoxy, alkylthio, oxo, amino, alkylamino, dialkylamino,




?or heteroaryl or heterocycloalkyl, optionally substituted with 1-17 substituents, each of the substituent is independently selected from the group consisting of hydrogen, hydroxy, halo, alkyl, alkoxy, cyano, haloalkyl, haloalkoxy, alkylthio, oxo, amino, alkylamino, dialkylamino,




?wherein




?is a resin;
J is independently at each occurrence selected from the group consisting of —C(O)NR6—,








R6 is each hydrogen, alkyl, arylalkyl




RN is aryl, alkyl, or arylalkyl;
R? is hydrogen, alkyl, arylalkyl, or haloalkyl;
D is independently at each occurrence an oligonucleotide;
Lb and Lc are independently at each occurrence selected from the group consisting of bond, —O—, —S—, —OC(O)—, —C(O)O—, —(CH2)nC(O)—, —(CH2)nC(O)C(O)—, —(CH2)nNR5C(O)C(O)—, —NR5(CH2)nC(O)C(O)—, optionally substituted (CH2)nC1-6 alkylene (CH2)n—, optionally substituted (CH2)nC(O)C1-6 alkylene (CH2)n—, optionally substituted (CH2)nNR5C1-6 alkylene (CH2)n—, optionally substituted (CH2)nC(O)NR5C1-6 alkylene (CH2)n—, optionally substituted (CH2)nNR5C(O)C1-6 alkylene (CH2)n—, optionally substituted (CH2)nC(O)OC1-6 alkylene (CH2)n—, optionally substituted (CH2)nOC(O)C1-6 alkylene (CH2)n—, optionally substituted (CH2)nOC1-6 alkylene (CH2)n—, optionally substituted (CH2)nNR5C1-6 alkylene (CH2)n-, optionally substituted (CH2)n—S—C1-6 alkylene (CH2)n—, and optionally substituted (CH2CH2O)n; wherein each alkylene is optionally substituted with 1 or 2 groups independently selected from the group consisting of halo, hydroxy, haloalkyl, haloalkoxy, alkyl, alkoxy, amino, carboxyl, cyano, nitro, NHFmoc;
each R5 is independently hydrogen, alkyl, arylalkyl,




?or and




RN is aryl, alkyl, or arylalkyl; X is O, S or NR8, R8 is hydrogen, hydroxy, OR9, NR10R11 alkyl, arylalkyl,




?wherein RN is aryl, alkyl, or arylalkyl; wherein R9, R10 and R11 are each independently hydrogen or alkyl; V1 and V2 are each independently




?W is




?Ring B is a 4-10 membered heterocycloalkyl, optionally substituted with 1-10 substituents, each of which is selected from the group consisting of hydrogen, hydroxy, halo, alkyl, alkoxy, cyano, haloalkyl, haloalkoxy, alkylthio, oxo, amino, alkylamino, dialkylamino, arylalkyl,




?wherein R12 is aryl, alkyl, or arylalkyl; R13 is hydrogen, hydroxy, OR16, NR17R18, alkyl, arylalkyl,




?RN is aryl, alkyl, or arylalkyl; R14 and R15 is each independently hydrogen, hydroxy, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, aryl, arylalkyl, or heteroaryl; Z is bond,




?R16 and R17 are each independently selected from the group consisting of hydrogen, hydroxy, halo, alkyl, alkoxy, cycloalkyl, cyano, alkylthio, amino, alkylamino, and dialkylamino; K is O, CHR18, CR18, N, or and NR18, wherein R18 is hydrogen or alkyl;
La, L1, L2, L3, L4, L5, L6, L7 and L8 are each independently a bond, —O—, —NR19—, —SO—, —SO2—, (CH2)n—,




?or a linking group selected from Table 1; Ring C is a 5-6 membered heteroaryl, optionally substituted with 1-4 substituents, each of which is independently selected from the group consisting of hydrogen, hydroxyl, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, cyano, alkylthio, amino, alkylamino, dialkylamino and Lb-J-Lc-D; wherein each R19, R20, and R21 is independently is selected from the group consisting of hydrogen, hydroxy, OR22, NR23R24, alkyl, arylalkyl,




?wherein RN is aryl, alkyl, or arylalkyl; wherein R22, R23, and R24 are each independently hydrogen or alkyl;
n is 0, 1, 2, 3, 4, 5 or 6; and
the Effector Domain has Formula (XIIa):




each ka, kb, kc, kd, ke, kf, kg, kh, and ki is independently 0 or 1;
each Xa, Xb, Xc, Xd, Xe, Xf, Xg, Xh, and Xi is independently a bond, —S—, —S—S—, —S(O)—, —S(O)2—, substituted or unsubstituted —(C1-C3) alkylene-, —(C2-C4) alkenylene-, —(C2-C4) alkynylene-, or




Ring E is phenyl or a 5-6 heteroaryl or heterocycloalkyl; wherein each w is independently 0, 1, or 2; each R1, R1a, R1b, R1c, R1d, R1e, R1f, R1g, R1h, R1i, and R4 is independently hydrogen, alkyl, arylalkyl or NR25, wherein R25 is hydrogen, hydroxy, OR26, NR27R28, alkyl, arylalkyl,




?wherein RN is aryl, alkyl, or arylalkyl; wherein R26, R27, and R28 are each independently hydrogen or alkyl; each R2, R3, R2a, R3a, R2b, R3b, R2c, R3c, R2d, R3d, R2e, R3e, R2f, R3f, R2g, R3g, R2h, R3h, R2i, and R3i is independently selected from the group consisting of hydrogen, halo, amino, cyano, nitro, haloalkyl, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted alkylamino, optionally substituted dialkylamino, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted arylalkyl, optionally substituted heteroarylalkyl and





US Pat. No. 11,066,415

COMPOSITIONS AND METHODS FOR REGULATING GLUCOSE HOMEOSTASIS AND INSULIN ACTION

UNIVERSITY OF VIRGINIA PA...


1. A method for regulating glucose homeostasis or treating type II diabetes, the method comprising administering to a subject in need thereof a pharmaceutical composition comprising a pharmaceutically acceptable carrier, optionally at least one additional therapeutic agent, and an effective amount of at least one compound having a structure of Formula I or Formula II:



wherein R1-R10 are all independently optional, and are each independently selected from the group consisting of H, halogen, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, and amino acid, wherein each group can be optionally substituted, or a pharmaceutically acceptable salt thereof, or




wherein R1-R2 are independently optional, and are each independently selected from the group consisting of H, halogen, hydroxy, acyl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclo, aryl, heteroaryl, alkoxy, amino, amide, thiol, sulfone, sulfoxide, oxo, oxy, nitro, carbonyl, carboxy, amino acid sidechain, and amino acid, wherein each group can be optionally substituted, or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,414

COT MODULATORS AND METHODS OF USE THEREOF

Gilead Sciences, Inc., F...


1. A method of treating an inflammatory disease in a subject in need thereof, comprising administering to the subject an effective amount of a compound of Formula I:



wherein
R1 is hydrogen, —O—R7, —N(R8)(R9), —C(O)—R7, —S(O)2—R7, —C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, heterocyclyl, aryl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, heterocyclyl, aryl, and heteroaryl may be optionally substituted with one to four Z1;

R2 is hydrogen, —C(O)—R7, —C(O)O—R7, —C(O)N(R7)2, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z2;

or R1 and R2 together with the nitrogen to which they are attached to form a heterocyclyl or heteroaryl, wherein each heterocyclyl or heteroaryl is optionally substituted with one to four Z2;
R3 is heterocyclyl or heteroaryl, wherein each heterocyclyl or heteroaryl is optionally substituted with one to four Z3;
R4 is heterocyclyl or heteroaryl, wherein each heterocyclyl or heteroaryl is optionally substituted with one to four Z4;
R5 is hydrogen, halo, —CN, —NO2, —O—R7, —N(R8)(R9), —S(O)—R7, —S(O)2R7, —S(O)2N(R7)2, —C(O)R7, —OC(O)—R7, —C(O)O—R7, —OC(O)O—R7, —OC(O)N(R10)(R11), —C(O)N(R7)2, —N(R7)C(O)(R7), C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-9 alkylthio, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-9 alkylthio, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z5;

R6 is hydrogen, —C(O)—R7, —C(O)O—R7, —C(O)N(R7)2, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z6;

each R7 is independently hydrogen, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, and heteroaryl may be optionally substituted with one to four Z7;

R8 and R9 at each occurrence are independently hydrogen, —S(O)2R10, —C(O)—R10, —C(O)O—R10, —C(O)N(R10)(R11), C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl;wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl may be optionally substituted with one to four Z8;

R10 and R11 at each occurrence are independently hydrogen, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl,wherein each C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, and heteroaryl optionally is substituted with one to four Z1b;

each Z1, Z2, Z3, Z4, Z5, Z6, Z7, and Z8 is independently hydrogen, oxo, halo, —NO2, —N3, —CN, thioxo, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O—R12, —C(O)—R12, —C(O)O—R12, —C(O)—N(R13)(R14), —N(R13)(R14), —N(R13)2(R14)+, —N(R12)C(O)—R12, —N(R12)C(O)O—R12, —N(R12)C(O)N(R13)(R14), —N(R12)S(O)2(R12), —NR12S(O)2N(R13)(R14), —NR12S(O)2O(R12), —OC(O)R12, —OC(O)—N(R13)(R14), —P(O)(OR12)2, —OP(O)(OR12)2, —CH2P(O)(OR12)2, —OCH2P(O)(OR12)2, —C(O)OCH2P(O)(OR12)2, —P(O)(R12)(OR12), —OP(O)(R12)(OR12), —CH2P(O)(R2)(OR12), —OCH2P(O)(R12)(OR12), —C(O)OCH2P(O)(R12)(OR12), —P(O)(N(R12)2)2, —OP(O)(N(R12)2)2, —CH2P(O)(N(R12)2)2, —OCH2P(O)(N(R2)2)2, —C(O))OCH2P(O)(N(R12)2)2, —P(O)(N(R12)2)(OR12), —OP(O)(N(R12)2)(OR12), —CH2P(O)(N(R12)2)(OR12), —OCH2P(O)(N(R12)2)(OR12), —C(O)OCH2P(O)(N(R12)2)(OR12), —P(O)(R12)(N(R12)2), —OP(O)(R12)(N(R12)2), —CH2P(O)(R12)(N(R12)2), —OCH2P(O)(R12)(N(R12)2), —C(O)OCH2P(O)(R12)(N(R12)2), —Si(R12)3, —S—R12, —S(O)R12, —S(O)(NH)R12, —S(O)2R12 or —S(O)2N(R13)(R14);wherein any alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z1a groups;

each Z1a is independently oxo, halo, thioxo, —NO2, —CN, —N3, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O—R12, —C(O)R12, —C(O)O—R12, —C(O)N(R13)(R14), —N(R13)(R14), —N(R13)2(R14)+, —N(R12)—C(O)R12, —N(R12)C(O)O(R12), —N(R12)C(O)N(R13)(R14), —N(R12)S(O)2(R12), —N(R12)S(O)2—N(R13)(R14), —N(R12)S(O)2O(R12), —OC(O)R12, —OC(O)OR12, —OC(O)—N(R13)(R14), —Si(R12)3, —S—R12, —S(O)R12, —S(O)(NH)R12, —S(O)2R12 or —S(O)2N(R13)(R14);wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z1b groups;

each R12 is independently hydrogen, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, aryl, heteroaryl or heterocyclyl,wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z1b groups;

R13 and R14 at each occurrence are each independently hydrogen, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, aryl, heteroaryl or heterocyclyl;wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with one to four Z1b groups, or R13 and R14 together with the nitrogen to which they are attached form a heterocyclyl, wherein said heterocyclyl is optionally substituted with one to four Z1b groups;

each R15 is independently halo, —CN, —NO2, —O—R7, —N(R8)(R9), —S(O)—R7, —S(O)2R7, —S(O)2N(R7)2, —C(O)R7, —OC(O)—R7, —C(O)O—R7, —OC(O)O—R7, —OC(O)N(R10)(R11), —C(O)N(R7)2, —N(R7)C(O)(R7), C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-9 alkylthio, C1-6 haloalkyl, C3-15 cycloalkyl, aryl, heterocyclyl, or heteroaryl; and
each Z1b is independently oxo, thioxo, hydroxy, halo, —NO2, —N3, —CN, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O(C1-9 alkyl), —O(C2-6 alkenyl), —O(C2-6 alkynyl), —O(C3-15 cycloalkyl), —O(C1-8 haloalkyl), —O(aryl), —O(heteroaryl), —O(heterocyclyl), —NH2, —NH(C1-9 alkyl), —NH(C2-6 alkenyl), —NH(C2-6 alkynyl), —NH(C3-15 cycloalkyl), —NH(C1-8 haloalkyl), —NH(aryl), —NH(heteroaryl), —NH(heterocyclyl), —N(C1-9 alkyl)2, —N(C2-6 alkenyl)2, —N(C2-6 alkynyl)2, —N(C3-15 cycloalkyl)2, —N(C1-8 haloalkyl)2, —N(aryl)2, —N(heteroaryl)2, —N(heterocyclyl)2, —N(C1-9 alkyl)(C2-6 alkenyl), —N(C1-9 alkyl)(C2-6 alkynyl), —N(C1-9 alkyl)(C3-15 cycloalkyl), —N(C1-9 alkyl)(C1-8 haloalkyl), —N(C1-9 alkyl)(aryl), —N(C1-9 alkyl)(heteroaryl), —N(C1-9 alkyl)(heterocyclyl), —C(O)(C1-9 alkyl), —C(O)(C2-6 alkenyl), —C(O)(C2-6 alkynyl), —C(O)(C3-15 cycloalkyl), —C(O)(C1-8 haloalkyl), —C(O)(aryl), —C(O)(heteroaryl), —C(O)(heterocyclyl), —C(O)O(C1-9 alkyl), —C(O)O(C2-6 alkenyl), —C(O)O(C2-6 alkynyl), —C(O)O(C3-15 cycloalkyl), —C(O)O(C1-8 haloalkyl), —C(O)O(aryl), —C(O)O(heteroaryl), —C(O)O(heterocyclyl), —C(O)NH2, —C(O)NH(C1-9 alkyl), —C(O)NH(C2-6 alkenyl), —C(O)NH(C2-6 alkynyl), —C(O)NH(C3-15 cycloalkyl), —C(O)NH(C1-8 haloalkyl), —C(O)NH(aryl), —C(O)NH(heteroaryl), —C(O)NH(heterocyclyl), —C(O)N(C1-9 alkyl)2, —C(O)N(C3-15 cycloalkyl)2, —C(O)N(C2-6 alkenyl)2, —C(O)N(C2-6 alkynyl)2, —C(O)N(C1-8 haloalkyl)2, —C(O)N(aryl)2, —C(O)N(heteroaryl)2, —C(O)N(heterocyclyl)2, —NHC(O)(C1-9 alkyl), —NHC(O)(C2-6 alkenyl), —NHC(O)(C2-6 alkynyl), —NHC(O)(C3-15 cycloalkyl), —NHC(O)(C1-8 haloalkyl), —NHC(O)(aryl), —NHC(O)(heteroaryl), —NHC(O)(heterocyclyl), —NHC(O)O(C1-9 alkyl), —NHC(O)O(C2-6 alkenyl), —NHC(O)O(C2-6 alkynyl), —NHC(O)O(C3-15 cycloalkyl), —NHC(O)O(C1-8 haloalkyl), —NHC(O)O(aryl), —NHC(O)O(heteroaryl), —NHC(O)O(heterocyclyl), —NHC(O)NH(C1-9 alkyl), —NHC(O)NH(C2-6 alkenyl), —NHC(O)NH(C2-6 alkynyl), —NHC(O)NH(C3-15 cycloalkyl), —NHC(O)NH(C1-8 haloalkyl), —NHC(O)NH(aryl), —NHC(O)NH(heteroaryl), —NHC(O)NH(heterocyclyl), —SH, —S(C1-9 alkyl), —S(C2-6 alkenyl), —S(C2-6 alkynyl), —S(C3-15 cycloalkyl), —S(C1-8 haloalkyl), —S(aryl), —S(heteroaryl), —S(heterocyclyl), —NHS(O)(C1-9 alkyl), —N(C1-9 alkyl)(S(O)(C1-9 alkyl), —S(O)N(C1-9 alkyl)2, —S(O)(C1-9 alkyl), —S(O)(NH)(C1-9 alkyl), —S(O)(C2-6 alkenyl), —S(O)(C2-6 alkynyl), —S(O)(C3-15 cycloalkyl), —S(O)(C1-8 haloalkyl), —S(O)(aryl), —S(O)(heteroaryl), —S(O)(heterocyclyl), —S(O)2(C1-9 alkyl), —S(O)2(C2-6 alkenyl), —S(O)2(C2-6 alkynyl), —S(O)2(C3-15 cycloalkyl), —S(O)2(C1-8 haloalkyl), —S(O)2(aryl), —S(O)2(heteroaryl), —S(O)2(heterocyclyl), —S(O)2NH(C1-9 alkyl), or —S(O)2N(C1-9 alkyl)2;wherein any alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl is optionally substituted with one to four halo, C1-9 alkyl, C1-8 haloalkyl, —OH, —NH2, —NH(C1-9 alkyl), —NH(C3-15 cycloalkyl), —NH(C1-8 haloalkyl), —NH(aryl), —NH(heteroaryl), —NH(heterocyclyl), —N(C1-9 alkyl)2, —N(C3-15 cycloalkyl)2, —NHC(O)(C3-15 cycloalkyl), —NHC(O)(C1-8 haloalkyl), —NHC(O)(aryl), —NHC(O)(heteroaryl), —NHC(O)(heterocyclyl), —NHC(O)O(C1-9 alkyl), —NHC(O)O(C2-6 alkynyl), —NHC(O)O(C3-15 cycloalkyl), —NHC(O)O(C1-8 haloalkyl), —NHC(O)O(aryl), —NHC(O)O(heteroaryl), —NHC(O)O(heterocyclyl), —NHC(O)NH(C1-9 alkyl), —S(O)(NH)(C1-9 alkyl), S(O)2(C1-9 alkyl), —S(O)2(C3-15 cycloalkyl), —S(O)2(C1-8 haloalkyl), —S(O)2(aryl), —S(O)2(heteroaryl), —S(O)2(heterocyclyl), —S(O)2NH(C1-9 alkyl), —S(O)2N(C1-9 alkyl)2, —O(C3-15 cycloalkyl), —O(C1-8 haloalkyl), —O(aryl), —O(heteroaryl), —O(heterocyclyl), or —O(C1-9 alkyl);

m is 0, 1, or 2;
or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof and a pharmaceutically acceptable carrier.

US Pat. No. 11,066,413

AMINOPYRIMIDINE FIVE-MEMBERED HETEROCYCLIC COMPOUND, AND INTERMEDIATE, PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF

GUANGZHOU MAXINOVEL PHARM...


1. An aminopyrimidine five-membered heterocyclic compound represented by formula I-1, a pharmaceutically acceptable salt, a tautomer, an enantiomer or a diastereomer or a prodrug thereof:



wherein, “” represents a single bond or a double bond;
when “” is a single bond, Z is N or CR5; R5 is H, D or C1-C20 alkyl;
when“” is double bond, Z is C;
X is O, CO or NR3;
Y is CO, CH2 or NR4;
R1 is selected from unsubstituted methyl, substituted or unsubstituted ethyl, substituted or unsubstituted n-propyl, substituted or unsubstituted isopropyl, substituted or unsubstituted n-butyl, substituted or unsubstituted isobutyl, substituted or unsubstituted tert-butyl, substituted or unsubstituted C6-C30 aryl or substituted or unsubstituted C2-C30 heteroaryl;
R2 is selected from substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted C6-C30 aryl or substituted or unsubstituted C2-C30 heteroaryl;
the C2-C30 heteroaryl in the substituted or unsubstituted C2-C30 heteroaryl refers to a C2-C30 heteroaryl comprising 1-4 heteroatoms which is selected from the group consisting of N, O or S;
the substituent in the substituted ethyl, the substituted n-propyl, the substituted isopropyl, the substituted n-butyl, the substituted isobutyl, the substituted tert-butyl of R1, the substituted C1-C20 alkyl group of R2, the substituted C6-C30 aryl or the substituted C2-C30 heteroaryl of R1 or R2 is selected from one or more of the group consisting of one or more halogens, C1-C20 alkyl, halogenated C1-C20 alkyl, oxo, hydroxyl, amino,





cyano, C1-C20 alkoxyl, halogenated C1-C20 alkoxyl and C1-C20 alkylthio; when the number of the substituent is more than one, the substituents are the same or different; wherein, each of Ra and Rb is independently H or C1-C20 alkyl; Rc is C1-C20 alkyl;R3 is C1-C20 alkyl or C3-C30 cycloalkyl;
R4 is H, C1-C20 alkyl or C3-C30 cycloalkyl;
m is 0, 1, 2 or 3;
n is 1, 2 or 3.

US Pat. No. 11,066,412

SUBSTITUTED PYRROLO[2,1-A]PHTHALAZINES AND BENZO[G]PYRROLO[2,1-A]PHTHALAZINES FOR THE TREATMENT OF CANCER

Academia Sinica, Taipei ...


1. A compound of formula (I):



or a pharmaceutically acceptable salt or stereoisomer thereof,

wherein:




wherein A is optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl, C(O)H, OH, O(alkyl), O(CH2)xN(Rb)2, OC(O)alkyl, O(aryl), and aryl;each R1 is independently alkyl, wherein each alkyl is optionally and independently substituted with one or more substituents independently selected from the group consisting of halo, OR, OC(O)CH3, OC(O)NHR, and OS(O)2R;
R2 is hydrogen, alkyl, cycloalkyl, aryl, or heteroaryl, wherein the aryl or heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of halo, CN, C1-6 alkyl, N(Rc)2, NO2, O(alkyl), —OCH2O—, —O(CH2)2O—, pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and 4-(piperido)piperidinyl;
R3 is NRARB or NHPhRc;
each R is independently hydrogen, alkyl, cycloalkyl, or aryl;
RA is hydrogen or C1-6 alkyl;
RB is hydrogen or C1-6 alkyl; or
RA and RB, taken together with the nitrogen atom to which they are attached, form pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-yl)piperidin-l-yl, or 4-(piperidin-4-yl) piperidin-l-yl, wherein the piperazin-l-yl or 4-(piperidin-4-yl)piperidin-l-yl is optionally substituted with one or more substituents independently selected from the group consisting of alkyl and (CH2)nC(O)NH(CH2)mNRARB;
Rc is hydrogen, halo, alkyl, alkenyl, alkynyl, NHC(O)Ra, NHC(O)ORa, O(alkyl), heterocyclyl, or aryl, wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of halo, alkyl, haloalkyl, alkenyl, C(O)H, OC(O)alkyl, O(aryl), and aryl, and further wherein the aryl is optionally substituted with one or more substituents independently selected from the group consisting of halo, CN, C1-6 alkyl, N(Rc)2, NO2, O(alkyl), —OCH2O—, —O(CH2)2O—, pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and 4-(piperido)piperidinyl;
Ra is C1-6 alkyl or aryl;
each Rb is independently C1-10alkyl, pyrrolidin-l-yl, piperidin-l-yl, piperazin-l-yl, morpholin-4-yl, 4-(piperidin-l-yl)piperidin-l-yl, or 4-(piperidin-4-yl)piperidin-l-yl;
each Rc is independently hydrogen or C1-10 alkyl;
m is 1, 2, 3, 4, or 5;
n is 1, 2, 3, 4, or 5; and
x is 1, 2, 3, 4, or 5.

US Pat. No. 11,066,411

[1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVE AS A2A RECEPTOR INHIBITOR

MEDSHINE DISCOVERY INC., ...


1. A compound represented by formula (I), or a pharmaceutically acceptable salt thereof,




whereinR1 is selected from the group consisting of H, CN, COOH, and





or is selected from the group consisting of C1-3 alkyl, C1-3 alkyl-O—C1-3 alkyl-, C1-3 alkyl-C(=O)NH-, and C3-6 cycloalkyl, each of which is optionally substituted by 1, 2 or 3 R;R2 is each independently selected from the group consisting of H, F, Cl, Br, I, OH, NH2, and CN, or is independently selected from the group consisting of C3-6 cycloalkyl, C1-6 alkyl, and C1-6 heteroalkyl, each of which is optionally substituted by 1, 2 or 3 R;
R3 is each independently selected from the group consisting of H, F, Cl, Br, I, OH, NH2, and CN, or is independently selected from the group consisting of C1-6 alkyl or C1-6 heteroalkyl, each of which is optionally substituted by 1, 2 or 3 R;
n is 0, 1, 2 or 3;
m is 0, 1, 2 or 3;
ring A is selected from the group consisting of 6- to 10-membered aryl, 5- to 10-membered heteroaryl, 5- to 10-membered heterocycloalkyl and 5- to 10-membered heterocycloalkenyl;
ring B is selected from the group consisting of phenyl and 5- to 6-membered heteroaryl;
R is selected from the group consisting of F, Cl, Br, I, OH, NH2, and CN, or is selected from the group consisting of C1-3 alkyl, C3-6 cycloalkyl, C3-6 cycloalkyl-NH—, 3- to 6-membered heterocycloalkyl, 3- to 6-membered heterocycloalkyl-O-, and phenyl, each of which is optionally substituted by 1, 2 or 3 R?;
R? is selected from the group consisting of F, Cl, Br, I, OH, NH2, Me, and





the heteroatom or the heteroatom group of the C1-6 heteroalkyl, 5- to 10-membered heteroaryl, 5- to 10-membered heterocycloalkyl, 3- to 6-membered heterocycloalkyl and 5- to 10-membered heterocycloalkenyl is each independently selected from the group consisting of N, O, S, NH, —C(?O)—, —C(?O)O- and —C(?O)NH—;the number of the heteroatom or the heteroatom group is each independently 1, 2, 3 or 4.

US Pat. No. 11,066,410

FUSED TRIAZOLO-PYRIMIDINE COMPOUNDS HAVING USEFUL PHARMACEUTICAL APPLICATION

3100 Central Expressway L...


1. A compound of Formula I or a pharmaceutically acceptable salt thereof:




whereinR1 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl, provided R1 is not cyclohexyl,
R2 is alkyl, aryl, heteroaryl, —N?CH-alkyl, —N?CH-aryl or —N?CH-heteroaryl, in which each of the alkyl, aryl and heteroaryl is optionally substituted,
R3 and R4 together with the nitrogen to which they are attached form a mono or bi-cyclic heterocyclyl or a bi-cyclic aryl, each of the mono, bi-cyclic heterocyclyl and bi-cyclic aryl is optionally substituted with one, two, three, or four groups selected from lower alkyl.

US Pat. No. 11,066,409

BICYCLIC NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME


1. A compound represented by Formula (I):



whereinZ1 is N;
Z2 is C(R5a)(R5a?)or N(R5b);
the dashed line represents the presence or absence of a bond;
when the dashed line represents the presence of a bond, then R5a? and R5b are absent;
R5a is a hydrogen atom, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkyloxy, substituted or unsubstituted alkenyloxy, substituted or unsubstituted alkynyloxy, substituted or unsubstituted alkylamino, substituted or unsubstituted alkenylamino, substituted or unsubstituted alkynylamino, substituted or unsubstituted aromatic carbocyclyl, or substituted or unsubstituted aromatic heterocyclyl;
R5a? is a hydrogen atom;
R5b is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl;
Ring Q is a substituted or unsubstituted 5-membered non-aromatic heterocycle or a substituted or unsubstituted 6-membered non-aromatic heterocycle;
Y1 is O;
R2a is a group represented by the formula: —(C(R2a?)(R2b?))n—R1;
R2b is a hydrogen atom, halogen, hydroxy, substituted or unsubstituted alkyl, or substituted or unsubstituted alkyloxy;
R2a? is each independently a hydrogen atom, halogen, hydroxy, substituted or unsubstituted alkyl, or substituted or unsubstituted alkyloxy;
R2b? is each independently a hydrogen atom, halogen, hydroxy, substituted or unsubstituted alkyl, or substituted or unsubstituted alkyloxy;
Ra? and R2b? which are attached to the same carbon atom may be taken together to form oxo;
R1 is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl;
X is N(R7a);
R7a is a hydrogen atom, substituted or unsubstituted alkyl, or substituted or unsubstituted alkylcarbonyl;
R2c is each independently a hydrogen atom, halogen, hydroxy, substituted or unsubstituted alkyl, or substituted or unsubstituted alkyloxy;
R2d is each independently a hydrogen atom, halogen, hydroxy, substituted or unsubstituted alkyl, or substituted or unsubstituted alkyloxy;
R2c and R2d which are attached to the same carbon atom may be taken together to form a substituted or unsubstituted non-aromatic carbocycle, or two of R2c may be taken together to form a substituted or unsubstituted non-aromatic carbocycle;
R3 is substituted or unsubstituted aromatic carbocyclyl, substituted or unsubstituted aromatic heterocyclyl, substituted or unsubstituted non-aromatic carbocyclyl, or substituted or unsubstituted non-aromatic heterocyclyl;
n is an integer from 0 to 4; and
m is an integer from 0 to 4,

or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,407

PREPARATION OF CERTAIN SUBSTITUTED 1H-PYRIDO[3',4':4,5]PYRROLO[1,2,3-DE]QUINOXALINES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

INTRA-CELLULAR THERAPIES,...


1. A method for preparing a compound of Formula 2F:




or a pharmaceutically acceptable salt thereof,
wherein:k is 1;
m is 1;
n is 1;
B is benzyl, triphenylmethyl, or toluenesulfonyl; or
B is a moiety of the formula:




wherein:P is —C(O)—, —C(O)O—, or —S(O)2—;
Z is C1-6alkyl, C1-6alkylaryl, OR, or aryl; and
R is C1-6alkyl, aryl, arylC1-6 alkyl, or heteroarylC1-6alkyl;

R5 is H;
R7, R8, and R9 are independently H;
—X—Y— is —(R?)N—CH2— or —(R?)N—C(O)—; and
R? is H or CH3;

comprising the steps of:A) reacting a compound of Formula 2E:





wherein:k is 1;
m is 1;
n is 1;
A is F, Cl, Br, or I;
B is benzyl, triphenylmethyl, or toluenesulfonyl; or
B is a moiety of the formula:







wherein:P is —C(O)—, —C(O)O—, or —S(O)2—;
Z is C1-6alkyl, C1-6alkylaryl, OR, or aryl; and
R is C1-6 alkyl, aryl, arylC1-6alkyl, or heteroarylC1-6alkyl;

R5 is H;
R7, R8, and R9 are independently H;
—X—Y— is —(R?)N—CH2— or —(R?)N—C(O)—; and
R? is H or CH3;

with:
(a) a transition metal catalyst selected from the group consisting of palladium, copper, nickel, platinum, ruthenium, and rhodium;
(b) a base; and optionally
(c) a monodentate or bidentate ligand selected from the group consisting of N,N-dimethylformamide, dimethylsulfoxide, 1-methyl-2-pyrrolidinone, an aryl alcohol, a 1,2-diamine, 2-(dimethylamino)glycine, (methylimino)diacetic acid, 8-aminoquinoline, a 1,2-aminoalcohol, an imidazolium carbene, 4-(dimethylamino)pyridine, 2-(aminomethyl)pyridine, 1,8-diazabicyclo[5.4.0]undec-7-ene, 4,7-diphenyl-1,10-phenanthroline, 4,7-dimethyl-1,10-phenanthroline, 5-methyl-1,10-phenanthroline, 5-chloro-1,10-phenanthroline, and 5-nitro-1,10-phenanthroline;
to give the compound of Formula 2F above; and
B) optionally reacting the compound of Formula 2F with an acid, to give a pharmaceutically acceptable salt of the compound of Formula 2F.

US Pat. No. 11,066,406

SMALL MOLECULE INHIBITORS OF THE JAK FAMILY OF KINASES

Janssen Pharmaceutica NV,...


1. A compound of formula




US Pat. No. 11,066,405

BICYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER

TEMPEST THERAPEUTICS, INC...


1. A compound of Formula Ib:



or a pharmaceutically acceptable salt, solvate, solvate of the salt, hydrate, a single stereoisomer, a mixture of stereoisomers, or a racemic mixture of stereoisomers thereof, wherein:
Ar is an aryl or a heteroaryl, wherein said aryl and said heteroaryl are each optionally substituted with 1 to 3 substituents independently selected from C1-C6 alkyl, C3-C7 cycloalkyl, heterocycle, aryl, heteroaryl, halogen, CN, ORb, SF5, and C1-C6 haloalkyl;
W is selected from C(?O)OR5, C(?O)NHOH, S(?O)2NHRb, S(?O)2NHC(?O)Rb, NHC(?O)NHSO2Rb, 1H-tetrazole, and C(?O)NHS(?O)2Rb;
X1, X2, X3, X4, and X5 are each independently N or CRa, wherein not more than 2 of X1, X2, X3, X4, and X5 are N;
R4 is selected from H, C1-C6 alkyl, halogen and C1-C6 haloalkyl;
R5 is selected from H and C1-C6 alkyl;
each Ra is independently selected from H, C1-C6 alkyl, halogen, ORb, CN, C3-C6 cycloalkyl, and C1-C6 haloalkyl;
Rb is selected from H, C1-C6 alkyl, C3-C6 cycloalkyl, and C1-C6 haloalkyl; and
n is 1, 2 or 3.

US Pat. No. 11,066,404

DIHYDROPYRIDO[2,3-D]PYRIMIDINONE COMPOUNDS AS CDK2 INHIBITORS

Incyte Corporation, Wilm...


1. A compound of Formula (I):




or a pharmaceutically acceptable salt thereof, wherein:R1 is selected from H, C1-6 alkyl, and C1-6 haloalkyl;
R2 is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, 5-10 membered heteroaryl-C1-4 alkyl, C(?O)Rb, C(?O)NRcRd, C(?O)ORa, C(?NRe)Rb, C(?NRe)NRcRd, S(?O)Rb, S(?O)NRcRd, NRcS(?O)2Rb, NRcS(?O)2NRcRd, S(?O)2Rb, and S(?O)2NRcRd, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R2A substituents;
each Ra, Rc, and Rd is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R2A substituents;
each Rb is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, each of which are optionally substituted with 1, 2, 3, or 4 independently selected R2A substituents;
each Re is independently selected from H, CN, OH, C1-4 alkyl, and C1-4 alkoxy;
each Rf is independently selected from H, C1-4 alkyl, and C1-4 haloalkyl;
R3 is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, each of which is optionally substituted with 1, 2, 3, or 4 independently selected R3A substituents;
R4, R5, R6, and R7 have the definitions in Group (a) or (b):
Group (a):
R4 and R5 are independently selected from halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
or, alternatively, R4 and R5, together with the carbon atom to which they are attached, form a 3, 4, 5, 6, or 7 membered cycloalkyl ring or a 3, 4, 5, 6, or 7 membered heterocycloalkyl ring, each of which is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
R6 and R7 are independently selected from H, D, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
or, alternatively, R6 and R7, together with the carbon atom to which they are attached, form a 3, 4, 5, 6, or 7 membered cycloalkyl ring or a 3, 4, 5, 6, or 7 membered heterocycloalkyl ring, each of which is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
Group (b):
R4 and R5 are independently selected from H, halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
or, alternatively, R4 and R5, together with the carbon atom to which they are attached, form a 3, 4, 5, 6, or 7 membered cycloalkyl ring or a 3, 4, 5, 6, or 7 membered heterocycloalkyl ring, each of which is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
R6 and R7 are independently selected from halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, and C3-6 cycloalkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
or, alternatively, R6 and R7, together with the carbon atom to which they are attached, form a 3, 4, 5, 6, or 7 membered cycloalkyl ring or a 3, 4, 5, 6, or 7 membered heterocycloalkyl ring, each of which is optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
each R2A is independently selected from H, D, halo, CN, NO2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, 5-10 membered heteroaryl-C1-4 alkyl, ORa1, SRa1, C(?O)Rb1, C(?O)NRc1Rd1, C(?O)ORa1, OC(?O)Rb1, OC(?O)NRc1Rd1, NRc1Rd1, NRc1C(?O)Rb1, NRc1C(?O)ORb1, NRc1C(?O)NRc1Rd1, C(?NRe)Rb1, C(?NRe)NRc1Rd1, NRc1C(?NRe) NRc1Rd1, NHORa1, NRc1S(?O)Rb1, NRc1S(?O)NRc1Rd1, S(?O)Rb1, S(?O)NRc1Rd1, NRc1S(?O)2Rb1, NRc1S(?O)2NRc1Rd1, S(?O)2Rb1, S(?O)(?NRf)Rb1, and S(?O)2NRc1Rd1, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R2B substituents;
each Ra1, Rc1, and Rd1 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R2B substituents;
each Rb1 is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, each of which are optionally substituted with 1, 2, 3, or 4 independently selected R2B substituents;
each R3A is independently selected from H, D, halo, CN, NO2, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, 5-10 membered heteroaryl-C1-4 alkyl, ORa2, SRa2, C(?O)Rb2, C(?O)NRc2Rd2, C(?O)ORa2, OC(?O)Rb2, OC(?O)NRc2Rd2,NRc2Rd2, NRc2C(?O)Rb2, NRc2C(?O)ORb2, NRc2C(?O)NRc2Rd2, C(?NRe)Rb2, C(?NRe)NRc2Rd2, NRc2C(?NRe)NRc2Rd2, NHORa2, NRc2 S(?O)Rb2, NRc2S(?O)NRc2Rd2, S(?O)Rb2, S(?O)NRc2Rd2, NRc2S(?O)2Rb2, NRc2S(?O)2NRc2Rd2, S(?O)2Rb2, S(?O)(?NRf)Rb2, and S(?O)2NRc2Rd2, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R3B substituents;
each Ra2, Rc2, and Rd2 is independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10 cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected R3B substituents;
each Rb2 is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-10cycloalkyl, C6-10 aryl, 4-10 membered heterocycloalkyl, 5-10 membered heteroaryl, C3-10 cycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl, 4-10 membered heterocycloalkyl-C1-4 alkyl, and 5-10 membered heteroaryl-C1-4 alkyl, each of which are optionally substituted with 1, 2, 3, or 4 independently selected R3B substituents;
each R2B and R3B is independently selected from H, D, halo, CN, NO2, C3-7 cycloalkyl, phenyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-7 cycloalkyl-C1-4 alkyl, phenyl-C1-4 alkyl, 4-7 membered heterocycloalkyl-C1-4 alkyl, 5-6 membered heteroaryl-C1-4 alkyl, ORa23, SRa23, C(?O)Rb23, C(?O)NRc23Rd23, C(?O)ORa23, OC(?O)Rb23, OC(?O)NRc23Rd23, NRc23Rd23, NRc23C(?O)Rb23, NRc23C(?O)ORb23, NRc23C(?O)NRc23Rd23, C(?NRe)Rb23, C(?NRe)NRc23Rd23, NRc23C(?NRe)NRc23Rd23, NHORa23, NRc23S(?O)Rb23, NRc23S(?O)NRc23Rd23, S(?O)Rb23, S(?O)NRc23Rd23, NRc23S(?O)2Rb23, NRc23S(?O)2NRc23Rd23, S(?O)2Rb23, S(?O)(?NRf)Rb23, and S(?O)2NRc23Rd23, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, phenyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-7 cycloalkyl-C1-4 alkyl, phenyl-C1-4 alkyl, 4-7 membered heterocycloalkyl-C1-4 alkyl, and 5-6 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
each Ra23, Rc23, and Rd23 is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, phenyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-7 cycloalkyl-C1-4 alkyl, phenyl-C1-4 alkyl, 4-7 membered heterocycloalkyl-C1-4 alkyl, and 5-6 membered heteroaryl-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, phenyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-7 cycloalkyl-C1-4 alkyl, phenyl-C1-4 alkyl, 4-7 membered heterocycloalkyl-C1-4 alkyl, and 5-6 membered heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, or 4 independently selected RG substituents;
each Rb23 is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C3-7 cycloalkyl, phenyl, 4-7 membered heterocycloalkyl, 5-6 membered heteroaryl, C3-7 cycloalkyl-C1-4 alkyl, phenyl-C1-4 alkyl, 4-7 membered heterocycloalkyl-C1-4 alkyl, and 5-6 membered heteroaryl-C1-4 alkyl, each of which are optionally substituted with 1, 2, 3, or 4 independently selected RG substituents; and
each RG is independently selected from OH, NO2, CN, halo, C1-3 alkyl, C2-3 alkenyl, C2-3 alkynyl, C1-3 haloalkyl, cyano-C1-3 alkyl, HO—C1-3 alkyl, C1-3 alkoxy-C1-3 alkyl, C1-3 alkoxy, C1-3 haloalkoxy, amino, C1-3 alkylamino, di(C1-3 alkyl)amino, thio, C1-3 alkylthio, C1-3 alkylsulfinyl, C1-3 alkylsulfonyl, carbamyl, C1-3 alkylcarbamyl, di(C1-3 alkyl)carbamyl, carboxy, C1-3 alkylcarbonyl, C1-3 alkoxycarbonyl, C1-3 alkylcarbonyloxy, C1-3 alkylcarbonylamino, C1-3 alkoxycarbonylamino, C1-3 alkylaminocarbonyloxy, C1-3 alkylsulfonylamino, aminosulfonyl, C1-3 alkylaminosulfonyl, di(C1-3 alkyl)aminosulfonyl, aminosulfonylamino, C1-3 alkylaminosulfonylamino, di(C1-3 alkyl)aminosulfonylamino, aminocarbonylamino, C1-3 alkylaminocarbonylamino, and di(C1-3 alkyl)aminocarbonylamino;
wherein “heterocycloalkyl” refers to monocyclic heterocycles or polycyclic heterocycles having 2, 3, or 4 fused, spirocyclic, or bridged rings, wherein at least one of the rings of the polycyclic heterocycle is a non-aromatic ring (saturated or partially unsaturated ring), wherein 1, 2, 3, or 4 of the ring-forming carbon atoms of the monocyclic heterocycle or polycyclic heterocycle is replaced by a heteroatom independently selected from N, O, S, and B; wherein the heterocycloalkyl group can contain one or more aromatic rings fused to (having a bond in common with) the non-aromatic heterocyclic ring; wherein the ring-forming carbon atoms and heteroatoms of the heterocycloalkyl group can be optionally substituted by one or more oxo or sulfido (C(O), S(O), C(S), or S(O)2); and wherein the heterocycloalkyl group can have one or more oxidized ring members; and
wherein “heteroaryl” refers to monocyclic aromatic heterocycles or polycyclic aromatic heterocycles having 2, 3, or 4 fused rings, wherein the monocyclic aromatic heterocycle or polycyclic aromatic heterocycle has 1, 2, 3, or 4 heteroatom ring members independently selected from N, O, S and B, and wherein any ring-forming N in a heteroaryl moiety can be an N-oxide.

US Pat. No. 11,066,403

SOLID FORM OF AZETIDINE DERIVATIVE AND PREPARATION METHOD THEREFOR AND USE THEREOF

SICHUAN KELUN-BIOTECH BIO...


19. A crystalline form of the compound of Formula (I), which is crystalline form B of the compound of Formula (I):



the XRPD spectrum of the crystalline form B comprises peaks at diffraction angles (2?) of about 6.4±0.2, 7.9±0.2, 8.4±0.2, 11.8±0.2, 12.7±0.2, 15.5±0.2, 16.0±0.2, 16.3±0.2, 16.9±0.2, 19.1±0.2 degrees.

US Pat. No. 11,066,402

3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5-DISUBSTITUTED-3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF C-MET PROTEIN KINASES

Rhizen Pharmaceuticals SA...


1. A compound of formula (IA-I)




or a tautomer, stereoisomer, enantiomer, diastereomer, a pharmaceutically acceptable salt, or N-oxide thereof; whereinX is CR1 or N;
D is monocyclic aryl; wherein D is substituted with a group E which is selected from —CONH—O—(CRxRy)p—ORx, and —CONH—O—(CRxRy)p-[cycloalkyl]-(CRxRy)p—ORx; and further D can optionally be substituted with one or more of Rz;
L2 is —(CRaRb)—;
Cy2 is substituted or unsubstituted heteroaryl;
each occurrence of R1 and R2 may be same or different and is independently selected from hydrogen, nitro, hydroxy, cyano, halogen, —ORa, —S(?O)q—Ra, —NRaRb, —C(?Y)—Ra, —CRaRb—C(?Y)—Ra, —CRaRb—Y—CRaRbRb, —C(?Y)—NRaRb, —NRaRb—C(?Y)—NRaRb, —S(?O)q—NRaRb—, —NRaRb—S(?O)q—NRaRb, —NRaRb—NRaRb, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl;
each occurrence of Y is independently selected from O, S, and NRa;
each occurrence of Ra and Rb may be same or different and are independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl, or when two Ra and/or Rb substituents are directly bound to a common atom, they may be joined to form a substituted or unsubstituted, saturated or unsaturated 3-10 member ring, which may optionally include one or more heteroatoms which may be same or different and are selected from O, NRc or S;
each occurrence of Rc is independently selected from hydrogen, nitro, hydroxy, cyano, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted C3-6 cycloalkyl, substituted or unsubstituted C3-6 cycloalkylalkyl, and substituted or unsubstituted C3-6 cycloalkenyl;
each occurrence of Rx and Ry is independently selected from hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (?O), thio (?S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocycyl, substituted or unsubstituted heterocyclylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, —COORz, —C(O)Rz, —C(S)Rz, —C(O)NRzRz, —C(O)ONRzRz, —NRzRz, —NRzCONRzRz, —N(Rz)SORz, —N(Rz)SO2Rz, —(?N—N(Rz)Rz), —NRzC(O)ORz, —NRzC(O)Rz—, —NRxC(S)Ry—NRzC(S)NRzRz, —SONRzRz—, —SO2NRzRz—, —ORz, —ORzC(O)NRzRz, —ORzC(O)ORz—, —OC(O)Rz, —OC(O)NRzRz, —RzNRzC(O)Rz, —RzORz, —RzC(O)ORz, —RzC(O)NRzRz, —RzC(O)Rz, —RzOC(O)Rz, —SRz, —SORz, —SO2Rz, and —ONO2, or any two of Rx and Ry which are directly bound to a common atom may be joined to form (i) a substituted or unsubstituted, saturated or unsaturated 3-14 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NRz or S, or (ii) an oxo (?O), thio (?S) or imino (?NRz); wherein
each occurrence of Rz is independently hydrogen, hydroxy, halogen, carboxyl, cyano, nitro, oxo (?O), thio (?S), substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted cycloalkenylalkyl, substituted or unsubstituted heterocycyl, substituted or unsubstituted heterocyclcyalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, and —ONO2, or any two of Rz which are directly bound to a common atom may be joined to form (i) a substituted or unsubstituted, saturated or unsaturated 3-14 membered ring, which may optionally include one or more heteroatoms which may be the same or different and are selected from O, NR? (where R? is H or alkyl) or S, or (ii) an oxo (?O), thio (?S) or imino (?NRz);
each occurrence of p independently represents 1, 2, 3, 4, 5, 6, 7 or 8; and
each occurrence of q independently represents 0, 1 or 2,

with the proviso that when Cy2 is substituted or unsubstituted heteroaryl, each occurrence of R1 and R2 is hydrogen, and E is —CONH—O—(CRxRy)p—ORx, then p is not 2.

US Pat. No. 11,066,401

PYRIMIDINE COMPOUND, CHLORIDE SALT THEREOF, AND MANUFACTURING AND APPLICATION OF SAME

Shenzhen Haiban Pharmaceu...


1. A hydrochloride salt of a compound shown in Formula (I), wherein the structure of the hydrochloride salt is shown in Formula (II):




US Pat. No. 11,066,400

COMPOUNDS FOR THE TREATMENT OF CANCER

Hoffmann-La Roche Inc., ...


1. A method for treating cancer comprising administering to a subject in need thereof an effective amount of a FoxM1 gene splicing modifier, wherein the FoxM1 gene splicing modifier is a compound of formula (IV), (V) or (VIII):



wherein X is —O— or —N(CH3)—; R? is cyano, pyrazolyl optionally substituted with methyl, or pyridinyl substituted with methyl and hydroxy; R? is hydrogen, methyl or methoxy; R?? is pyrazolyl optionally substituted with methyl, or pyridinyl substituted with methyl and hydroxy; Ru is hydrogen, chloro or fluoro; and Rv is hydrogen, chloro or fluoro;
or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,399

FERROPORTIN INHIBITORS

Vifor (International) AG,...


1. A pharmaceutical composition comprising a compound having the formula



or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,397

PROTEASOME INHIBITORS AND USES THEREOF

CORNELL UNIVERSITY, Itha...


1. A compound of Formula (I):




whereinR is H or C1-6 alkyl;
R1 is selected from the group consisting of monocyclic and bicyclic aryl, biphenyl, monocyclic and bicyclic heteroaryl, wherein monocyclic and bicyclic aryl, biphenyl, monocyclic and bicyclic heteroaryl can be optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, —OH, aryl, heteroaryl, non-aromatic heterocycle, and non-aromatic heterocycle substituted with ?O;
R2 is independently selected at each occurrence thereof from the group consisting of C1-2 alkyl, alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, monocyclic and bicyclic heterocyclyl, and —(CH2)mC(O)NHR4, wherein alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, monocyclic and bicyclic heterocyclyl can be optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, —OH, —NO2, —CF3, —OC1-6 alkyl, alkyl, alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, and monocyclic and bicyclic heterocyclyl;
R3 is selected from the group consisting of H, —SOpR5, —C(O)(CH2)kAr, —SO2Ar, —SO2C3-8 cycloalkyl, —C(O)(CH2)kHet, and —C(O)C1-6 alkyl, wherein aryl (Ar) and heteroaryl (Het) can be optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from halogen or C1-6 alkyl;
R4 is selected from the group consisting of H, C1-6 alkyl, and C3-8 cycloalkyl, wherein C3-8 cycloalkyl can be optionally substituted with —CF3;
R5 is selected from the group consisting of alkyl, alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, and monocyclic and bicyclic heterocyclyl, wherein alkyl, alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, and monocyclic and bicyclic heterocyclyl can be optionally substituted from 1 to 3 times with a substituent selected independently at each occurrence thereof from the group consisting of halogen, cyano, —OH, —NO2, —CF3, —OC1-6 alkyl, alkyl, alkenyl, monocyclic and bicyclic aryl, monocyclic and bicyclic heteroaryl, and monocyclic and bicyclic heterocyclyl;
k is 0 or 2;
m is 1 or 2;
n is 1, 2, or 3; and
p is 1 or 2;

or an oxide thereof, a pharmaceutically acceptable salt thereof, a solvate thereof, or a prodrug thereof.

US Pat. No. 11,066,396

3-ARYL- HETEROARYL SUBSTITUTED 5-TRIFLUOROMETHYL OXADIAZOLES AS HISTONEDEACETYLASE 6 (HDAC6) INHIBITORS


1. A compound of formula (I):



or a pharmaceutically acceptable salt thereof wherein;
X represents phenyl, wherein said phenyl is optionally substituted with one or two fluoro;
Z is —N;
R1 and R2 can combine together with the nitrogen atom to which they are attached to form a six membered monocyclic, heterocyclic non-aromatic ring optionally interrupted by 1 heteroatoms O, wherein said heterocyclic ring is optionally substituted with 1 to 2 groups of Ra;
Ra is selected from the group consisting of H, phenyl and ?O, wherein said phenyl is optionally substituted with 1 group Rb;
Rb is halo,
n represents 0.

US Pat. No. 11,066,395

DIMETHYLAMINOETHANOL SALT OF A GLP-1 RECEPTOR MODULATOR

RECEPTOS LLC, New York, ...


1. A compound having the following structure:




US Pat. No. 11,066,394

SOLID FORMS OF AN HPK1 INHIBITOR

Incyte Corporation, Wilm...


1. A solid form of Compound 1 having the formula:



wherein the solid form has crystalline Form I, and wherein the solid form has at least one characteristic X-ray powder diffraction (“XRPD”) peak selected from about 6.7, about 9.9, about 13.4, about 14.1, about 15.5, about 18.3, about 19.9, and about 20.4 degrees 2-theta.

US Pat. No. 11,066,393

INDOLIN-2-ONE DERIVATIVES

Hoffmann-La Roche Inc., ...


1. A method for the treatment of CNS diseases related to positive and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, inflammatory retinal diseases, balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy, which method comprises administering an effective amount of a compound of formula (I)




whereinA is phenyl or a five or six membered heteroaryl group, containing one or two N atoms, selected from





or the amide group —C(O)—NR1R2 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from



R1 and R2 are independently selected from hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, —(CH2)2-lower alkoxy, oxetanyl, cycloalkyl, or CH2-cycloalkyl, which cycloalkyl rings are optionally substituted by halogen;or R1 and R2 may form together with the N atom to which they are attached the group






andR3 is hydrogen or lower alkyl;
or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,392

INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE

Bristol-Myers Squibb Comp...


1. A compound of formula I or formula II or formula III



whereinX is CH, CR4, or N;
R1 is C1-6alkyl, C0-6alk-O—C1-6alkyl, C0-6alk-O—C1-6alk-O—C1-6alkyl, C0-6alk-CN, or C0-6alk-heterocycloalkyl;
R2 is H, —NH2; —NH(C1-6alkyl); —N(C1-6alkyl)(C1-6alkyl), C1-6alkyl, d1-d13-C1-6alkyl, C1-6alkoxy, d1-d13-C1-6alkoxy, OH, halo, heterocycloalkyl, or heteroaryl;
R3 is pyridyl; pyrimidinyl; quinolinyl; or naphthyridinyl, wherein the pyridyl, pyrimidinyl, quinolinyl, or naphthyridinyl is optionally substituted on any atom with 1, 2 or 3 R substituents that are independently C1-6alkyl, d1-d13-C1-6alkyl, haloC1-6alkyl, haloC1-6alkoxy, C1-6alkoxy, d1-d13-C1-6alkoxy, OH, or halo;
R4 is NH2; —NH(C1-6alkyl); —N(C1-6alkyl)(C1-6alkyl), C1-6alkyl; C1-6alkoxy, OH, halo, heterocycloalkyl, or heteroaryl;
or a stereoisomer thereof or a tautomer thereof;
or a pharmaceutically acceptable salt thereof.


US Pat. No. 11,066,391

ATORVASTATIN DERIVED HMG-COA REDUCTASE DEGRADATION INDUCING COMPOUND

UPPTHERA, Incheon (KR)


1. A compound represented by the following Formula I:ULM-Linker-PTM,??[Formula I]
wherein:
ULM is CRBN or VHL E3 ubiquitin ligase binding moiety,
PTM is




Linker is a group that chemically links ULM and PTM,
wherein the compound is selected from the group consisting of:














or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,388

INDAZOLE-3-CARBOXAMIDES AND THEIR USE AS WNT/B-CATENIN SIGNALING PATHWAY INHIBITORS

BioSplice Therapeutics, I...


1. A method of treating cancer in a subject, the method comprising administering to the subject a therapeutically effective amount of a compound of Formula Ia, or a pharmaceutically acceptable salt thereof:



wherein:
R3 is selected from the group consisting of 3-pyridylR6, 5-pyrimidinylR6, and 4-pyridazinylR6;
R5 is selected from the group consisting of -heteroarylR7;
R6 is a substituent selected from the group consisting of -(C1-2 alkyl)heterocyclylR8 and -heterocyclylR8;
R7 is 1-2 substituents each independently selected from the group consisting of H, C1-3alkyl, halide, —NH2, —OCF3, —CF3, —CN, —OR10, -(C1-2 alkyl)heterocyclylR9, -heterocyclylR9, and —SO2R11;
R8 is 1-2 substituents each independently selected from the group consisting of H, C1-3alkyl, halide, and —OR12;
each R9 is 1-2 substituents each independently selected from the group consisting of H, C1-3alkyl, halide, amino, —OCF3, —CF3, —CN, and —OR12;
R10 is selected from the group consisting of H and C1-3alkyl;
R11 is C1-3alkyl; and
each R12 is independently selected from the group consisting of H and C1-3alkyl.

US Pat. No. 11,066,386

CGRP RECEPTOR ANTAGONISTS

Eli Lilly and Company, I...


1. A compound of the formula:




or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,384

CRYSTALLINE FORMS OF ARN-509, PREPARATION METHOD AND USE THEREOF

Crystal Pharmaceutical (S...


1. A crystalline form CS8 of ARN-509,



wherein the X-ray powder diffraction pattern shows characteristic peaks at 2theta values of 7.9±0.2°, 12.4±0.2°, and 19.0±0.2° using CuK? radiation.

US Pat. No. 11,066,383

INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE

Bristol-Myers Squibb Comp...


1. A compound of formula I or formula II



whereinX is N;
T is CH;
R1 is H, halo, or C1-C6haloalkyl;
R1A is H, halo, or C1-C6haloalkyl;
Y is N;
n is 0, 1, 2, 3, or 4;
W is CR4 wherein R4 is H or (C1-C6alkyl);
V is C1-C6alkylene optionally substituted with one, two, or three substituents independently selected from C1-C6alkyl and C3-C6cycloalkyl;
R2 is H or C1-C6alkyl;
Z is a bond or C1-C6alkylene optionally substituted with one, two, or three substituents independently selected from C1-C6alkyl and C3-C6cycloalkyl;B is aryl optionally substituted with 1, 2, or 3 R substituents independently selected from —OH, C1-C6alkyl, C1-C6haloalkyl, halo, —OC1-C6alkyl, —OC1-C6haloalkyl, —CN, aryl, or —Oaryl; or C3-C12cycloalkyl optionally substituted with 1, 2, or 3 R substituents independently selected from —OH, C1-C6alkyl, C1-C6haloalkyl, halo, —OC1-C6alkyl, —OC1-C6haloalkyl, —CN, aryl, or —Oaryl;



or a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a tautomer thereof, or a solvate thereof.

US Pat. No. 11,066,382

ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING SAME

SOLUS ADVANCED MATERIALS ...


1. A compound of the following Chemical Formula 3, 4, or 5:



wherein, in Formulae 3 to 5,
R1 to R6 and R8 are each independently selected from the group consisting of hydrogen, deuterium, halogen, a cyano group, a nitro group, a C1˜C40 alkyl group, a C2˜C40 alkenyl group, a C2˜C40 alkynyl group, a C3˜C40 cycloalkyl group, a heterocycloalkyl group having 3 to 40 nuclear atoms, a C6˜C60 aryl group, a heteroaryl group having 5 to 60 nuclear atoms, a C1˜C40 alkyloxy group, a C6˜C60 aryloxy group, a C3˜C40 alkylsilyl group, a C6˜C60 arylsilyl group, a C1˜C40 alkylboron group, a C6˜C60 arylboron group, a C6˜C60 arylphosphanyl group, a C6˜C60 mono or diarylphosphynyl group and a C6˜C60 arylamine group, or bond to adjacent groups to form a fused ring;
the R1 to R6 and R8 alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, aryloxy group, alkyloxy group, cycloalkyl group, heterocycloalkyl group, arylamine group, alkylsilyl group, alkylboron group, arylboron group, arylphosphanyl group, mono or diarylphosphynyl group and arylsilyl group are each independently unsubstituted or substituted with one or more types of substituents selected from the group consisting of deuterium, halogen, a cyano group, a nitro group, a C1˜C40 alkyl group, a C2˜C40 alkenyl group, a C2˜C40 alkynyl group, a C6˜C60 aryl group, a heteroaryl group having 5 to 60 nuclear atoms, a C6˜C60 aryloxy group, a C1˜C40 alkyloxy group, a C6˜C60 arylamine group, a C3˜C40 cycloalkyl group, a heterocycloalkyl group having 3 to 40 nuclear atoms, a C1˜C40 alkylsilyl group, a C1˜C40 alkylboron group, a C6˜C60 arylboron group, a C6˜C60 arylphosphanyl group, a C6˜C60 mono or diarylphosphynyl group and a C6˜C60 arylsilyl group, and when substituted with a plurality of substituents, these are the same as or different from each other;
Y1 to Y12 are each independently C(H) or C(R9), and at least one of them is C(R9);
R9 is a substituent of the following Chemical Formula 6:




in Chemical Formula 6,
* means a part where a bond is formed;
L1 and L2 are each independently selected from the group consisting of a direct bond, a C6˜C18 arylene group and a heteroarylene group having 5 to 18 nuclear atoms;
R10 is selected from the group consisting of halogen, a cyano group, a nitro group, a C6˜C40 alkyl group, a C2˜C40 alkenyl group, a C2˜C40 alkynyl group, a C3˜C40 cycloalkyl group, a heterocycloalkyl group having 3 to 40 nuclear atoms, a C6˜C60 aryl group, a heteroaryl group having 5 to 60 nuclear atoms, a C1˜C40 alkyloxy group, a C6˜C60 aryloxy group, a C3˜C40 alkylsilyl group, a C6˜C60 arylsilyl group, a C1˜C40 alkylboron group, a C6˜C60 arylboron group, a C6˜C60 arylphosphanyl group, a C6˜C60 mono or diarylphosphynyl group and a C6˜C60 arylamine group, or bonds to adjacent groups to form a fused ring; and
the L1 and L2 arylene group and heteroarylene group, and the R10 alkyl group, alkenyl group, alkynyl group, aryl group, heteroaryl group, aryloxy group, alkyloxy group, cycloalkyl group, heterocycloalkyl group, arylamine group, alkylsilyl group, alkylboron group, arylboron group, arylphosphanyl group, mono or diarylphosphynyl group and arylsilyl group are each independently unsubstituted or substituted with one or more types of substituents selected from the group consisting of deuterium, halogen, a cyano group, a nitro group, a C1˜C40 alkyl group, a C2˜C40 alkenyl group, a C2˜C40 alkynyl group, a C6˜C60 aryl group, a heteroaryl group having 5 to 60 nuclear atoms, a C6˜C60 aryloxy group, a C1˜C40 alkyloxy group, a C6˜C60 arylamine group, a C3˜C40 cycloalkyl group, a heterocycloalkyl group having 3 to 40 nuclear atoms, a C1˜C40 alkylsilyl group, a C1˜C40 alkylboron group, a C6˜C60 arylboron group, a C6˜C60 arylphosphanyl group, a C6˜C60 mono or diarylphosphynyl group and a C6˜C60 arylsilyl group, and when substituted with a plurality of substituents, these are the same as or different from each other.

US Pat. No. 11,066,379

GRACILIN A AND CONGENERS AS IMMUNOSUPPRESSIVE AND NEUROPROTECTIVE AGENTS

Universidade de Santiago ...


21. A compound having the formula:




US Pat. No. 11,066,378

CAFFEIC ACID DERIVATIVES FOR ANTI-ANGIOGENESIS

Taipei Medical University...


1. A compound, which is




or a stereoisomer thereof, or an enantiomer thereof or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,375

MICROBIOCIDAL OXADIAZOLE DERIVATIVES

SYNGENTA PARTICIPATIONS A...


1. A compound of formula (I):



wherein
n is 1 or 2;
A1 represents N or CR1, wherein R1 is hydrogen, halogen, methyl, ethyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, or difluoromethoxy;
A2 represents N or CR2, wherein R2 is hydrogen, halogen, methyl, ethyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, or difluoromethoxy;
A3 represents N or CR3, wherein R3 is hydrogen or halogen;
A4 represents N or CR4, wherein R4 is hydrogen or halogen; and
wherein 0, 1 or 2 of A1, A2, A3 and A4 are N;
R5 and R6 are independently selected from hydrogen, C1-4alkyl, halogen, cyano, trifluoromethyl and difluoromethyl, or R5 and R6 together with the carbon atom they share form a cyclopropyl;
R7 is hydroxy, C1-4alkyl, C1-4haloalkyl, C1-4alkoxy, hydroxyC1-4alkyl, C1-2alkoxyC1-4alkyl, C1-2haloalkoxyC1-4alkyl, C3-6alkenyl, C3-4alkynyl, C3-6alkenyloxy, C3-6alkynyloxy, C3-6haloalkenyl, C3-6haloalkenyloxy, C1-4alkylcarbonyloxy, C1-4haloalkylcarbonyloxy, C1-4alkoxycarbonyloxy, C1-4alkylcarbonyloxyC1-4alkyl, C1-4haloalkylcarbonyloxyC1-4alkyl or C1-4alkoxycarbonyloxyC1-4alkyl; or
R7 is C3-6cycloalkyl, C3-6cycloalkylC1-2alkyl, C3-6cycloalkylC1-2alkoxy, phenylC1-2alkyl, phenylC1-2alkoxy, heteroaryl, heteroarylC1-2alkyl, heteroarylC1-2alkoxy, heterocyclyl, heterocyclylC1-2alkyl, heterocyclylC1-2alkoxy, C3-6cycloalkylcarbonyloxy, heterocyclylcarbonyloxy, phenylcarbonyloxy, C3-6cycloalkylcarbonyloxyC1-4alkyl, heterocyclylcarbonyloxyC1-4alkyl or phenylcarbonyloxyC1-4alkyl, wherein the heteroaryl moiety is a 5- or 6-membered monocyclic aromatic ring which comprises 1, 2, 3 or 4 heteroatoms individually selected from N, O and S, the heterocyclyl moiety is a 4- to 6-membered non-aromatic ring which comprises 1 or 2 heteroatoms individually selected from N, O and S, and wherein any of said cycloalkyl, phenyl, heteroaryl and heterocyclyl moieties are optionally substituted by 1 or 2 substituents selected from cyano, fluoro, chloro, bromo, methyl, difluoromethyl, trifluoromethyl, methoxy, ethoxy, or difluoromethoxy;
R8 is —NR14R15, wherein R14 is hydrogen, cyano, C1-6alkyl, C1-6alkoxy, C2-6alkenyl, C2-6alkynyl, C3-6alkenyloxy, C3-6alkynyloxy, cyanoC1-6alkyl, C1-6haloalkyl, C1-6haloalkenyl, hydroxyC1-6alkyl, C1-4alkoxyC1-6alkyl, C1-4haloalkoxyC1-6alkyl, C1-4alkoxyC1-4alkoxyC1-6alkyl, aminoC1-6alkyl, N—C1-4alkylaminoC1-6alkyl, C1-6alkylcarbonylC1-6alkyl, C1-6alkylcarbonylC2-6alkenyl, C1-6alkoxycarbonylC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, N—C1-4alkylaminocarbonylC1-6alkyl, N,N-diC1-4alkylaminocarbonylC1-6alkyl, C1-4alkylsulfanylC1-6alkyl, C1-6alkylsulfonylC1-6alkyl or C1-6alkylsulfonylaminoC1-6alkyl; or
R14 is C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, C3-8cycloalkylC1-6alkoxy, C3-6cycloalkyloxy, wherein the cycloalkyl moiety is optionally partially unsaturated, phenyl, phenylC1-6alkyl, phenylC1-6alkoxy, heteroaryl, heteroarylC1-6alkyl, heteroarylC1-6alkoxy, wherein the heteroaryl moiety is a 5- or 6-membered monocyclic aromatic ring which comprises 1, 2, 3 or 4 heteroatoms individually selected from N, O and S, heterocyclyl, heterocyclylC1-6alkyl or heterocyclylC1-6alkoxy wherein the heterocyclyl moiety is a 4- to 6-membered non-aromatic ring which comprises 1, 2 or 3 heteroatoms individually selected from N, O and S,
wherein for R14, any cycloalkyl, phenyl, heteroaryl, heterocyclyl moiety is optionally substituted by 1, 2 or 3 substituents, which may be the same or different, selected from R16; wherein
R16 is cyano, halogen, hydroxy, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4haloalkyl, C2-4haloalkenyl, C1-4alkoxy, C1-2alkoxyC1-2alkyl, C1-4haloalkoxy, C3-4alkenyloxy, C3-4alkynyloxy, N—C1-4alkylamino, N,N-diC1-4alkylamino, C1-4alkylcarbonyl, C1-4alkoxycarbonyl, carbonylamino, N—C1-4alkylaminocarbonyl, N,N-diC1-4alkylaminocarbonyl or C1-4alkoxycarbonylamino;
and wherein, when R14 is substituted C3-8cycloalkyl, C3-8cycloalkylC1-6alkyl, C3-8cycloalkylC1-6alkoxy, heterocyclyl, heterocyclylC1-6alkyl or heterocyclylC1-6alkoxy, R16 may also represent oxo on the C3-8cycloalkyl or heterocyclyl moiety;
R15 is hydrogen, C1-4alkyl, C3-4alkynyl, C1-4alkoxyC1-4alkyl, cyanoC1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-2alkyl; or
R14 and R15, together with the nitrogen atom to which they are bonded, form a 4-, 5- or 6-membered cycle optionally containing an additional heteroatom or group selected from O, S, S(O)2, oxo (?O) and NR17; wherein
R17 is hydrogen, methyl, methoxy, formyl or acyl; or
a salt or an N-oxide thereof.

US Pat. No. 11,066,374

METHOD FOR PRODUCING KAKEROMYCIN AND DERIVATIVES THEREOF

OP BIO FACTORY CO., LTD.,...


1. A compound represented by formula (4):



wherein
R is (1) a group represented by formula (A):





wherein R1 and R2 are the same or different and each is a C1-20 alkyl group, a C6-20 aryl group optionally substituted by a halogen atom, or a C7-20 aralkyl group, (2) a C1-20 alkyl group, (3) a C6-20 aryl group, or (4) a C7-20 aralkyl group, andn is 1,

or a salt thereof.

US Pat. No. 11,066,373

MORPHIC FORMS OF HEXADECYLOXYPROPYL-PHOSPHONATE ESTERS AND METHODS OF SYNTHESIS THEREOF

Chimerix, Inc., Durham, ...


1. A method of synthesizing morphic Form II of Compound 1:




comprising:(i) contacting a mixture of (S)—N1-[(2-hydroxy-3-triphenylmethoxy)propyl]cytosine (Compound 2) with P-[[[4-methylphenyl)sulfonyl]oxy]methyl]-, mono[3-(hexadecyloxy)propyl]ester, sodium salt (Compound 4) in the presence of a suitable base and in a suitable organic solvent, at a suitable reaction temperature;
(ii) extracting the crude product with a suitable organic solvent and concentrating the mixture to give crude phosphonic acid, [[(S)-2-(4-amino-2-oxo-1(2H)-pyrimidinyl)-1-(hydroxymethyl)-2-(triphenylmethoxy)ethyl]methyl]mono[3-(hexadecyl oxy)propyl] ester (Compound 3);
(iii) diluting crude Compound 3 in methanol and re-concentrating the resulting solution to remove the residual suitable organic solvent of step (ii);
(iv) contacting crude Compound 3 with a suitable deprotecting agent in an organic solvent to give crude Compound 1; and
(v) recrystallizing crude Compound 1 using a suitable solvent system.

US Pat. No. 11,066,372

DEUTERATED BENZIMIDAZOLE COMPOUND AND MEDICAL USE THEREOF

Sumitomo Dainippon Pharma...


1. A compound of formula (I):




or a pharmaceutically acceptable salt thereof, whereinR1a, R1b, R1c and R1d are independently hydrogen, halogen, cyano, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylamino (wherein the alkyl and the alkyl moiety in the alkoxy and the alkylamino may be independently substituted with 1 to 5 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and 3- to 7-membered non-aromatic heterocyclyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), C3-7 cycloalkyl, C3-7 cycloalkoxy, C3-7 cycloalkylamino (wherein the cycloalkyl and the cycloalkyl moiety in the cycloalkoxy and the cycloalkylamino may be independently substituted with 1 to 5 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), C6-10 aryl, C6-10 aryloxy, 5- to 12-membered heteroaryl, or 5- to 12-membered heteroaryloxy (wherein the aryl and the aryl moiety in the aryloxy, and the heteroaryl and the heteroaryl moiety in the heteroaryloxy may be independently substituted with 1 to 5 substituents selected independently from the group consisting of halogen, cyano, C1-4 alkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, 3- to 7-membered non-aromatic heterocyclyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C1-4 alkylthio optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, and C1-4 alkylsulfonyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A), provided that at least one of R1a, R1b, R1c and R1d is the above C6-10 aryl, C6-10 aryloxy, 5- to 12-membered heteroaryl or 5- to 12-membered heteroaryloxy,
R2 and R3 are independently hydrogen, C1-6 alkyl (which may be independently substituted with 1 to 5 substituents selected independently from the group consisting of cyano, halogen, hydroxy group, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), or C3-10 cycloalkyl,
R4 is hydrogen, C1-6 alkyl (which may be substituted with 1 to 3 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and 3- to 7-membered non-aromatic heterocyclyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), or C3-7 cycloalkyl (which may be independently substituted with 1 to 3 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B),
m is 0, 1, or 2,
L is CR7R8 provided that when m is 2, each CR7R8 is independently the same or different,
R7 and R8 are independently hydrogen, hydroxy group, C1-4 alkyl, C1-4 alkoxy (wherein the alkyl and the alkyl moiety in the alkoxy may be independently substituted with 1 to 3 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and 3- to 7-membered non-aromatic heterocyclyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), C3-7 cycloalkyl, or C3-7 cycloalkoxy (wherein the cycloalkyl and the cycloalkyl moiety in the cycloalkoxy may be independently substituted with 1 to 3 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B), or
in R2, R3 and —OR4, R2 and R3 may be combined together with the carbon atom to which they are attached to form the following group of formula (II) with —OR4





in formula (II),e and f are independently 1, 2 or 3,
R4 is as defined above,
V is single bond or oxygen atom,
R5a, R5b, R5c, and R5d are independently hydrogen, halogen, hydroxy group, C1-4 alkyl, or C1-4 alkoxy, wherein the alkyl and the alkyl moiety in the alkoxy may be independently substituted with 1 to 3 substituents selected independently from the group consisting of halogen, hydroxy group, C1-4 alkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group A, C3-7 cycloalkyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, C3-7 cycloalkoxy optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B, and 3- to 7-membered non-aromatic heterocyclyl optionally-substituted with 1 to 3 substituents selected independently from Substituent-group B,
Substituent-group A is independently halogen, hydroxy group, C1-4 alkoxy, C3-7 cycloalkyl, or C3-7 cycloalkoxy,
Substituent-group B is independently halogen, hydroxy group, C1-4 alkyl, C1-4 alkoxy, C3-7 cycloalkyl, or C3-7 cycloalkoxy, and further any 1 to 6 hydrogen atoms in the compound of formula (I) may be replaced with deuterium atoms.

US Pat. No. 11,066,371

PYRIDINE COMPOUND, MAKING, AND USE THEREOF

UNITED ARAB EMIRATES UNIV...


1. A method for treating a damaged gastric wall of a human, comprising exposing gastric stem cells to an effective amount of a substituted pyridine derivative selected from compounds of formula (I)




wherein:R1 is selected from the group consisting of C1-C6 alkyl, C3-C5 cycloalkyl, and C1-C6 haloalkyl;
R2 is selected from the group consisting of C1-C6 alkyl, 5-membered heterocyclyl, and phenyl;
R3 and R4 are independently selected from the group consisting of H, C1-C6 alkyl, C3-C5 cycloalkyl, C1-C6 alkoxy, halo, NO2, NH2, OH, CN, haloalkyl, SO3H, SO2NH2, COOH, and CONH2;
X is S or O;

thereby inducing differentiation of the gastric stem cells into gastric functional cells.

US Pat. No. 11,066,370

KINASE INHIBITOR COMPOUNDS, COMPOSITIONS, AND METHODS OF TREATING CANCER

ICAHN SCHOOL OF MEDICINE ...


1. A compound of Formula (I) having the following structure:



or a stereoisomer, pharmaceutically acceptable salt, or oxide, wherein
R is aryl optionally substituted n times with R13;
R1 is H;
R2 is H;
R3 is halogen;
R4 is H;
R5 is H, halogen, or C1-C6 alkyl;
R6 is C1-C6 alkyl;
X is NH;
Y is;




Z is C(R12);
R12 is H, halogen, or C1-C6 alkyl;
R13 is selected independently at each occurrence thereof from the group consisting of H, CH2F, CHF2, CClF2, CBrF2, CIF2, CF3, C2F5, C3F7, and C4F9; and
n is 1 to 5.

US Pat. No. 11,066,369

N-(PYRIDIN-2-YL)PYRIDINE-SULFONAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE

Novartis AG, Basel (CH)


1. A pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt thereof,



wherein:ring A is phenyl;
ring B is pyridinyl;
R1 and R2 are each independently hydrogen, nitrile, C1-4alkoxy, halogen, C1-4alkyl, halo-substituted-C1-4alkyl, C3-6 cycloalkyl or halo-substituted-C1-4alkoxy;
R3 and R4 are each independently hydrogen, nitrile, CD3, C3-6 cycloalkyl, C4-6 heterocycle, C1-4alkoxy, halogen, C1-4alkyl, halo-substituted-C1-4alkyl, hydroxy-substituted-C1-4alkyl or halo-substituted-C1-4alkoxy;
n is 1 or 2;
R5 is —NR7R8, —OR9 or R10;
R6 is hydrogen, hydroxy, C1-2alkyl, C1-2alkoxy, hydroxy-substituted-C1-2alkyl, halogen or amino;
m is 1 or 2;
R7 is hydrogen, C1-6alkyl, C3-6 cycloalkyl, a fully or partially saturated 4 to 7-membered heterocycle, wherein said 4 to 7-membered heterocycle is optionally substituted with 1 to 4 substituents each independently selected from halogen, hydroxy, C1-4alkyl, C1-4alkoxy, halo-substituted-C1-4alkyl, hydroxy-substituted-C1-4alkyl, halo-substituted-C1-4alkoxy, oxo, nitrile, C3-6cycloalkyl, C4-6 heterocycle, NHR11, —C(O)—R13, —C(O)NHR11, C1-3alkyl-C(O)NHR11 and —C(O)O—R12;
R8 is hydrogen or C1-4alkyl;
R9 is hydrogen, C3-6 cycloalkyl or a fully or partially saturated 4 to 7-membered heterocycle each ring is optionally substituted with one to four substituents each independently selected from halogen, hydroxy, C1-4alkyl, C1-4alkoxy, halo-substituted-C1-4alkyl, hydroxy-substituted-C1-4alkyl, halo-substituted-C1-4alkoxy, oxo, nitrile, C3-6 cycloalkyl, C4-6 heterocycle, NHR11, —C(O)—R13, —C(O)NHR11, C1-3alkyl-C(O)NHR11 and —C(O)O—R12;
R10 is a fully or partially saturated 4 to 10-membered heterocycle optionally substituted with one to four substituents each independently selected from halogen, hydroxy, C1-4alkyl, C1-4alkoxy, halo-substituted-C1-4alkyl, hydroxy-substituted-C1-4alkyl, halo-substituted-C1-4alkoxy, oxo, nitrile, C3-6 cycloalkyl, C4-6 heterocycle, NHR11, —C(O)—R13, —C(O)NHR11, C1-3alkyl-C(O)NHR11, —C(O)C1-3alkyl-NHR11 and —C(O)O—R12, wherein said C3-6 cycloalkyl and C4-6 heterocycle are optionally substituted with 1 to 3 substituents each independently selected from hydroxy, halogen, amino, C1-4alkyl, halo-substituted-C1-4alkyl and hydroxy-substituted-C1-4alkyl;
R11 is hydrogen, C1-4alkyl or C0-3alkyl-C(O)O—R14;
R12 is hydrogen, C1-4alkyl or C1-3alkyl-C(O)—NHR14;
R13 is C1-4alkyl, wherein said alkyl is optionally substituted with amino; and
R14 is hydrogen or C1-4alkyl,


a CFTR modulator selected from:N-(2-(5-chloro-2-methoxy-phenylamino)-4?-methyl-[4, 5?]bithiazolyl-2?-yl)-benzamide;
N-(2,4-di-tert-butyl-5-hydroxyphenyl)-1,4-dihydro-4-oxoquinoline-3-carboxamide;
N-[2-(1,1-Dimethylethyl)-4-[1,1-di(methyl-d3)ethyl-2,2,2-d3]-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide;
(((3-((3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)carbamoyl)-1H-pyrazol-1-yl)methoxy)methyl)phosphonic acid;
3-[6-({[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}amino)-3-methylpyridin-2-yl]benzoic acid;
N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-3-carboxamide;
1-(2,2-difluoro-1,3-benzodioxol-5-yl)-N-[1-[(2R)-2,3-dihydroxypropyl]-6-fluoro-2-(2-hydroxy-1,1-dimethylethyl)-1H-indol-5-yl]-cyclopropanecarboxamide;
4-((2R,4R)-4-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropane-1-carboxamido)-7-(difluoromethoxy)chroman-2-yl)benzoic acid;
4-(3-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropane-1-carboxamido)isoquinolin-1-yl)benzoic acid;
N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluromethyl)-1,4-dihydroquinoline-3-carboxamide;
3-[5-(2-fluorophenyl)-1,2,4-oxadiazol-3-yl]benzoic acid;
5,7-Dihydroxy-3-(4-hydroxyphenyl)chromen-4-one;
N-(2-(tert-butyl)-5-hydroxy-4-(2-(methyl-d3)propan-2-yl-1,1,1,3,3,3-d6)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide;
N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-5-carboxamide;
3-Chloro-4-(6-hydroxyquinolin-2-yl)benzoic acid,
and
(S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide;

and a pharmaceutically acceptable carrier.

US Pat. No. 11,066,368

PROCESS FOR THE PREPARATION AND PARTICLE SIZE REDUCTION OF PIRFENIDONE

Laurus Labs Limited, Hyd...


1. A process for preparation of pirfenidone of Formula (I),




having a particle size distribution characterized by D90 from 50 microns to 500 microns, comprising:a) reacting 5-methyl-1H-pyridin-2-one of Formula (II),





with bromobenzene of Formula (III),




in the presence of a copper catalyst and a base in an organic solvent to provide pirfenidone, wherein the bromobenzene contains about 0.2% or more by weight of dibromobenzene;b) isolating the pirfenidone; and
c) reducing the particle size of the isolated pirfenidone to arrive at the particle size distribution,
wherein the particle size reduction of step c) comprises wet milling the isolated pirfenidone of step b) using one of a colloid mill, ultrasonicator, and high speed homogenizer device, and
wherein the size-reduced pirfenidone recovered after the wet milling is characterized by a particle size distribution of D10 greater than about 10 ?m and less than about 50 ?m, D50 greater than about 35 ?m and less than about 150 ?m, and D90 greater than about 85 ?m and less than about 300 ?M.

US Pat. No. 11,066,366

HYDROPHILIC FENTANYL DERIVATIVES

Allegheny-Singer Research...


1. A compound according to Formula Ia or Formula Ib:




wherein :each R1 is independently selected from the group consisting of halo, hydroxyl, lower alkyl, amino, carboxyl, and trifluoromethyl;
n is 0, 1 or 2;
m is 1 or 2;
R2 is —(L)x-R3, in which:x is 1;
L is a linking group selected from the group consisting of —(CH?CH)a-, —(CH?CR)b—, and —C?C—, wherein:a is 1, 2 or 3; and
b is 1, 2 or 3;

R3 is —X1—X2—Z,in which:


X1 is —C(?O)—,
X2 is selected from —O—, and —NH—; and
Z is an oligomer selected from the group consisting of —(CH2CH2—O)m—H, and —(CH2CH2—O)m—CH3 wherein m is from 1 to 20; and
each R is independently selected from H and methyl.

US Pat. No. 11,066,365

1-CYANO-PYRROLIDINE COMPOUNDS AS USP30 INHIBITORS

Mission Therapeutics Limi...


1. A compound having the formula (IIA):



a tautomer thereof, or a pharmaceutically acceptable salt of said compound or tautomer,
wherein:
R2 represents a hydrogen atom or C1-C3 alkyl;
R3, R4 and R5 each independently represent a hydrogen atom, optionally substituted C1-C3 alkyl, or C1-C3 alkoxy group, wherein the optional substituents of alkyl of R3, R4 and R5, which may be the same or different, are selected from C1-C3 alkoxy, halogen, hydroxyl, thiol, cyano, amino, amido, nitro and SF5;
R1 and R8 each independently represent a hydrogen atom or C1-C3 alkyl;
R9 represents a hydrogen atom, a fluorine atom, hydroxyl, C1-C3 alkyl, C1-C3 alkoxy group, or cyclopropyl;
R10 represents a hydrogen atom;
Y represents a covalent bond;
R12 is a 6 to 14-membered heteroaryl ring, which comprises 1, 2 or 3 heteroatoms independently selected from nitrogen, oxygen and sulfur, which is substituted with one or more of -Q1-(R13)p, wherein:
p is 0 or 1;
Q1 is selected from halogen, cyano, oxo, a covalent bond, —NR14R15—, —NR14CO—, an oxygen atom, C1-C6 alkoxy, —NR14—, —NR14COR15, C1-C6 alkyl, C1-C3 alkylene, wherein the alkyl and alkoxy are optionally substituted with fluorine;
R14 and R15 each independently represent a hydrogen atom or C1-C3 alkyl;
when p is 1, R13 represents a 4 to 10-membered, monocyclic or bicyclic, heteroaryl or heterocyclyl ring, which comprises 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulfur; or R13 represents phenyl, naphthyl, or a 3 to 8-membered cycloalkyl ring;
wherein R13 is optionally substituted with one or more substituents selected from halogen, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkyl, oxo, cyano, -Q2-R17, -Q2-COR17, Q2-CONR17R18, and -Q2-CO2R17;
Q2 represents a covalent bond or an oxygen atom; and
R17 and R18 each independently represent hydrogen, C1-C6 alkyl, cyclopropyl, phenyl, or a 4 to 10-membered, monocyclic or bicyclic, heterocyclyl or heteroaryl ring, which comprises 1, 2 or 3 heteroatoms selected from nitrogen, oxygen and sulfur; wherein said phenyl, heterocyclyl, or heteroaryl ring, may be optionally substituted with one or more substituents, which may be the same or different, selected from chloro and fluoro.

US Pat. No. 11,066,364

NLRX1 LIGANDS

LANDOS BIOPHARMA, INC., ...


1. A compound of formula Z having an A ring, a B ring, a C ring, and a D ring, or a salt thereof, wherein:Z is:




X in each instance is CH;
Y in each instance is O;
A1, A2, A3, and A4 in each instance are independently selected from the group consisting of N and C, with the proviso that at least one of A1 and A3 on the A ring is C and A2 on the A ring is C;
A5 in each instance is N;
R5 in each instance is absent;
R1, R2, R3, and R4, when present, are in each instance independently selected from the group consisting of hydrogen, hydroxy, halo, carboxyl, amino, alkyl, alkoxy, acyl, aryl, and any combination of the foregoing, with the proviso that any of R1, R2, R3, and/or R4 on a given ring is absent when A1, A2, A3, and/or A4 on the given ring, respectively, is N.

US Pat. No. 11,066,363

SUBSTITUTED 6,11-DIHYDRO-5H-BENZO[B]CARBAZOLES AS INHIBITORS OF ALK AND SRPK

DANA-FARBER CANCER INSTIT...


2. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of the compound of claim 1, or a pharmaceutically acceptable salt, stereoisomer, or tautomer.

US Pat. No. 11,066,362

METHOD FOR PRODUCING PYRROLE COMPOUND

Takeda Pharmaceutical Com...


1. A method for producing a compound represented by the formula




wherein R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, a chlorine atom or a fluorine atom, R3 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and R4 is an alkyl group, or a salt thereof, comprising
(1) subjecting a compound represented by the formula




wherein each symbol is as defined above, or a salt thereof to a reduction reaction, and then to a cyclization reaction to give a compound represented by the formula




wherein each symbol is as defined above, or a salt thereof, wherein the reduction reaction is a continuous hydrogenation in a fixed bed reactor filled with a supported metal catalyst,
(2) subjecting the obtained compound to a reduction reaction, and then to hydrolysis to give a compound represented by the formula




wherein each symbol is as defined above, or a salt thereof,
(3) reacting the obtained compound with a compound represented by the formulaR3—SO2—X??(V)

wherein R3 is as defined above, and X is a leaving group, or a salt thereof to give a compound represented by the formula




wherein each symbol is as defined above, or a salt thereof, and
(4) reacting the obtained compound with a compound represented by the formulaR4—NH2??(VII)
wherein R4 is as defined above, or a salt thereof.

US Pat. No. 11,066,361

DIFLUOROLACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASES AND CONDITIONS

CAYMAN CHEMICAL COMPANY, ...


1. A compound of formula (6.1)



wherein:
L1 isa) C3-C7alkylene, C3-C7alkenylene, or C3-C7alkynylene; or
b) —(CH2)n1-G2-(CH2)p—, —(CH2)n2—C?C-G2-, or —(CH2)n2—C(R12)?C(R12)-G2-,
wherein n1 is 2, 3, 4, or 5, n2 is 1, 2, or 3, p is 0, 1, 2, or 3, and n1+p=2, 3, 4, 5, or 6;

G2 is




R1 is a protected carboxylic acid;
R12, at each occurrence, is independently H or C1-C4alkyl; and
R20 is H or a hydroxyl protecting group.

US Pat. No. 11,066,360

HUMAN PLASMA KALLIKREIN INHIBITORS

BioCryst Pharmaceuticals,...


1. A method of treating a disease or condition characterized by unwanted plasma kallikrein activity, comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt thereof:




wherein, independently for each occurrence:R1 represents —OH, —ORc, —NH2, —NHRc, —NRcRd, alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, halo, haloalkyl, cycloalkyl, (cycloalkyl)alkyl, —C(O)Rc, —C(O)OH, —C(O)ORc, —OC(O)Rc, —C(O)NH2, —C(O)NHRc, —C(O)NRcRd, —NHC(O)Rc, or —NRcC(O)Rd; or two geminal occurrences of R1 taken together with the carbon to which they are attached represent —C(O)—; or two vicinal or geminal occurrences of R1 taken together form an optionally substituted fused or spirocyclic carbocyclic or heterocyclic ring;
W is —C(O)NH— or —C(O)N(Rc)—;
R2 represents optionally substituted aryl or heteroaryl;
V represents optionally substituted aryl or heteroaryl;
Z is absent or represents one or more substituents independently selected from the group consisting of halo, haloalkyl, —NO2, —CN, —C(O)Rc, —C(O)OH, —C(O)ORc, —OC(O)Rc, —C(O)NH2, —C(O)NHRc, —C(O)NRcRd, —NHC(O)Rc, —N(Rc)C(O)Rd, —OS(O)p(Rc), —NHS(O)p(Rc), and —NRcS(O)p(Rc);
X represents —C(NH2)—, —C(NH(Rc))—, —C(NRcRd)—, —C(NHS(O)pRc)—, —C(NHC(O)Rc)—, —C(NHC(O)NH2)—, —C(NHC(O)NHRc)—, —C(NHC(O)NRcRd)—, —C(OH)—, —C(O(alkyl))-, —C(N3)—, —C(CN)—, —C(NO2)—, —C(S(O)nRa)—, —C[—C(?O)Rc]—, —C[—C(?O)NRcRd]—, —C[—C(?O)SRc]—, —C[—S(O)Rc]—, —C[—S(O)2Rc]—, —C[S(O)(ORc)]—, —C[—S(O)2(ORc)]—, —C[—SO2NRcRd]—, —C(halogen)-, —C(alkyl), —C((cycloalkyl)alkyl), —C(alkenyl)-, —C(alkynyl)-, or —C(aralkyl)-;
R3 represents optionally substituted aryl, heteroaryl, cycloalkyl, or heterocycloalkyl;
R3a is absent or represents one or more substituents independently selected from the group consisting of halo, hydroxy, alkyl, —CF3, —OCF3, alkoxy, aryl, heteroaryl, aryloxy, amino, aminoalkyl, —C(O)NH2, cyano, —NHC(O)alkyl, —SO2alkyl, —SO2NH2, cycloalkyl, —(CH2)rORa, —NO2, —(CH2)rNRaRb, —(CH2)rC(O)Ra, —NRaC(O)Rb, —C(O)NRcRd, —NRaC(O)NRcRd, —C(?NRa)NRcRd, —NHC(?NRa)NRcRd, —NRaRb, —SO2NRcRd, —NRaSO2NRcRd, —NRaSO2alkyl, —NRaSO2Ra, —S(O)pRa, —(CF2)rCF3, —NHCH2Ra, —OCH2Ra, —SCH2Ra, —NH(CH2)2(CH2)rRa, —O(CH2)2(CH2)rRa, or —S(CH2)2(CH2)rRa;
Y represents a bond; or —Y—R4 represents optionally substituted -alkylene-R4, —CH2C(O)—R4, —CH2NH—R4, —CH2N(alkyl)-R4, —CRaRb—R4, —NH—R4, —NHCH2—R4, —NHC(O)—R4, —N(alkyl)-R4, —N(alkyl)CH2—R4, —N((CH2)2OH)—R4, —N((cycloalkyl)alkyl)R4, -heterocyclyl-R4, —OR4, —OCH2—R4, —OC(O)—R4, —OC(O)NRaRb, —SCH2R4, or —SR4;
R4 represents hydrogen, hydroxy, optionally substituted alkyl, cycloalkyl, (heterocycloalkyl)alkyl, (cycloalkyl)alkyl, —CH2OH, —CH(alkyl)OH, —CH(NH2)CH(alkyl)2, aryl, aralkyl, heteroaryl, heteroaralkyl, —CH2S(alkyl), amino, or cyano; or —(CRaRb)r(CRaRb)p— fused to the 4-position of the ring bearing Z to form a 5- to 7-membered heterocyclic ring with optional substituents; or,
when R3 is phenyl, R4 can represent —NRa— fused to the position ortho to X on that phenyl;
each Ra and Rb is independently H, alkyl, alkenyl, alkynyl, aralkyl, (cycloalkyl)alkyl, —C(?O)Rc, —C(?O)ORc, —C(?O)NRcRd, —C(?O)SRc, —S(O)Rc, —S(O)2Rc, —S(O)(ORc), or —SO2NRcRd;
Rc and Rd represent, independently for each occurrence, optionally substituted alkyl, alkenyl, alkynyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, (cycloalkyl)alkyl, heterocycloalkyl, (heterocycloalkyl)alkyl, —C(O)alkyl, or —S(O)p(alkyl); or Rc and Rd can be taken together to form an optionally substituted heterocyclic ring;





can represent



r is 0, 1, 2, or 3;
n is an integer from 0 to 6;
p is 0, 1, or 2; and
the disease or condition characterized by unwanted plasma kallikrein activity is selected from the group consisting of stroke, inflammation, reperfusion injury, acute myocardial infarction, deep vein thrombosis, post fibrinolytic treatment condition, angina, edema, angioedema, hereditary angioedema, sepsis, arthritis, hemorrhage, blood loss during cardiopulmonary bypass, inflammatory bowel disease, diabetes mellitus, retinopathy, diabetic retinopathy, diabetic macular edema, diabetic macular degeneration, age-related macular edema, age-related macular degeneration, proliferative retinopathy, neuropathy, hypertension, brain edema, increased albumin excretion, macroalbuminuria, and nephropathy.

US Pat. No. 11,066,359

BIODEGRADABLE SURFACTANTS AND RELATED COMPOSITIONS, METHODS AND SYSTEMS

LAWRENCE LIVERMORE NATION...


1. A method of modifying a tunable biodegradable surfactant having a first aHLB value to obtain a tuned biodegradable surfactant having a second aHLB value, the method comprising:providing the tunable biodegradable surfactant having the first aHLB value, the tunable biodegradable surfactant comprising an amphiphilic heteroatom containing hydrocarbon and optionally at least one counterion (Z), the amphiphilic heteroatom containing hydrocarbon comprising
a hydrophilic head portion of containing a maximum number of a hydrophilic functional group with a positive Group Number on the hydrocarbon the hydrophilic function group comprising at least one tunable moiety, and
a hydrophobic tail portion containing the maximum number of a hydrophobic group of atoms with a negative Group Number on the hydrocarbon and forming a contiguous terminal section of the biodegradable surfactant; and
modifying the at least one tunable moiety of the tunable biodegradable surfactant to obtain the tuned biodegradable surfactant comprising at least one tuned moiety and having the second aHLB value and optionally the at least one counterion (Z),

wherein the amphiphilic heteroatom containing hydrocarbon has Formula (X):



in which
represents a single or double bond when R21 is H, and a single bond when R21 is other than H;
X is selected from one of O, NH, or NCH3;
Y is selected from C2-C8 linear or branched alkyl, C4-C8 cycloalkyl, C2-C8 linear or branched heteroalkyl, C4-C8 heterocycloalkyl, C4-C8 heteroalkyl heterocycloalkyl, C4-C8 aryl alkyl, C4-C8 alkyl aryl, C4-C8 heteroaryl alkyl, and C4-C8 alkyl heteroaryl groups, optionally substituted with 1-6 tuning moieties independently selected from sulfate, sulfonate, phosphate, phosphonate, carboxylate, amine, C1-C2 alkyl amine, C1-C2 dialkyl amine, C1-C2 trialkyl ammonium, pyridinium, hydroxyl, acetyloxy, C1-C2 alkoxy;
R20 is a C11-C21 linear or branched alkyl, alkenyl, or alkynyl group; and
R21 is selected from H, sulfate, sulfonate, phosphate, phosphonate, carboxylate, amine, C1-C2 alkyl amine, C1-C2 dialkyl amine, C1-C2 trialkyl ammonium, pyridinium, hydroxyl, acetyloxy, C1-C2 alkoxy; and
the at least one counterion (Z) is selected from the group selected from the group consisting of proton, ammonium, C-C4 tetraalkyl ammonium, sodium (I), potassium (I), cesium (I), magnesium (II), calcium (II), zinc (II), inorganic sulfate (SO42?), inorganic phosphate (PO43?), tetrafluorborate, hexafluorophospate, p-toluenesulfonate, benzenesulfonate, nitrate, trifluoroacetate, fluoride, chloride, bromide, and iodide or any combinations thereof;

wherein the at least one counterion (Z) is selected from the group selected from the group consisting of proton, ammonium, C-C4 tetraalkyl ammonium, sodium (I), potassium (I), cesium (I), magnesium (II), calcium (II), zinc (II), inorganic sulfate (SO42-), inorganic phosphate (PO43-), tetrafluorborate, hexafluorophospate, p-toluenesulfonate, benzenesulfonate, nitrate, trifluoroacetate, fluoride, chloride, bromide, and iodide or any combinations thereof;
and whereinaHLB=20*Gh/(Gh?Gt)??(1)

in whichGh is the Group Number of the head portion of the amphiphilic heteroatom containing hydrocarbon,
Gt is the Group Number of the tail portion of amphiphilic heteroatom containing hydrocarbon.

US Pat. No. 11,066,358

COMPOSITIONS OF ESSENTIALLY PURE FORM IV OF N-((R)-2,3-DIHYDROXYPROPOXY)-3,4-DIFLUORO-2-(2-FLUORO-4-IODO-PHENYLAMINO)-BENZAMIDE AND USES THEREOF

WARNER-LAMBERT COMPANY LL...


1. A crystalline composition that is essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide of Formula (I)




US Pat. No. 11,066,357

BENZOANNULENE DERIVATIVES AS ANTIVIRAL AGENTS

SOUTHERN RESEARCH INSTITU...


1. A compound having a structure represented by a formula:



wherein each of m and n is independently selected from 0 and 1;
wherein Q is selected from CH and N;
wherein Z is selected from NH and CH2;
wherein R1 is selected from hydrogen, —OH, C1-C4 alkyl, C1-C4 haloalkoxy, and C1-C4 alkoxy;
wherein R2 is hydrogen; and
wherein R3 is C2-C5 heteroaryl substituted with 0, 1, 2, or 3 groups independently selected from halogen, —CN, —NH2, —OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, (C1-C4 alkyl)Ar1, and Ar1;wherein Ar1, when present, is selected from cycloalkyl, monocyclic aryl, heterocycloalkyl, and heteroaryl, and is substituted with 0, 1, 2, or 3 groups independently selected from halogen, C1-C4 alkyl, and C1-C4 haloalkyl;

or wherein R3 is a structure represented by a formula:





wherein each of R4a, R4b, R4c, and R4d is independently selected from hydrogen, halogen, —CN, —NH2, —OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, and Ar2;wherein Ar2, when present, is selected from cycloalkyl, monocyclic aryl, heterocycloalkyl, and heteroaryl, and is substituted with 0, 1, 2, or 3 groups independently selected from halogen, C1-C4 alkyl, and C1-C4 haloalkyl;

wherein R5 is selected from hydrogen, halogen, —CN, —NH2, —OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, (C1-C4)(C1-C4) dialkylamino, —(C1-C4 alkyl)CO2H, and Ar3; andwherein Ar3, when present, is selected from cycloalkyl, monocyclic aryl, heterocycloalkyl, and heteroaryl, and is substituted with 0, 1, 2, or 3 groups independently selected from halogen, C1-C4 alkyl, and C1-C4 haloalkyl;


or wherein each of R2 and R3 are covalently bonded together and, together with the intermediate atoms, comprise a 3- to 6-membered heterocycloalkyl substituted with 0, 1, 2, or 3 groups independently selected from halogen, —CN, —NH2, —OH, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 cyanoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, C1-C4 alkylamino, and (C1-C4)(C1-C4) dialkylamino;
provided that when n is 1 and R1 is hydrogen, then R3 is not pyridinyl,
provided that when n is 1, then R5 is not hydrogen,
or provided that when R5 is hydrogen, then R1 is not hydrogen,
or a pharmaceutically acceptable salt thereof.

US Pat. No. 11,066,356

DEVICE AND METHOD FOR THE DESALINATION OF WATER BY MEANS OF THERMAL DEIONISATION AND LIQUID-PHASE ION EXTRACTION LIQUID

ADIONICS, Thiais (FR)


1. A method for treating water comprising the extraction of at least two ionic species, the at least two ionic species comprising an anionic species and a cationic species and being present in the water to be treated, the method comprising the following steps:a) mixing in a first reactor, at a first temperature, a hydrophobic organic liquid phase and the water to be treated, the water to be treated being in the liquid state, in order to subsequently obtain a treated liquid water and a hydrophobic organic liquid phase charged with the at least two ionic species,
the hydrophobic organic liquid phase comprising:
at least a first protic and hydrophobic organic compound allowing anionic species solvation and whose pKa in water at 25° C. is at least 9 and at least lower than 15 at 25° C., the first protic and hydrophobic organic compound being a compound of Formula (B):




in which at least one of the radicals RA, RB, RC, RD and RE, which are identical or different, is a halogen atom or an electron-withdrawing group or a halogenated radical, of the following group: F, Cl, Br, CmF2m+1 with m?4, where m is a non-zero integer; CF2CF2CpH2p+1 with p?4, where p is an integer; CF2CpH2p+1 with p?4, where p is an integer; CH2CpF2p+1 with p?4, where p is an integer; OCH2CF3; C(?O)CF3; CmHnFpClqBrs with m?4, where n, p, q, s are integers of which at least p, q or s is non-zero; C(?O)OCmH2m+1 with m?4, where m is an integer; and C(?O)CmH2m+1 with m?4, where m is an integer,
the remaining radical(s) RA, RB, RC, RD and RE are chosen, identical or different, from the following non-electron withdrawing radicals: H; CH3; CH2CH3; CH2CH2CpF2p+1 with p?4, where p is an integer; CmH2m?1 with m?10, where m is a non-zero integer; and CmH2m+1 with m?10, where m is a non-zero integer;
where only one of the radicals RA to RE may be one of these last two radicals CmH2m?1 and CmH2m+1; and wherein X is selected from the following radicals: OH; NH—R?;




where R? and R?, is chosen from the following radicals: H; CnH2n?1 with n?4, where n is a non-zero integer; CnH2n+1 with n?4, where n is a non-zero integer; CH2CH2CpF2p+1 with p?4, where p is an integer; CH2CpF2p+1 with p?4, where p is an integer; CF2CpH2p+1 with p?4, where p is an integer; CF2CF2CpH2p+1 with p?4, where p is an integer; CmF2m+1 with m?4, where m is a non-zero integer; CmHnFpClqBrs with m?4, where n, p, q, s are integers of which at least p, q or s is non-zero; and an aryl radical of formula (b):




where RA, RB, RC, RD and RE, which may be identical or different, are as defined above in formula (B);
and wherein R?? is selected from the following radicals: CmH2m+1 with m?20, where m is an integer; CmH2m?1 with m?20, where m is a non-zero integer; CmHnFpClqBrs with m?10, where n, p, q, s are integers of which at least p, q or s is non-zero; CH2CH2CpF2p+1 with p?4, where p is an integer; CH2CpF2p+1 with p?4, where p is an integer; CF2CpH2p+1 with p?4, where p is an integer; CF2CF2CpH2p+1 with p?4, where p is an integer; CmF2m+1 with m?4, where m is a non-zero integer; and an aryl radical of formula (b):




where RA, RB, RC, RD and RE, which may be identical or different, are as defined above in formula (B); and
at least a second hydrophobic organic compound allowing cation extraction and having a complexing constant of the cationic species whose log K value, in methanol at 25° C., is greater than 2 and less than 11;
b) separating of the treated liquid water and of the organic liquid phase charged with the at least two ionic species,
c) mixing, at a second temperature, in the liquid phase, in a second reactor, of the organic liquid phase, charged with the at least two ionic species, with regeneration liquid water, for subsequent production of a regenerated organic liquid phase and of a regeneration liquid water charged with the at least two ionic species, the second temperature being higher than the first temperature and the difference between the first and second temperatures ranging from 30° C. to 150° C.

US Pat. No. 11,066,355

BRANCHED TAIL LIPID COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS

ModernaTX, Inc., Cambrid...


1. A compound of Formula (1-1):




or its N-oxide, or a salt or isomer thereof,wherein R?a is R?branched or R?cyclic; wherein

R?branched is




and R?cyclic is:




and
R?b is




wherein




denotes a point of attachment;wherein Ra? and Rb? are each independently a C2-12 alkyl or C2-12 alkenyl;
R2 and R3 are each independently selected from the group consisting of C1-14 alkyl and C2-14 alkenyl;
R4 is —(CH2)2OH;
each R? independently is a C1-12 alkyl or C2-12 alkenyl;
Ya is a C3-6 carbocycle;
R*?a is selected from the group consisting of C1-15 alkyl and C2-15 alkenyl; and
s is 2 or 3.

US Pat. No. 11,066,354

PROCESS FOR MONO N-ALKYLATION OF AMINOPHENOL

SABIC GLOBAL TECHNOLOGIES...


1. A process for the preparation of a compound represented by formula (I)




wherein
X is selected from the group consisting of —H, a halogen, linear or branched C1-C7 alkyl group, linear or branched C1-C5 alkoxy group, —NO2 and —CN and
Y is a linear or branched C1-C7 alkyl group,
comprising the steps of:
a) reacting a compound represented by formula (II) with a compound represented by (III) to obtain an intermediate product,




wherein X is as defined with respect to formula (I),




wherein Z is H, —CH3 or —C2H5,
b) reacting the intermediate product of step a) with a compound represented by Y2SO4 (IV) wherein Y is as defined with respect to formula (I) to obtain a salt and
c) hydrolyzing the salt of step b) to obtain the compound of formula (I).

US Pat. No. 11,066,351

ORGANIC COMPOUND, THREE-DIMENSIONAL ORGANIC FRAMEWORK FORMED BY USING ORGANIC COMPOUND, SEPARATION SIEVE AND OPTICAL LAYER, WHICH COMPRISE ORGANIC FRAMEWORK, AND OPTICAL DEVICE COMPRISING OPTICAL LAYER AS OPTICAL AMPLIFICATION LAYER

IUCF-HYU (INDUSTRY-UNIVER...


1. A three-dimensional organic structure comprising a plurality of unit organic molecules which are self-assembled to form the three-dimensional organic structure,wherein each of the unit organic molecules has at least one aromatic ring, a first pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring, and a second pair of substituents being connected to immediately adjacent positions of substitutable positions of the aromatic ring,
wherein the substituents have terminal groups, respective of which is independently selected from the group consisting of —CRcRdRe, —OH, —COOH, —CHO, —SH, —COCRcRdRe, —COOCRcRdRe, —CRc?CRdRe, —CN, —N?C?O, —C?N?N—CRcRdRe, —C?CRa, —NHCRcRdRe, and —NH2, wherein Rc, Rd, and Re are, independently of each other, H, F, Cl, Br, or I,
wherein the unit organic molecules contained in one layer of the three-dimensional structure are self-assembled by physical interaction between the terminal groups of the first pair of the substituents included in one unit organic molecule and the terminal groups of the second pair of the substituent groups included in another unit organic molecule among the unit organic molecules,
wherein the unit organic molecules contained in one layer and the unit organic molecules contained in another adjacent layer of the three-dimensional structure are self-assembled by pi-pi interactions between the aromatic rings,
wherein the three-dimensional organic structure is an organic crystal,
wherein the unit organic molecules has an organic compound of the following Chemical Formula 1:




in Chemical-Formula 1,
-A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 form one of the pairs of substituents being connected immediately adjacent positions among substitution positions of Ar,
X1 and X2 are the terminal groups,
A1 and A2 are, independently of each other, —O— or —S—,
L1 and L2 are, independently of each other, -E-,





E, E1, and E2 are, independently of each other, O or S, n1 and n2 are, independently of each other, 0 or 1,Y1 and Y2 are, independently of each other,





a1, a2, a3, b1, and b2 are, independently of each other, integers of 0 to 30, and a1+a2+a3+b1+b2 is an integer of 3 to 30,P1, P2, and P3 are, independently of each other, —CRaRb— or —(CRaRb)rO—, r is an integer of 1 to 3,
Q1 and Q2 are, independently of each other, q1-(p1)c1-q2-(p2)c2-q3, q1 and q3 are, independently of each other, —O— or —S—, q2 is —CH?CH—, —C?C—, —N?N—,





in which the hydrogen group bonded to the carbon is substituted with F, Cl, Br, or I, or unsubstituted, p1 and p2 are, independently of each other, —CRaRb—, c1 and c2 are, independently of each other, an integer of 0 to 2,Ra and Rb are, independently of each other, H, F, Cl, Br, or I,
Rc, Rd, and Re are, independently of each other, H, F, Cl, Br, or I,
U is one selected from the group consisting of a hydroxyl group, fluorine, chlorine, iodine, a substituted or unsubstituted alkyl group having 1 to 15 carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 15 carbon atoms, a substituted or unsubstituted cycloalkyl group having 3 to 15 carbon atoms, a substituted or unsubstituted alkenyl group having 2 to 15 carbon atoms, and a substituted or unsubstituted alkynyl group having 2 to 15 carbon atoms,
o is an integer between 0 and 16,
m is an integer of 2 to 8, and
the aromatic ring (Ar) is selected from the group consisting of an aromatic ring of the following Structural Formula 3, an aromatic ring of the following Structural Formula 6, an aromatic ring of the following Structural Formula 8, an aromatic ring of the following Structural Formula 10 and an aromatic ring of the following Structural Formula 12:




in Structural Formula 3, T1 to T14 are all C; or some of T1 to T14 are N, P, B or Si independently of each other and remainders are C,
G1, G3, G5, G6, G7, G8, G10, G12, G13, and G14 represent substitution positions of the aromatic ring,
a first pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G6 and G7 positions,
a second pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G13 and G14 positions,
U is bonded to any one of remaining G1, G3, G5, G8, G10, and G12 positions or not, and
o is an integer of 0 to 6;




in Structural Formula 6, T1 to T13 are all C; or some of T1 to T13 are N, P, B or Si independently of each other and remainders are C,
G1, G2, G4, G5, G7, G8, G10, and G11 represent substitution positions of the aromatic ring,
a first pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G4 and G5 positions,
a second pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G10 and G11 positions,
U is bonded to any one of remaining G1, G2, G7, and G8 positions or not, and
o is an integer of 0 to 4;




in Structural Formula 8, T1 to T14, T16 and T17 are all C; or some of T1 to T14, T16 and T17 are N, P, B or Si independently of each other and remainders are C,
G1, G2, G4, G5, G7, G8, G9, G11, G12, and G14 represent substitution positions of the aromatic ring,
a first pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G4 and G5 positions,
a second pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G11 and G12 positions,
U is bonded to any one of remaining G1, G2, G7, G8, G9, and G14 positions or not, and
o is an integer of 0 to 6;




in Structural Formula 10, T1 to T18 are all C; or some of T1 to T18 are N, P, B or Si independently of each other and remainders are C,
G1, G2, G3, G6, G7, G8, G9, G12, G13, G14, G15, and G18 represent substitution positions of the aromatic ring,
a first pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G1 and G2 positions,
a second pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G7 and G8 positions,
a third pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G13 and G14 positions,
U is bonded to any one of remaining G3, G6, G9, G12, G15, and G18 positions or not, and
o is an integer of 0 to 6;




in Structural Formula 12, T1 to T24 are all C; or some of T1 to T24 are N, P, B or Si independently of each other and remainders are C,
G1, G3, G4, G6, G7, G9, G10, G12, G13, G15, G16, and G18 represent substitution positions of the aromatic ring,
a first pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G6 and G7 positions,
a second pair of -A1-(L1)n1-Y1—X1 and -A2-(L2)n2-Y2—X2 are bonded to G15 and G16 positions,
U is bonded to any one of remaining G1, G3, G4, G9, G10, G12, G13, and G18 positions or not, and
o is an integer of 0 to 8.

US Pat. No. 11,066,347

PURIFICATION AND LIQUEFACTION OF BIOGAS BY COMBINATION OF A CRYSTALLIZATION SYSTEM WITH A LIQUEFACTION EXCHANGER


1. A process for production of liquid methane from biogas that comprises methane, water, and carbon dioxide, said process comprising the steps of:condensing amounts of water from a biogas feed stream by lowering a temperature of the biogas feed gas stream in a condensing exchanger to a temperature of between ?57° C. and ?75° C.;
recovering a water-depleted feed gas stream from the condensing exchanger having a water content lower than that of the raw feed gas stream;
injecting the water-depleted feed gas stream into a bottom portion of a CO2 crystallizer system;
feeding a stream predominantly comprising liquid methane into a top portion of the CO2 crystallizer countercurrentwise to the injected feed gas stream, thereby crystallizing amounts of CO2 contained in the injected water-depleted feed gas stream;
recovering gaseous methane from the upper portion of the CO2 crystallizer;
liquefying the recovered gaseous methane with liquefaction exchanger, a cooling power of the liquefaction exchanger being supplied by a refrigerant;
recovering a stream of liquid methane at an outlet of the liquefaction exchanger; and
filtering solid CO2 particles from the recovered stream of liquid methane to produce a CO2-depleted stream of liquid methane having a CO2 content of between 2 ppm and 1000 ppm.

US Pat. No. 11,066,346

METHOD AND SYSTEM FOR OBTAINING ONE OR MORE OLEFINS

LINDE AKTIENGESELLSCHAFT,...


1. Method (100, 200) of obtaining one or more olefins, in which, using an oxidative coupling of methane (10), a gas mixture comprising hydrogen, methane, carbon monoxide and higher-boiling hydrocarbons than methane is formed and is subjected to a low-temperature separation (1-5), characterized in that the low-temperature separation (1-5) is conducted using a rectification column (2) having a first separation region (21), a second separation region (22) arranged above the first separation region (21), and a condenser-evaporator (23), wherein the gas mixture is cooled, fed at least partly as first separation feed into the first separation region (21) and subjected to a first rectification in the first separation region (21) to form a first tops gas and a first bottoms liquid, wherein, using a first proportion of the first tops gas in the condenser-evaporator (23), a condensate which is recycled to the first separation region and, using a second proportion of the tops gas, a second separation feed which is fed into the second separation region (22) are formed, and wherein the second separation feed is subjected to a second rectification in the second separation region (22) to form a second tops gas and a second bottoms liquid.

US Pat. No. 11,066,345

PROCESSES FOR INCREASING AN OCTANE VALUE OF A GASOLINE COMPONENT

UOP LLC, Des Plaines, IL...


1. A process for increasing an octane value of a gasoline component, the process comprising:separating a naphtha feed in a naphtha splitter into a stream comprising C6 and lighter boiling hydrocarbons, a C7 stream comprising C7 hydrocarbons including C7 paraffins and methylcyclohexane, and a heavy stream comprising C8 hydrocarbons;
dehydrogenating at least a portion of the stream comprising C7 hydrocarbons in a first dehydrogenation zone to form an intermediate dehydrogenation effluent comprising the C7 paraffins and toluene, the first dehydrogenation zone comprising a catalyst and operated under conditions to convert methylcyclohexane to toluene and minimize cracking reactions;
dehydrogenating the intermediate dehydrogenation effluent in a second dehydrogenation zone to form a C7 dehydrogenation effluent, the C7 dehydrogenation zone comprising a catalyst and the C7 dehydrogenation effluent comprising C7 olefins, wherein the C7 dehydrogenation effluent has an increased olefins content compared to an olefins content of the intermediate dehydrogenation effluent; and,
blending the C7 dehydrogenation effluent as a gasoline component in a gasoline pool.

US Pat. No. 11,066,344

METHODS AND SYSTEMS OF UPGRADING HEAVY AROMATICS STREAM TO PETROCHEMICAL FEEDSTOCK

SAUDI ARABIAN OIL COMPANY...


1. A system for conversion of alkyl-bridged non-condensed alkyl multi-aromatic compounds to alkyl mono-aromatic compounds, the system comprising:a first separator adapted to receive a feed stream containing one or more of heavy alkyl aromatic compounds and one or more alkyl-bridged non-condensed alkyl multi-aromatic compounds having at least two benzene rings connected by an alkyl bridge group with at least two carbons and the benzene rings being connected to different carbons of the alkyl bridge group, and produces a first product stream containing C9 and C10 compounds and a second product stream containing one or more of heavy alkyl aromatic compounds and alkyl-bridged non-condensed alkyl multi-aromatic compounds;
a hydrodearylation reactor fluidly coupled to the first separator and adapted to receive a hydrogen stream and the second product stream and to produce a third product stream in presence of a catalyst, the third product stream containing one or more alkyl mono-aromatic compounds; and
a second separator fluidly coupled to the hydrodearylation reactor and adapted to receive the third product stream and to produce a benzene-containing stream, a toluene-containing stream, a C8-rich stream, and a bottoms C9+ stream, the system adapted to combine the first product stream containing C9 and C10 compounds from the first separator and the bottoms C9+ stream from the second separator.

US Pat. No. 11,066,342

FERTILIZER COMPOSITION AND METHODS OF MAKING AND USING SAME

SABIC GLOBAL TECHNOLOGIES...


1. A fertilizer core particle having an outer surface and comprising one or more fertilizer additives, from about 45 wt % to about 99 wt % of one or more binders, and from about 30 wt % to about 50 wt % of one or more pH buffering agents, wherein the one or more binders comprises from 40 wt % to 60 wt % of Plaster of Paris and from 5 wt % to 10 wt % of flour comprising bleached wheat flour based on the weight of the fertilizer core particle, and wherein the one or more fertilizer additive comprises from more than 0 wt % to 5 wt % of N-(n-butyl) thiophosphoric triamide based on the weight of the fertilizer core particle.

US Pat. No. 11,066,340

FERTILIZERS CONTAINING SLOW AND FAST RELEASE SOURCES OF BORON

The Mosaic Company, Plym...


11. A method of forming a fertilizer product comprising a plurality of granules, each granule containing multiple sources of boron, the method comprising:providing a source of potassium;
adding a first source of boron having a first solubility configured to release boron primarily during a first part of a growing season to the source of potassium;
adding a second source of boron having a second solubility less than the first source configured to release boron primarily during a second part of the growing season to the primary nutrient source, wherein the second source of boron comprises a calcium based source of boron;
compacting the source of potassium, the first source of boron, and the second source of boron to form a fertilizer composition; and
crushing the compacted fertilizer composition to form the plurality of granules.

US Pat. No. 11,066,339

ARTICLE FOR HIGH TEMPERATURE SERVICE

General Electric Company,...


1. An article, comprising:a substrate comprising a ceramic matrix composite;
a first layer disposed over the substrate, the first layer comprising a substantially interconnected silicon source material comprising elemental silicon, and a secondary material, wherein the elemental silicon is present in the first layer in a range from about 10% by volume to about 70% by volume; and
a second layer disposed over the first layer, the second layer comprising a membrane material in mass transfer communication with the silicon source material, wherein the membrane material comprises a silicide, silicon carbide, silicon boride, a carbosilicide, or a combination comprising any one or more of these, wherein the second layer includes at least 80% by volume of the membrane material;
wherein, for a given temperature above about 1200 degrees Celsius, silicon diffusion through the membrane material exceeds the rate at which oxygen diffuses through silica.

US Pat. No. 11,066,337

INORGANIC FOAM BASED ON CALCIUM SULFOALUMINATE


1. A process for preparing an inorganic foam comprising the steps of(1) mixing(i) at least one group of inorganic particles;
(ii) at least one amphiphilic compound;
(iii) at least one inorganic binder mixture comprising(iiia) at least one calcium sulfoaluminate mixture, and optionally
(iiib) at least one further inorganic binder selected from the group consisting of hydraulic binders, latent hydraulic binders, pozzolanic binders, and mixtures thereof;

(iv) water; and optionally
(v) at least one additive; and

(2) foaming the resulting foam formulation by chemical, physical or mechanical foaming; wherein the at least one calcium sulfoaluminate mixture contains a) ye'elimite (4CaO×3Al2O3×SO3) and optionally belite (2CaO×SiO2) and b) anhydrite (CaSO4), calcium sulfate hemihydrate (CaSO4×0.5H2O) and/or gypsum (CaSO4×2H2O), in a weight ratio of a):b) of from 90:10 to 60:40.

US Pat. No. 11,066,336

HONEYCOMB STRUCTURE

NGK Insulators, Ltd., Na...


1. A honeycomb structure comprising:a plurality of prismatic columnar honeycomb segments;
bonding layers that bond side faces of the plurality of honeycomb segments with respect to each other; and
a circumferential wall that is disposed to surround the plurality of honeycomb segments bonded with the bonding layers in a state where the plurality of honeycomb segments are arrayed in a grid pattern, wherein
each of the honeycomb segments includes porous partition walls disposed to surround a plurality of cells extending from an inflow end face to an outflow end face in an axial direction and a segmented outer wall disposed to surround the partition walls,
an end of each of the cells in each of the honeycomb segments is plugged by a plugging portion at any one of the inflow end face and the outflow end face,
the bonding layers include bottomed-hollow voids which extend toward an internal side in the axial direction from the inflow end face or the outflow end face and which are formed only at intersections that bond the honeycomb segments in the grid pattern, and
a ratio of a depth of each void in the axial direction to a length of each honeycomb segment in the axial direction is 5% or more.

US Pat. No. 11,066,335

ARTICLES FOR CREATING HOLLOW STRUCTURES IN CERAMIC MATRIX COMPOSITES

GENERAL ELECTRIC COMPANY,...


1. A method of fabricating a composite component comprising: at least partially covering a core having an organic binder and at least a silicon component with a reinforcing fiber material, wherein the core is a non-fugitive hollow core which includes at least one portion having a non-linear geometry, wherein the non-fugitive hollow core is formed by:(a) contacting a cured portion of a workpiece with a liquid photopolymer;
(b) irradiating a portion of the liquid photopolymer adjacent to the cured portion through a window contacting the liquid photopolymer; and
(c) removing the workpiece from the uncured liquid photopolymer; wherein the non-fugitive hollow core comprises at least one hollow passage, wherein the hollow passage defines at least one cooling passage, wherein at least partially covering the core further comprises:
placing the non-fugitive hollow core on at least one first layer of the reinforced fiber material, wherein the reinforced fiber material is pre-impregnated with a ceramic matrix precursor material, wherein the at least one first layer comprises a plurality of layers of either fabric or pre-impregnated fabric with a matrix precursor: and
adding at least one second layer of pre-impregnated reinforcing fiber material on top of the non-fugitive hollow core, wherein the at least one second layer comprises a plurality of layers of fabric or pre impregnated fabric, wherein the at least one first layer and the at least one second layer are densified to consolidate the at least one first layer and the at least one second layer of reinforcing fiber material.

US Pat. No. 11,066,334

BINDERLESS CBN SINTERING WITH CUBIC PRESS

SCHLUMBERGER TECHNOLOGY C...


1. A method of sintering a binderless cubic boron nitride body, comprising:providing a boron nitride particle mixture into a pressure chamber, the boron nitride particle mixture comprising a first type of boron nitride particles and boron nitride filler particles, the first type of boron nitride particles comprising a cubic boron nitride particle mixture having a multi modal particle size distribution, the boron nitride filler particles comprising hexagonal boron nitride particles; and
sintering the boron nitride particle mixture in the pressure chamber to form the binderless cubic boron nitride body, the sintering comprising:generating a pressure in the pressure chamber of less than 7.7 GPa; and
heating the boron nitride particle mixture to a temperature ranging from 1900° C. to 2300° C.,

wherein the binderless cubic boron nitride body has a density of at least 97 percent.

US Pat. No. 11,066,333

CERAMIC COMPOSITE MATERIALS, ARTICLES, AND METHODS

The Florida State Univers...


1. A method of forming a composite material, the method comprising:providing a mixture comprising (i) ultra-high temperature ceramic particles and (ii) a liquid preceramic precursor;
heating the mixture at a temperature for a time effective to cure the liquid preceramic precursor to form a solid mixture;
subjecting the solid mixture to one or more forces to form particles of the solid mixture; and
pressing the particles of the solid mixture into a mold having a pre-selected shape to form the composite material.

US Pat. No. 11,066,332

DIELECTRIC CERAMIC COMPOSITION AND CERAMIC ELECTRONIC COMPONENT

SHOEI CHEMICAL INC., Tok...


1. A dielectric ceramic composition comprising a first component and a second component, wherein:the dielectric ceramic composition is a sintered compact obtained by mixing a dielectric raw material for the first component obtained by calcining starting materials for the first component and a raw material for the second component, and firing them;
the first component comprises: an oxide of Ca in a content of 0 to 35.85 mol % in terms of CaO; an oxide of Sr in a content of 0 to 47.12 mol % in terms of SrO; an oxide of Ba in a content of 0 to 51.22 mol % in terms of BaO; an oxide of Ti in a content of 0 to 17.36 mol % in terms of TiO2; an oxide of Zr in a content of 0 to 17.36 mol % in terms of ZrO2; an oxide of Sn in a content of 0 to 2.60 mol % in terms of SnO2; an oxide of Nb in a content of 0 to 35.32 mol % in terms of Nb2O5; an oxide of Ta in a content of 0 to 35.32 mol % in terms of Ta2O5; and an oxide of V in a content of 0 to 2.65 mol % in terms of V2O5, at the specified content based on the total number of moles of the first component in terms of the above oxides;
the first component comprises at least one selected from the oxide of Ca, the oxide of Sr, and the oxide of Ba, at least one selected from the oxide of Ti and the oxide of Zr, and at least one selected from the oxide of Nb and the oxide of Ta; and wherein, based on a total number of moles of the first component in terms of the above oxides, a total content of the oxide of Ca in terms of CaO, the oxide of Sr in terms of SrO, and the oxide of Ba in terms of BaO is 48.72 to 51.22 mol %; a total content of the oxide of Ti in terms of TiO2, the oxide of Zr in terms of ZrO2, and the oxide of Sn in terms of SnO2 is 15.97 to 17.36 mol %; and a total content of the oxide of Nb in terms of Nb2O5, the oxide of Ta in terms of Ta2O5, and the oxide of V in terms of V2O5 is 31.42 to 35.31 mol %; and
the dielectric ceramic composition comprises at least an oxide of Mn in a content of more than 0% by mass and 3.5% by mass or less in terms of MnO with respect to the total mass of the first component in terms of the above oxides as the second component.

US Pat. No. 11,066,331

MATERIAL INCLUDING BORON SUBOXIDE AND METHOD OF FORMING SAME


1. A material, having a body comprising B6Ox, wherein the body has a thickness of at least 2 mm; and wherein the B6Ox comprises lattice constant a and lattice constant c, wherein A represents a value of constant a, and C represents a value of constant c, wherein C is at most 12.318, wherein A is at least 5.386.

US Pat. No. 11,066,328

LOW REFLECTIVITY COATING AND METHOD AND SYSTEM FOR COATING A SUBSTRATE

SURREY NANOSYSTEMS LIMITE...


1. A method of coating a substrate with carbon nanostructures to produce a non-transparent coating, including the steps of:(i) coating a substrate with a polymer solution which is a polymer dissolved in a first solvent;

(ii) providing a suspension of carbon nanostructures in a second solvent;(iii) spray-coating the suspension onto the substrate so that the carbon nanostructures are incorporated into the polymer solution;
(iv) drying the substrate to evaporate the first and second solvents to leave a coating of polymer and carbon nanostructures;
(v) plasma etching the coating to selectively remove at least some of said polymer in order to leave the carbon nanostructures.

US Pat. No. 11,066,327

VACUUM COMPATIBLE ELECTRICAL INSULATOR

General Fusion Inc., Bri...


11. A plasma system comprising:a vacuum vessel;
a first electrode and a second electrode mounted in the vacuum vessel and spaced apart to form a gap therein between, the first and second electrodes operable to apply a voltage between the first and the second electrodes; and
an electrical insulator mounted between the two electrodes, the electrical insulator comprising an electrically insulating glass substrate with at least one face surface, and an electrically insulating ceramic layer coating at least a portion of the at least one face surface, the ceramic layer configured to be exposed to plasma inside the vacuum vessel and to protect the portion of the at least one face surface from the plasma.

US Pat. No. 11,066,323

GLASS WITH HIGH SURFACE STRENGTH

Corning Incorporated, Co...


1. An alkali aluminosilicate glass article comprising: a compressive stress layer extending from a surface of the alkali aluminosilicate glass to a depth of layer (DOL), the compressive stress layer having a maximum compressive stress of at least 400 MPa at the surface, wherein the alkali aluminosilicate glass article comprises:from about 58 mol % to about 65 mol % SiO2;
from about 0.5 mol % to about 3 mol % P2O5;
at least about 11 mol % Al2O3;
Na2O; and
Li2O,
wherein the ratio of the amount of Li2O(mol %) to Na2O(mol %) (Li2O/Na2O) is less than 1.0, and wherein the alkali aluminosilicate glass article is free of B2O3,
wherein the alkali aluminosilicate glass article comprises a relationship R2O(mol %)+R?O(mol %)?Al2O3(mol %)?P2O5(mol %) that is greater than 0 mol %, wherein R2O=the total amount of Li2O and Na2O present in the alkali aluminosilicate glass article and R?O is a total amount of divalent metal oxides present in the alkali aluminosilicate glass article, and
wherein at least one of:
(i) the glass article further comprises a thickness and a central region extending from the DOL to a depth equal to 0.5 times the thickness, and wherein the central region is free of K2O; or
(ii) the alkali aluminosilicate glass article comprises less than 1 mol % K2O,
wherein the alkali aluminosilicate glass article comprises a liquidus viscosity of at least 200 kPoise.

US Pat. No. 11,066,322

SELECTIVELY HEAT-TREATED GLASS-CERAMIC FOR AN ELECTRONIC DEVICE

APPLE INC., Cupertino, C...


1. An electronic device comprising:a display;
a housing;
a cover sheet affixed to the housing and covering the display, the cover sheet comprising:a first region having an optical haze and a first median crystal size;
a second region positioned over the display having a second median crystal size that is smaller than a crystal size that causes scattering of light; and
a third region positioned between the first region and the second region, the third region defining a transition between the first region and the second region and including crystals that range in size from the first median crystal size to the second median crystal size, the transition having a gradient of crystal sizes between the first region and the second region, the gradient defining a uniform profile extending from a top surface of the cover sheet to a bottom surface of the cover sheet.


US Pat. No. 11,066,321

MOLD, MOLDING APPARATUS, PRODUCTION METHOD OF MOLDED BODY, AND MOLDED BODY

AGC INC., Chiyoda-ku (JP...


1. A molded body which is a plate-like molded body having a first region and a second region provided on an outer periphery of the first region,wherein a radius of curvature of the second region is smaller than a radius of curvature of the first region, and
when a main surface of the molded body on the side of a direction where the second region is bent relative to the first region is defined as a first main surface, and a main surface on an opposite side thereto is defined as a second main surface, in a top view of the molded body seen from the second main surface side, in a case where a long-side direction of the molded body is defined as an m-axis, a short-side direction orthogonal to the m-axis is defined an n-axis, a center of gravity of the molded body is defined as a central point (m,n)=(0,0), a long-side dimension of the molded body is defined as M, and a short-side dimension of the molded body is defined as N, a stress integral value S in a plate thickness direction on a line segment A joining a point (M/4,0) and a point (?M/4,0) and a line segment B joining a point (0,N/4) and a point (0,?N/4) is 0.1 MPa or more and 3.0 MPa or less.

US Pat. No. 11,066,320

COVER GLASS AND A MANUFACTURING METHOD THEREOF USING GLASS WOOL

SAMSUNG DISPLAY CO., LTD....


1. A cover glass including glass wool, the cover glass comprising:a first area; and
a second area connected to the first area and bent away from the first area,
wherein the second area includes a plurality of protrusions and valleys between the protrusions which are adjacent, and
wherein the second area further includes the glass wool to fill the valleys between the protrusions.

US Pat. No. 11,066,319

METHOD AND FACILITY FOR MANUFACTURING A FIBERGLASS MATERIAL


1. A process for manufacturing a glass fiber product in which molten glass is converted into a glass fiber product, said process comprising the steps of:producing molten glass in a melting furnace heated by combustion of a fuel with a rich oxidizer having an oxygen content of 80 vol % to 100 vol %, with generation of heat and flue gases, said generated flue gases being discharged from the melting furnace at a temperature between 1000° C. and 1600° C.;
heating air by heat exchange with the discharged flue gases in a primary heat exchanger to produce hot air, the hot air being at a temperature between 500° C. and 800° C.; and
before the rich oxidizer and the fuel are combusted, preheating the rich oxidizer and/or the fuel by heat exchange with the hot air in a secondary heat exchanger to correspondingly produce preheated rich oxidizer and/or preheated fuel and also moderated air that is obtained from the hot air, the moderated air being at a temperature between 200° C. and 500° C., the molten glass being converted into a glass fiber product by:
spinning the molten glass into at least one stream;
attenuation of the at least one stream into one or more filaments;
collecting the filament or filaments;
optionally sizing the filament or filaments upstream of their collection;
optionally applying adhesive to the filament or filaments before or after their collection, followed by a drying of the applied adhesive using a drying agent;
optionally crosslinking dried adhesive-treated collective filament or filaments and;
optionally texturing the filament or filaments or strands containing them,
wherein: the moderated air resulting from the secondary heat exchanger is employed during conversion of the molten glass into the glass fiber product in at least one of the following stages:
during the attenuation of the at least one stream in the form of one or more attenuation gas currents,
during the sizing of the filament or filaments upstream of their collection in the form of a spraying agent for a sizing agent,
during application of adhesive to the filament or filaments before or after their collection in the form of a spraying agent for an adhesive binder, during the drying of the filament or filaments by using the moderated air as the drying agent, and during the texturing of the filament or filaments or the strands containing them in the form of a texturing gas current.

US Pat. No. 11,066,317

SYSTEM FOR REMOVAL OF NITRATE AND CHROME FROM WATER


1. A process to remove nitrates and chrome from water, which process comprises:passing incoming nitrate and chrome contaminated water through a nanofiltration membrane;
pumping retentate liquid rejected from the nanofiltration membrane to effluent or returning to the nanofiltration membrane;
delivering permeate from said nanofiltration membrane through a well screen upper collector in an open atmospheric bed having a strong base ion exchange resin;
extracting, with a pump, said permeate through said ion exchange resin, through a gravel layer beneath said resin in said open atmospheric bed and from said open atmospheric bed; and
periodically regenerating said strong base ion exchange resin.

US Pat. No. 11,066,315

INDUCED SLUDGE BED ANAEROBIC REACTOR SYSTEM


1. An induced bed bioreactor (“IBR”) system comprising:a vessel configured to induce a sludge bed;
a septum located within the vessel, the septum comprising a plurality of vanes configured to minimize clogging of the vessel based on an orientation of each adjacent pair of the plurality of vanes, where the orientation comprises maintaining a distance p between the each adjacent pair of vanes that is greater than a maximum rigid dimension of clogging waste anticipated to enter the vessel; and
a macerator coupled to the vessel and configured to limit the maximum rigid dimension of the clogging waste to a particular maximum size, where the distance p is substantially the same as or greater than the particular maximum size.

US Pat. No. 11,066,314

WATER TREATMENT AERATOR HAVING BUBBLE DIFFUSER

BioMicrobics, Inc., Lene...


1. An aerator assembly for wastewater treatment, said aerator assembly comprising:an upright draft tube including a sidewall and presenting an open top tube end and an open bottom tube end,
said sidewall including a circumferential groove that defines an inwardly projecting rib adjacent the bottom tube end; and
an air supply assembly including an air supply conduit connectable to a source of air,
said air supply assembly further including a diffuser body that has an inlet aperture and a bubble generator fluidly connected to the inlet aperture,
said inlet aperture being fluidly connected to the air supply conduit such that the bubble generator is configured to receive air from the source of air,
said bubble generator comprising a plurality of air openings,
said diffuser body enclosed within the sidewall and having a periphery that sealingly engages the rib so as to restrict an upward flow of wastewater through the draft tube past the diffuser body.

US Pat. No. 11,066,312

METHOD AND APPARATUS FOR SEPARATING LOW DENSITY PARTICLES FROM FEED SLURRIES

NEWCASTLE INNOVATION LIMI...


1. Apparatus for separating low density particles from feed slurries, said apparatus comprising: a separation chamber having an upper region, a lower region, a perforated upper end defining an upper boundary of the upper region, and a lower end defining a lower boundary of the lower region;a wash water feeder arranged above the perforated upper end of the separation chamber, the wash water feeder fluidly communicating with the upper region of the separation chamber and being configured to force wash water under pressure through the perforated upper end and into the upper region of the separation chamber such that the wash water directly contacts the low density particles in the upper region of the separation chamber in the absence of a free surface between the low density particles in the upper region of the separation chamber and the perforated upper end;
a plurality of inclined channels located in the lower region of the separation chamber;
a conduit extending into the separation chamber, the conduit having an inlet end configured for receiving slurry and a discharge end for discharging a bubbly mixture into the separation chamber;
an inlet arranged to feed the gas into the conduit and being configured to allow the gas and the slurry to mix within the conduit and discharge as the bubbly mixture from the discharge end of the conduit;
the conduit being arranged and configured so that during operation of the apparatus, the bubbly mixture flows through the separation chamber and into the inclined channels such that the low density particles escape the downward bubbly mixture flow and slide up the downwardly facing inclined surfaces of the inclined channels while higher density particles in the bubbly mixture travel down the inclined channels;
a first outlet arranged in the separation chamber above the inclined channels and discharge end and being configured to allow concentrated suspensions of the low density particles to be removed from the separation chamber in a foam froth, and
a second outlet arranged in the separation chamber below the inclined channels and being configured to allow the higher density particles to be removed from the separation chamber at a controlled rate;
wherein during operation of the apparatus, the bubbly mixture forms a fluidized bed of bubbles in the separation chamber above the inclined channels.

US Pat. No. 11,066,311

METHOD OF USING A FILTER MEDIA FOR FILTRATION

Brita I.P, Oakland, CA (...


1. A method of using a filter media for filtration, comprising:1. providing a housing having,a frame extending along a longitudinal axis from a first end to a second end to define a channel within the frame, wherein the frame includes a first plurality of radial openings through a surface of the frame, wherein the first plurality of openings are defined between a plurality of first support members of the frame extending between the first end and the second end and one or more second support members of the frame that connect to one or more first support members of the plurality of first support members, wherein the plurality of first support members extend to and between a first end cap at the first end and a second end cap at the second end, wherein the frame defines a slot that extends parallel to the longitudinal axis and located entirely within a radial outer periphery defined by the first and second support members; and
a casing secured about at least a portion of the frame and at least partially covering at least a portion of the frame while maintaining a space between at least a portion of the casing and at least a portion of the frame, the casing comprising a second plurality of radial openings in fluid communication with the channel via the first plurality of radial openings in the frame, wherein the second plurality of radial openings in the casing, the first plurality of radial openings in the frame, the channel, and an aperture in the first end of the frame form a fluid flow path; and

2. providing an activated carbon filter media as the filter media, wherein the filter media is not granular, a foam, or a block positioned in the space between the frame and the casing such that at least a portion of the filter media presents a curved surface to a fluid to be filtered; and
positioning a first end and a second end of the filter media in the slot formed by the frame to attach the filter media to the frame;
wherein the fluid can flow through the fluid flow path and pass through the filter media at the curved surface.

US Pat. No. 11,066,310

TUNGSTEN PENTACHLORIDE CONDITIONING AND CRYSTALLINE PHASE MANIPULATION


1. A WCl5-containing composition having 10% weight of WCl5 to 40% weight of WCl5 in the form of Phase 1 crystal structure WCl5 as determined by X-ray diffraction.

US Pat. No. 11,066,309

DIRECT SYNTHESIS OF HIGH-ASPECT RATIO ZEOLITE NANOSHEETS

Regents of the University...


1. A material comprising:a planar layer of MFI zeolite; and
a MFI zeolite particle embedded in the planar layer of MFI zeolite,
wherein the planar layer has a thickness in a range between 4 nm and 10 nm for at least 70% of a basal area of the planar layer.

US Pat. No. 11,066,308

PREPARATION OF METAL DIBORIDE AND BORON-DOPED POWDERS

United Technologies Corpo...


1. A method for producing a powder for use in high temperature ceramic applications, the method comprising:producing a boriding gas stream from a first powder in a first fluidizing bed reactor;
delivering the boriding gas stream to a second fluidized bed reactor through a conduit fluidly connecting the first and second fluidized bed reactors, the second fluidized bed reactor containing a second powder selected from the group consisting of metal oxides, metal hydroxides, and alloys;
fluidizing the second powder in the second fluidized bed reactor; and
mixing the second powder with the boriding gas stream such that a metal boride powder or boron-doped powder is formed.

US Pat. No. 11,066,307

POLYANION ACTIVE MATERIALS AND METHOD OF FORMING THE SAME


1. A method of forming a polyanion active material comprising:providing a carbon source;
providing a mobile ion source;
providing an active metal material;
providing a network material;
providing a flux material;
mixing the carbon source, mobile ion source, active metal material, flux material and network material;
heating the mixture to a predetermined temperature in a non-oxidizing atmosphere forming a reaction product; and
washing the reaction product forming a carbon coated polyanion active material.

US Pat. No. 11,066,306

DIATOMACEOUS ENERGY STORAGE DEVICES

Printed Energy Pty Ltd, ...


1. A frustule comprising:a plurality of perforations through the frustule; and
a layer of silver nanostructures substantially covering at least interior and exterior surfaces of the frustule,
wherein the frustule is included in an electrode.

US Pat. No. 11,066,305

POROUS SILICON MANUFACTURED FROM FUMED SILICA

ionobell Inc, San Jose, ...


1. A silicon material comprising:a primary structure comprising silicon nanoparticles with primary sizes between about 2 nanometers (nm) and about 150 nm;
a secondary structure comprising clusters of the silicon nanoparticles, the clusters having a cluster size between about 100 and 1000 nm; and
a tertiary structure comprising agglomers of the clusters, the agglomers having an agglomer size between about 2 micrometer (?m) and 50 ?m;
wherein the nanoparticles cooperatively form primary pores within the clusters.

US Pat. No. 11,066,304

POLYMER GRAFTED GRAPHENE AND METHOD FOR PREPARATION THEREOF

LG Chem, Ltd.


1. Graphene in which a polymer structure represented by the following Chemical Formula 1 or 2 is bonded to the surface of the graphene:



in Chemical Formula 1,
n is an integer of 0 to 20,
m1 is an integer of 1 to 10000,
R1 and R2 are each independently hydrogen, or C1-4 alkyl,
R3 is hydrogen, C1-30 alkyl, C1-30 hydroxyalkyl, or




R4 is C2-5 alkylene,
l is an integer of 1 to 10000,
* means a bond covalently bonded to the surface of the graphene,




in Chemical Formula 2,
n is an integer of 0 to 20,
m1 is an integer of 1 to 10000,
m2 is an integer of 1 to 10000,
R1, R?1, R2, and R?2 are each independently hydrogen, or C1-4 alkyl,
R3 and R?3 are each independently hydrogen, C1-30 alkyl, C1-30 hydroxyalkyl, or




R4 is C2-5 alkylene,
l is an integer of 1 to 10000,
* means a bond covalently bonded to the surface of the graphene,
with the proviso that at least one of R1 and R?1; R2 and R?2; and R3 and R?3 is different from each other.

US Pat. No. 11,066,303

ELECTROCHEMICALLY EXPANDED MATERIALS AND REACTOR AND METHOD FOR PRODUCING THE SAME


1. A reactor configured to deliver electric current to a parent material to produce expanded parent material, the reactor comprising:an electrically insulating container, comprising:
an expandable chamber configured to contain the parent material, wherein the expandable chamber is configured to expand in at least one direction in order to accommodate expansion of the parent material as it transitions to the expanded parent material, while also maintaining pressure on the parent material and any expanded parent material sufficient to maintain the conditions necessary to generate the expanded parent material;
an electrolyte chamber configured to be in fluid communication with an electrolyte solution; and
a porous membrane separating the expandable chamber and the electrolyte chamber configured to allow ions to pass through the porous membrane but not the parent material and any expanded parent material; wherein the porous membrane is configured to contain the pressure of the expanded parent material; and
an electrical system, comprising:a first electrode configured to be in electrical communication with an interior of the expandable chamber and any parent material disposed in the expandable chamber; and
a second electrode configured to be in electrical communication with the electrolyte chamber and any electrolyte solution disposed in the electrolyte chamber.


US Pat. No. 11,066,302

METHOD FOR PRODUCING INORGANIC OXIDE IN FORM OF THIN FILM

KAO CORPORATION, Tokyo (...


1. A method for producing an inorganic oxide in a form of a thin film, the method comprisingproviding a stream of a first liquid having an inorganic oxide precursor dissolved therein,
providing a separate stream of a second liquid having a substance dissolved therein, the substance reacting with the inorganic oxide precursor of the first liquid to form an inorganic oxide derived from the inorganic oxide precursor, and
bringing said first liquid and said second liquid into contact with each other,
wherein a segment size of a cross-section perpendicular to a flow direction of the first liquid at a time of contact between the first and second liquids is maintained at 500 ?m or smaller, thereby providing an inorganic oxide in the form of a thin film having an average thickness of 0.01 ?m or larger and 1.5 ?m or smaller.

US Pat. No. 11,066,301

SYSTEM FOR EXTRACTING GASEOUS MOLECULES FROM AIR


1. A system for separating and storing molecules, atoms and/or ions from air, comprising:at least one air collecting means, comprisingat least one collecting tank configured to receive molecules, atoms and/or ions separated from air through an inlet; and
at least two membranes serially fit in the inlet of the collecting tank at an appropriate distance from each other and configured to let a specified pre-determined size of molecules, atoms and/or ions to pass through the at least two membranes;

at least one storing tank for storing the separated molecules, atoms and/or ions, and
at least one outlet,wherein a first of the at least two membranes filters out gaseous molecules that have a size smaller than a first pre-determined size and a second of the at least two membranes filters out gaseous molecules that have a second pre-determined size, wherein the second pre-determined size is smaller than the first pre-determined size.


US Pat. No. 11,066,300

METHOD OF OPERATING A SYNGAS PLANT FOR A WIDE RANGE OF HYDROGEN AND CO CO-PRODUCTION


1. A method for achieving a gas with a variable hydrogen to carbon monoxide ratio in a system comprising:a warm raw syngas stream, a first syngas cooler,
a second syngas cooler,
a water/gas shift reactor,
an acid gas scrubber,
a temperature swing adsorber
a carbon monoxide separator, and
a hydrogen separator,

the method comprising:splitting the warm raw syngas stream into a first portion and a second portion, the second portion having a hydrogen portion flowrate, and the warm raw syngas stream having a total syngas flow rate,
sending the first portion of the warm raw syngas stream to the first syngas cooler, then to the acid gas scrubber, temperature swing adsorber, and carbon monoxide separator, thereby producing a first hydrogen enriched stream and a carbon monoxide rich stream having a carbon monoxide portion flowrate,
sending the second portion of the warm raw syngas stream to the water/gas shift reactor, thereby producing a shifted syngas stream, then sending the shifted syngas stream to the second syngas cooler, thereby producing a second hydrogen enriched stream,
combining the first hydrogen enriched stream and the second hydrogen enriched stream and sending the combined stream to the hydrogen separator, thereby producing a product hydrogen stream having a hydrogen flowrate,
varying the hydrogen flowrate by varying the second portion flowrate, while maintaining a constant total syngas flow rate.

US Pat. No. 11,066,299

CATALYST COMPOSITIONS HAVING ENHANCED ACIDITY FOR STEAM REFORMING PROCESSES

SAUDI ARABIAN OIL COMPANY...


1. A method for steam reforming over an enhanced-acidity modified red mud catalyst composition, the method comprising the steps of:providing a methane feed and a steam feed to react in a steam reforming reaction over the enhanced-acidity modified red mud catalyst composition at a temperature between about 500° C. to about 1000° C. and a pressure between about 5 bar and 20 bar to produce synthesis gas comprising H2 and CO, the enhanced-acidity modified red mud composition prepared by a homogeneous precipitation process comprising the steps of:
providing an unmodified caustic red mud waste material produced from an alumina extraction process from bauxite ore;
dissolving in water the unmodified caustic red mud waste material and neutralizing pH of the unmodified red mud waste material with an acid comprising hydrochloric acid;
combining nickel oxide, the nickel oxide present at between about 5 wt. % to about 40 wt. % of the enhanced-acidity modified red mud catalyst composition; and
combining a Periodic Table Group VIB metal oxide, the Group VIB metal oxide present at between about 1 wt. % and about 30 wt. % of the enhanced-acidity modified red mud catalyst composition.

US Pat. No. 11,066,298

SYSTEMS AND METHODS FOR PRODUCTION AND SEPARATION OF HYDROGEN AND CARBON DIOXIDE

8 Rivers Capital, LLC, D...


1. A process for hydrogen production, the process comprising:reacting a hydrocarbon feed and oxygen in a reactor unit to form a product gas stream comprising H2+CO;
passing at least a portion of the product gas stream comprising H2+CO through a steam generating boiler to add steam to the product gas stream comprising H2+CO;
converting the product gas stream comprising H2+CO in at least one reactor to form CO2 and thus form a stream comprising H2+CO2;
processing the stream comprising H2+CO2 in a pressure swing adsorber, wherein the stream comprising H2+CO2 processed in the pressure swing adsorber comprises at least 40 mol % CO2, to separate out H2 and provide a product stream formed of substantially pure hydrogen and also provide an H2-depleted waste gas stream comprising the CO2 formed in the at least one reactor;
forming a liquid CO2 product stream in a low temperature separation unit operating with auto-refrigeration by passing the H2-depleted waste gas stream comprising CO2 therethrough such that at least 50 mol % of the CO2 in the waste gas stream comprising CO2 is separated into the liquid CO2 product stream; and
recycling a vapor phase stream from the low temperature separation unit.

US Pat. No. 11,066,297

MEMS PACKAGES AND METHODS OF MANUFACTURE THEREOF

Taiwan Semiconductor Manu...


1. A package, comprising:a microelectromechanical systems (MEMS) structure comprising a capping structure bonded to a MEMS device, wherein the capping structure comprises a substrate and an oxide layer, the substrate having a cavity disposed in a first surface thereof, wherein the oxide layer lines the cavity, and wherein the oxide layer is interposed between the substrate of the capping structure and the MEMS device, the capping structure being bonded to the MEMS device by one or more first inter-device connectors, the first inter-device connectors comprising a eutectic material, wherein peripheral edges of the first inter-device connectors are aligned with peripheral edges of the capping structure, wherein the MEMS structure further comprises a standoff region extending away from the capping structure, wherein a first surface of the standoff region closest to the MEMS device has a first width, wherein a second surface of a first one of the first inter-device connectors closest to the capping structure has a second width, wherein the first surface contacts the second surface, and wherein the second width is less than the first width;
a device substrate comprising a plurality of first devices formed therein, wherein the device substrate is attached to the MEMS structure by an adhesive between the MEMS structure and the device substrate;
a through via adjacent the device substrate and electrically coupled to the plurality of first devices; and
an encapsulant contacting sidewalls of the device substrate, the adhesive, and the through via.

US Pat. No. 11,066,296

METHODS, APPARATUS, AND SYSTEMS FOR FABRICATING SOLUTION-BASED CONDUCTIVE 2D AND 3D ELECTRONIC CIRCUITS

Iowa State University Res...


1. A method of fabricating a 2D or 3D conductive pattern or circuit in a substrate having a length, width, and thickness including but not limited to millimeter and micrometer scales without requiring post-processing steps comprising:a. providing a substrate with a predetermined pattern or circuit of three-dimensional structural features in the thickness of the substrate to create three-dimensional open or closed microchannels in directions of any of the length, width, and thickness of the substrate, the microchannels having surfaces; and
b. coating at least some of said microchannel surfaces of selected said microchannels by:i. controlling flow of a liquid comprising viscous or solution-form carbon-based conductive materials or nano-materials, through the selected said microchannels to control filling of the selected channels with the liquid by one or more of:1. flow direction;
2. flow volume;
3. flow rate;
4. concentration of particles in the solution;
5. size of the particles in the solution;
6. solution viscosity;
7. capillary action; and

ii. adhering the electrically-conductive components of the liquid at a controlled thickness and coverage of the surfaces of the selected said microchannels;

c. without needing any postprocessing using chemicals or lasers or use of elevated temperatures;

further comprising transferring the conductive three-dimensional pattern or circuit to a second substrate by:a. placing a polymer solution over the conductive three-dimensional pattern;
b. curing the polymer solution in place to;i. create a second substrate;
ii. promote adherence of the conductive three-dimensional pattern to the second substrate;

c. transferring the conductive three-dimensional pattern to the second substrate by separating the second substrate from the first substrate.

US Pat. No. 11,066,295

MICROMECHANICAL COMPONENT HAVING AN OSCILLATOR, A METHOD FOR THE MANUFACTURE THEREOF, AND A METHOD FOR EXCITING A MOTION OF AN ADJUSTABLE ELEMENT ABOUT A ROTATIONAL AXIS

Robert Bosch GmbH, Stutt...


1. A micromechanical component, comprising:a mount;
an adjustable element connected via at least one spring to the mount; and
an actuator device configured to excite a first oscillatory motion of the adjustable element about a first axis of rotation relative to the mount, and to simultaneously excite a second oscillatory motion of the adjustable element, which is excited into the first oscillatory motion, about a second axis of rotation relative to the mount, the second axis of rotation being oriented obliquely to the first axis of rotation;
wherein the adjustable element is configured by the at least one spring to be adjustable on the mount in such a way that the adjustable element is able to be adjusted relative to the mount, in response to an angular momentum caused by the adjustable element, which is set into the first oscillatory motion, being set into the second oscillatory motion, about a rotational axis, which is oriented orthogonally to the first axis of rotation and orthogonally to the second axis of rotation.

US Pat. No. 11,066,294

MICRO-ELECTRO-MECHANICAL ACTUATOR DEVICE OF PIEZOELECTRIC TYPE AND APPARATUS INTEGRATING THE MICRO-ELECTRO-MECHANICAL ACTUATOR DEVICE

STMicroelectronics S.r.l....


1. A micro-electro-mechanical (MEMS) actuator device, comprising:a frame;
a first functional sub-structure positioned within the frame and mechanically coupled thereto by supporting elements, the first functional sub-structure being subdivided into first and second portions, the first portion being subdivided into first and second sub-portions separated from one another by a first through trench, the second portion being subdivided into first and second sub-portions separated from one another by a second through trench;
first and second piezo-electric structures respectively carried by the first and second sub-portions of the first portion;
third and fourth piezo-electric structures respectively carried by the first and second sub-portions of the second portion; and
a third through trench extending between the frame and the first functional sub-structure except for regions in which the supporting elements are present.

US Pat. No. 11,066,293

SPRING FEEDING DEVICE, APPARATUS FOR FORMING A STRING OF POCKET SPRINGS, AND METHOD OF FEEDING SPRINGS


1. A spring feeding device configured to feed a spring for pocketing the spring, the spring feeding device comprising:a feeding member delimiting a channel,
a pusher configured to push the spring along the channel delimited by the feeding member, and
a drive mechanism configured to concurrently displace both the feeding member and the pusher such that the feeding member and the pusher move in opposite directions to reduce a travel path of the pusher compared to a device having a stationary channel thereby reducing a cycle time.

US Pat. No. 11,066,292

DEVICE FOR TRANSFERRING A FLUID TO A SHIP

NEXANS, Courbevoie (FR)


1. Device for transferring a fluid from a mooring area to a ship, comprising:an articulated supporting structure, which has at least one first and one second support, which are connected pivotably to one another by at least one pivot joint and which each have a longitudinal axis, wherein the first support is fixed on the mooring area in such a way that the longitudinal axis of said support can be rotated substantially vertically and the first support can be rotated about the longitudinal axis thereof, and wherein the second support is pivotable in a vertical plane,
at least one guide element, which is fixed on the supports or on the at least one pivot joint, and
a first flexible line, which is supported by means of the guide element and is guided substantially in the vertical plane,wherein the device furthermore comprises a second flexible line, which is arranged substantially in a horizontal plane around the first support and is connected to the first flexible line by means of a rigid tube section connected in a fixed manner to the first support.


US Pat. No. 11,066,291

FLUSH AND WINTERIZING SYSTEM


1. An apparatus comprising: a valve comprising an inlet, an outlet, and an uptake inlet; a spool located in a valve body and coupled to a handle, and the spool is configured to selectively, by the positioning of the handle, direct flow between the inlet, the outlet, and the uptake inlet; an uptake conduit comprising an uptake conduit valve connector, configured to couple with the uptake inlet, and a conduit, configured to allow fluid to flow therethrough; and a circuit attachment comprising a circuit connector and a valve connector; wherein the uptake conduit and the circuit attachment are coupled to the valve; and the uptake conduit further comprises an entry apparatus comprising a conduit connection and a debris guard; wherein the debris guard is configured to actuate from an open position to a closed position.

US Pat. No. 11,066,290

ELECTRIC FUEL SHUTOFF DEVICE

CHEMOIL CORPORATION, Okl...


1. A fuel flow control device, comprising:an enclosure containing control circuity;
a valve having an inlet and an outlet, the valve moveable between an open position and a closed position, the open position configured to permit fuel flow through the valve and the closed position configured to block fuel flow through the valve;
a valve actuator operable to move the valve between the open position and the closed position;
an electric fuel sensor disposed in a sensor housing and comprising a shaft, the shaft comprising a slot such that the electric fuel sensor senses fuel when the slot is submerged in fuel;
an adapter cap configured to couple the fuel flow control device to the fuel tank; and
a battery configured to power the control circuity, the valve actuator, and the electric fuel sensor,
wherein the control circuity comprises logic configured to move the valve between the open position and the closed position in response to a signal provided by the electric fuel sensor.

US Pat. No. 11,066,289

KEG CLOSURE WITH ATTACHED VENTING SYSTEM

Petainer Large Container ...


1. A closure for admitting a pressurised gas into a headspace of a beverage keg, the closure comprising:a venting aperture that is configured to provide fluid communication between the headspace of the beverage keg and an exterior of the closure, wherein the venting aperture is provided in a housing wall of a housing component that defines at least a portion of a valve housing of the closure;
a barrier configured to seal the venting aperture such that the closure is able to retain the pressurised gas within the beverage keg in an unvented configuration, wherein the barrier is configured to rupture and/or to become at least partially detached from the closure by internal pressure from within the beverage keg in order to switch the closure into a vented configuration in which the venting aperture is no longer sealed by the barrier; and
a head portion configured for attachment to a filling head or dispense head, wherein the head portion is formed separately to the housing wall as part of a separate attachment part, and wherein the head portion includes an annular wall extending around at least a portion of the housing wall, the annular wall at least partially protecting the venting aperture and the barrier.

US Pat. No. 11,066,288

SYSTEMS AND METHODS FOR DISPENSING A BEVERAGE STORED IN A COLLAPSIBLE BEVERAGE CONTAINER


1. A beverage dispensing system for dispensing a beverage stored in a collapsible beverage container, said collapsible beverage container defining a beverage filled space, a gas-filled head space and a beverage outlet in communication with said beverage filled space for extracting said beverage from said beverage filled space, said beverage dispensing system comprising:a base part including a beverage container connector for connecting to said beverage outlet of said collapsible beverage container;
a tapping device for extracting said beverage from said beverage filled space and a tapping line extending from said beverage container connector to said tapping device; and
a lid connectable to said base part, said lid and said base part defining a sealed inner space for accommodating and encapsulating said collapsible beverage container,
wherein said lid is flexible and said beverage dispensing system further comprises a vacuum pump in fluid communication with said inner space for depressurizing said inner space for causing said flexible lid to apply a force onto said collapsible beverage container, thereby collapsing said collapsible beverage container and forcing said beverage from said beverage filled space through said tapping line and out through said tapping device.

US Pat. No. 11,066,287

NITROGEN GENERATOR AND USES THEREOF

AUTOMATIC BAR CONTROLS, I...


1. A self-contained dispense system for preparation and dispensation of a specialty nitrogen infused beverage, comprising as components:means for infusing nitrogen into a liquid to provide a nitrogen infused liquid, wherein the nitrogen infused liquid is the nitrogen infused beverage or is used to prepare the nitrogen infused beverage;
means to dispense the nitrogen infused beverage; and
a system to continuously supply nitrogen gas to the means for infusing nitrogen, wherein the system to supply nitrogen gas comprises:a compressed air feed;
a nitrogen membrane separator;
a nitrogen storage unit;
a pressure control unit; and
a release valve for nitrogen from the nitrogen storage unit,

wherein
a foot print of the system to supply nitrogen gas is less than four square feet,
a height of the system to supply nitrogen gas is less than one foot, and
a volume of the nitrogen storage unit is from 10 to 100 cubic inches.

US Pat. No. 11,066,286

WATER DISPENSING SYSTEM FOR FURNITURE


1. A water-dispensing system for furniture comprisinga water storage reservoir, a pump, a valve, a first retractable hose, and a second retractable hose;
wherein the water-dispensing system for furniture further comprises a plurality of vessel structures;
wherein each of the plurality of vessel structures is a mechanical structure that contains the water;
wherein the plurality of vessel structures automatically refills the water;
wherein the water-dispensing system for furniture is configured for use with an item of furniture;
wherein the water-dispensing system for furniture mounts in the item of furniture;
wherein the plurality of vessel structures further comprises a first vessel structure;
wherein the first vessel structure further comprises a first vessel and a first vessel holder;
wherein the first vessel holder contains the first vessel;
wherein the first vessel holder further comprises a first vessel holder valve and a first vessel holder pan;
wherein the first vessel holder pan is a prism-shaped negative space that is formed in the first vessel holder;
wherein the first vessel holder valve forms a portion of a fitting that attaches the first vessel to the first retractable hose such that the first vessel receives water from the first retractable hose;
wherein the inner dimension of the first vessel holder pan is greater than the outer dimension of the first vessel such that the first vessel inserts into the first vessel holder pan.

US Pat. No. 11,066,285

DISPENSING APPARATUS FOR AGING AND STORING WINE IN FLEXIBLE CONTAINERS


1. A system for dispensing and storing liquid comprising:a flexible bladder for holding a liquid and a sediment that settles out of the liquid;
a dip tube head component coupled to the flexible bladder in an airtight manner so that the liquid is held in the bladder in an airtight manner; and
means for dispensing the liquid from the flexible bladder by dispensing a portion of the liquid from an upper surface of the liquid in the bladder before portions of the liquid below the portion of the liquid from the upper surface so that the liquid at the upper surface is dispensed prior to portions of the liquid below that portion throughout a dispensing process, wherein the liquid without the settled sediment is dispensed from the device,
wherein the means for dispensing the liquid comprises a perforated dip tube extension coupled to the dip tube head component and configured to extend into the flexible bladder to a bottom wall of the bladder,
wherein the dip tube head component comprises a fill/drain port and a sample port in direct communication with the perforated dip tube extension via a chamber formed in the dip tube head component, and
wherein the perforated dip tube extension further comprises a solid end cap configured to close a distal end of the perforated dip tube extension and prevent liquid and sediment from entering the distal end of the perforated dip tube extension.

US Pat. No. 11,066,284

ARTICLE TRANSPORT VEHICLE

Daifuku Co., Ltd., Osaka...


1. An article transport vehicle comprising:a travel portion configured to travel along a travel path;
a support portion configured to support a container; and
a moving mechanism configured to move the support portion along a lateral width direction which crosses the travel path as seen along a vertical direction,
wherein the moving mechanism is configured to move the support portion to a projected position at which the support portion is projected along the lateral width direction with respect to the travel portion, and to a retracted position at which the support portion is closer to the travel portion than at the projected position,
wherein the support portion includes a support member configured to support a bottom surface of a container from below, a movable member configured to be moved along the lateral width direction by the moving mechanism, and a vertically moving mechanism configured to move the support member along the vertical direction with respect to the movable member,
wherein the container includes a main body portion which has an opening which faces a direction along the lateral width direction when the container is supported by the support portion, and a lid for closing the opening,
wherein the article transport vehicle further comprises one or more fall preventing members configured to prevent a lid of a supported container which is the container that is supported by the support member from falling, and a movement coupling mechanism configured to move the one or more fall preventing members when the support member is moved,
wherein each of the one or more fall preventing members is located on the opposite side of the lid of the supported container from the main body portion, and is configured to be movable to a preventing position in which the fall preventing member protrudes upward with respect to a lower end of the lid, and to a retracted position in which the fall preventing member is retracted so as to be located lower than the lower end of the lid,
wherein the movement coupling mechanism is configured to move the one or more fall preventing members from respective retracted positions to respective preventing positions when the support member is raised, and to move the one or more fall preventing members from respective preventing positions to respective retracted positions when the support member is lowered,
wherein each of the one or more fall preventing members comprises a preventing portion extending along a first direction perpendicular to the lateral width direction and a pivot arm portion extending along a second direction which is perpendicular to the lateral width direction and different from the first direction,
wherein the preventing portion of each of the one or more fall preventing members has a portion that overlaps the lid of the supported container when the fall preventing member is in the preventing position, and does not overlap the lid of the supported container when the fall preventing member is in the retracted position, and
wherein the pivot arm portion of each of the one or more fall preventing members is located lower than the corresponding preventing portion when the fall preventing member is in the restricting position and when the fall preventing member is in the retracted position.

US Pat. No. 11,066,283

SUSPENSION SYSTEM FOR AN AUTOMATED GUIDE VEHICLE


1. An automated guided vehicle for transporting one or more objects, the automated guided vehicle comprising:a chassis;
a suspension system, the suspension system comprising a pair of first arms each coupled to the chassis via a first coupling, and a second arm coupled to the chassis via a second coupling, wherein the pair of first arms are independently pivotable relative to the chassis and about a first pivot axis, and the second arm is pivotable relative to the chassis and about a second pivot axis;
one or more first movement structures associated with the pair of first arms; and
one or more second movement structures associated with the second arm, wherein the second arm is arranged transverse relative to the pair of first arms, the first pivot axis and second pivot axis are transverse to each other, wherein each of the pair of first arms includes a drive wheel and a guiding wheel attached to and provided at opposite ends of the respective first arm;
wherein the chassis defines a longitudinal axis and a transverse axis, the pair of first arms are arranged parallel to the longitudinal axis, and the second arm is arranged parallel to the transverse axis; and
wherein the chassis is further arranged to maintain an average pitch angle of each of the pair of first arms by the independent pivoting action of the pair of first arms so as to improve stability and traction of the automated guided vehicle by keeping the drive wheel and the guiding wheel on the ground.

US Pat. No. 11,066,282

SYSTEM AND METHOD FOR MANEUVERING A MOBILE DRIVE UNIT

Amazon Technologies, Inc....


1. A method for transporting an inventory holder comprising:docking a mobile drive unit with the inventory holder;
while the mobile drive unit and the inventory holder are docked together, controlling at least a first actuator to move the mobile drive unit and the inventory holder in a first translational direction; and
controlling at least a second actuator to selectively rotate the inventory holder while the mobile drive unit and the inventory holder move in the first translational direction.

US Pat. No. 11,066,281

CONSTRUCTION MACHINE

KOBELCO CONSTRUCTION MACH...


1. A construction machine comprising:a lower travelling body configured to move on ground; and
an upper slewing body supported by the lower travelling body in a slewable manner, wherein
the lower travelling body includes:a truck frame including a front surface part and a rear surface part, the truck frame supporting the upper slewing body;
one pair of left and right side frames each supporting a crawler that allows circling movement, the one pair of left and right side frames being respectively coupled to both ends of a left and right direction of the truck frame to extend in a front and rear direction more than the truck frame;
one pair of front and rear travelling body weights each including a weight upper surface part facing upward and one pair of left and right weight side surfaces respectively disposed facing the one pair of left and right side frames, the one pair of front and rear travelling body weights being respectively disposed on a front side and a rear side of the truck frame between the one pair of left and right side frames; and
at least one pair of front and rear scaffolding members each including a scaffolding upper surface part facing upward, the at least one pair of front and rear scaffolding members being respectively installed in the one pair of front and rear travelling body weights to project to sides of the side frames more than the weight side surfaces, and

the scaffolding upper surface part and the weight upper surface part are disposed in line with each other along the left and right direction, and form a moving passage that allows a worker to move between the one pair of left and right side frames.

US Pat. No. 11,066,280

CONTAINER CRANE CONTROL SYSTEM

ABB Schweiz AG, Baden (C...


1. A container crane control system comprising:a camera configured to be fixedly mounted to a crane to obtain a series of captured images;
a video output configured to provide a video signal including a series of cropped image respectively based on the series of captured images; and
a control device configured to, for at least part of the captured images and the respective cropped image, receive an input signal indicating a current height of a load of the crane, wherein the control device is configured to control a position of the respective cropped image within the captured image based on the current height of the load.

US Pat. No. 11,066,279

MOTION COMPENSATING CRANE FOR USE ON AN OFFSHORE VESSEL

ITREC B.V., Schiedam (NL...


1. A motion compensating crane for use on an offshore vessel in floating condition having a hull with a design waterline, wherein the crane comprises:a main boom pivotally connected at an inner end thereof about a substantially horizontal boom pivot axis, said main boom having a tip end remote from said inner end;
a main boom luffing assembly adapted to set an angle of the main boom within a main boom working angle range, wherein the main boom has a length and a main boom working angle range such that the tip end thereof is positionable in a position wherein the tip end is at least 100 meters above the design waterline of the hull of the vessel;
a rigid jib frame pivotally connected to the tip end of the main boom about a substantially horizontal jib frame pivot axis;
a level setting assembly adapted to set the rigid jib frame in a levelled position whilst the main boom has any angle within said main boom working angle range, wherein the rigid jib frame is provided with one or more X-direction tracks that each extend perpendicular to the horizontal jib frame pivot axis and which are each substantially horizontal in said levelled position of the rigid jib frame;
a mobile carrier supported by said one or more X-direction tracks and movable relative thereto in an X direction;
a motor powered X-motion displacement actuator assembly adapted to move said mobile carrier in said X-direction relative to said one or more X-direction tracks, wherein the mobile carrier is provided with one or multiple parallel Y-direction tracks that extend perpendicular to said X-direction tracks;
a mobile jib hoist cable suspension member supported by said one or more Y-direction tracks and movable relative thereto in an Y direction;
a motor powered Y-motion displacement actuator assembly adapted to move said mobile jib hoist cable suspension member in said Y-direction relative to said one or more Y-direction tracks;
a jib hoist winch and a jib hoist cable driven by said jib hoist winch, which jib hoist cable depends from said mobile jib hoist cable suspension member, wherein an object suspension device is suspended from said jib hoist cable; and
a Z-direction heave motion compensation device that acts on the jib hoist cable and is integrated in the jib hoist winch and/or comprises a jib hoist cable engaging member that is arranged and adapted to act on the jib hoist cable.

US Pat. No. 11,066,278

CONVEYANCE ELEMENT FOR A CONVEYOR

OTIS ELEVATOR COMPANY, F...


1. A conveyance element for a conveyor, the conveyance element being configured for being moved in a conveying direction and comprising:an outer side configured for accommodating and supporting passengers; and
an opposing inner side facing away from the outer side;
wherein at least a portion of the inner side is a concave portion having a concave shape along the conveying direction;
wherein the concave portion has a polygonal cross-section.

US Pat. No. 11,066,277

GAP-REDUCING SILL ASSEMBLY FOR AN ELEVATOR CAR

OTIS ELEVATOR COMPANY, F...


1. An elevator car assembly, comprising:a cab;
at least one door that is moveable to open or close an opening into the cab;
a sill beneath the at least one door;
a sill plate having a first end and a second end;
at least one support arm secured to the sill plate, wherein the at least one support arm is secured to the sill plate near one end of the at least one support arm and an opposite end of the at least one support arm includes a surface configured as a pinion near each end of the sill plate;
a mounting bracket, the at least one support arm being supported on the mounting bracket to allow the at least one support arm to pivot relative to the mounting bracket; and
a first linear actuator near the first end of the sill plate and a second linear actuator near the second end of the sill plate, each linear actuator having a stationary portion that is secured to the mounting bracket in a selected position and a moving portion that moves in a vertical direction, wherein the moving portion of each linear actuator is configured as a rack that cooperates with the pinion near the corresponding end of the sill plate to cause the at least one support arm to pivot relative to the mounting bracket as the rack moves relative to the mounting bracket to thereby cause the sill plate to pivot from a stored position at least partially beneath the sill to an actuated position where the sill plate is aligned with the sill.

US Pat. No. 11,066,276

ENHANCED DOOR DETECTION

OTIS ELEVATOR COMPANY, F...


1. A door control system comprising:a sensor having a field of view in proximity to a door threshold of an entrance to an occupancy area, wherein the sensor is adapted to detect objects in the door threshold and a landing area proximate to the door threshold;
wherein the sensor is operated based on a movement of a door in the door threshold, wherein operating the sensor comprises adjusting the field of view of the sensor as a door closes across the door threshold; and
based at least upon detecting an object within a portion of the door threshold or the landing area, the sensor operable to signal a door operation controller to perform an action.

US Pat. No. 11,066,275

CONVEYANCE BELT FOR A CONVEYOR

OTIS ELEVATOR COMPANY, F...


1. Conveyance belt for a conveyor,the conveyance belt extending in a conveyance direction and comprising a plurality of cavities, wherein each of the cavities is configured for form-fittingly accommodating a corresponding insert for connecting the conveyance belt with a conveyance element of the conveyor;
wherein the conveyance belt comprises plurality of teeth and the cavities are formed in at least some of the teeth;
wherein each of the cavities has a smaller dimension in a direction extending parallel to the conveyance direction, and a larger dimension in a direction extending orthogonally to a conveyance direction.

US Pat. No. 11,066,274

ELECTROMAGNETIC SAFETY TRIGGER

OTIS ELEVATOR COMPANY, F...


1. A selectively operable braking device for an elevator system including a car and a plurality of guiderails, comprising:a safety brake disposed on the car and adapted to be wedged against one of the guiderails when moved from a non-braking state into a braking state;
a rod operably coupled to the safety brake, the rod configured to move the safety brake between the non-braking state and braking state;
a magnetic brake operably coupled to the rod and disposed adjacent to the guiderail, the magnetic brake configured to move between a rail-engaging position and a rail-non-engaging position, said magnetic brake, when in the rail-engaging position contemporaneously with motion of the car, moving the rod in a direction to thereby move the safety brake from the non-braking state into the braking state; and
an electromagnetic component, the electromagnetic component configured to move the magnetic brake from the rail-engaging position to the rail-non-engaging position upon receipt of a resetting signal;
wherein the electromagnetic component further comprises a retention apparatus configured to move the electromagnetic component in a direction parallel to an actuation axis, wherein the actuation axis is perpendicular to a direction of travel of the car;
wherein the retention apparatus further comprises a biasing member configured to apply a force to the electromagnetic component in the direction parallel to the actuation axis.

US Pat. No. 11,066,273

ELEVATOR OVERTRAVEL TESTING SYSTEMS AND METHODS

OTIS ELEVATOR COMPANY, F...


1. An elevator system comprising:a first guide rail and a second guide rail;
an overtravel feature on at least one of the first or second guide rails, the overtravel feature located a first distance from a top surface of the respective guide rail;
an elevator car moveable along the first and second guide rails, the elevator car including a car guidance element; and
a control unit configured to perform an overtravel distance test, the control unit configured to:
measure a landing position of the elevator car relative to a landing in an elevator shaft;
drive the elevator car upward along the first and second guide rails above the landing;
measure a second distance, the second distance being a distance of travel of the elevator car between the landing position and a location of the overtravel feature by detecting an interaction of the elevator car with the overtravel feature;
combine the first distance and the second distance to calculate a measured overtravel distance;
compare the measured overtravel distance with a predetermined overtravel setpoint; and
generate a failure indicator when the calculated measured overtravel distance is less than the overtravel setpoint.

US Pat. No. 11,066,272

CABLE STORAGE AND HANDLING SYSTEMS AND METHODS

ROLLS-ROYCE CANADA LIMITE...


1. A levelwind cable guide for guiding a cable having a minimum bend radius onto a drum, said cable guide comprising an elongated chute having contoured surfaces defining a cavity extending through a length of the chute, wherein the contoured surfaces include no bend having a radius smaller than the minimum bend radius of the cable, wherein the contoured surfaces comprise a contoured ceiling defining an upper boundary of the cavity, a contoured floor defining a lower boundary of the cavity, and opposing lateral walls defining lateral boundaries of the cavity.

US Pat. No. 11,066,271

METHOD FOR OPERATING A TEXTILE MACHINE AND A TEXTILE MACHINE


1. A method for operating a textile machine with several identical workstations which each have a basic requirement for negative pressure for regular production operation and an additional requirement for negative pressure following an interruption to production at a workstation, and wherein the textile machine comprises a vacuum system with limited suction force to exert the negative pressure on the workstations,whereby a minimum negative spinning pressure (pmin) is set, wherein, at said minimum negative spinning pressure (pmin), an absolute value of the negative spinning pressure (pmin) is at its lowest level during standard operation; and
whereby the number of workstations to be supplied with additional negative pressure simultaneously is limited so that the minimum negative pressure (pmin) is met,
characterised in that
a sub-negative spinning pressure (psub) is set, wherein an absolute value of the sub-negative spinning pressure (psub) is below the absolute value of the minimum negative spinning pressure (pmin) and
upon the occurrence of a specified event, the number of workstations simultaneously supplied with additional negative pressure is temporarily limited so that the sub-negative pressure (psub) is met.

US Pat. No. 11,066,270

SHEET FOLDING APPARATUS AND IMAGE FORMING APPARATUS

CANON FINETECH NISCA INC....


8. A sheet folding apparatus for folding sheets, comprising:a feeding-roller pair configured to transport sheets;
a folding-roller pair arranged downstream from the feeding-roller pair, for nipping a prescribed part of the sheet and fold the sheet;
a transport path having a first passage for guiding the sheet to the folding-roller pair, and a second passage inclined downward, for guiding the sheet from the feeding-roller pair to the first passage;
a loop-forming space provided below the first passage, for receiving a sheet loop between the feeding-roller pair and the folding-roller pair;
a pushing member arranged at a location below the second passage and in the neighborhood of the first passage, for pushing the sheet to move to a position where the folding-roller pair nips a prescribed part of the sheet; and
a control section configured to control the feeding-roller pair, folding-roller pair and pushing member, the control section including controlling the feeding-roller pair and folding-roller pair so as to form a sheet loop, and then moving the pushing member so that a prescribed part of the sheet is nipped by the folding-roller pair.

US Pat. No. 11,066,269

SHEET FOLDING PROCESSING APPARATUS AND IMAGE FORMING SYSTEM INCLUDING THE SAME

CANON FINETECH NISCA INC....


1. A sheet folding processing apparatus comprising:a conveyance unit which conveys a sheet in a conveyance direction;
a folding unit including a nipping portion which performs folding processing to nip a predetermined part of the sheet conveyed by the conveyance unit and to form a fold line at the predetermined part;
a loop forming space for forming a loop on the sheet between the conveyance unit and the folding unit;
a pushing plate which contacts the loop formed in the loop forming space and is movable between a guide position for guiding the predetermined part to the nipping portion of the folding unit and a retracting position closer to the conveyance unit than the guide position; and
an additional folding unit which performs fold line reinforcing processing to reinforce the fold line formed by the folding unit,
wherein the conveyance unit conveys the sheet in the conveyance direction after the folding processing is performed on the sheet by the folding unit, and the additional folding unit performs the fold line reinforcing processing on the fold line after a rear end of the sheet in the conveyance direction passes through the conveyance unit.

US Pat. No. 11,066,268

BINDING DEVICE, POST-PROCESSING APPARATUS, AND IMAGE FORMING SYSTEM

RICOH COMPANY, LTD., Tok...


1. A binding device comprising:a stacking device configured to receive sheets;
a sheet alignment member configured to align the sheets on the stacking device;
a binder configured to bind the sheets on the stacking device;
a binder moving device configured to move the binder; and
a retreat device configured to retreat the sheet alignment member from a range of movement of the binder in response to a pressing force acting on the sheet alignment member in a direction of movement of the binder, the retreat device including:a retreat mechanism configured to retreat, from the range of movement of the binder, an interfering portion of the sheet alignment member in response to interference with the binder moved by the binder moving device; and
a restoration mechanism configured to return the interfering portion of the sheet alignment member to a state before the interference, when the interference is resolved by the retreat mechanism, and

wherein the retreat mechanism is configured to rotate the interfering portion of the sheet alignment member along the direction of movement of the binder in accordance with movement of the binder.

US Pat. No. 11,066,267

RECORDING MATERIAL PROCESSING APPARATUS OR IMAGE FORMING SYSTEM EACH OF WHICH EXECUTES STAPLING PROCESS

Canon Kabushiki Kaisha, ...


14. An image forming system comprising:an image forming unit configured to form an image on a recording material;
a processing tray in which the recording material on which the image has been formed by the image forming unit is to be placed;
a detecting unit configured to detect the recording material placed in the processing tray;
a stapling unit configured to execute a stapling process for the recording material placed in the processing tray;
an instructing unit configured to output an execution instruction of the stapling process by the stapling unit;
a control unit configured to control switching between a first mode that executes the stapling process for a first recording material conveyed from the image forming unit to the processing tray and a second mode that, in a state in which the detecting unit has detected a second recording material inserted in the processing tray from an outside of a main body of a main body apparatus, waits for the execution instruction from the instructing unit and, upon receipt of the execution instruction, executes the stapling process;
a switching unit configured to switch a position of the stapling unit among a plurality of positions;
a notifying unit configured to provide notification of a placement position of the second recording material in the processing tray corresponding to each of the plurality of positions;
a discharging unit configured to discharge the first recording material or the second recording material for which the stapling process has been executed by the stapling unit, from the processing tray through a discharging port; and
a discharge tray in which the first recording material or the second recording material discharged by the discharging unit is placed,
wherein the discharging port is configured such that the second recording material can be inserted from the outside of the main body of the main body apparatus into the processing tray through the discharging port,
wherein the discharging unit is a roller capable of moving between a contact position where the roller comes in contact with the first recording material or the second recording material placed in the processing tray and a separated position where the roller is separated from the first recording material or the second recording material placed in the processing tray, and
wherein, in a case of having switched to the first mode, the control unit makes the roller move to the contact position and, in a case of having switched to the second mode, the control unit makes the roller move to the separated position.

US Pat. No. 11,066,266

CUTTING DEVICE, PRINTER AND METHOD FOR DETECTING OPERATION ERROR

TOSHIBA TEC KABUSHIKI KAI...


1. A cutting device comprising:a cutter having a movable piece that is configured to cut a medium;
a drive mechanism configured to change a position or posture of the movable piece;
a counting module configured to count a number of times the position or posture of the movable piece changes;
a determination module configured to variably determine a reference speed according to the number of times; and
a detection module configured to detect an operation error of the cutter according to a comparison result between a speed at which the position or posture of the movable piece is changed and the reference speed.

US Pat. No. 11,066,265

VALUE NOTE CASSETTE

Wincor Nixdor Internation...


1. A value note cassette, comprising:a first storage area for storing first notes of value of a first value note type, wherein the first notes of value are storable in the first storage area in a first orientation, and
a second storage area for storing second notes of value of a second value note type, which second storage area is separate from the first storage area,characterized in that the second notes of value are storable in the second storage area in a second orientation, and
wherein the first orientation is orthogonal to the second orientation,

further characterized in that a switch arrangement is provided,
wherein in a first switch position of the switch arrangement notes of value fed to the value note cassette are feedable to a first transport path, and
wherein in a second switch position of the switch arrangement the notes of value fed to the value note cassette are feedable to a second transport path, and
wherein the first transport path comprises a first transport unit and the second transport path comprises a second transport unit
further characterized in that the second transport unit comprises a circulating belt arrangement with an endless belt guided over rollers serving as deflecting elements,
characterized in that the second transport unit comprises a guiding element, wherein the guiding element is designed and arranged such that it separates a rear section, as viewed in transport direction, of a second note of value stored in the second storage area and bearing against the endless belt from a front section, as viewed in transport direction, of a further second note of value during feeding into the second storage area.

US Pat. No. 11,066,264

METHOD FOR AUTOMATICALLY REPLACING REELS IN AN UNWINDING ASSEMBLY AND RELATIVE UNWINDING ASSEMBLY

Fameccanica.Data S.p.A., ...


1. A method for automatically replacing a first reel with a second reel containing, respectively, a first web and a second web, each including an inner surface and an outer surface opposite to each other, wherein said first web feeds a production machine along a feed direction with said inner surface of said first web facing towards a predefined reference direction, and wherein said second web is intended to replace said first web, so that along said feed direction said inner surface of said second web faces towards said predefined reference direction, said method comprises:positioning a head section of said second web with respect to a tail section of said first web, wherein said inner surfaces, or said outer surfaces, are partly facing each other in a junction zone;
joining a portion of said head section with a portion of said tail section at said junction zone to form a transverse junction band;
feeding said second web towards said production machine along said feed direction with said inner surface facing towards said predefined reference direction; and
cutting said transverse junction band, thereby separating waste portions joined together from said first web and said second web joined together.

US Pat. No. 11,066,263

SHEET CONVEYING DEVICE AND IMAGE FORMING APPARATUS INCORPORATING THE SHEET CONVEYING DEVICE

Ricoh Company, Ltd., Tok...


1. A sheet conveying device comprising:a pair of rotary bodies configured to convey a sheet and to correct a skew of the sheet;
a detector configured to detect a side edge of the sheet in a width direction of the sheet, the detector including a downstream sensor downstream from the pair of rotary bodies in a conveyance direction of the sheet; and
a controller configured to control the pair of rotary bodies to,perform a primary skew correction in which the pair of rotary bodies is configured to (i) rotate from a reference position around a shaft in an opposite direction, which is opposite to a predetermined direction, before the pair of rotary bodies holds the sheet, and (ii) rotate in the predetermined direction around the shaft after the pair of rotary bodies holds the sheet, and
perform a secondary skew correction performed after the primary skew correction in which the pair of rotary bodies is configured to rotate around the shaft while the pair of rotary bodies conveys the sheet and after a leading edge of the sheet arrives at the downstream sensor.


US Pat. No. 11,066,262

APPARATUS AND METHOD FOR SINGLING SHEET MATERIAL


1. A singling apparatus for singling sheet material, the singling apparatus comprising:a sheet store for receiving a sheet stack of sheets to be singled, wherein the sheet store includes a singling gap, said singling gap being formed and arranged to deliver a sheet out of the sheet store to a transport mechanism;
a singling device comprising a separation roller, the separation roller comprising partially on its rotational surface a contact area to periodically contact and transport the sheet from the sheet store to the transport mechanism; and
a position indication device coupled to the separation roller and comprising an alignment indication arranged in correlation with an angle position of the contact area of the separation roller, the alignment indication indicating an alignment of the contact area relative to the singling gap and/or the sheet;
wherein the position indication device is arranged on the separation roller.

US Pat. No. 11,066,261

SHEET CONTAINER AND IMAGE FORMING APPARATUS

Canon Kabushiki Kaisha, ...


1. A sheet container to contain a sheet, the sheet container comprising:a support unit including a plurality of engaged portions and configured to support the contained sheet; and
a regulation unit movable with respect to the support unit, wherein the regulation unit is configured to come into contact with an end of the sheet to regulate the sheet in position,
wherein the regulation unit includes an operating member to be operated, a holding member configured to hold the operating member, a fixing member movable in cooperation with the operating member, and a cover configured to cover the operating member,
wherein the fixing member is movable between an engaging position at which the fixing member engages with one of the plurality of engaged portions and a non-engaged position at which the fixing member does not engage with one of the plurality of engaged portions,
wherein the operating member is configured to be engageable with the cover,
wherein the regulation unit is kept fixed to the support unit by the fixing member engaging with one of the plurality of engaged portions, with the cover engaging with the operating member,
wherein the holding member has a positioning hole, and the support unit has a fixing hole, and
wherein the regulation unit is fixed in such a manner that the holding member is fixed in the fixing hole of the support unit with a screw through the positioning hole.

US Pat. No. 11,066,260

SHEET LOADING DEVICE AND IMAGE FORMING APPARATUS INCORPORATING THE SHEET LOADING DEVICE

RICOH COMPANY, LTD., Tok...


1. A sheet loading device comprising:a device body to load a sheet;
a guide disposed extending in a sheet conveying direction in the device body;
a restricting body to move along the guide of the device body and to restrict a position of an end portion of the sheet; and
a securing body extending perpendicularly from the restricting body to attach to the restricting body and the guide and detach from the restricting body and the guide, the securing body having an engaging body,
the engaging body of the securing body engaging with the guide at an arbitrary position on the guide in the sheet conveying direction,
the restricting body being secured to the device body according to engagement of the engaging body of the securing body with the guide of the device body, wherein the securing body includes a rotatable switching body to rotate the engaging body relative to the securing body, wherein in a first position the engaging body is in a position parrallel to the sheet conveying direction of the guide and in a second position the engaging body is orthogonal to the guide.

US Pat. No. 11,066,259

DUST CONTROL SYSTEMS FOR BULK MATERIAL CONTAINERS

Halliburton Energy Servic...


1. A container system, comprising:a support structure, wherein the support structure comprises a frame;
an outlet coupled to the frame;
a dust control enclosure coupled to the outlet, wherein the dust control enclosure comprises a flexible and collapsible material;
a container disposed on the frame, wherein the container stores bulk material, and wherein the dust control enclosure forms a seal between the container and the outlet;
a discharge gate of the container for discharging the bulk material from the container, wherein the dust control enclosure forms a seal between the container and the outlet, and wherein the dust control enclosure is configured to control dust emissions associated with the discharge of the bulk material; and
one or more actuators disposed on the support structure, wherein the one or more actuators are configured to actuate the discharge gate.

US Pat. No. 11,066,258

CONTROL SYSTEM AND CONTROL METHOD FOR ROTARY CAR DUMPERS

VALE S.A., Rio de Janeir...


1. A method of operating a rotary car dumper, comprising:a) determining a silo level of at least one silo of at least one feeder by a silo level control to be at a first level or a second level; and
b) adjusting the silo level, when the silo level is determined to be at:a first level, by increasing a cycle time of a discharge of material by a positioning car control;
a second level, by:measuring a current, torque, position, speed, and acceleration of a positioning car by a positioning car control and verifying whether the cycle time can be decreased by increasing forces of the positioning car;
decreasing the cycle time based on the positioning car control determining that the cycle time can be reduced; and
decreasing an output flow of the material from the at least one feeder by a feeder flow control based on the positioning car control determining that the cycle time cannot be reduced;

wherein the second level is determined by measuring the silo level that is less than the first level and less than a minimal level, wherein the minimal level is less than the first level and greater than the second level; and

c) repeating a) and b) to maintain the silo level at the minimal level, calculated by flow set point.

US Pat. No. 11,066,257

CONTAINER TRANSPORT SYSTEM


5. A container transport system comprising:a vehicle having a subframe assembly coupled thereto, the subframe assembly including a lifting arm and a clamping arm, the clamping arm configured to clamp onto a corner fitting of a cargo container, the lifting arm configured to raise a portion of the cargo container, the vehicle includes a truck bed, the truck bed includes the subframe assembly coupled thereunder, the clamping arm includes a clamping portion having an extended connection, the clamping arm configured to clamp onto the corner fitting of the cargo container with the extended connection extending entirely through the corner fitting;
a jack stand for inserting below the cargo container, and the lifting arm is configured to lower for tilting the cargo container on the jack stand, the jack stand configured as a fulcrum; and
a container trailer configured for positioning below the cargo container, and the lifting arm is configured to raise for pivoting the cargo container on the jack stand and lowering the cargo container onto the container trailer, the container trailer includes a horizontal rail, the lifting arm configured to pivot the cargo container on the jack stand and lower the cargo container onto the horizontal rail of the container trailer.

US Pat. No. 11,066,256

GRAIN BIN POWERSWEEP WITH SUMP SHAFT APERTURE SEALING COVER PLATE ASSEMBLY

CTB, Inc., Milford, IN (...


1. A grain bin powersweep with a sump shaft aperture sealing cover plate assembly comprising:a grain bin sump including a sloped wall designed to shed grain toward a sump basin;
an unload conveyor positioned below a floor of the grain bin and operable to move grain out of the sump basin;
a sweep conveyor positioned above the floor of the grain bin and operable to move grain toward the sump basin;
a below floor gearbox positioned below the sloped wall and operably coupled to the unload conveyor;
an above floor gearbox positioned above the sloped wall and operably coupled to the sweep conveyor;
a coupling shaft extending through a non-circular sump shaft aperture in the sloped wall to couple the below floor gearbox to the above floor gearbox, the coupling shaft extending vertically;
a pair of seal cover plates forming a horizontal wall extending perpendicular to the coupling shaft, the horizontal wall having a circular sealing aperture therein and through which the coupling shaft extends.

US Pat. No. 11,066,255

VACUUM CONVEYING SYSTEM FOR BULK MATERIAL, IN PARTICULAR PLASTIC GRANULES


1. A vacuum conveying system for bulk material, the vacuum conveying system comprising:at least two storage locations;
at least two consumers;
supply conduits and discharge conduits connecting the at least two storage locations and the at least two consumers to each other;
at least one vacuum source configured to produce a vacuum flow/airflow;
a central material conduit comprising a first end and an opposite second end and extending straight from the first end to the second end, wherein the central material conduit comprises valves arranged sequentially one after another along a length of the central material conduit from the first end to the opposite second end, wherein the supply conduits and the discharge conduits each have one of the valves associated therewith, and wherein the valves are configured to actuate conveying paths of the bulk material from the at least two storage locations to the at least two consumers;
wherein the valves have a first position and a second position, wherein in the first position the valves open the central material conduit to provide a straight through passage, and wherein in the second position the valves supply the vacuum flow/air flow to the central material conduit or conduct the vacuum flow/air flow away from the central material conduit.

US Pat. No. 11,066,254

DISTRIBUTION RAMP FOR DRY AGRICULTURAL PRODUCT APPLICATOR

CNH Industrial Canada, Lt...


1. A distribution ramp system for a dry agricultural product applicator with a pneumatic conveyance system through which particulate material of a dry agricultural product is guided from an upstream bulk storage system to downstream nozzles for delivery onto an agricultural field, the distribution ramp system comprising:a product delivery line of the pneumatic conveyance system, the product delivery line including a circumferential sidewall that defines a wall segment; and
a distribution ramp with a ramp body mounted against the product delivery line wall segment; the ramp body including:a first end that defines a front end facing an upstream direction;
a second end that defines a back end facing a downstream direction; and
a ramp surface extending between the front and back ends, the ramp surface inclined with respect to the product delivery line wall segment to guide particulate material flowing along the product delivery line wall segment upwardly away from the product delivery line wall segment while traveling along the ramp surface;

a mounting arrangement at a point of engagement between the ramp body and the product delivery line to positionally lock the ramp body with respect to the product delivery line and wherein the mounting arrangement includes:
a projection; and
a receptacle;with the projection received in the receptacle to longitudinally and transversely locate the distribution ramp with respect to the product delivery line;

wherein:the projection defines a first projection extending from the distribution ramp;
the receptacle defines a first receptacle extending into the product delivery line circumferential sidewall; and

mounting arrangement further includes:a second projection extending from the distribution ramp;

a second receptacle extending into the product delivery line circumferential sidewall that receives the second projection of the distribution ramp;wherein:

each of the first and second projections defines a height dimension;
the product delivery line circumferential sidewall defines a thickness dimension; and
the height dimensions of the first and second projections are greater than the thickness dimension of the product delivery line circumferential sidewall;
the first and second receptacles are defined by first and second openings extending through the entire thickness dimension of the product delivery line circumferential sidewall; and
the first and second projections of the distribution ramp extend entirely through the first and second openings and beyond the product delivery line circumferential sidewall.

US Pat. No. 11,066,253

CONTAINER DUMPING MODULE

INTELLIGRATED HEADQUARTER...


1. A container dumping module comprising:a frame assembly;
a drive assembly mechanically coupled to the frame assembly; and
a cradle assembly suspended on the drive assembly, wherein the cradle assembly comprises:one or more finger-like structures having a top portion and a bottom portion in orthogonal planes, provided at a lower end of the cradle assembly, wherein the bottom portion supports at least a portion of bottom face of a container in one of a home position, a work position, and a transit position during a rotational motion of the cradle assembly;
a first support plate and a second support plate positioned at an upper end of the cradle assembly to support at least a portion of a top face of the container in one of the home position, the work position, and the transit position; and
a third support plate positioned perpendicular to the first support plate and the second support plate to support at least a portion of a side face of the container in one of the home position, the work position, and the transit position, wherein the home position, the work position, and the transit position is determined based on a type of item handled by the cradle assembly of the container dumping module;
wherein the one or more finger-like structures, the first support plate, the second support plate, and the third support plate are mechanically coupled to each other with a support bracket, and
a guide structure coupled to the support bracket to guide the container into the cradle assembly, wherein the guide structure comprises a protruding portion extending away from the one or more finger-like structures, and wherein the protruding portion comprises an angled cut to guide the container.


US Pat. No. 11,066,252

SUCTION GRIPPING DEVICE


1. A suction gripping device comprising:a support arm;
a head comprising at least a suction gripping element, an inlet for fluid passage and a channelling system for passage of fluid predisposed internally of the head so as to place the inlet and the at least a suction gripping element in mutual communication, the head being mounted on the support arm in such a way as to be translatable alternatively along the support arm in order to displace the suction gripping element at least between a picking-up position of an object and a release position of the object;
at least a manifold element, having a substantially longitudinal extension and being predisposed so as to be arranged parallel to the support arm superiorly or inferiorly thereto, along the extension thereof and so as to be connected to a suction source in order to be maintained in depression, the manifold element having a side thereof facing towards the head and comprising, along a portion of length at least equal to the entity of the translation of the head between the picking-up position and the release position, a single opening for passage of fluid or a series of openings for passage of fluid, each opening of the series of openings being arranged one consecutively after another;
seal means which are predisposed along the side of the manifold element at the opening or the series of openings so as to prevent the passage of fluid between the outside and the inside of the manifold element and enable maintaining the inside of the manifold element in depression;
a fluid distributor group, comprising a chamber, a front wall, a rear wall, a first window for passage of fluid in the rear wall communicating with the chamber and a second window for passage of fluid in the front wall communicating with the chamber, the fluid distributor group being mounted on the head so as to be interposed between the inlet present in the head and the side of the manifold element, the front wall being opposite and in proximity of the side of the manifold element, so that the distributor group translates along the side without there being any contact between the front wall and the side during the translation of the head along the support arm, the first window for passage of fluid being in communication with the inlet and the second window for passage of fluid being located at the seal means, the fluid distributor group further comprising, internally of the chamber, spacer means which are predisposed and configured so as to maintain a portion of the seal means distanced from the side of the manifold element in such a way as to place the inside of the manifold element in fluid-dynamic communication with the chamber via the second window for passage of fluid and therefore with the inlet, via the first window for passage of fluid, and thus maintain the channelling system in depression for activation in suction of the gripping element, the spacer means being further predisposed in such a way, during the translation of the head along the support arm and the sliding of the distributor group along the side of the manifold element, as to distance, and maintain distanced from the side of the manifold element, the portion of the seal means which, during the sliding of the distributor group along the side of the manifold element, is at the second window for passage of fluid of the distributor group, so as to constantly maintain the inside of the manifold element in fluid communication with the chamber and therefore, via the first window for passage of fluid, with the inlet and thus maintain the channelling system in depression for enabling the gripping element to suction-grip an object and to maintain the suction grip of the object during the translation of the head along the support arm, at least between the picking-up position and the release position.

US Pat. No. 11,066,251

BOARD CONVEYOR

SIEMPELKAMP MASCHINEN- UN...


1. A conveyor for transporting a board along a path in a transport direction between treatment stations, the conveyor comprising:an upstream conveyor section;
a downstream conveyor section spaced downstream in the direction from and aligned with the upstream section and defining therewith a horizontal support plane;
a center conveyor section between the upstream and downstream conveyor sections, the upstream, downstream, and center sections each being provided with rollers or belts for moving the board from the upstream section through the center section into the downstream section;
means for moving the center conveyor section transversely of the direction from a pass-through position aligned and level with the upstream and downstream sections to an offset position spaced therefrom horizontally or vertically;
a platform underneath the center section and moveable vertically between an upper offset position spaced below from the plane and a lower flush position level with the plane; and
lift means for moving the platform vertically between the upper offset and lower flush positions; and
means for, when the center section is in the offset position and the platform is in the lower flush position, either pulling a board off the platform and onto the downstream section or for guiding and depositing a board from the upstream section onto the platform.

US Pat. No. 11,066,250

APPARATUS FOR UNSCRAMBLING RANDOMLY ARRANGED CONTAINERS COMPRISING EXTRACTION MEANS INDEPENDENT OF EACH OTHER

RONCHI MARIO S.P.A., Ges...


1. An apparatus for unscrambling articles, in particular containers (100) fed randomly to an inlet of said apparatus, comprising:a transport system (20) for transporting the articles fed to the inlet, designed to transport through the apparatus articles arranged randomly on a transport plane,
pick and release devices (31;32) for picking and releasing the articles (100), configured to pick up the articles arranged randomly on the transport system (20) and release them to an extraction system (50) with a predefined orientation and/or position;
said extraction system (40;140,50) for extracting the articles (100) arranged with a predefined orientation and/or position;
a detection system (60) designed to detect the position and the arrangement of the articles (100) in transit on the transport system and to provide the information for controlling the pick and release devices (30);
a unit (500) for processing and controlling the components and the drives of the apparatus, designed in particular to receive the information about the position and/or arrangement of the articles and to control the pick and release devices (30);

wherein the extraction system comprises:a support plane (40;140) for supporting the articles (100) being extracted;
means (50;150) for extracting the articles (100), designed to pick up the articles released by the pick and release devices (31;32) and transport them on the support plane (40;140) towards the outlet (“O”) of the apparatus;

wherein said extraction means comprise a plurality of grippers (50;150), each comprising a pair of jaws (51;151) and each gripper (50;150) is displaceable along a fixed guide (55) independently of one or more of the other grippers (50;150);
and wherein said guide (55) is arranged inclined with respect to the plane of the transport system (20) and/or the support plane (40;140) of the extraction system, so as to prevent relative interference between said grippers (50;150) and the transport plane and/or the support plane (10;140) of the extraction system.

US Pat. No. 11,066,249

LOADING TABLE ROLLER BRUSH ASSEMBLY

OSBORN, LLC, Richmond, I...


1. A transport roller brush assembly comprising:an arcuate tube defined by an inner surface and an outer surface and wherein a radius of curvature of the inner surface approximates a radius of a roller whose opposite ends are supported by a frame;
a plurality of brush wires that extend in an outward radial direction beyond the outer surface of the arcuate tube and are oriented to engage material translated over the arcuate tube;
a first collar and a second collar that are each associated with a respective longitudinal end of the arcuate tube and constructed to secure the arcuate tube to the roller; and
at least one seam defined by each of the arcuate tube, the first collar, and the second collar and that extends in a longitudinal direction such that the arcuate tube, the first collar, and the second collar engage the roller from a radial direction relative to the longitudinal direction.

US Pat. No. 11,066,248

ARTICLE TRANSPORT DEVICE

Daifuku Co., Ltd., Osaka...


1. An article transport device for transporting an article from a receiving location to a delivery location comprising:a transport vehicle configured to move back and forth between the receiving location and the delivery location;
a path forming portion configured to connect the receiving location to the delivery location and to form a path through which the transport vehicle moves; and
a load receiving base provided at at least the receiving location,
wherein:
the transport vehicle includes a transport placing base on which an article is to be placed, and a lift device configured to raise and lower the transport placing base to a first height and to a second height that is lower than the first height,
the load receiving base is a base on which an article is to be placed, and is fixed at a third height that is between the first height and the second height,
the transport vehicle receives an article at the receiving location as a result of the article being placed onto the transport placing base positioned at the first height, or as a result of the transport placing base being raised from the second height to the first height with the article placed on the load receiving base, and the article being placed onto the transport placing base, and delivers the article at the delivery location, and
when the transport vehicle performs restoration movement to move from the delivery location to the receiving location, the lift device performs a restoration operation that differs in accordance with whether or not an article is present on the load receiving base at the receiving location.

US Pat. No. 11,066,247

POWERSWEEP INCLUDING GEARBOX SHIFTER MECHANISM

CTB, Inc., Milford, IN (...


1. A grain bin powersweep comprising:a grain bin unload conveyor positioned under a floor of a grain bin;
a grain bin sweep conveyor positioned above the floor of the grain bin;
a gearbox positioned under the floor of, and at the center of, the grain bin and having an external shift coupling movable between a drive position in which the sweep conveyor is operably engaged with the unload conveyor, and a neutral position in which the sweep conveyor is operably disengaged from the unload conveyor;
a shifter arm coupled to the external shift coupling;
a control rod extending from a handle at an exterior of the grain bin to the center of the grain bin, the control rod being axially movable between a corresponding drive position and a corresponding neutral position;
a pair of biasing members operably positioned at the center of the grain bin and between the control rod and the shifter arm to bias the shifter arm in opposite directions;
a neutral positioning recess and a drive positioning recess at the exterior of the grain bin into which the control rod is selectively positionable;
wherein a biasing force of a first biasing member of the pair of biasing members acts against an opposite biasing force of a second biasing member of the pair of biasing members to bias the control rod into the neutral positioning recess to retain the external shift coupling and the control rod in the neutral position and the corresponding neutral position, respectively, and wherein the opposite biasing force of the second biasing member of the pair of biasing members acts against the biasing force of the first biasing member of the pair of biasing members to bias the control rod into the drive positioning recess to retain the external shift coupling and the control rod in the drive position and the corresponding drive position, respectively.

US Pat. No. 11,066,246

EXTENDIBLE CONVEYOR WITH IRREGULAR PARCEL HANDLING

Siemens Logistics LLC, D...


1. An extendible conveyor system comprising:an extendible conveyor configured to extend into a container;
at least one belt on the extendible conveyor configured to transport an irregular parcel from the container to a base end of the extendible conveyor; and
a transfer mechanism configured to move the irregular parcel from the at least one belt to a shelf,
wherein the transfer mechanism is configured to restrain the at least one belt when the irregular parcel is being moved to the shelf.

US Pat. No. 11,066,245

CONVEYOR TRUSS ELEVATION APPARATUS, SYSTEMS, AND METHODS

Superior Industries, Inc....


1. A conveyor strut for modifying the elevation of a conveyor truss relative to a conveyor undercarriage, comprising:a lower frame having a first pair of supports connected by a first plurality of braces, said lower frame pivotally coupled to the conveyor undercarriage by a first pair of pivot supports;
an intermediate frame slidingly engaged with said lower frame, said intermediate frame having a second pair of supports connected by a second plurality of braces;
an upper frame slidingly engaged with said intermediate frame, said upper frame pivotally coupled to the conveyor truss by a second pair of pivot supports; and
at least a first actuator coupled to at least one of said upper frame and said lower frame, said first actuator configured to alternately extend and retract the strut in order to alternately raise and lower the conveyor truss relative to the conveyor undercarriage.