US Pat. No. 10,428,439

PREDICTIVE CAPABILITY FOR ELECTROPLATING SHIELD DESIGN

Intel Corporation, Santa...

1. A method of electroplating, comprising:placing a substrate in a tank comprising a plating solution, an anode, and a base shield, the base shield having a plurality of openings in an array having a two-dimensional coordinate system; and
electroplating a material on the substrate, wherein at least one of the number of the plurality of openings, the diameter of the plurality of openings, or the location of the plurality of openings in the base shield is determined by a method comprising:
running a simulated plating process on a substrate using a base shield between the substrate and an anode in a bath, the base shield comprising a plurality of openings therethrough defining an array comprising a two coordinates;
after running the simulated plating process, determining if a predetermined criterion for the simulated plating process is satisfied; and
if the predetermined criterion is not satisfied, adjusting one or more of the plurality of openings, wherein adjusting the openings of the array comprises adjusting at least one of the two coordinates and an area of one or more of the openings.

US Pat. No. 10,428,438

SUBSTRATE PROCESSING METHOD AND TEMPLATE

TOKYO ELECTRON LIMITED, ...

15. A template for use in performing a predetermined processing on a processing region of a substrate, the template comprising:a template body configured to face the processing region of the substrate;
a passage formed in the template body and configured to distribute a processing liquid to the processing region of the substrate, the passage including a surface which defines the passage;
a first insulating material provided either on the surface of the passage or within the passage;
a first indirect electrode to which a first voltage from a power source connected between the first indirect electrode and a counter electrode that is provided in the processing region of the substrate is applied in order to cause processing target ions included in the processing liquid to migrate to the counter electrode, wherein the first indirect electrode is disposed on the first insulating material such that the first insulating material covers the first indirect electrode and the first indirect electrode does not come into contact with the processing liquid flowing through the passage; and
a direct electrode connected to the counter electrode through the power source, and to which the first voltage from the power source is applied in order to cause the processing target ions that have migrated to the counter electrode to be oxidized or reduced, wherein the direct electrode is provided on the surface of the passage above the first insulating material and the first indirect electrode or provided on the first insulating material within the passage.

US Pat. No. 10,428,437

WEAR-RESISTANT COATING PRODUCED BY ELECTRODEPOSITION AND PROCESS THEREFOR

MTU AERO ENGINES AG, Mun...

1. A coating, wherein the coating is wear-resistant and comprises an electrodeposited matrix which comprises from 15% by weight to 50% by weight Co, from 15% by weight to 50% by weight Ni, from 10% by weight to 30% by weight Cr, and from 1% by weight to 10% by weight Al, and in which first particles comprising hard material particles and/or slip material particles are incorporated in a proportion of from 5% by volume to 40% by volume.

US Pat. No. 10,428,436

INDIUM ELECTROPLATING COMPOSITIONS CONTAINING AMINE COMPOUNDS AND METHODS OF ELECTROPLATING INDIUM

Rohm and Haas Electronic ...

1. A method comprising:a) providing a substrate comprising a nickel layer;
b) contacting the substrate with an indium electroplating composition comprising one or more sources of indium ions, citric acid, salts thereof or mixtures thereof, and one or more amine compounds in amounts of 0.1 ppm to 100 ppm having a formula:

where R1 is chosen from hydrogen; (CH2)aNR4R5 where R4 and R5 are independently chosen from hydrogen and linear or branched (C1-C4)alkyl and a is an integer of 1 to 4 (CH2CHR6—O)xH or salts thereof where R6 is chosen from hydrogen or linear of branched (C1-C4)alkyl and x is an integer from 1 to 20; carboxy(C1-C4)alkyl or salts thereof; or (CH2CHR6—O)p(CH2CHR9—O)xH or salts thereof where R9 is hydrogen or linear or branched (C1-C4)alkyl; R2 is chosen from hydrogen; linear or branched (C1-C4)alkyl; (CH2CHR6—O)yH of salts thereof where R6 is defined as above and y is an integer of 1 to 20; carboxy(C1-C4)alkyl or salts thereof; or (CH2CHR6—O)q(CH2CHR10—O)yH or salts thereof where R10 is hydrogen or linear or branched (C1-C4)alkyl; R3 is chosen from cocoalkyl; R?—O—(CH2)m where R? is chosen from linear or branched, saturated or unsaturated (C1-C20)alkyl, m is an integer of 1 to 4; (CH2)mNR7R8 where R7 is (CH2CHR6—O)p(CH2CHR9—O)xH or salts thereof and R8 is (CH2CHR6—O)q(CH2CHR10—O)yH or salts thereof; p and q are integers from 1-20; and G is (CH2CHR6—O)zH or salts thereof where z is an integer from 1 to 20 and n is 0 or 1; and wherein the indium electroplating composition is free of alloying metals; and
c) electroplating an indium metal layer on the nickel layer of the substrate with the indium electroplating composition.

US Pat. No. 10,428,435

METHOD FOR MODIFYING AN ELECTRICALLY CONDUCTIVE OXIDE SURFACE, USE FOR ELECTRODEPOSITION OF COPPER ON SAID SURFACE

1. Method for modifying the surface of an Indium Tin Oxide (ITO) substrate, said method comprising the following steps consisting in:i) bringing into contact the surface of said ITO substrate with a solution containing at least one copper ion (Cu2+) and at least ammonia then washing and optionally drying the surface of said ITO substrate thus obtained;
ii) bringing into contact the surface of said ITO substrate obtained following step (i) with a solution containing sodium tetraborohydride then washing and optionally drying the surface of said ITO substrate, whereby the ITO substrate surface that is obtained after step (ii) is a modified surface that does not present nanoparticles or clusters of copper.

US Pat. No. 10,428,433

METHOD TO REGENERATE OXYGEN TRAPS

CENTRE NATIONAL DE LA REC...

1. A method to regenerate an oxygen trap using an electric current, comprising at least the following steps:a) circulating, by a circuit and a voltage source, an electric current in a material of the trap to reduce the material;
b) measuring, by an ammeter, a value Im of said electric current and estimating a derivative dIm/dt of the measured current Im in relation to time;
c) estimating, by a calculator, a length (?) of material reduced by said electric current, as a function of the value of said current (Im) and of said derivative (dIm/dt);
d) stopping, by a switch, circulation of the current when the length of reduced material is at least equal to a threshold value (?s).

US Pat. No. 10,428,432

CATALYST LAYERS AND ELECTROLYZERS

Dioxide Materials, Inc., ...

1. A catalyst layer for an electrochemical device comprising a catalytically active element and an ion conducting polymer wherein said ion conducting polymer comprises:(a) positively charged cyclic amine groups; and
(b) polymers or copolymers of styrene, and wherein the weight of the ion conducting polymer in the catalyst layer is less than 64% of the weight of the catalytically active element.

US Pat. No. 10,428,431

MULTI-LAYER WATER-SPLITTING DEVICES

AQUAHYDREX PTY LTD, Nort...

1. A water splitting device comprising at least one cathode and at least one anode, wherein at least one liquid-permeable and gas-permeable spacer layer is positioned between the at least one cathode and the at least one anode, and wherein the water splitting device is arranged so that liquid electrolytes can permeate through the at least one liquid-permeable and gas-permeable spacer layer and thus be in fluid communication with both the at least one cathode and the at least one anode, wherein the spacer layer comprises embossed structures defining microfluidic plumbing structures configured for transmission of gas.

US Pat. No. 10,428,430

MARINE UTILITY CAST IRON ANODE

1. A marine utility anode sled, comprising:at least two generally parallel lateral members having lateral member centerlines and made of an anodic material;
at least two generally parallel longitudinal members attached to reside generally perpendicular to the lateral members and having longitudinal member centerlines above the lateral member centerlines of the lateral members and made of an anodic material; and
at least one electrical cable in electrical communication with the anodic material of both the lateral members and longitudinal members.

US Pat. No. 10,428,428

MICROWAVE PLASMA AND ULTRAVIOLET ASSISTED DEPOSITION APPARATUS AND METHOD FOR MATERIAL DEPOSITION USING THE SAME

International Business Ma...

1. A method for depositing a material on a substrate, the method comprising:feeding a precursor gas into a processing space in which the substrate is arranged;
feeding a reactive gas into the processing space;
operating an ultraviolet radiation assembly comprising an ultra violet source unit, an optical window and a movable protective shutter configured to generate and emit ultraviolet radiation into the processing space in combination with operating a microwave radiation assembly comprising a microwave power source and a microwave applicator that comprises an annular waveguide configured to generate and emit microwave radiation into the processing space, wherein the emitted ultraviolet radiation and the emitted microwave radiation that enter into the processing space containing the substrate collectively excite at least the reactive gas that is fed into the processing space containing the substrate, wherein the annular waveguide comprises an outer cylindrical wall and an inner cylindrical wall comprising a plurality of slots, wherein each of the plurality of slots of the inner cylindrical wall comprises a dielectric window within each slot; and
depositing the material on the substrate in the processing space from a reaction of the excited reactive gas and the precursor gas.

US Pat. No. 10,428,427

FABRICATION METHOD FOR TWO-DIMENSIONAL MATERIALS

NATIONAL CHIAO TUNG UNIVE...

1. A fabrication method for two-dimensional materials, comprising the following steps:forming an amorphous thin film having at least one element on a substrate;
forming at least one capping layer on the amorphous thin film; and
annealing the amorphous thin film to form a two-dimensional material film after the capping layer is formed, wherein the two-dimensional material film is a crystalline material formed from the at least one element;
wherein the step for forming the capping layer comprises:
forming a first capping layer on the amorphous thin film by using evaporation; and
forming a second capping layer on the first capping layer by using plasma-enhanced chemical vapor deposition,
wherein a density of the second capping layer is larger than a density of the first capping layer.

US Pat. No. 10,428,426

METHOD AND APPARATUS TO PREVENT DEPOSITION RATE/THICKNESS DRIFT, REDUCE PARTICLE DEFECTS AND INCREASE REMOTE PLASMA SYSTEM LIFETIME

APPLIED MATERIALS, INC., ...

1. A twin-chamber deposition system, comprising: a pair of processing chambers; a first remote plasma system in selective fluid communication with a showerhead disposed within each of the processing chambers, the first remote plasma system comprising two remote plasma chambers that are each configured exclusively for a respective one of the pair of processing chambers; and a second remote plasma system in selective fluid communication with each of the pair of processing chambers, wherein the first remote plasma system is configured for deposition precursors and the second remote plasma system is configured for cleaning precursors.

US Pat. No. 10,428,425

FILM DEPOSITION APPARATUS, METHOD OF DEPOSITING FILM, AND NON-TRANSITORY COMPUTER-READABLE RECORDING MEDIUM

Tokyo Electron Limited, ...

1. A film deposition apparatus for sequentially supplying at least two reaction gases, which mutually react, into a chamber to deposit a film on a substrate, the film deposition apparatus comprising:a turntable configured to be rotatable and include a concave portion on an upper surface, a bottom portion of the concave portion having a through hole;
a substrate supporting member configured to be attachable to and detachable from the concave portion, an upper surface of the substrate supporting member being configured to mount the substrate, a lower surface of the substrate supporting member being configured to have a first protruding portion;
a drive mechanism configured to move up and down the turntable, and revolve the turntable;
a lid member located inside the chamber and lower than the turntable, an upper surface of the lid member having a second protruding portion; and
a control unit configured to, after the drive mechanism moves down the turntable, revolve the turntable to cause the first protruding portion to contact the second protruding portion and cause the substrate supporting member to move to be spun a predetermined angle relative to the turntable.

US Pat. No. 10,428,424

TRAY DEVICE, REACTION CHAMBER AND MOCVD APPARATUS

BEIJING NAURA MICROELECTR...

1. A tray device, comprising:a large tray; a rotating shaft; a small tray; and a supporting disk,
wherein
the rotating shaft is connected with a center of the large tray and is configured to drive the large tray to rotate about the rotating shaft,
a tray groove configured to place the small tray therein is provided on the large tray, and
the supporting disk is located under the large tray, a sliding mechanism is provided between the supporting disk and the small tray, and, when the small tray revolves along with the large tray, the small tray is driven to spin in response to a sliding operation of the sliding mechanism, and the small tray is supported by the supporting disk by means of the sliding mechanism,
the sliding mechanism comprises a first sliding groove and a sliding pin, the first sliding groove being formed at an upper surface of the supporting disk, the first sliding groove being a closed track, an upper end of the sliding pin being fixedly connected to a first position other than a center of the small tray, a lower end of the sliding pin contacting the first sliding groove, and the sliding pin being configured to move along the first sliding groove, and when the large tray rotates about the rotating shaft, the first sliding groove on the supporting disk being fixed.

US Pat. No. 10,428,423

METHOD AND APPARATUS FOR DEPOSITING ATOMIC LAYERS ON A SUBSTRATE

1. A method of depositing an atomic layer on a substrate, the method comprising:supplying a precursor gas from a precursor-gas supply comprised in a drum; the drum being rotatable with respect to a sealing piece that receives gas from a gas source, wherein one of the drum and sealing piece comprises one or more gas feed channels in fluid connection with the precursor-gas supply, wherein the other of the drum and sealing piece comprises one or more circumferential grooves in its surface sealed by the one of the drum and sealing piece thereby preventing a fluid flowpath in a radial direction and leaving a fluid flow path in a circumferential direction, wherein during the supplying the precursor gas from the precursor-gas supply towards the substrate, the gas feed channels abut the sealed grooves, wherein a part of the gas flow path is formed by the sealed grooves, and wherein at least one sealed groove is provided with one or more separations separating adjacent zones of process gas feeds in the sealed groove, thus allowing zones to provide for mutually differing process gas compositions; and
providing a relative motion between the precursor-gas supply and the substrate to have the precursor gas react on the substrate so as to form an atomic layer by rotating the drum along a rotation trajectory while supplying the precursor gas; thus depositing a stack of atomic layers of a gradient composition,
wherein the at least one groove is formed by an upstanding wall that is sealed by an abutting face of one of the sealing piece or the drum, and
wherein the separations are recessed relative to the upstanding wall thereby forming a flow restriction relative the abutting face in order to provide a controlled cross flow between adjacent zones.

US Pat. No. 10,428,422

FILM-FORMING METHOD

PHILTECH Inc., Tokyo (JP...

1. A film-forming method for forming a film in a film-forming apparatus including (i) a first accumulation mechanism in which a first source gas is accumulated and a second accumulation mechanism in which a second source gas is accumulated, (ii) a first instantaneously-heating unit connected to the first accumulation mechanism that heats the first source gas, and a second instantaneously-heating unit connected to the second accumulation mechanism that heats the second source gas, wherein each of the first and second instantaneously-heating units heats each of the first and second source gases respectively by causing each of the first and second source gases to vertically collide with a flow path wall of a flow path formed on a surface of a heat exchange substrate electrically heated to cause heat exchange between each of the first and second source gases and the flow path wall, and (iii) a reaction chamber in which a substrate whose temperature is lower than a heating temperature of each of the first and second instantaneously-heating units is placed, comprising:generating first gas molecular species by causing the first source gas in an amount accumulated in the first accumulation mechanism to pass through the first instantaneously-heating unit, and generating second gas molecular species by causing the second source gas in an amount accumulated in the second accumulation mechanism to pass through the second instantaneously-heating unit;
sharply raising a partial pressure of the first gas molecular species and a partial pressure of the second gas molecular species by projectingly supplying the first gas molecular species and the second gas molecular species so that the partial pressures of the first and second gas molecular species make projecting peaks to the reaction chamber in which the substrate has been placed, which has been depressurized, and which has a constant capacity;
bringing the first gas molecular species or the second gas molecular species into reaction by alternately repeatedly guiding the first gas molecular species or the second gas molecular species to a surface of the substrate; and
forming a compound film on the surface of the substrate by supplying the first and second gas molecular species with repeated depressurization and projecting supply.

US Pat. No. 10,428,421

SELECTIVE DEPOSITION ON METAL OR METALLIC SURFACES RELATIVE TO DIELECTRIC SURFACES

ASM IP Holding B.V., Alm...

1. A method for selectively depositing a material on a first metal or metallic surface of a substrate relative to a second surface dielectric surface of the substrate, the method comprising one or more deposition cycles comprising:contacting the substrate with a first vapor-phase precursor comprising a metal halide at a temperature equal to or above about 225° C., wherein the metal halide is selected from fluorides or chlorides of Nb, Ta, Mo, W, V, Cr;
contacting the substrate with a second vapor-phase precursor comprising water or H2O2; and
optionally repeating the contacting steps until a desired thickness of material is deposited on the first metal or metallic surface;
wherein the material is deposited on the first metal or metallic surface relative to the second dielectric surface with a selectivity of above about 50%.

US Pat. No. 10,428,420

METHOD FOR CONTROLLING A PROCESSING SYSTEM

APPLIED MATERIALS, INC., ...

1. A method, comprising:flowing a precursor gas into a processing chamber;
injecting an inert gas directly into an exhaust line at a location between the processing chamber and an abatement system downstream of the processing chamber, wherein the inert gas bypasses the processing chamber; and
controlling the flow of the inert gas based on the flow of the precursor gas, wherein the flowing of the inert gas is controlled in response to a change to the flowing of the precursor gas.

US Pat. No. 10,428,419

COMBINATION CVD/ALD METHOD, SOURCE AND PULSE PROFILE MODIFICATION

ASM IP Holding B.V., Alm...

1. A method of operating a system having a reactor configured to deposit a thin film, said method comprising:providing a first amount of a reactant from a reactant source vessel to a reaction space of the reactor at a first volumetric flow rate,
subsequently providing a pulse flow of a second amount of the reactant to the reaction space at a second volumetric flow rate which is greater than said first volumetric flow rate, the pulsed flow comprising a pulse time duration,
removing at least a portion of the second amount of the reactant from the reaction space via delivery of a purge gas to the reaction space,
wherein the providing a first amount of a reactant, providing a pulsed flow of the second amount of the reactant, and removing a portion of the second amount of the reactant are repeated multiple times to deposit the thin film, and
wherein each pulsed flow of the second amount of the reactant entering the reaction space includes less than half of a total amount of the second reactant within a first half of the pulse time duration, thereby initially providing a low partial pressure pulsed flow of the second reactant to the reaction space during each pulsed flow.

US Pat. No. 10,428,418

METAL MATERIAL AND A METHOD FOR USE IN FABRICATING THEREOF

CITY UNIVERSITY OF HONG K...

1. A metal material comprising a plurality of metal particles arranged in a structure having at least two phases including a crystalline phase and an amorphous phase; wherein the crystalline phase is arranged to form a plurality of spherical crystalline structures and the amorphous phase is arranged to surround the spherical crystalline structures such that the spherical crystalline structures are substantially free of dislocation.

US Pat. No. 10,428,416

COATING FILM, MANUFACTURING METHOD FOR SAME, AND PVD DEVICE

NIPPON ITF, INC., Kyoto ...

1. A coating film of a sliding member, coated on a substrate surface, whereina hard carbon layer is formed continuing in columns-shape perpendicular to the substrate when observed in a cross-sectional bright-field TEM image,
the hard carbon layer is formed using a PVD method,
the ID/IG ratio is 1-6 when the hard carbon layer is measured using Raman spectroscopy, said ratio being the ratio of the Raman spectrum D band peak area intensity and G band peak area intensity,
a nano indentation hardness of the columnar hard carbon layer is 10 GPa to 35 GPa, and
the columnar hard carbon layer consists of amorphous hard carbon, or consists of amorphous hard carbon and graphite crystals.

US Pat. No. 10,428,412

ARTIFICIAL AGING OF STRAINED SHEET METAL FOR STRENGTH UNIFORMITY

FORD MOTOR COMPANY, Dear...

1. A method, comprising:forming a sheet of solution heat-treated, quenched, and aged 6xxx series aluminum having a sheet average yield strength of at least 100 MPa into a component;
attaching the component to an assembly;
painting at least a portion of the assembly; and
heat treating the assembly to cure the paint and to increase a component average yield to at least 240 MPa,
the heat treating step consists of a first heat treatment at a temperature of 170° C. to 190° C. for 5 to 15 minutes, followed by a second heat treatment at a temperature of 140° C. to 160° C. for 5 to 15 minutes, followed by a third heat treatment at a temperature of 130° C. to 150° C. for 5 to 15 minutes.

US Pat. No. 10,428,411

AIR QUENCHED HEAT TREATMENT FOR ALUMINUM ALLOYS

Ford Global Technologies,...

1. A method of processing an air-quenchable aluminum alloy component, comprising:sequentially performing operations of
progressive die stamping a sheet of an air-quenchable aluminum alloy to form a component,
solution heat treating the component,
air-quenching the component at a rate of 6° C./s to 25° C./s, and
artificially aging the component, including heat treating the component at 235° C. to 255° C., to a yield strength of at least 200 MPa.

US Pat. No. 10,428,409

HOT-ROLLED STEEL SHEET WITH EXCELLENT PRESS FORMABILITY AND PRODUCTION METHOD THEREOF

NIPPON STEEL CORPORATION,...

1. A hot-rolled steel sheet with excellent press formability, consisting of, in mass %,C: 0.03 to 0.10%,
Si: 0.6 to 1.5%,
Mn: 0.5 to 2.0%,
Nb: 0-0.08%,
Ti: 0-0.2%,
W: 0-0.5%,
Mo: 0-0.4%,
Cu: 0-1.2%,
Ni: 0-0.6%,
Cr: 0-1.0%,
B: 0-0.005%,
Ca: 0-0.01%, and
REM: 0-0.01%, andhaving a balance of Fe and unavoidable impurities,as impurities,P: limited to 0.05% or less,
S: limited to 0.01% or less,
Al: limited to 0.30% or less,
N: limited to 0.01% or less,wherein the hot-rolled steel sheet has a tensile strength of at least 540 MPa, and wherein in the steel sheet, the X-ray random intensity ratios of {211} plane parallel to a surface of the steel sheet at the ½ thickness position, the ¼ thickness position, and the ? thickness position in the thickness direction from the surface are 1.5 or less, 1.3 or less, and 1.1 or less, respectively, andwherein in the metallic structure of said steel sheet, the area fraction of ferrite is 70% or more, the area fraction of bainite is 30% or less, the area fraction of either one or both of martensite having an area of 0.1 ?m2 or more and retained austenite having an area of 0.1 ?m2 or more is 2% or less, andwith regard to respective average intervals, average diameters and number densities of a cementite having an area of 0.1 ?m2 or more, an inclusion having an area of 0.05 ?m2 or more and either one or both of the martensite and the retained austenite, a void formation/connection index L defined by formula 1 is 11.5 or more:

n?, ni and nMA: number densities of the cementite, the inclusion and either one or both of the martensite and the retained austenite, respectively, and the unit is pieces/?m2;
D?, Di and DMA: average diameters of the cementite, the inclusion and either one or both of the martensite and the retained austenite, respectively, and the unit is ?m; and
L?, Li and LMA: average intervals of the cementite, the inclusion and either one or both of the martensite and the retained austenite, respectively, and the unit is ?m.

US Pat. No. 10,428,407

CYLINDRICAL MEMBER MADE OF FLAKE GRAPHITE CAST IRON

TPR CO., LTD., Tokyo (JP...

1. A cylindrical member made of flake graphite cast iron,the flake graphite cast iron comprising a composition containing, in terms of mass %, 2.85% or more and 3.35% or less of C, 1.95% or more and 2.55% or less of Si, 0.45% or more and 0.8% or less of Mn, 0.03% or more and 0.25% or less of P, 0.15% or less of S, 0.15% or more and 0.55% or less of Cr, 0.15% or more and 0.65% or less of Mo, 0.15% or more and 0.65% or less of Ni, and the balance of Fe and inevitable impurities,
wherein the cylindrical member has a thickness of 3.5 mm or less.

US Pat. No. 10,428,406

WEAR RESISTANT AND CORROSION RESISTANT COBALT-BASED ALLOY POWDERS AND APPLICATIONS THEREOF

KENNAMETAL INC., Latrobe...

1. An article comprising:a metallic substrate; and
an alloy coating adhered to the metallic substrate via high velocity oxygen fuel (HVOF) spraying or high velocity air fuel (HVAF) spraying followed by sintering, the alloy coating comprising 15-25 wt. % chromium, 15-20 wt. % molybdenum, 0-15 wt. % tungsten, 10-20 wt. % nickel, 2.5-3.5 wt. % boron, 2.5-4.5 wt. % silicon, 1-2 wt. % carbon and the balance cobalt, wherein microstructure of the alloy comprises Co—Mo—Si Laves phases and intermetallic phases including metal borides and metal carbides.

US Pat. No. 10,428,405

EXTRACTANT AND METHOD FOR EXTRACTING AND SEPARATING YTTRIUM

XIAMEN INSTITUTE OF RARE ...

1. A method for the extraction and separation of yttrium, comprising:(1) mixing an extractant with a diluent to obtain an organic solution,
wherein the extractant is a compound or a mixture of compounds of formula (1):

wherein,
X is P or N; and
all of R1, R2, R3, and R4 are n-butyl, or one of R1, R2, R3, and R4 is n-tetradecyl and the other three of R1, R2, R3, and R4 are n-butyl;
(2) in a first extraction step, mixing the organic solution obtained in step (1) with an aqueous solution containing yttrium and other rare earth compounds to undergo selective extraction, so that yttrium remains in an aqueous phase while the other rare compounds are extracted into an organic phase; and
(3) in a back-extraction step, mixing the organic phase obtained from step (2) with an aqueous inorganic acid solution to extract the other rare earth compounds from the organic phase into the aqueous inorganic acid solution, wherein a molar concentration of the inorganic acid in the aqueous inorganic acid solution is 0.005 mol/l to 0.5 mol/l.

US Pat. No. 10,428,404

METHOD OF CONVERTING COPPER CONTAINING MATERIAL

OUTOTEC (FINLAND) OY, Es...

1. A method of converting copper containing material to blister copper comprising the following steps:(a) providing copper containing material comprising copper sulfides and iron sulfides, whereby the copper containing material comprises at least 35 wt % copper of the total weight of the copper containing material;
(b) reacting the copper containing material in a furnace with an oxygen containing gas, in the absence of flux, to effect oxidation of iron sulfide and copper sulfide, and controlling injection of the oxygen containing gas and the temperature so that a resulting converter slag is in a molten phase to obtain blister copper and converter slag, wherein in step (b) the oxygen partial pressure (pO2) is from 1 to 100 Pa.

US Pat. No. 10,428,403

METHOD FOR MANUFACTURING GRAIN-ORIENTED ELECTRICAL STEEL SHEET

JFE STEEL CORPORATION, C...

1. A method for manufacturing a grain-oriented electrical steel sheet, the method comprising:heating a steel slab having a composition that contains, in mass %, C: 0.08% or less, Si: 4.5% or less, and Mn: 0.5% or less, and that contains, in mass ppm, S: less than 50 ppm, Se: less than 50 ppm, O: less than 50 ppm, N: less than 60 ppm, and sol.A1: less than 100 ppm, and the balance consisting of Fe and incidental impurities;
subjecting the steel slab to hot rolling to obtain a hot rolled sheet;
optionally subjecting the hot rolled sheet to hot band annealing;
subjecting the hot rolled sheet to cold rolling either once, or twice or more with intermediate annealing performed therebetween, to thereby obtain a cold rolled sheet having a final thickness;
subjecting the cold rolled sheet to decarburization annealing to obtain a decarburization annealed sheet;
applying an annealing separator mainly composed of MgO on a surface of the decarburization annealed sheet; and
then subjecting the decarburization annealed sheet to secondary recrystallization annealing,
wherein the cold rolling comprises final cold rolling with a total cold rolling reduction being set to 85% or more and a rolling reduction per pass being set to 32% or more,
wherein the final cold rolling includes one or more passes followed by a final pass and uses work rolls having a mean surface roughness Ra of 0.25 ?m or less in at least one of the one or more passes other than the final pass, and
wherein the method further comprises, before initiating the final cold rolling, and after the hot rolling or the hot band annealing, heating both widthwise edges of the steel sheet to be subjected to the final cold rolling to a temperature from 100° C. to 400° C.

US Pat. No. 10,428,402

METHOD FOR HOT FORMING THIN SEMI-FINISHED PRODUCTS

1. A method for hot forming a semi-finished product of steel, the method comprising:heating the semi-finished product to a forming temperature;
conveying the semi-finished product to a forming tool;
forming at least one structure in the semi-finished product that increases rigidity of the semi-finished product, the at least one structure being formed at least partially in a trimming region of the semi-finished product, the trimming region defined as a portion of the semi-finished product that is removed resulting from cutting along a cutting line on the semi-finished product;
hot forming, hardening, or press hardening the semi-finished product in the forming tool after the at least one structure has been formed in the semi-finished product;
removing the trimming region from the semi-finished product thereby removing the structure wherein no remnants of the at least one structure remain on the semi-finished, formed and trimmed semi-finished product of steel; and
forming the semi-finished product into an A-pillar, a B-pillar, or a C-pillar of a motor vehicle.

US Pat. No. 10,428,401

THERMAL TREATMENT PROCESS OF A STEEL SHEET AND DEVICE FOR ITS IMPLEMENTATION

ArcelorMittal, Luxembour...

1. A thermal treatment process for a ferrous alloy sheet comprising the steps of:performing a thermal treatment on a running ferrous alloy sheet by immersing the ferrous alloy sheet into at least one molten oxides bath, the molten oxides bath having a viscosity lower than 3·10?1 Pa·s, a surface of the bath being in contact with a non-oxidizing atmosphere, the molten oxides being inert towards iron and a difference (?T) between a temperature of the ferrous alloy sheet at an entry of the bath and a temperature of the bath being between 25° C. and 900° C.; and
eliminating residues of molten oxides remaining on surfaces of the ferrous alloy sheet at an exit of the bath.

US Pat. No. 10,428,399

IMMERSION PROBE AND ASSEMBLY OF IMMERSION SUBLANCE AND IMMERSION PROBE FOR A CONVERTER FURNACE

ECIL MET TEC LTDA., Pied...

1. An immersion assembly for a converter furnace comprising: an immersion sublance comprising: a guide comprising a guide connecting end; and a sublance holder comprising a first coupling end and a second coupling end; wherein the guide connecting end of the guide is coupled to the first coupling end of the sublance holder; and wherein the sublance holder extends longitudinally from the first coupling end to the second coupling end; and an immersion probe comprising: a casing comprising an upper portion and having an internal cavity; and an adjustable portion located in the internal cavity, the adjustable portion comprising a connecting portion, an elastic portion, and a fixed portion, wherein the connecting portion is attached to the elastic portion and the elastic portion is attached to the fixed portion; and wherein the adjustable portion extends longitudinally along the internal cavity of the casing from the connecting portion to the fixed portion; wherein the second coupling end of the sublance holder of the immersion sublance is connected to the connecting portion of the adjustable portion of the immersion probe; wherein the connecting portion comprises a connector attached to a connection base, wherein the connector is located within the internal cavity of the casing, and wherein the connection base is attached to the elastic portion; wherein the elastic portion is disposed between the fixed portion and the connecting portion so that compression of the elastic portion decreases a length of the adjustable portion after a first contact point is established between a surface of the connection base of the connecting portion and a surface of the second coupling end of the sublance holder; and wherein the elastic portion is configured to compress until a second contact point is established between the upper portion of the casing of the immersion probe and the guide connecting end of the guide of the immersion sublance.

US Pat. No. 10,428,381

METHODS FOR DETECTION OF NUCLEOTIDE MODIFICATION

Cambridge Epigenetix Limi...

1. A method comprising:contacting a sample comprising a 5-hydroxymethylcytosine with a perruthenate oxidizing agent, wherein said perruthenate oxidizing agent selectively converts said 5-hydroxymethylcytosine to 5-formylcytosine.

US Pat. No. 10,428,379

NUCLEOTIDE ANALOGS FOR SEQUENCING

IBIS BIOSCIENCES, INC., ...

1. A nucleotide analog comprising:a) a nucleotide comprising a phosphate moiety, a base, and a sugar;
b) a photocleavable terminating moiety attached to the nucleotide by a first photocleavable linker, wherein said photocleavable terminating moiety is electrochemically detectable by accepting or donating at least one electron during an electrochemical reaction; and
c) a second photocleavable terminating moiety attached to the nucleotide by a second photocleavable linker.

US Pat. No. 10,428,377

METHODS OF DETECTING LOW COPY NUCLEIC ACIDS

CALIPER LIFE SCIENCES, IN...

8. A method of detecting a low copy nucleic acid of interest in a sample that comprises a higher copy additional nucleic acid that is different from the low copy nucleic acid, the method comprising:aliquotting the sample into a plurality of reaction mixtures, which reaction mixtures comprise a plurality of zero copy reaction mixtures comprising zero copies of the nucleic acid of interest and at least one single copy reaction mixture comprising a single copy of the nucleic acid of interest;
simultaneously subjecting the zero and single copy reaction mixtures in parallel to an amplification reaction while flowing each of the plurality of reaction mixtures through one of a plurality of channels of a microfluidic device;
detecting the nucleic acid of interest in the single copy reaction mixture;
wherein at least one of the plurality of reaction mixtures is formulated in an aqueous phase of an emulsion comprising aqueous droplets suspended in and surrounded by an immiscible liquid.

US Pat. No. 10,428,375

NUCLEIC ACID AMPLIFICATION AND DETECTION APPARATUS AND METHOD

AXXIN PTY LTD, Melbourne...

1. A nucleic acid amplification and detection apparatus, including:a support configured to receive a plurality of reaction vessels containing respective samples of one or more nucleic acids to be amplified, the support being rotatable about an axis of rotation and the reaction vessels being received in the support at respective receiving locations distributed about the axis of rotation;
a temperature control component thermally coupled to the support and configured to control the temperature of the support in order to amplify the nucleic acids contained in the reaction vessels while received in the support;
a plurality of measurement components configured to measure respective characteristics of the nucleic acids within the reaction vessels at respective measurement locations distributed about the axis of rotation, wherein the measurement components are arranged radially outward with respect to the reaction vessels;
a stepper motor coupled to the support and configured to rotate the support about the axis of rotation; and
a sample position controller coupled to the stepper motor and being configured to:
(i) cause the stepper motor to rotate the support about the axis of rotation in an oscillatory manner to cause mixing of the contents of the reaction vessels; and
(ii) cause the stepper motor to selectively position and hold a selected one of the plurality of reaction vessels at a selected one of the plurality of measurement locations to allow a corresponding one of the plurality of measurement components to perform a corresponding measurement on a corresponding sample.

US Pat. No. 10,428,374

LIQUID DISPENSING DEVICE

Kimantech, LLC, Salt Lak...

1. A liquid dispensing system, comprising:a support member;
a plurality of penetrating tips fixedly coupled to the support member, each penetrating tip operable to penetrate a container having a liquid disposed therein and create an opening in a portion of the container to dispense the liquid; and
a plurality of receptacles, each receptacle comprising a well of an electrophoresis gel configured to receive the liquid dispensed from the container.

US Pat. No. 10,428,372

PROBE SYSTEM FOR REAL-TIME QUANTITATIVE AND QUALITATIVE ANALYSIS OF BIOMATERIAL, REACTION CHAMBER WITH SAID PROBE SYSTEM, AND ANALYSIS METHOD THEREOF

SUGENTECH, INC., Daejeon...

1. A method for real-time quantitative and qualitative analysis of a biomaterial, comprising:(a) introducing a test sample into a reaction chamber,
wherein the reaction chamber has a top opening and the test sample accommodated therein and is hermetically closed with a cap installed at the opening after introduction of the test sample, wherein a bottom surface of the reaction chamber comprises an optically transmissive window having an optically transmissive flat surface; a biochip is formed on the optically transmissive window; a target probe-reporter probe linker, which comprises a target probe, which has a sequence complementary to a target nucleic acid sequence to be detected, and comprises a first fluorophore and a first quencher, and a reporter probe linked to an end of the target probe and having a sequence non-complementary to the target nucleic acid sequence, is accommodated in the reaction chamber; and the biochip comprises a capture probe having a complementary sequence capable of hybridizing with the non-complementary sequence of the reporter probe and comprising a second fluorophore and a second quencher;
(b) hybridizing and amplifying,
wherein, when the target probe is hybridized with target nucleic acids of the test sample, a first fluorescence signal is generated from the first fluorophore of the target probe while the target probe is digested with a polymerase having nuclease activities, the reporter probe is digested from the target probe with the polymerase having the nuclease activities to be released into the reaction chamber, and the capture probe having the complementary sequence is hybridized with the non-complimentary sequence of the reporter probe released into the reaction chamber to emit a second fluorescence signal due to a structural change of the capture probe caused by an extension reaction; and
(c) detecting the first and second fluorescence signals,
wherein quantitative analysis of the target nucleic acids from the first fluorescence signal is performed, and qualitative analysis of the target nucleic acids from the second fluorescence signal is performed.

US Pat. No. 10,428,371

FLUORESCENT LABELED SINGLE-STRANDED NUCLEIC ACID AND USE THEREOF

KABUSHIKI KAISHA DNAFORM,...

1. A labeled single-stranded nucleic acid comprising at least two fluorescent atomic group pairs that exhibit an exciton effect within each fluorescent atomic group pair, whereinan emission peak wavelength of a fluorescent atomic group pair J is shorter than an excitation peak wavelength of a fluorescent atomic group pair K,
the fluorescent atomic group pair J and the fluorescent atomic group pair K are both cations,
the fluorescent atomic group pairs J and K have a Förster resonance energy transfer (FRET) effect between each other,
each of a base having the fluorescent atomic group pair J or K that exhibits an exciton effect has a structure represented by the following formula (16), (16b), (17), or (17b):
where in the formulae (16), (16b), (17), and (17b),Z11 and Z12 are each a fluorescent atomic group that exhibits an exciton effect, and may be identical to or different from each other,
Z11 and Z12 constitute a fluorescent atomic group pair,
B is an atomic group having a natural nucleobase skeleton or an artificial nucleobase skeleton, wherein the natural nucleobase is adenine, guanine, cytosine, thymine or uracil,
E is:
(i) an atomic group having a deoxyribose skeleton, a ribose skeleton, or a structure derived from either one of them, or
(ii) an atomic group having a peptide structure or a peptoid structure,
L1, L2, and L3 are each a linking atom or a linking atomic group, having any number of main chain atoms, each may or may not contain each of C, N, O, S, P, and Si in the main chain, each may or may not contain each of a single bond, a double bond, a triple bond, an amide bond, an ester bond, a disulfide bond, an imino group, an ether bond, a thioether bond, and a thioester bond in the main chain, and may be identical to or different from each other,
D is CR, N, P, P?O, B, or SiR where R is a hydrogen atom, an alkyl group, or any substituent, and
b is a single bond, a double bond, or a triple bond, or alternatively,
in the formulae (16) and (16b), L1- and L2 are each a linker, L3, D, and b may not be present, and L1 and L2 may be bound directly to B, provided that:
in the formulae (16) and (17), E is an atomic group described in the item (i), and at least one O atom in a phosphoric acid linkage may be substituted with an S atom;
in the formulae (16b) and (17b), E is an atomic group described in the item (ii);
in the formulae (17) and (17b), the respective Bs may be identical to or different from each other, and the respective Es may be identical to or different from each other; and
the base having the fluorescent atomic group pair J and the base having the fluorescent atomic group pair K are contained in the labeled single-stranded nucleic acid at a distance at which there are from 1 to 5 bases between the base having the fluorescent atomic group pair J and the base having the fluorescent atomic group pair K.

US Pat. No. 10,428,370

UNIVERSAL METHOD FOR EXTRACTING NUCLEIC ACID MOLECULES FROM A DIVERSE POPULATION OF ONE OR MORE TYPES OF MICROBES IN A SAMPLE

Sun Genomics, Inc., San ...

1. A method comprising:extracting genetic material from any microbes present in a first sample obtained from the subject by: i) mixing the sample with a first lysis solution comprising a detergent, and a chelator; ii) adding a second lysis solution having a lysozyme to the mixture of step i); and iii) adding a third lysis solution comprising a chaotropic agent, to the mixture of step ii);
subjecting the genetic material extracted from the first sample to metagenomics analysis;
diagnosing the subject as having dysbiosis based on the metagenomics analysis of the first sample;
administering a probiotic to the subject to treat the dysbiosis;
extracting genetic material from any microbes present in a second sample obtained from the subject in the same manner as the extraction of genetic material from the first sample;
performing metagenomics analysis on the extracted genetic material from the second sample; and
assessing effectiveness of the dysbiosis treatment; and
administering a modified probiotic which is formulated specifically to the dysbiosis in the subject and based on the assessment of effectiveness, to the subject to treat the dysbiosis.

US Pat. No. 10,428,369

ANALYZING MICRODROPLET OUTLINE SIZE AND ADJUSTING CHANNEL PRESSURE TO ALTER MICRODROPLET SIZE

Bio-Rad Laboratories, Inc...

1. A method of analyzing a microdroplet, comprising:forming a microdroplet in a microfluidic channel;
obtaining a projected image of the microdroplet in the microfluidic channel, wherein the image includes a microdroplet outline;
measuring an outside diameter of the microdroplet outline;
measuring an inside diameter of the microdroplet outline;
analyzing the size of the microdroplet by using a midpoint diameter of the microdroplet outline, wherein the midpoint diameter is the average of the outside diameter and the inside diameter; and
adjusting pressure inside the microfluidic channel to alter the size of the microdroplet.

US Pat. No. 10,428,368

METHODS FOR ENRICHING FOR A POPULATION OF RNA MOLECULES

New England Biolabs, Inc....

1. A method of enriching for a population of RNA molecules in a mixture of RNAs, comprising:(a) adding a labeled GMP to the 5? end of 5?-diphosphorylated or 5?-triphosphorylated RNA molecules in a sample by incubating the sample with a labeled GTP and a capping enzyme, wherein the labeled GTP is of Formula (I):

 wherein the base is guanine, R is a linker and L is desthiobiotin; and
(b) enriching for RNA comprising the desthiobiotin.

US Pat. No. 10,428,367

PORTABLE GENETIC DETECTION AND ANALYSIS SYSTEM AND METHOD

ILLUMINA, INC., San Dieg...

1. A portable genetic detector system comprising:a plurality of portable detectors, wherein each portable detector comprises:
a housing;
an interface disposed on or in the housing and configured to receive input from an operator to control operation of the portable detector;
a sample receiving component disposed on or in the housing and configured to receive a biological sample wherein the biological samples are different from one another;
a reader disposed on or in the housing and configured to detect nucleic acids of interest in the biological sample to generate sample data;
a control system disposed on or in the housing and programmed to control the operation of the portable detector;
a locator configured to generate location information of the portable detector;
a transceiver disposed on or in the housing and configured to output the sample data generated by the reading component, wherein the sample data comprises data identifying nucleotides present in the biological sample; and
a display disposed on or in the housing and configured to display information related to the operation of the portable detector; anda remote processing system in communication with each of the plurality of portable detectors and separate from the plurality of portable detectors, wherein the remote processing system comprises:communications circuitry configured to receive the sample data and the location information from each of the plurality of portable detectors; and
a processor programmed to assemble a nucleic acid sequence of at least one biological sample based on the sample data; determine a sequence coverage for one or more regions of a genome based on sequence; and provide instructions to stop operation of the control system of each of the plurality of portable detectors when the sequence coverage has achieved a threshold and to provide new instructions to a subset of the plurality of portable detectors to analyze respective new biological samples, wherein the subset is selected based on the location information.

US Pat. No. 10,428,365

QUANTITATIVE STERILE FIELD ANALYSIS SYSTEM

1. A settle plate holder for a settle plate to collect airborne particulates in an operating room, said settle plate holder comprising:a planar circular base for securing a settle plate, said planar circular base having a top face and two opposing plate securing flanges extending perpendicularly from said top face and each having an upper abutting lip;
said planar circular base devoid of a side wall; and
a protective cover allowing airflow over a placed settle plate, said protective cover hingeably coupled to said planar circular base, said protective cover comprising two parallel arms extending across a substantial length of said planar circular base and an arcuate wire centered upon said two parallel arms.

US Pat. No. 10,428,345

CORN PLANT EVENT MON87460 AND COMPOSITIONS AND METHODS FOR DETECTION THEREOF

Monsanto Technology LLC, ...

3. A corn seed comprising the polynucleotide of SEQ ID NO: 2 or a complement thereof.

US Pat. No. 10,428,328

RESTORATION OF THE CFTR FUNCTION BY SPLICING MODULATION

YISSUM RESEARCH DEVELOPME...

1. A method for improving at least one clinical parameter of Cystic Fibrosis in a patient in need thereof, the method comprising administering a therapeutically effective amount of a synthetic polynucleotide molecule to said patient,wherein the synthetic polynucleotide molecule comprises a nucleotide sequence having a sequence of at least 18 consecutive nucleotide bases,
wherein said synthetic polynucleotide molecule binds to a pre-messenger RNA (pre-mRNA) transcript of the Cystic Fibrosis Trans-membrane conductance Regulator (CFTR) gene and suppresses exon 10 exclusion from the mature CFTR mRNA, and
wherein said nucleotide sequence is complementary to the nucleotide sequence set forth in SEQ ID NO: 2, or to a fragment thereof.

US Pat. No. 10,428,325

IDENTIFICATION OF ANTIGEN-SPECIFIC B CELL RECEPTORS

Adaptive Biotechnologies ...

1. A method for identifying antigen-specific B-cell receptor (BCR) sequences comprising:(A) incubating a plurality of B-cells with an antigen library displayed by an organism capable of displaying antigens;
(B) distributing the B-cells bound to antigens of the antigen library into a plurality of aliquots;
(C) isolating nucleic acids from B-cells bound to antigens of the antigen library and from the organism displaying said antigens;
(D) sequencing the following elements from each of the aliquots;
(i) B-cell heavy chain sequence,
(ii) B-cell light chain sequence, and
(iii) a nucleotide sequence encoding the antigen bound to the BCR; and
(E) identifying the sequenced elements of (D) that occur together in more than one aliquot thereby identifying antigen-specific BCR sequences.

US Pat. No. 10,428,323

REAGENTS AND METHODS FOR ESTERIFICATION

Wisconsin Alumni Research...

1. A method for esterifying one or more carboxylic acid groups in an organic or biological molecule which comprises contacting the organic or biological molecule with a compound of formula I:
or salts thereof, where:
R is an alkyl, alkenyl, alkynyl group or hydrogen,
RA is an alkyl or alkoxy at the para position on the indicated phenyl ring, and
RM is an alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or arylalkyl group which is optionally substituted with one or more alkyl, alkoxy, aryl, alkylaryl, halogen, haloalkyl, or haloalkoxy group.

US Pat. No. 10,428,309

SYSTEMS AND METHODS FOR PRODUCING STEM CELLS AND DIFFERENTIATED CELLS

New York Stem Cell Founda...

1. A method for the automated generation and/or manipulation of stem cells, the method comprising:a) providing an automated system having controller software,
b) culturing multiple different samples of cells, wherein the cells comprise adult somatic cells,
c) determining the proliferation rate or cell doubling time of individual cell samples from among the multiple different samples of cells utilizing an automated device having controller software for determining the proliferation rate or cell doubling time,
d) freezing individual cell samples from among the multiple different samples of cells,
e) selecting from the individual cell samples a subset of samples having similar proliferation rates or cell doubling times,
f) thawing the subset of samples selected in step (e),
g) plating the subset of samples in a multi-well plate,
h) culturing the subset of samples until they reach a desired confluency,
i) contacting the cultured subset of samples with one or more reprogramming factors in order to produce iPSCs, and
j) sorting the iPSCs and consolidating the sorted iPSCs to produce a pooled iPSC sample, wherein (a) to (j) are performed on the automated system via the controller software.

US Pat. No. 10,428,305

MODIFIED NATURAL KILLER CELLS THAT EXPRESS IL15 AND USES THEREOF

National University of Si...

1. A natural killer (NK) cell that expresses all or a functional portion of interleukin-15 (IL-15), wherein the all or a functional portion of the IL-15 is fused to all or a portion of a transmembrane protein that anchors the expressed IL-15 as a cell membrane-bound polypeptide (mbIL15) of the NK cell, and wherein the all or a functional portion of IL-15 promotes one or more of:(i) NK cell survival,
(ii) regulation of NK cell and T cell activation and proliferation, and
(iii) support of NK cell development from hematopoietic stem cells.

US Pat. No. 10,428,301

SYSTEM, APPARATUS AND METHOD FOR MATERIAL PREPARATION AND/OR HANDLING

Keck Graduate Institute, ...

1. A system to perform lysis, the system comprising:a container having at least one chamber to hold a material to be lysed and a lysing particulate material, the chamber having:
a first opening to provide fluid communication with the chamber from an exterior thereof and to receive the material to be lysed;
a second opening to provide fluid communication with the chamber from an exterior thereof and to provide an exit to the chamber for the material to be lysed;
a first filter positioned adjacent the second opening, the first filter having a plurality of apertures sized to pass the material that has been lysed and to block the lysing Particulate material;
a second filter positioned adjacent the first opening, the second filter having a plurality of apertures sized to pass the material to be lysed and to block the lysing particulate material;
a medium that includes the lysing particulate material and a fluid;
an impeller having a number of blades received in the chamber of the container; and
a micromotor coupled to the impeller, in operation, the micromotor turns the impeller which causes the impeller to agitate the material to be lysed in the chamber along with the medium that includes the lysing particulate material and the fluid to mechanically lyse the material.

US Pat. No. 10,428,300

CELL CULTURING DEVICE

HITACHI, LTD., Tokyo (JP...

1. An automatic cell culture system comprising:a culture vessel comprising a first vessel and a second vessel, the first vessel being positioned within the second vessel and having a culture surface formed of a permeable membrane;
wherein the first vessel comprises a first port configured to supply a liquid into the first vessel and discharge a gas from the first vessel, and a second port configured to discharge a liquid from the first vessel;
wherein the second vessel comprises a third port configured to supply a liquid into the second vessel and discharge a gas from the second vessel, and a fourth port configured to discharge a liquid from the second vessel;
the culture vessel further comprising:
at least one flow channel for discharging the gas discharged from the first port and the third port to outside air at atmospheric pressure;
at least one filter provided in the at least one flow channel; and
at least one collecting unit disposed between the first port and the third port, and the at least one filter in the at least one flow channel, the at least one collecting unit collecting moisture from the discharged gas.

US Pat. No. 10,428,299

MIXING DEVICE FOR MIXING THE CONTENTS OF A CONTAINER

Sartorius Stedim Biotech ...

1. A mixing device (1) for mixing contents of a container (12), the container having a removal side (17) that defines a side of the container (12) designated for collection and removal of the contents of the container (12), comprising:a container support (3) configured for supporting the container (12); and
a moving device (5) connected to the container support (3) and operative for generating movement of the container support (3) so that the contents of the container (12) can be mixed when the container support (3) is in a mixing position; wherein:
the container support (3) has a positioning device (11) designed to position the container (12) in a predetermined or predeterminable position on the container support (3), so that the removal side (17) of the container (12) is arranged substantially along a predetermined line (19) of the container support (3),
the container support (3) is mounted to be pivotable about a removal pivot axis (21) relative to the moving device (5) to move the container (12), which can be positioned on the container support (3), into a removal position,
the removal pivot axis (21) is arranged at a pivot axis angle of over 0° to 45° to the predetermined line (19) of the container support (3) so that the container (12) positioned on the container support (3) can be moved from the mixing position by means of a pivoting movement of the container support (3) about the removal pivot axis (21) into the removal position in which the removal side (17) is located on a lower side of the container (12) and also inclined toward a removal region (23) on the removal side (17) of the container (12).

US Pat. No. 10,428,298

METHANOL SLICING OF WINE

James Fred Salzman, Anna...

1. A method for reducing methanol content in a fermented solution, comprising:a. heating a fermented solution in a vacuum vessel to a fixed temperature, the fermented solution occupying a portion of the volume of the vessel;
b. lowering a boiling point of the solution by pulling a vacuum within the vessel to create a vapor; and
c. extracting the vapor, thereby producing a reduced methanol fermented solution without substantially reducing ethanol content.

US Pat. No. 10,428,297

WATER-SOLUBLE UNIT DOSE ARTICLES MADE FROM A COMBINATION OF DIFFERENT FILMS

MONOSOL, LLC, Merrillvil...

1. A water-soluble unit dose article comprising at least one sealed compartment, the water-soluble unit dose article comprisinga first water soluble film comprising a first water soluble resin;
and a second water soluble film comprising a second water soluble resin;
wherein the first film is sealed to the second film to form the at least one sealed compartment;
wherein the first water soluble resin comprises at least one polyvinyl alcohol homopolymer or at least one polyvinyl alcohol copolymer or a blend thereof, the at least one polyvinyl alcohol homopolymer or at least one polyvinyl alcohol copolymer or blend thereof having a 4% solution viscosity in demineralized water at 25° C. in a range of about 8 cP to about 40 cP, or about 12 cP to about 30 cP, or about 14 cP to about 25 cP;
wherein the second water soluble resin comprises at least one polyvinyl alcohol homopolymer or at least one polyvinyl alcohol copolymer or a blend thereof, the at least one polyvinyl alcohol homopolymer or at least one polyvinyl alcohol copolymer or blend thereof having a 4% solution viscosity in demineralized water at 25° C. in a range of about 4 cP to about 35 cP, or about 10 cP to about 20 cP, or about 10 cP to about 15 cP, or about 12 cP to about 14 cP; and
wherein the 4% solution viscosity in demineralized water at 25° C. of the at least one polyvinyl alcohol homopolymer or the at least one polyvinyl alcohol copolymer or the blend thereof of the first water soluble resin is greater than the 4% solution viscosity in demineralized water at 25° C. of the at least one polyvinyl alcohol homopolymer or the at least one polyvinyl alcohol copolymer or the blend thereof of the second water soluble resin and the difference between the 4% solution viscosity in demineralized water at 25° C. of the at least one polyvinyl alcohol homopolymer or the at least one polyvinyl alcohol copolymer or the blend thereof of the first water soluble resin and the 4% solution viscosity in demineralized water at 25° C. of the at least one polyvinyl alcohol homopolymer or the at least one polyvinyl alcohol copolymer or the blend thereof of the second water soluble resin is about 2 cP to about 20 cP, or about 3 cP to about 15 cP, or about 4 cP to about 12 cP;
provided that when the sealed compartment contains a fabric care or household care composition and a film comprises a blend of a polyvinyl alcohol homopolymer resin and an anionic polyvinyl alcohol copolymer resin, then both then first water soluble film and the second water soluble film comprise blends that include 65 wt. % or greater of an anionic polyvinyl alcohol copolymer resin, based on the total weight of polyvinyl alcohol resins in the blend; and
provided that when the sealed compartment contains a fabric care or household care composition and a film comprises a blend of at least two anionic polyvinyl alcohol copolymer resins, then both then first water soluble film and the second water soluble film comprise blends of at least two anionic polyvinyl alcohol copolymer resins.

US Pat. No. 10,428,295

FABRIC WRINKLE REDUCTION COMPOSITION

Colgate-Palmolive Company...

1. A fabric conditioner composition comprising:a cationic fabric softener, which is an esterquat having the formula:

wherein:
R4 is an aliphatic hydrocarbon group having from 8 to 22 carbon atoms,
R2 and R3 represent (CH2)S—R5,
R5 is an alkoxy carbonyl group containing from 8 to 22 carbon atoms, benzyl, phenyl, C1-C4 alkyl substituted phenyl, OH, or H,
R6 is benzyl, phenyl, C1-C4 alkyl substituted phenyl, OH, or H,
q, s, and t, are each independently an integer from 1 to 3, and
X? is a softener compatible anion; and
0.02 to 0.04% by weight of an amino-functional, epoxide group containing silicone polymer having a weight average molecular weight of 400,000 to 900,000 that exhibits a capability of reducing the number of fabric wrinkles same as a composition that has 5% by weight of the same silicone polymer.

US Pat. No. 10,428,291

ASHLESS OIL ADDITIVES AND THEIR USE AS TBN BOOSTERS

Cummins Filtration IP, In...

1. An engine oil composition, comprising:an engine oil; and
an ashless oil additive comprising at least one diazabicyclo or triazabicyclo compound, wherein the diazabicyclo or triazabicyclo compound comprises at least three tertiary amines.

US Pat. No. 10,428,289

METHODS FOR MAKING AND DISTRIBUTING BATCHES OF BUTANE-ENRICHED GASOLINE

1. An automated method of generating key performance indicators of a butane blending operation comprising:a) providing a central information processing unit that maintains hourly time;
b) providing a petroleum conduit and a flow of petroleum through said conduit;
c) providing a butane supply and a butane blending system on said petroleum conduit;
d) detecting points in time when said butane blending system stops and resumes operation;
e) associating said points in time with said hourly time, and generating data corresponding to segments of hourly time when said butane blending system stopped and resumed operation during a given time frame (“inoperative time segments”).

US Pat. No. 10,428,287

SUBSEA FLUID PROCESSING SYSTEM

AKER SOLUTIONS AS, Lysak...

1. A subsea fluid processing system configured to receive a wellstream flow, the subsea fluid processing system comprising:a pressure control device configured to regulate a pressure of the wellstream flow;
a gas-liquid separator unit configured to receive the wellstream flow downstream of the pressure control device and to provide a liquid stream and a gas stream;
a first membrane separator configured to receive the gas stream and to provide a retentate stream and a permeate stream;
a compressor configured to receive the permeate stream and to provide a compressed permeate stream;
a discharge cooler configured to receive the compressed permeate stream and to provide a cooled compressed permeate stream for injection into a subsurface reservoir; and
a heat exchanger configured to transfer heat from the compressed permeate stream to the wellstream flow,
wherein, a density of the cooled compressed permeate stream is higher than a density of the compressed permeate stream.

US Pat. No. 10,428,286

ASSOCIATIVE POLYMERS FOR USE IN A FLOW AND RELATED COMPOSITIONS, METHODS AND SYSTEMS

CALIFORNIA INSTITUTE OF T...

1. A framing associative polymer comprising:a linear, branched, or hyperbranched polymer backbone having at least two ends and a functional group presented at two or more ends of the at least two ends of the linear, branched, or hyperbranched polymer backbone;wherein the linear, branched, or hyperbranched polymer backbone is substantially soluble in a host non-polar composition,wherein a number of the functional groups presented at the two or more ends is formed by associative functional groups each capable of undergoing an associative interaction with another associative functional group in the non-polar composition with an association constant (k), wherein
in which Rg is the radius of gyration of the framing associative polymer in the non-polar composition in nanometers, Na is Avogadro's constant; and nF is the average number of the associative functional groups in the framing associative polymer,wherein a longest span of the framing associative polymer has a contour length Lf, such that ½ Lbf?Lf
in which Fbf is the rupture force of the framing associative polymer in nanonewtons, Re is the Reynolds number, d is the characteristic length of the flow in meters, p is the viscosity of the host non-polar composition ?h or the viscosity of the associative non polar composition ?a in Pa·s, and ? is the density of the host non-polar composition ?h or the viscosity of the associative non polar composition ?a in kg/m3,
wherein when c?2 c*, ? is the viscosity of the host non-polar composition ?h, ? is the density of the host non-polar composition ?h, and when c>2 c*, ? is the viscosity of the associative non-polar composition ?a, and ? is the density of the associative non-polar composition ?a,
and wherein

in which Mw is the weight-average molecular weight, Rg is the radius of gyration, and Na is Avogadro's constant.

US Pat. No. 10,428,285

METHOD AND APPARATUS FOR PROCESSING OF CARBON-CONTAINING FEED STOCK INTO GASIFICATION GAS

1. A downdraft gasification method comprising the steps ofproviding a loading mechanism trunk,
providing a drying zone
providing a plasticization zone
providing a pyrolysis zone
providing a combustion zone
providing a reforming zone
providing a slag discharge zone
supplying feedstock,
forcing said feedstock through said loading mechanism trunk as well as through each of said drying zone, pyrolysis zone, combustion zone, reforming zone and slag discharge zone with a loading mechanism that comprises an elongated loading mechanism trunk and a feedstock feeder,
causing said feedstock being forced through said loading mechanism trunk to form a plug that substantially hermetically separates said drying zone, said plasticization zone, said pyrolysis zone, said combustion zone, said reforming zone and said slag discharge zone from the atmosphere;
causing formation and separation of steam from said feedstock in said drying zone,
causing pyrolysis gases to form in said pyrolysis zone,
separating substantially all of said pyrolysis gases from said feedstock in said pyrolysis zone, thereby causing separation of carbon char residue;
and forming gasification gases.

US Pat. No. 10,428,284

GROUP III BASE STOCKS AND LUBRICANT COMPOSITIONS

EXXONMOBIL RESEARCH AND E...

1. A method for producing a diesel fuel and a base stock, comprising:providing a feed stock comprising a vacuum gas oil feed;
hydrotreating the feed stock under first effective hydrotreating conditions to produce a first hydrotreated effluent;
hydrotreating the first hydrotreated effluent under second effective hydrotreating conditions to produce a second hydrotreated effluent;
fractionating the second hydrotreated effluent to produce at least a first diesel product fraction and a bottoms fraction;
hydrocracking the bottoms fraction under effective hydrocracking conditions to produce a hydrocracked effluent;
dewaxing the hydrocracked effluent under effective catalytic dewaxing conditions to produce a dewaxed effluent, the dewaxing catalyst including at least one non-dealuminated, unidimensional, 10-member ring pore zeolite, and at least one Group VI metal, Group VIII metal or combination thereof;
hydrotreating the dewaxed effluent under third effective hydrotreating conditions to produce a third hydrotreated effluent; and
fractionating the third hydrotreated effluent to form at least a second diesel product fraction and a base stock product fraction, wherein the Group III lubricant base stock product fraction includes greater than or equal to 95 wt. % saturated hydrocarbons, a kinematic viscosity at 100° C. between 5 cSt and 12 cSt and has a ratio of multi-ring naphthenes to single ring naphthenes (2R+N/1RN) of less than about 0.59, and a ratio of branched carbons to straight chain (BC/SC) carbons less than or equal to 0.26.

US Pat. No. 10,428,282

METHOD FOR SIMULTANEOUSLY ELIMINATING ISOBUTANAL AND ETHANOL FROM OLEFINIC FEEDSTOCKS BY ADSORPTION ON A POROUS REFRACTORY OXIDE-BASED MATERIAL

IFP Energies nouvelles, ...

1. A method for purifying an olefinic feedstock that comprises olefins with 4 carbon atoms and impurities including isobutanal, ethanol, and acetone, wherein said method comprises:a) pretreatment that comprises at least one acetone elimination; and
b) simultaneously eliminating isobutanal and ethanol by running the pretreated feedstock obtained from a) over at least one fixed bed with at least one adsorbent that comprises at least one porous refractory oxide-based material,
wherein b) operates at a temperature of between 0 and 200° C., at a pressure of 0.1 to 10 MPa, and with an hourly volumetric flow rate (VVH) of the pretreated feedstock obtained from a) over the fixed bed of between 0.1 and 10 h?1.

US Pat. No. 10,428,276

FEED MIXTURE FOR PRODUCING HYDROCARBONS

1. A process for producing hydrocarbons comprising:combining one or more carbonaceous feedstocks with water and an additional component of a texturing agent to obtain a feed mixture;
pressurizing said feed mixture to a pressure substantially in a range of 150 to 375 bar; and
heating the pressurized feed mixture to a temperature substantially in a range of 300 to 430° C.,
wherein the texturing agent is adapted to stabilize the feed mixture to prevent separation and further to maintain the feed mixture as a homogenous mixture during the pressurizing step,
wherein the texturing agent is adapted to be converted or degraded during the hydrocarbon production process, and
wherein the texturing agent comprises a derivative of a cellulosic material and is selected from microcrystalline cellulose (MCC), nanocrystalline cellulose (NCC), polyanionic cellulose (PAC), a derivative of methylcellulose, and a combination thereof.

US Pat. No. 10,428,274

LIQUID CRYSTAL ALIGNMENT AGENT FOR PHOTO-ALIGNMENT, ALIGNING MEMBER, AND RETARDATION MEMBER

NISSAN CHEMICAL INDUSTRIE...

1. A liquid crystal alignment agent for photo-alignment, the liquid crystal alignment agent containing (A) a resin having a side chain including a structure of Formula (1) below, and (B) a compound of Formula (2) below,
in Formula (1), X1 is a benzene ring which may be substituted with a substituent, wherein the substituent is one or more of an alkyl group, a haloalkyl group, an alkoxy group, a halogen atom, a cyano group and a nitro group, and R is a substituent selected from OH and NH2;

in Formula (2), any 3-5 of R1, R2, R3, R4 and R5 are each independently a substituent selected from a hydrogen atom, a halogen atom, C1-6 alkyl, C1-6 haloalkyl, C3-8 cycloalkyl, C3-8 halocycloalkyl, C2-6 alkenyl, C2-6 haloalkenyl, C3-8 cycloalkenyl, C3-8 halocycloalkenyl, C2-6 alkynyl, C2-6 haloalkynyl, C1-6 alkoxy, C1-6 haloalkoxy, (C1-6 alkyl)carbonyl, (C1-6 haloalkyl)carbonyl, (C1-6 alkoxy)carbonyl, (C1-6 haloalkoxy)carbonyl, (C1-6 alkyl)aminocarbonyl, (C1-6 haloalkyl)aminocarbonyl, di(C1-6 alkyl)aminocarbonyl, cyano and nitro, and when any 3 or 4 of R1, R2, R3, R4 and R5 are as defined above, the remaining one or two of R1, R2, R3, R4 and R5 is/are a group of Formula (3) below,

in Formula (3), the dashed line is a bond, R6 is C1-30 alkylene, phenylene, or a divalent carbocyclic ring or heterocyclic ring, one or a plurality of hydrogen atoms of the alkylene, phenylene, or divalent carbocyclic ring or heterocyclic ring is optionally substituted with a fluorine atom, and when R6 is C1-3 alkylene, —CH2CH2— of R6 is optionally replaced by —CH?CH—, —CH2— of R6 is optionally replaced by phenylene or a divalent carbocyclic ring or heterocyclic ring, and is optionally replaced by —O—, —NHCO—, —CONH—, —COO—, —OCO—, —NH—, —NHCONH—, or —CO—, provided these groups are not adjacent to each other, and R7 is a hydrogen atom or a methyl group, and n is an integer of 0 or 1.

US Pat. No. 10,428,272

BARK AND WOOD FIBER GROWING MEDIUM

Profile Products, L.L.C.,...

21. A growing medium comprising:about 100 weight % fibrous pine wood components,
wherein the growing medium has a dry bulk density of 12.01 to 20.02 kg/m3 and wet bulk density of about 120 kg/m3 or lower.

US Pat. No. 10,428,270

HYBRID FLUORESCENT MATERIAL AND METHOD OF PRODUCING SAME

NICHIA CORPORATION, Anan...

1. A method of producing a hybrid fluorescent material comprising:dispersing Lu3Al5O12:Ce fluorescent material particles in a first solution;
mixing the first solution in a second solution, the second solution including a mixture of a first metallic salt containing at least one element selected from the group consisting of yttrium, gadolinium, and terbium, a second metallic salt containing aluminum and/or gallium, and a third metallic salt containing cerium,
wherein the mixing attaches (Y,Gd,Tb)3(Al,Ga)5O12:Ce fluorescent material precursor particles on surfaces of the Lu3Al5O12:Ce fluorescent material particles to obtain a hybrid fluorescent material precursor;
separating the hybrid fluorescent material precursor particles from the first and second solutions; and
calcining the hybrid fluorescent material precursor particles to obtain a hybrid fluorescent material of Lu3Al5O12:Ce fluorescent material particles covered by (Y,Gd,Tb)3(Al,Ga)5O12:Ce fluorescent material,
wherein the first solution contains ammonium hydrogen carbonate or ammonium carbonate.

US Pat. No. 10,428,269

INDENOTRIPHENYLENE DERIVATIVE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

5. An organic electroluminescence device, comprising a pair of electrodes composed of a cathode and an anode, and a light emitting layer and one or more organic thin film layers between the pair of electrodes, wherein at least one of the light emitting layer and the organic thin film layer comprises the indenotriphenylene derivative of claim 1.

US Pat. No. 10,428,268

ORGANIC ELECTROLUMINESCENCE ELEMENT

UDC Ireland Limited, Dub...

1. A light emitting organic thin film comprising at least one compound represented by Formula (PQ-1) and at least one compound represented by Formula (BN-1):
wherein, in Formula (PQ-1), each of Ra, Rb and Rc independently represents a hydrogen atom or an alkyl group, any one of Ra, Rb and Rc represents a hydrogen atom and the remaining two represent an alkyl group, each of R1 to R5 independently represents a hydrogen atom, an alkyl group, a phenyl group, a fluorine atom or a cyano group, and each of Rx and Ry represents a methyl group;
in Formula (BN-1), Ar1 represents an arylene group that may have a substituent Z, Ar2 represents a tetracenyl group that may have a substituent Z, each of R101 to R113 represents a hydrogen atom, an alkyl group, a cycloalkyl group, or a phenyl group that may have a substituent Z;
the substituent Z represents an alkyl group, an alkenyl group, an aryl group, an aromatic heterocyclic group, an alkoxy group, an aryloxy group, a fluorine atom, a silyl group, an amino group, a cyano group or a combination thereof.

US Pat. No. 10,428,267

METHODS FOR PRODUCING SOLID CERAMIC PARTICLES USING A MICROWAVE FIRING PROCESS

CARBO CERAMICS, INC., Ho...

1. A method for forming sintered substantially round and spherical pellets, comprising:forming substantially round and spherical green pellets from raw materials comprising water and kaolin clay; and
sintering the green pellets in a microwave furnace at a temperature of from about 1350° C. to about 1620° C. for a time at peak temperature of from about 20 to about 200 minutes, to form a proppant having a bulk density of from about 1.3 to about 1.6 g/cm3 and a crush percent at 7500 psi of from about 1.5 to about 3.5.

US Pat. No. 10,428,266

FORMING PROPPANT-FREE CHANNELS IN PROPPED VERTICALLY ORIENTED FRACTURES

Halliburton Energy Servic...

1. A method of treating a subterranean formation having a vertically oriented fracture disposed at true vertical or deviated up to 30° from true vertical comprising:providing a treatment fluid comprising an aqueous base fluid, a gelling agent, proppant particulates, and swellable particulates having an unswelled form and a swelled form,
wherein the density of the treatment fluid comprising the aqueous base fluid, the gelling agent, and the proppant particulates is about 0.75 g/cm3 to about 1.25 g/cm3,
wherein the density of the swellable particulates is about 95% to about 105% of the density of the transmit fluid, and
wherein the treatment fluid is a homogenous mixture upon introduction into the vertically oriented fracture;
placing the treatment fluid into the vertically oriented fracture;
swelling the swellable particulates at a first location against walls of the vertically oriented fracture, thereby forming a first swelled particulates plug;
swelling the swellable particulates at a second location above or below the first location against the walls of the vertically oriented fracture, thereby forming a second swelled particulates plug; and
settling the proppant particulates atop the first swelled particulates plug and the second swelled particulates plug,
wherein if the second swelled particulates plug is formed above the first swelled particulates plug, a proppant-free channel is formed below the second swelled particulates plug and above the settled proppant particulates atop the first swelled particulates plug, and
wherein if the second swelled particulates plug is formed below the first swelled particulates plug, a proppant-free channel is formed below the first swelled particulates plug and above the settled proppant particulates atop the second swelled particulates plug.

US Pat. No. 10,428,265

SELECTIVE ACIDIZING OF A SUBTERRANEAN FORMATION

Halliburton Energy Servic...

1. A method of acidizing a subterranean formation, comprising:pumping an acid-resisting treatment composition comprising a surface modification agent comprising at least one of a tackifying agent or resin, a hydroxy-reactive organosilicon compound, or a phosphonate compound into the subterranean formation, wherein the acid-resisting treatment composition further comprises about 0.001 wt % to about 10 wt % of a viscosifier; then
producing an at least partially acid-resistant coating comprising the surface modification agent or a reaction product thereof on at least a part of the subterranean formation; and then
pumping an acidizing composition into the subterranean formation, wherein the acidizing composition at least one of etches and dissolves another part of the subterranean formation substantially free of the acid-resistant coating.

US Pat. No. 10,428,264

BREAKER COATED PARTICULATES FOR USE IN SUBTERRANEAN FORMATION OPERATIONS

Halliburton Energy Servic...

1. A method comprising:preparing a viscosified treatment fluid comprising a base fluid, a gelling agent, and breaker coated particulates (BCPs),
wherein the BCPs comprise particulates at least partially coated with a first layer of a stabilization agent followed by a second layer of a breaker, wherein the second layer of the breaker forms a chemical bond with the first layer of the stabilization agent, and
wherein the stabilization agent is present in the range of about 0.1% to about 5% v/w % of the particulates;
introducing the viscosified treatment fluid into a subterranean formation;
activating the breaker to reduce a viscosity of the viscosified treatment fluid; and
forming a particulate pack in the subterranean formation with the BCPs.

US Pat. No. 10,428,263

LOW TEMPERATURE WATERLESS STIMULATION FLUID

LINDE AKTIENGESELLSCHAFT,...

1. A method of treating a subsurface formation, comprising:increasing a pressure of an unfractionated hydrocarbon liquid mixture;
cooling the pressurized unfractionated hydrocarbon liquid mixture to a temperature at or below 0 degrees Fahrenheit;
mixing the cooled and pressurized unfractionated hydrocarbon liquid mixture with a foaming agent and a gas to form a waterless stimulation fluid comprising foam, wherein the unfractionated hydrocarbon liquid mixture comprises ethane, propane, butane, isobutane, pentane, and less than 1 percent methane, and wherein the unfractionated hydrocarbon liquid mixture is a byproduct of a de-methanized hydrocarbon stream; and
injecting the waterless stimulation fluid into the subsurface formation at the temperature at or below 0 degrees Fahrenheit to thermally fracture the subsurface formation.

US Pat. No. 10,428,261

RESIN COMPOSITE WITH OVERLOADED SOLIDS FOR WELL SEALING APPLICATIONS

CSI TECHNOLOGIES LLC, Ho...

1. A method of formulating a sealant to span an opening and form a seal with surfaces around the opening at a sealing location; comprising:selecting a fluid material capable of contacting and adhering to the surfaces around the opening and which reacts to form a solid material as a result of reaction thereof; and
selecting and intermixing at least one solid particulate material with the fluid material to form a composite;
locating the composite at the sealing location prior to the formation of the solid material, and wherein the at least one solid particulate material to move migrates within the composite to form a solids enhanced portion and a solids depleted portion of the composite at the sealing location;
wherein the solids enhanced portion has at least one of the following properties:
a thermal expansion factor of 45 or less;
an exothermic factor of 1.1 or less;
a heat flow factor of 5.5 or less;
a heat duration factor of 55 or less; and
a set time/cool down factor of 1.0 or less.

US Pat. No. 10,428,260

CURABLE COMPOSITION AND RESIN FOR TREATMENT OF A SUBTERRANEAN FORMATION

HALLIBURTON ENERGY SERVIC...

1. A method of treating a subterranean formation, comprising:placing a curable composition into the subterranean formation as an alternative to cement, the curable composition comprising:
40 to 80 wt. %, based on the total weight of the curable composition, of an epoxy silane monomer;
5 to 50 wt. %, based on the total weight of the curable composition, of a hardener; and
1 to 40 wt. %, based on the total weight of the curable composition, of a carrier fluid; and
curing the curable composition in the subterranean formation to form an epoxy silane resin, wherein the epoxy silane resin adheres to a casing disposed in the subterranean formation, thereby cementing or plugging the subterranean formation.

US Pat. No. 10,428,259

DOWNHOLE FLUIDS AND METHODS OF USE THEREOF

Halliburton Energy Servic...

1. A downhole fluid comprising:a smectite clay;
a hydroxylated polymer;
a cation;
the smectite clay, the hydroxylated polymer and the cation together in an amount sufficient to render the downhole fluid thermally thixotropic at a temperature of 400° F.; and
at least one additional downhole fluid component that is an aqueous component with a pH of at least 9, a density control additive, or a viscosity control material.

US Pat. No. 10,428,258

BARRIER PILLS

Halliburton Energy Servic...

1. A method comprising:introducing a first fluid into a wellbore;
introducing a clay-based barrier pill into the wellbore, wherein the barrier pill comprises:
a strong base selected from the group consisting of a hydroxide base, quick lime, and any combination thereof,
a naturally occurring hectorite clay, and
a naturally occurring secondary clay comprising at least one clay selected from the group consisting of an attapulgite clay, a sepiolite clay, a palygorskite clay, and any combination thereof, wherein the barrier pill has a clay concentration between about 8 and about 20 pounds per barrel, and wherein a gel strength of the barrier pill is substantially maintained or increased, or decreases less than a gel strength of the barrier pill without the secondary clay, when the barrier pill is exposed to one or more salts; and
introducing a second fluid into the wellbore.

US Pat. No. 10,428,257

THERMAL INTERFACE MATERIAL WITH ION SCAVENGER

Honeywell International I...

1. An electronic component comprising:a heat sink having a copper surface;
an electronic chip;
a thermal interface material positioned between the heat sink and electronic chip and including a first surface in direct contact with the copper surface of the heat sink, the thermal interface material including:
at least one elastomeric polymer;
at least one thermally conductive filler present in a total amount between 75 wt. % and 95 wt. %, based on a total weight of the thermal interface material; and
at least one ion scavenger.

US Pat. No. 10,428,256

RELEASABLE THERMAL GEL

Honeywell International I...

1. A thermal gel comprising:a first component including:
a primary silicone oil;
an inhibitor;
a catalyst; and
at least one thermal conductive filler;
a second component including:
a primary silicone oil;
a crosslinking silicone oil; and
at least one thermal conductive filler;
wherein the primary silicone oil of the first component is a vinyl silicone oil, the primary silicone oil of the second component is a vinyl silicone oil, and the crosslinking silicone oil of the second component is a hydrosilicone oil;
wherein the thermal gel is releasable from a substrate upon which the thermal gel is applied;
wherein the total content of the thermally conductive fillers in the thermal gel is between 75 wt. % and 95 wt. %; and
wherein the weight ratio between the first component and the second component is between 0.5:1 and 2:1.

US Pat. No. 10,428,255

SHAPED ABRASIVE PARTICLE AND METHOD OF FORMING SAME

1. A particulate material comprising:a shaped abrasive particle having a body comprising a first major surface, a second major surface, and a side surface extending between the first major surface and second major surface, wherein the side surface comprises a fractured region located on a portion of the side surface, wherein the fractured region is spaced apart from an edge defining the first major surface and abutting an edge defining the second major surface, and wherein the fractured region has a height (hfr) that is less than a height of the body (hc) on the side surface.

US Pat. No. 10,428,253

PHOTOSENSITIVE RESIN COMPOSITION, FILM ADHESIVE, ADHESIVE SHEET, ADHESIVE PATTERN, SEMICONDUCTOR WAFER WITH ADHESIVE LAYER, AND SEMICONDUCTOR DEVICE

Hitachi Chemical Company,...

1. A photosensitive resin composition comprising:an alkali-soluble resin having a phenolic hydroxyl group as an end group and a phenolic hydroxyl group as a side chain group (A);
a radiation-polymerizable compound (B); and
a photoinitiator (C);
wherein a glass transition temperature of the alkali-soluble resin is 40° C. to 120° C.

US Pat. No. 10,428,249

ADHESIVE COMPOSITION AND FILM ROLL

DEXERIALS CORPORATION, T...

1. A film roll comprising:an adhesive film comprising a phenoxy resin, an epoxy resin, a latent curing agent, an acrylic rubber having a carboxyl group or a glycidyl group, and a butadiene rubber, in which the acrylic rubber phase-separates from the epoxy resin at a normal temperature of 20° C.±15° C. and is compatible with the epoxy resin at a predetermined temperature of 40 to 80° C.; and
a reel in which the adhesive film is wound around a roll core,
wherein the epoxy resin is a bisphenol-type epoxy resin,
wherein the latent curing agent is an imidazole-type latent curing agent,
wherein the acrylic rubber content is 40 pts. mass or more and 60 pts. mass or less with respect to 100 pts. mass of epoxy resin,
wherein the latent curing agent is a microcapsule type, and
wherein the latent curing agent content is 80 pts. mass or more and 120 pts. mass or less with respect to 100 pts. mass of epoxy resin.

US Pat. No. 10,428,247

ADHESIVE COMPOSITION FOR TOUCH SENSOR AND OPTICAL LAMINATE USING THE SAME

DONGWOO FINE-CHEM CO., LT...

1. An adhesive composition for a touch sensor comprising: a photopolymerizable compound; a titanocene-based compound as a photoinitiator; and a phosphoric acid-based compound or a phosphonic acid-based compound as a curing accelerator,wherein the phosphoric acid-based compound is a compound of the following Chemical Formula 1:

wherein
R1 is hydrogen or methyl group,
R2 is a C1-C6 alkylene group,
n is an integer of 1 to 3, and
m is an integer of 1 to 10; and
wherein the phosphonic acid-based compound is a compound of the following Chemical Formula 2:

wherein
R3 is a C1-C6 alkyl group or an aryl group, and
R4 is hydrogen, a C1-C6 alkyl group, or an aryl group.

US Pat. No. 10,428,245

MOISTURE- AND HEAT-CROSSLINKABLE POLYURETHANE-BASED ADHESIVE COMPOSITION COMPRISING A LOW CONTENT OF ISOCYANATE MONOMER

BOSTIK SA, La Plaine St ...

1. A crosslinkable adhesive composition comprising:a) from 40 to 60 wt % of at least one polyurethane obtainable by a polyaddition reaction:
of at least one aromatic or aliphatic diisocyanate that is:
a1) isophorone diisocyanate,
a2) 2,4-toluene diisocyanate,
a3) diphenylmethane-2,4?-diisocyanate,
a4) an allophanate derivative of hexamethylene diisocyanate of formula (I):

in which:
p is an integer in the range from 1 to 2;
q is an integer in the range from 0 to 9;
R represents a hydrocarbon chain, saturated or unsaturated, cyclic or acyclic, linear or branched, comprising from 1 to 20 carbon atoms;
R3 represents a divalent alkylene group, linear or branched, having from 2 to 4 carbon atoms;
or a mixture of said aromatic or aliphatic diisocyanates,
with at least one polyether diol, with or without the presence of at least one reaction catalyst, at a reaction temperature T1 below 95° C., in anhydrous conditions, and in amounts of diisocyanate(s) and of polyether diol(s) leading to an NCO/OH molar ratio, designated r1, in the range from 1.6 to 1.9; said polyurethane having formula (II)
in which:R1 represents an aliphatic or aromatic divalent group:
a1?) a divalent group derived from isophorone diisocyanate:

a2?) a divalent group derived from 2,4-toluene diisocyanate:

a3?) a divalent group derived from diphenylmethane-2,4?-diisocyanate:
ora4?) a divalent group derived from an allophanate of hexamethylene diisocyanate (HDI) of formula (III):

in which:
p is an integer in the range from 1 to 2;
q is an integer in the range from 0 to 9;
R represents a hydrocarbon chain, saturated or unsaturated, cyclic or acyclic, linear or branched, comprising from 1 to 20 carbon atoms;
R3 represents a divalent alkylene group, linear or branched, having from 2 to 4 carbon atoms;
R2, which may be identical to or different from R3, represents a divalent alkylene group, linear or branched, having from 2 to 4 carbon atoms;
n is a non-zero integer such that the number-average molecular weight of the polyether block of formula [OR2]n— is in the range from 2000 to 12000 g/mol;
m is an integer such that the number-average molecular weight of the polyurethane is in the range from 3000 to 21000 g/mol;
b) from 39 to 59 wt % of at least one compatible tackifying resin, with a number-average molecular weight in the range from 200 Da to 5000 Da, and selected from the resins obtained by one of the following methods:
b1) polymerization of terpene hydrocarbons in the presence of Friedel-Crafts catalysts, followed by reaction with phenols,
b2) polymerization of alpha-methylstyrene, followed by reaction with phenols; and
c) from 0.01 to 1 wt % of at least one crosslinking catalyst, said percentages being expressed by weight relative to the total weight of the adhesive composition.

US Pat. No. 10,428,244

CABLE WINDING TAPE, IN PARTICULAR FOR AN ENGINE COMPARTMENT OF AN AUTOMOTIVE VEHICLE

1. A cable wrapping tape comprising a strip carrier (1) consisting of fabric, the carrier on at least one side having a self-adhering adhesive layer (2) consisting of a pressure-sensitive adhesive, wherein the fabric of the carrier (1) consists of a yarn (3a, 3b) consisting of a polyamide material and having a yarn linear density of at least 280 dtex, the yarn (3a, 3b) forming warps and wefts in the fabric of the carrier, wherein the yarn (3a, 3b) is formed from 24 to 80 filaments (4) twisted with one another about a central longitudinal axis (X-X) of the yarn (3a, 3b) in an S-twist or in a Z-twist wherein the filaments (4) of the twisted yarn (3a, 3b) have a number of twists based on a meter length (T/m) in the range of 140 to 260 and whereby the filaments (4) of the twisted yarn (3a, 3b) of the warps have a greater number of twists based on a meter length (T/m) than the filaments (4) of the twisted yarn (3a, 3b) of the wefts, and wherein the cable wrapping tape meets abrasion class F, according to LV 312 both on a mandrel having a 5 mm diameter and on a mandrel having a 10 mm diameter.

US Pat. No. 10,428,243

METHOD OF UTILIZING THIN FILM PRESSURE SENSITIVE STRIPS TO MEASURE PRESSURE APPLIED TO A SEAL

FORD MOTOR COMPANY, Dear...

1. A method of assembling a vehicle comprising:identifying critical fit areas between a closure member and a closure member frame;
adhering plural pressure indicator tapes to a peripheral seal in the critical fit areas;
closing the closure member against the seal to produce a marking on the pressure indicator tapes; and
comparing visually the marking to a reference pressure intensity scale to establish an observed pressure intensity level.

US Pat. No. 10,428,242

SLURRY COMPOSITION FOR CHEMICAL MECHANICAL POLISHING

SAMSUNG ELECTRONICS CO., ...

1. A slurry composition for chemical mechanical polishing, the slurry composition comprising:ceramic polishing particles;
a dispersion agent;
a pH control agent and
an additive having affinity with silicon nitride, the additive having affinity with silicon nitride including a group that forms a covalent bond with an amine group of silicon nitride or an electrostatic interaction bond with an amine group of silicon nitride, the group not forming a hydrogen bond with a hydroxyl group in the dispersion agent.

US Pat. No. 10,428,241

POLISHING COMPOSITIONS CONTAINING CHARGED ABRASIVE

Fujifilm Electronic Mater...

1. A polishing composition, comprisinga) a cationic abrasive comprising alumina, silica, titania, zirconia, a co-formed product thereof, or a mixture thereof, wherein the cationic abrasive comprises terminal groups of formula (I):
—Om—X—(CH2)n—Y  (I),in which m is an integer from 1 to 3; n is an integer from 1 to 10; X is Al, Si, Ti, or Zr; and Y is a cationic amino group or a cationic thiol group;b) an acid or base; and
c) water;
wherein the polishing composition has a pH of about 2 to about 7, is free of a cationic polymer, and is substantially free of a halide salt; and
wherein the polishing composition has a first rate of removal of silicon oxide, a second rate of removal of silicon nitride, and a ratio of the first rate to the second rate is at least about 2:1.

US Pat. No. 10,428,240

METHOD FOR PREPARING SLURRY COMPOSITION AND SLURRY COMPOSITION PREPARED THEREBY

KCTECH CO., LTD., Anseon...

1. A method of preparing a slurry composition, the method comprising:preparing a raw material slurry composition by mixing cerium oxide abrasive particles, a dispersant and water;
pulverizing the cerium oxide abrasive particles in the raw material slurry composition;
removing massive particles and agglomerated particles from the raw material slurry composition by putting the raw material slurry composition containing the pulverized cerium oxide abrasive particles into a separation device comprising a horizontal cylindrical rotating body and centrifuging the raw material slurry composition; and
obtaining a massive particles and agglomerated particles-removed slurry composition,
wherein a particle size ratio of the abrasive particles in the massive particles and agglomerated particles-removed slurry composition is 0.3 to 1.0 by Equation 1:
(B2?A2)/(B1?A1),  [Equation 1]
wherein A1 denotes D1 particle size before classification,
B1 denotes D99 particle size before classification,
A2 denotes D1 particle size after classification, and
B2 denotes D99 particle size after classification.

US Pat. No. 10,428,239

RESIN COMPOSITION, RESIN FILM, METHOD FOR PRODUCING RESIN FILM, METHOD FOR PRODUCING SEMICONDUCTOR DEVICE, AND SEMICONDUCTOR DEVICE

SHIN-ETSU CHEMICAL CO., L...

1. A method for producing a resin film comprising:coating two or more a delamination films with a resin composition to produce two or more resin-formed films each having a resin composition layer on each of the delamination films, and
superimposing the resin composition layers of the two or more resin-formed films with each other; wherein the resin composition comprises:
(A) a silicone resin containing a constitutional unit shown by the following composition formula (1) and having a weight average molecular weight of 3,000 to 500,000,
wherein R1 to R4 each independently represent a monovalent hydrocarbon group having 1 to 8 carbon atoms, with the proviso that the both of R3 and R4 are not methyl groups at the same time; “m” and “n” are each independently an integer of 0 to 300; the both of “a” and “b” are positive numbers satisfying a+b=1; each of “X” independently represents a divalent linking group shown by the following general formula (2) or a divalent linking group shown by the following general formula (3), with the proviso that part of or all of the “X” in the formula are divalent linking group(s) shown by the following general formula (2), and when the molar number of a unit shown by the following general formula (2) is defined as “c”, and the molar number of a unit shown by the following general formula (3) is defined as “d”, a ratio between the “c” and the “d” is in a range of 0?d?1 when the “c” is assumed to be 1;wherein R5 represents a hydrogen atom or a methyl group, and “p” is an integer of 0 to 7;wherein R6 represents a hydrogen atom or a methyl group, R7 and R8 each independently represent a monovalent hydrocarbon group having 1 to 8 carbon atoms, with the proviso that the both of R7 and R8 are not methyl groups at the same time, “q” and “r” are each independently an integer of 0 to 300, and “k” is an integer of 0 to 7;(B) an epoxy resin-curing agent; and
(C) a filler;wherein the mass fraction of the component (C) is 50 to 95% by mass based on the total mass.

US Pat. No. 10,428,238

RESIN COMPOSITION, POLYIMIDE FILM AND METHOD FOR MANUFACTURING POLYIMIDE FILM

Zhen Ding Technology Co.,...

1. A method for manufacturing a polyimide film comprising:providing a resin composition, the resin composition comprising a modified polyimide compound, an epoxy resin, and a solvent, wherein the modified polyimide compound has a chemical structural formula of

 the Ar? represents diphenyl sulfone having a chemical structural formula of

 the modified polyimide compound has a degree of polymerization n of about 1 to about 50, the epoxy resin and the modified polyimide compound are in a molar ratio of about 0.1:1 to about 1:1;
coating the resin composition on a surface of a base, and heating the resin composition to cause the modified polyimide compound and the epoxy resin to undergo a polymerization reaction; and
drying the resin composition after the polymerization reaction and separating the dried resin composition from the base, thereby forming the polyimide film.

US Pat. No. 10,428,235

PROCESS FOR PREPARING TRANSPARENT/SEMI-TRANSPARENT COLOR DISPERSIONS AND THE COLOR DISPERSIONS MADE THEREOF

Dow Global Technologies L...

1. A process for making a transparent/semi-transparent color dispersion comprisinga first step of contacting water, a first colorant, and a polysaccharide selected from methylcellulose, hydroxypropylmethylcellulose, and a mixture thereof to form a first colorant dispersion;
wherein the first colorant dispersion comprises based on total weight of the first colorant dispersion, from 0.05 wt. % to 10 wt. % of the first colorant, and from 0.05 wt. % to 10 wt. % of the polysaccharide; and
a second step of contacting the first colorant dispersion with a protective composition comprising an aqueous dispersion of polymer particles, clay, and a peptizing agent to form a dispersion of protected first colorant particles;
wherein the composition comprises based on total weight of the protective composition, from 10 wt. % to 70 wt. % of the polymer particles, from 0.05 wt. % to 10 wt. % of the clay, and from 0.05 wt. % to 2 wt. % of the peptizing agent;
wherein the weight to weight ratio of the first colorant dispersion to the protective composition is from 1:30 to 5:1; and
wherein the transparent/semi-transparent aqueous color dispersion contains substantially no organic solvent.

US Pat. No. 10,428,234

LIQUID METAL INK

United States of America ...

1. A method for forming a conductive trace on a substrate, the method comprising the steps of:combining a metallic liquid comprising gallium with a solvent to produce a metallic liquid mixture,
stimulating the metallic liquid mixture to produce a colloidal suspension of discrete metallic liquid particles surrounded by the solvent,
aerosolizing colloidal suspension with a carrier gas, and
passing the aerosolized colloidal suspension through a nozzle to deposit the discrete metallic liquid particles onto the substrate, and
annealing the deposited discrete metallic liquid particles,
thereby producing the conductive trace, where the conductive trace has a contiguous core of the metallic liquid within a solid skin having an electrical conductivity of less than 1 S/cm that bounds the liquid core.

US Pat. No. 10,428,232

INK SET, IMAGE FORMING METHOD, AND IMAGE FORMING APPARATUS

Ricoh Company, Ltd., Tok...

1. An ink set comprising:an ink A, comprising water, an organic solvent A, a self-dispersible pigment, an anionic resin particle, and an amine compound having a boiling point of 120-200 degrees C.; and
an ink B, comprising water, an organic solvent B, and a resin-coated pigment,
wherein, a mass content ratio of the anionic resin particle to the amine compound in the ink A is from 10:1 to 100:1, and
a mass content ratio of the resin-coated pigment to the amine compound in the ink A is from 10:1 to 150:1.

US Pat. No. 10,428,229

AQUEOUS COATING MATERIAL AND METHOD FOR MANUFACTURING THE SAME

INDUSTRIAL TECHNOLOGY RES...

1. An aqueous coating material, comprising:an aqueous resin; and
a surfactant, having a hydrophilic segment of poly(alkylene glycol), a hydrophobic segment of siloxane, and a terminal hydrophilic group,
wherein the surfactant is formed by reacting (a) hydrolyzed siloxane compound with (b1 amino crosslinker, and the terminal hydrophilic group is amino group,
wherein the siloxane compound has a chemical formula:

wherein each of R1 is independently of C1-6alkyl group,
R2 is C2-10 alkylene group,
R3 is C2-4 alkylene group,
R4 is H or C1-4 alkyl group,
m=0-10,
n=1-10, and
=2-50;
wherein (b1) amino crosslinker has a chemical formula:

wherein each of R5 is independently of C1-6 alkyl group,
R6 is C1-10 alkylene group,
R7 is C2-4 alkylene group, and
q=0 or 1.

US Pat. No. 10,428,227

ANTISTATIC COMPOSITION FOR VEHICLE, VEHICLE, AND METHOD FOR MANUFACTURING VEHICLE

Nihon Tokushu Toryo Co., ...

1. An antistatic composition for a vehicle, consisting of a nickel powder and a polyolefin resin, which contains 2.5 to 15 vol. % of the nickel powder as a pigment volume concentration (vol. %),wherein the polyolefin is an acid-modified polyolefin or a chlorinated polyolefin.

US Pat. No. 10,428,222

SYSTEMS AND METHODS FOR CREATING DURABLE LUBRICIOUS SURFACES VIA INTERFACIAL MODIFICATION

LiquiGlide Inc., Cambrid...

1. An article, comprising:a substrate,
a liquid disposed on the substrate, the liquid having an average thickness and being immiscible with a contacting phase;
a first plurality of particles disposed in the liquid and having an average dimension between about 5 ?m and about 40 ?m and configured to remain in the liquid during use; and
a second plurality of particles disposed in the liquid and having an average dimension greater than about 20 ?m and greater than the average thickness of the liquid and configured to migrate to the contacting phase during use, wherein the first plurality of particles are hydrophobic and the second plurality of particles are hydrophilic.

US Pat. No. 10,428,221

LIQUID POLYMERIZABLE COMPOSITION COMPRISING AN ANHYDRIDE DERIVATIVE MONOMER AND MINERAL NANOPARTICLES DISPERSED THEREIN, AND ITS USE TO MANUFACTURE AN OPTICAL ARTICLE

ESSILOR INTERNATIONAL, C...

1. A liquid polymerizable composition comprising:a liquid monomer composition containing a monomer of formula (I):

wherein:
R and R?, identical or different, represent a hydrogen atom or a methyl group,
X is —O—, —S—, —NR1- or —CR2R3-,
R1 is selected from the group consisting of aryl, heteroaryl, aryl C1-C6 alkyl and heteroaryl C1-C6 alkyl, R2 and R3, identical or different, are selected from the group consisting of aryl, heteroaryl, aryl C1-C6 alkyl, heteroaryl C1-C6 alkyl, aryloxy, arylthio, aryl C1-C10 alkyloxy, heteroaryl C1-C10 alkyloxy, aryl C1-C10 alkylthio, and heteroaryl C1-C10 alkylthio, and
mineral nanoparticles homogeneously dispersed in said monomer composition, wherein said mineral nanoparticles consist of a material selected from the group consisting of ZnS, ZrO2, TiO2 and BaTiO3.

US Pat. No. 10,428,220

PARTICLES FOR ELECTROPHORETIC DISPLAYS

Merck Patent GmbH, Darms...

1. An electrophoretic fluid comprising coloured polymer particle consisting of monomer units of 0.5 -5% by weight based on the total weight of the polymerizable composition except solvent, of at least one polymerisable light stabiliser, monomer units of at least one monomer, monomer units of at least one polymerisable dye, optionally at least one core particle, optionally monomer units of at least one charged co-monomer, and optionally, monomer units of at least one crosslinking co-monomer, and optionally of at least one optionally polymerizable steric stabilizer, and wherein the coloured polymer particle has a colorfastness of ?6 according to the Blue Wool Scale.

US Pat. No. 10,428,209

FLAME RETARDANT COMPOUND INCLUDING HOST-GUEST COMPLEX

Corning Optical Communica...

18. A flame retardant cable comprising:at least one communication element;
a polymeric jacket that surrounds the at least one communication element;
wherein the polymeric jacket is formed from a flame retardant compound comprising:
a polymer base resin;
a cyclodextrin host compound; and
a guest compound including at least one atom of a transition metal, wherein the cyclodextrin host compound and the guest compound form a host-guest complex, wherein the host-guest complex acts to inhibit at least one of smoke release and smoke formation when exposed to heat, and wherein the host-guest complex is distributed within the polymer base resin.

US Pat. No. 10,428,203

PNEUMATIC TIRE

SUMITOMO RUBBER INDUSTRIE...

1. A pneumatic tire, formed from a rubber composition, the rubber composition comprising:a hydrogenated styrene-butadiene copolymer which is a random copolymer of a styrene and a 1,3-butadiene, wherein the styrene-butadiene hydrogenated copolymer has a degree of hydrogenation of the butadiene units of 90 mol % to 99 mol %, and a styrene content of 30% by mass or more;
silica; andat least one ofa first silane coupling agent represented by the following Formula (2-1):
whereinR101 represents a monovalent group selected from —Cl, —Br, —OR106, —O(O?)CR106, —ON?CR106R107, —ON?CR106R107, —NR106R107 or —(OSiR106R107 )h(OSiR106R108),where R106, R107, and R108 may be the same or different, and each represent a hydrogen atom or a C1-C18 monovalent hydrocarbon group, and h has a value, on average, of 1 to 4;
R102 represents R101, a hydrogen atom, or a C1-C18 monovalent hydrocarbon group;
R103 reprersents R101, R102, a hydrogen atom, or the group: —[O(R109O)j]0.5—, where R109 represents a C1-C18 alkylene group, and j represents an integer of 1 to 4;
R104 represents a C1-C18 divalent hydrocarbon group;
R105 represents a C1-C18 monovalent hydrocarbon group; and
x, y, and z are numbers satisfying the following relations: x+y+2z=3, 0?x?3, 0?y?2, and 0 ?z?1,ora second silane coupling agent comprising a linking unit A represented by Formula (2-2) below and a linking unit B represented by Formula (2-3) below:
whereinx represents an integer of 0 or more;
y represents an integer of 1 or more;
R201 represents a hydrogen atom, a halogen atom, a branched or unbranched C1-C30 alkyl group, a branched or unbranched C2-C30 alkenyl group, a branched or unbranched C2-C30 alkynyl group, or the alkyl group in which a terminal hydrogen atom is replaced with a hydroxy group or a carboxyl group; and
R202 represents a branched or unbranched C1-C30 alkylene group, a branched or unbranched C2-C30 alkenylene group, or a branched or unbranched C2-C30 alkynylene group; and R201 and R202 may together form a cyclic structure,
the rubber composition comprising, per 100% by mass of a rubber component, 90% to 100% by mass or more of the hydrogenated copolymer,
the silica being present in amounts of 45 to 100 parts by mass relative to 100 parts by mass of the rubber component, and
the first silane coupling agent and/or the second silane coupling agent being present in a combined amount of 1 to 10 parts by mass relative to 100 parts by mass of the silica.

US Pat. No. 10,428,197

CARBON AND ELASTOMER INTEGRATION

Lyten, Inc., Sunnyvale, ...

1. A compound comprising:an elastomer material;
a filler material;
at least one additive material; and
at least one accelerant material;
wherein the filler material comprises a graphene-based carbon material, wherein the graphene-based carbon material comprises:
carbon particles comprising graphene comprising up to 15 layers; and
particles of a nano-mix additive;
wherein:
the particles of the nano-mix additive are integrated with the carbon particles on a particle level such that the particles of the nano-mix additive and the carbon particles form aggregates together; and
the aggregates have a median size from 1 to 50 microns.

US Pat. No. 10,428,195

POLYMERIC MATERIAL FOR AN INSULATED CONTAINER

Berry Plastics Corporatio...

1. An insulative material comprising a first polymer material, a second polymer material, a chemical blowing agent, and a nucleating agent, whereinthe second polymer material is at least about 15 wt % of the insulative material
the chemical blowing agent is up to about 2 wt % of the insulative material,
the nucleating agent is up to about 2 wt % of the insulative material, and
wherein the insulative material is non-aromatic and has a density of about 0.01 g/cm3 to about 0.19 g/cm3, and
wherein the first polymer material comprises a polypropylene homopolymer,
wherein the second polymer material comprises a polypropylene homopolymer.

US Pat. No. 10,428,194

MODIFIED ACRYLIC RESIN CURED PRODUCT, AND LAMINATE THEREOF, AND PRODUCTION METHODS THEREFOR

MITSUI CHEMICALS, INC., ...

1. A modified acrylic resin cured product (C) obtained by treating the surface of a cured product (X) composed of an acrylic resinwith a compound (A) comprising, in the molecule,
one or more of anionic hydrophilic groups forming an ion pair with an onium ion of an amino silicone, and
one or more of groups selected from the group consisting of groups containing a polymerizable carbon-carbon double bond, amino groups, mercapto groups, and hydroxyl groups,
wherein the amino silicone has a molecular weight of 100 to 1,000,000 and is one or more selected from compounds represented by the following general formulae (a1) to (a3):
General Formula (a1):

wherein in the formula (a1), R1 to R8 are independently a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; n010 is an integer of 0 to 10; n0100 is an integer of 0 to 100; n02 is an integer of 0 to 2; n13 is an integer of 1 to 3; n02+n13=3; #1 and #2 represent bonding hands; and #1 and #2 are bonded together;
General Formula (a2):

wherein in the formula (a2), R1 to R11 are independently a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group; n01000 is an integer of 0 to 1000; n110 is an integer of 1 to 10; n010 is an integer of 0 to 10; n12 is an integer of 1 to 2; n01 is an integer of 0 to 1; n01+n12=2; #1 and #2 represent bonding hands; #1 and #2 are bonded together; and the compounds represented by the formula (a2) do not include the compounds represented by the formula (a1);
General Formula (a3):

wherein in the formula (a3), R1 to R5 are independently a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxy group); n01000 is an integer of 0 to 1000; n010 is an integer of 0 to 10; n01 is an integer of 0 to 2; n12 is an integer of 1 to 3; n01+n12=3; n01s and n12s each may be the same as or different from one another; #1 and #2 represent bonding hands; and #1 and #2 are bonded together.

US Pat. No. 10,428,192

CARBON FIBER REINFORCED MOLDING MATERIAL AND SHAPED PRODUCT

Teijin Limited, Osaka-Sh...

1. A plate-shaped carbon fiber reinforced molding material comprising a thermoplastic resin, carbon fibers (A) and carbon fibers (B), wherein: i) the carbon fibers (A) have fiber lengths ranging from 0.01 mm to less than 3 mm, ii) the carbon fibers (B) have fiber lengths ranging from 3 mm to less than 100 mm, iii) 1.3

US Pat. No. 10,428,185

THERMOPLASTIC ELASTOMER HYDROGELS

Colorado State University...

1. A block copolymer hydrogel, comprising:a glass formed from a dry blend comprising polystyrene-poly(ethylene oxide) diblock copolymer (SO) and polystyrene-poly(ethylene oxide)-polystyrene triblock copolymer (SOS) in a molar ratio from between 95:5 and 1:99 SO/SOS; and
a liquid medium at a concentration between about 32:1 and about 2:1 liquid medium/SO—SOS by weight, the liquid medium comprising at least one room-temperature ionic liquid (RTIL);
the block copolymer hydrogel having a fatigue resistance to at least 500,000 compression cycles, wherein the compression cycles operate with at least 12% compression at a frequency of about 1 Hz, and the compression cycles operate with at least 50% compression at least every eleventh cycle and wherein the fatigue resistance is characterized by a modulus recoverable to at least 80% of its value before the compression cycles were run.

US Pat. No. 10,428,184

METHOD FOR PRODUCING A SUPERHYDROPHOBIC MEMBRANE OR SURFACE COATING OF A SUBSTRATE

Universitaet Bayreuth, B...

1. Method for producing a superhydrophobic membrane or surface coating of a substrate from an aqueous phase comprising the following steps:a) Preparing an aqueous dispersion by dispersing particles of hydrophobic polymer(s) in an aqueous solution of protic polymer(s), wherein the protic polymer(s) and the hydrophobic polymer(s) are present in a weight ratio of protic polymer(s):hydrophobic polymer(s) in a range of 5:95 to 22:78,
b) electrospinning the dispersion of step a) onto a carrier for producing the membrane or onto the surface for producing the surface coating thereby producing at least one fiber and a nonwoven fabric from the fiber,
c) subjecting the nonwoven fabric to a sol-gel process, wherein a precursor/precursors of the sol-gel comprise(s) an alkoxysilane, and
d) curing the nonwoven fabric obtained by step c) at a temperature in a range of 50° C. to 150° C.

US Pat. No. 10,428,183

ROOM TEMPERATURE-CURABLE RESIN COMPOSITION CONTAINING AN ALUMINUM CHELATE COMPOUND

SHIN-ETSU CHEMICAL CO., L...

1. A room temperature-curable resin composition comprising:(A) 100 parts by mass of an alkoxysilyl-ethylene group terminated polymer having in one molecule at least one structure represented by the following general formula:
wherein each of R1 and R2 represents a substituted or unsubstituted monovalent hydrocarbon group having 1 to 12 carbon atoms, R1 and R2 being either identical to or different from each other; and a represents 2 or 3; and(D) 0.001 to 15 parts by mass of an aluminum chelate compound having a ?-ketoester and a ?-diketone.

US Pat. No. 10,428,182

SULFIDE-BASED POLYMER, FILM COMPRISING SAME AND METHOD FOR PREPARING SAME

LG CHEM, LTD., Seoul (KR...

1. A polymer comprising:a first unit represented by the following Chemical Formula 1; and
a second unit represented by the following Chemical Formula 2:

wherein, in Chemical Formulae 1 and 2, R1 to R9 are the same as or different from each other, and each independently hydrogen;
deuterium; a halogen group; a substituted or unsubstituted alkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted aryl group; or a substituted or unsubstituted heterocyclic group, or adjacent substituents bond to each other to form a substituted or unsubstituted aromatic cyclic group;
a to h are each an integer of 0 to 4, i is an integer of 0 to 8;
when a to i are 2 or greater, substituents in the parentheses are the same as or different from each other; and
m and n are each an integer of 1 to 1000.

US Pat. No. 10,428,181

POROUS CROSS-LINKED PARTIALLY ALIPHATIC POLYIMIDE NETWORKS

OHIO AEROSPACE INSTITUTE,...

1. A porous cross-linked partially aliphatic polyimide network comprising a polyamic acid oligomer that (i) comprises a repeating unit of a dianhydride and a diamine and terminal functional groups, (ii) has an average degree of polymerization of 10 to 70, (iii) has been cross-linked via a cross-linking agent, comprising three or more cross-linking groups, at a balanced stoichiometry of the cross-linking groups to the terminal functional groups, and (iv) has been chemically imidized to yield the porous cross-linked polyimide network, wherein the polyimide network is partially aliphatic based on one or both of the following:(a) the diamine comprises: (i) a first diamine at 5 to 95% (mol %) and (ii) a second diamine at 5 to 95% (mol %), wherein (1) the first diamine comprises a first diamine linear aliphatic backbone chain comprising carbon atoms and optionally one or more oxygen atoms therein, extending a length of 3 to 30 atoms, and having a ratio of carbon:oxygen of 2:1 to 3:0, and (2) the second diamine does not comprise any linear aliphatic backbone chain extending a length of 3 or more atoms; or
(b) the dianhydride comprises: (i) a first dianhydride at 5 to 95% (mol %) and (ii) a second dianhydride at 5 to 95% (mol %), wherein (1) the first dianhydride comprises a first dianhydride linear aliphatic backbone chain comprising carbon atoms and optionally one or more oxygen atoms therein, extending a length of 3 to 30 atoms, and having a ratio of carbon:oxygen of 2:1 to 3:0, and (2) the second dianhydride does not comprise any linear aliphatic backbone chain extending a length of 3 or more atoms.

US Pat. No. 10,428,179

POLYMERIC MATERIALS

VICTREX MANUFACTURING LIM...

1. A process for the production of a polymeric material having a repeat unit of formula—O-Ph-O-Ph-CO-Ph-  Iand a repeat unit of formula—O-Ph-Ph-O-Ph-CO-Ph-  II
wherein Ph represents a phenylene moiety, said process comprising polycondensing a mixture of at least one dihydroxybenzene compound and at least one dihydroxybiphenyl compound in the molar proportions 65:35 to 95:5 with at least one dihalobenzophenone in the presence of sodium carbonate and potassium carbonate wherein:
(i) the mole % of said potassium carbonate is 4% and is defined as

US Pat. No. 10,428,177

WATER ABSORBING OR WATER SOLUBLE POLYMERS, INTERMEDIATE COMPOUNDS, AND METHODS THEREOF

Sirrus, Inc., Loveland, ...

1. A grafted polymer comprising:i. a first component including a polymer formed by polymerizing the alkene groups of one or more monomers including a 1,1-diester-1-alkene compound, attached to;
ii. a second component that is a hydrophilic component, wherein the hydrophilic component includes a cation or a water-soluble polymer;
wherein the grafted polymer has a network structure.

US Pat. No. 10,428,176

THERMOSETTING ALKOXYSILYL COMPOUND HAVING TWO OR MORE ALKOXYSILYL GROUPS, COMPOSITION AND CURED PRODUCT COMPRISING SAME, USE THEREOF, AND METHOD FOR PREPARING ALKOXYSILYL COMPOUND

KOREA INSTITUTE OF INDUST...

1. A composition of an alkoxysilyl compound having two or more alkoxysilyl groups selected from the group consisting of the following Formulae AI to II:
in Formulae AI to DI, substituents a and b are each independently selected from the group consisting of the following Formulae S1 and S2, hydrogen, and a C1-10 alkenyl group, substituents c to f are each independently selected from the group consisting of the following Formula S1, hydrogen, a C1-10 alkyl group, a C1-10 alkenyl group, and a C6-30 aryl group, and at least two substituents among a to f are selected from the group consisting of the following Formulae S1 and S2;
in Formula AI, Y is —CH2—, —C(CH3)2—, —C(CF3)2—, —S— or —SO2—;
in Formulae EI and II, at least two substituents of g to i are selected from the group consisting of the following Formulae S1 and S2, and the remainder thereof is hydrogen, a C1-10 alkyl group, a C1-10 alkenyl group, or a C6-30 aryl group;
in Formulae FI to HI, at least two substituents of g to j are selected from the group consisting of the following Formulae S1 and S2, and the remainder thereof are hydrogen, a C1-10 alkyl group, a C1-10 alkenyl group, or a C6-30 aryl group;
in Formula HI, M is —CH2—, —C(CH3)2—, —C(CF3)2—, —S— or —SO2—; and
a meta position of oxygen in the above Formula II is substituted with a linear or branched C1-10 alkyl group,
—(CH2)z—SiR1R2R3  [Formula S1]
—CONH(CH2)z—SiR1R2R3  [Formula S2]
in Formulae S1 and S2, at least one of R1 to R3 is a linear or branched C1-10 alkoxy group, the other thereof is a linear or branched C1-10 alkyl group, and z is an integer of 3 to 10;
at least one filler selected from the group consisting of inorganic particles and fibers; and
an epoxy resin;
wherein a molar ratio of an alkoxy group of the alkoxysilyl compound to an epoxy group of the epoxy compound is 0.90-10:1.

US Pat. No. 10,428,171

CYCLIC DYNAMIC POLYUREAS FOR POLYMERIC UREA PROCESSING

THE BOARD OF TRUSTEES OF ...

1. A cyclic oligomer or polymer corresponding to formula (Ia) or (Ib)
wherein L and M are independently selected from aryl, (C1-C20)alkyl, (C4-C10)cyclolalkyl, (C1-C20)alkyl(C4-C10)cycloalkyl, (C1-C20)alkyl(C4-C10)cycloalkyl(C1-C20)alkyl, (C6-C10)aryl, (C1-C20)alkyl(C6-C10)aryl, (C1-C20)alkyl(C6-C10)aryl(C1-C20)alkyl, (C2-C20)alkyl-PEG-(C2-C20)alkyl, —(C1-C20)alkylO(C1-C20)alkyl-, —(C1-C20)alkylS(C1-C20)alkyl-, —NR4—, ?N—, —C(R5)2—, —NC(?O)(C1-C20)alkyl-, —C(?O)(C1-C20)alkyl-, —C(?O)—(NR4)—, —S(?O)2O—, —S(?O)2—(C1-C20)alkyl-, —OS(?O)2O(C1-C20)alkyl-, —S(?O)2NR4—, —S(?O)(C1-C20)alkyl-, —P(?O)(OR4)O—, —C(S)—(C1-C20)alkyl-, —C(O)O(C1-C20)alkyl-, —C(?O)O—, —C(?S)O(C1-C20)alkyl-, —C(?O)S(C1-C20)alkyl-, —C(?S)S(C1-C20)alkyl-, —C(O)NR4—(C1-C20)alkyl-, and —C(?NR4)NR4—;
each R1, R2, R3 and R4 are independently selected from the group consisting of aryl, (C1-C20)alkyl, (C4-C10)cyclolalkyl, (C1-C20)alkyl(C4-C10)cycloalkyl, (C1-C20)alkyl(C4-C10)cycloalkyl(C1-C20)alkyl, (C2-C20)alkyl-PEG-(C2-C20)alkyl, and H;
each R5 is independently selected from F, Cl, Br, and I;
and x is an integer from about 2 to about 500.

US Pat. No. 10,428,169

POLYMER, COMPOSITION, OPTICAL FILM, AND LIQUID CRYSTAL DISPLAY DEVICE

FUJIFILM Corporation, To...

1. A branched polymer, comprising:(i) a mesogenic group-containing monomeric first component selected from the group consisting of a compound represented by General Formula (X) and a compound represented by General Formula (I),
Qx1-Lx1-Cyx1-Lx2?Cyx2-Lx3?nxCyx3-Lx4-Qx2   General Formula (X)
in the formula, QX1 and QX2 each independently represent a polymerizable group, LX1 and LX4 each independently represent a divalent linking group, LX2 and LX3 each independently represent a single bond or a divalent linking group, CyX1, CyX2, and CyX3 represent a divalent cyclic group, and nx represents an integer of 0 to 3,

in General Formula (I), Y11, Y12 and Y13 each independently represent a methine which may be substituted or a nitrogen atom, L1, L2, and L3 each independently represent a single bond or a divalent linking group, H1, H2, and H3 each independently represent General Formula (I-A) described below or General Formula (I-B) described below, and R1, R2, and R3 each independently represent General Formula (I-R) described below,

in General Formula (I-A), YA1 and YA2 each independently represent methine which may have a substituent or a nitrogen atom, XA represents an oxygen atom, a sulfur atom, methylene, or imino, * represents a bonding position with respect to an L1 side to an L3 side in General Formula (I) described above, and ** represents a bonding position with respect to an R1 side to a R3 side in General Formula (I) described above,

in General Formula (I-B), YB1 and YB2 each independently represent methine which may have a substituent or a nitrogen atom, XB represents an oxygen atom, a sulfur atom, methylene, or imino, * represents a bonding position with respect to an L1 side to an L3 side in General Formula (I) described above, and ** represents a bonding position with respect to an R1 side to a R3 side in General Formula (I) described above, and
*?Lr1-Q2?n1Lr2-Lr3-Q1   General Formula (I-R)
in General Formula (I-R), * represents a bonding position with respect to an H1 side to an H3 side in General Formula (I), Lr1 represents a single bond or a divalent linking group, Q2 represents a divalent group having at least one type of cyclic structure, n1 represents an integer of 0 to 4, Lr2 and Lr3 each independently represent a divalent linking group, Q1 represents a polymerizable group or a hydrogen atom, and here, at least two of a plurality of Q1's represent a polymerizable group; and
(ii) a fluorine-containing monomeric second component represented by General Formula (a) described below,

in General Formula (a), Ra1 represents a hydrogen atom or an alkyl group having 1 to 20 carbon atoms, and Ra2 represents an alkyl group having 1 to 20 carbon atoms or an alkenyl group having 1 to 20 carbon atoms in which at least one carbon atom has a fluorine atom as a substituent.

US Pat. No. 10,428,168

COMPOSITION FOR POLYMERIZATION, METHOD FOR PRODUCING SAME, COMPOSITION FOR A COATING CONTAINING COMPOSITION FOR POLYMERIZATION, METHOD FOR PRODUCING COMPOSITION FOR A COATING USING COMPOSITION FOR POLYMERIZATION, AND METHOD FOR PRODUCING COATING

FUJIFILM Corporation, To...

1. A composition for polymerization, comprising:a monomer represented by the following Formula (I); and
water,
wherein a moisture content is equal to or higher than 3% by mass and less than 10% by mass,

wherein R represents a hydrogen atom or a methyl group.

US Pat. No. 10,428,167

ESTERIFIED POLY(VINYL ACETAL) RESIN COMPOSITIONS, LAYERS, AND INTERLAYERS HAVING ENHANCED PROPERTIES

Solutia Inc., St. Louis,...

1. An acetoacetylized polymer comprising units having the structure:
wherein R? is hydrogen, a substituted or unsubstituted C1 to C12 alkyl, a substituted or unsubstituted C6 to C14 aryl, a substituted or unsubstituted C6 to C14 alkaryl, or a combination thereof, “x” is from about 52 to about 78 mole %, “y” is from about 26 to about 45 mole %, “z” is from about 0 to about 20 mole %, and “a” is present in an amount greater than 0 to 45 mole % such that 0?y?a?10 mole % and x+y+z=100; wherein the glass transition temperature of the acetoacetylized polymer is less than the glass transition temperature of the non-acetoacetylized polymer, or wherein the loss factor at the glass transition temperature of the acetoacetylized polymer is less than the loss factor at the glass transition temperature of the non-acetoacetylized polymer, or wherein both the glass transition temperature of the acetoacetylized polymer is less than the glass transition temperature of the non-acetoacetylized polymer and the loss factor at the glass transition temperature of the acetoacetylized polymer is less than the loss factor at the glass transition temperature of the non-acetoacetylized polymer.

US Pat. No. 10,428,165

SYSTEMS AND PROCESSES FOR POLYACRYLIC ACID PRODUCTION

Novomer, Inc., Boston, M...

1. An integrated system for producing polyacrylic acid (PAA) and superabsorbent polymer (SAP) from ethylene, comprising:an oxidative reactor, comprising:
an inlet configured to receive ethylene,
an oxidative reaction zone configured to convert ethylene to ethylene oxide (EO), and
an outlet configured to provide an EO stream comprising the EO;
a central reactor, comprising:
an inlet configured to receive EO from the EO stream of the oxidative reactor, and carbon monoxide (CO) from a CO source,
a central reaction zone configured to convert EO to beta propiolactone (BPL) or polypropiolactone (PPL), or a combination thereof, and
an outlet configured to provide a carbonylation stream comprising the BPL, or a carbonylation stream comprising the PPL, or a combination thereof;
one or more of (i), (ii) and (iii):
(i) a first reactor, comprising:
an inlet configured to receive BPL from the carbonylation stream of the central reactor,
a first reaction zone configured to convert BPL to acrylic acid (AA), and
an outlet configured to provide an AA stream comprising the AA,
(ii) a second (a) reactor, comprising:
an inlet configured to receive BPL from the carbonylation stream of the central reactor,
a second (a) reaction zone configured to convert BPL to PPL, and
an outlet configured to provide a PPL stream comprising the PPL, and
a second (b) reactor, comprising:
an inlet configured to receive the PPL stream of the second (a) reactor,
a second (b) reaction zone configured to convert at least some of the PPL to AA, and
an outlet configured to provide an AA stream comprising the AA, and
(iii) a third reactor, comprising:
an inlet configured to receive PPL from the carbonylation stream of the central reactor,
a third reaction zone configured to convert PPL to AA, and
an outlet configured to provide an AA stream comprising the AA;
a fourth reactor, comprising:
an inlet configured to receive the AA stream of one or more of the first, second (b) and third reactor,
a fourth reaction zone configured to convert AA to polyacrylic acid (PAA), or a salt thereof, and
an outlet configured to provide a PAA stream comprising the PAA, or a salt thereof;
a fifth reactor, comprising:
an inlet configured to receive PAA, or a salt thereof, from the PAA stream of the fourth reactor,
a fifth reaction zone configured to directly convert the PAA, or a salt thereof, to superabsorbent polymer (SAP), and
an outlet configured to provide a SAP stream comprising the SAP; and
a controller to independently modulate production of the EO, BPL, PPL, AA, PAA and SAP.

US Pat. No. 10,428,164

PRINTING MATERIAL FOR THREE-DIMENSIONAL PRINTING APPARATUS

XYZprinting, Inc., New T...

1. A printing material for a three-dimensional printing apparatus, comprising:a wire comprising a core and a shell;
wherein a Shore hardness of the core is A45-A90;
the shell covers the core, wherein a Shore hardness of the shell is D40-D85, and the Shore hardness of the shell is higher than the Shore hardness of the core;
a volume percentage of the shell is 10% to 30%, and a volume percentage of the core is 70% to 90%,
wherein the wire has a diameter of 1.7 mm to 3.1 mm.

US Pat. No. 10,428,160

COLORIMETRIC HYDROGEL BASED NANOSENSOR FOR DETECTION OF THERAPEUTIC LEVELS OF IONIZING RADIATION

ARIZONA BOARD OF REGENTS ...

6. An apparatus comprising:a substantially colorless hydrogel to receive a low dose of radiation and form a radiated hydrogel having a color; and
a detector optically coupled to the radiated hydrogel, wherein the radiated hydrogel comprises a plasmonic nanoparticle.

US Pat. No. 10,428,138

ANTIBODY AND ANTIBODY-CONTAINING COMPOSITION

Ostrich Pharma KK, Kyoto...

1. A lotion, comprising:ostrich antibodies which specifically bind to a surface protein of a virus, wherein the virus comprises any one of HPV type 6, 11, 16 or 18; and
water, glycerol, ethanol, sodium polyacrylate, hydroxyethyl cellulose, phenoxyethanol, EDTA-2Na, paraben, polysorbate 80, and fatty acid sorbitan.

US Pat. No. 10,428,132

TUMOR NECROSIS FACTOR-RELATED APOPTOSIS-INDUCING LIGAND VARIANT, AS WELL AS A PREPARATION METHOD AND USE THEREOF

WEST CHINA HOSPITAL, SICH...

1. A tumor necrosis factor-related apoptosis-inducing ligand variant, characterized in that the variant is a fusion protein of a tumor necrosis factor-related apoptosis-inducing ligand and an F3 peptide, and the F3 peptide is fused to the N-terminus or C-terminus of the tumor necrosis factor-related apoptosis-inducing ligand by a linker.

US Pat. No. 10,428,122

TUBERCULOSIS COMPOSITIONS AND METHODS OF TREATING OR PREVENTING TUBERCULOSIS

International AIDS Vaccin...

1. A fusion protein comprising at least four or five Mycobacterium tuberculosis (Mtb) antigens, wherein the Mtb antigens are chosen from Rv1009, Rv3136, Rv3615c, Rv2628, Rv2034, and Rv3136 N-terminus, and wherein the fusion protein is chosen from:Rv1009-Rv2628-Rv3615c-Rv3136;
Rv1009-Rv2034-Rv2628-Rv3615c-Rv3136;
Rv1009-Rv3615c-Rv2034-Rv2628;
Rv3615c-Rv2034-Rv2628-Rv1009;
Rv2034-Rv3615c-Rv2628-Rv3136;
Rv3136-Rv2628-Rv3615c-Rv2034;
Rv1009-Rv3136Nt-Rv2628-Rv2034-Rv3615c;
Rv2034-Rv3615c-Rv3136Nt-Rv2628-Rv1009;
Rv3615c-Rv2628-Rv1009-Rv3136Nt-Rv2034;
Rv1009-Rv2628-Rv3136Nt-Rv2034-Rv3615c;
Rv2628-Rv3136Nt-Rv1009-Rv2034-Rv3615c; and
Rv2628-Rv3136Nt-Rv2034-Rv3615c-Rv1009.

US Pat. No. 10,428,112

MULTIPLEXED SAME TYPE-ANTIGENIC PEPTIDE

RIKEN, Wako-shi, Saitama...

1. A multiplexed same type-antigenic peptide comprising a dendritic core and B-cell recognition peptides, wherein the multiplexed same type-antigenic peptide comprises 4 to 8 B-cell recognition peptides of the same type, which are bound to the terminal ends of the dendritic core directly or via a spacer, and production of a class-switched antibody is induced by directly stimulating B cells in vivo in the absence of a T cell epitope; wherein the dendritic core has the following structure:

US Pat. No. 10,428,109

PROCESS FOR THE PREPARATION OF 1,5-BENZOTHIAZEPINE COMPOUNDS

1. A process for the preparation of a compound of formula (I):
comprising reacting a compound of formula (II):

with a compound of formula (III):

wherein
R6 is a suitable protecting group;
to obtain a compound of formula (IV):

and deprotecting said compound of formula (IV) to obtain the compound of formula (I).

US Pat. No. 10,428,108

DIFLUOROKETAMIDE DERIVATIVES

Hoffmann-La Roche Inc., ...

1. A compound of formula (I)
wherein:
R1 is alkyl, optionally substituted cycloalkyl, haloalkyl, optionally substituted heterocycloalkylalkyl optionally substituted arylalkyl or optionally substituted heteroarylalkyl, wherein each moiety is optionally substituted by one to three substituents independently selected from halogen, alkyl, haloalkyl, cycloalkyl, cyano, hydroxyl, alkoxy, haloalkoxy or phenyl;
R2, R3 R4, R6, R7 and R9 are independently selected from hydrogen, alkyl or cycloalkyl;
R5 is optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, wherein each moiety is optionally substituted by one to three substituents independently selected from halogen, alkyl, haloalkyl, cycloalkyl, cyano, hydroxyl, alkoxy, haloalkoxy or phenyl;
R8 is optionally substituted adamantylalkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted dicycloalkylalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted arylalkenyl, optionally substituted diarylalkyl, optionally substituted aryloxyalkyl, optionally substituted diaryloxyalkyl, optionally substituted arylaryloxyalkyl, optionally substituted heteroarylaryloxyalkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heteroarylalkenyl, optionally substituted arylheteroarylalkyl, optionally substituted arylheteroaryloxyalkyl or optionally substituted aryloxyheteroarylalkyl, wherein each moiety is optionally substituted by one to three substituents independently from selected halogen, alkyl, haloalkyl, cycloalkyl, cyano, hydroxyl, alkoxy, haloalkoxy or phenyl;
wherein a heterocycloalkyl moiety is a ring system of 4 to 9 ring atoms, comprising 1, 2, or 3 ring heteroatoms selected from N, O and S, the remaining ring atoms being carbon, heteroaryl moiety is a ring system of 5 or ring atoms, comprising 1, 2, 3 or 4 heteroatoms selected from N, O and S; the remaining ring atoms being carbon and an aryl moiety is a monovalent aromatic carbocyclic mono- or bicyclic ring system comprising 6 to 10 carbon ring atoms;
or, a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,106

PHOSPHATE REPLACEMENT MRNA CAP ANALOGS

ModernaTX, Inc., Cambrid...

1. An RNA molecule having a 5? end comprising a compound of formula (III):
wherein
indicates the attachment point of the 5? end to the RNA molecule;B1 is
whereinindicates the attachment point of B1 to the compound;Ra, Rb, and Rc are H;
R1 is CH3;
B2 is
whereinindicates the attachment point of B2 to the compound;Rd, Re, and Rf are H;
X1 is N or N+(CH3);
X2 is O;
R20, R21, R22, and R23 are H;
R27 and R28 are OH;
R2 is OR3;
R3 is H or CH3; and
Y2 is
whereinindicates the attachment points of Y2 to the compound.

US Pat. No. 10,428,105

ALKYNYL NUCLEOSIDE ANALOGS AS INHIBITORS OF HUMAN RHINOVIRUS

Novartis AG, Basel (CH)

1. The compound:
or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,103

LABELLED NUCLEOTIDES

Illumina Cambridge Limite...

1. A nucleoside or nucleotide comprising a base attached to a detectable label via a phosphine-cleavable linker comprising a disulfide, wherein the nucleoside or nucleotide comprises a ribose or deoxyribose moiety with a hydroxyl protecting group attached to the 2? or 3? oxygen atom, and wherein the protecting group is azidomethyl.

US Pat. No. 10,428,102

GLYCOLIPIDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR USE IN THERAPY

THE UNIVERSITY OF NOTTING...

1. A compound of Formula Ie:or a pharmaceutically acceptable salt thereof, for use in medicine,wherein:
R1 a carbohydrate group;
R2 is selected from hydrogen, a C1-C24 alkyl or a C1-C24 derivative of an alkyl group, a C2-C24 alkenyl or a C2-C24 derivative of an alkenyl group, and a C2-C24 alkynyl group or a C2-C24 derivative of an alkynyl group;
R3 is selected from hydrogen, a C1-C24 alkyl or a C1-C24 derivative of an alkyl group, a C2-C24 alkenyl or a C2-C24 derivative of an alkenyl group, and a C2-C24 alkynyl group or a C2-C24 derivative of an alkynyl group;
X is either absent or is -O-, -NRa-, -S- or -CRaRb-, wherein Ra and Rb are independently selected from the group consisting of hydrogen and C1-C4 alkyl; and
n is an integer from 1 to 6;
wherein said derivative of alkyl, alkenyl or alkynyl group is composed of said alkyl, alkenyl or alkynyl group wherein one or more of the hydrogen atoms in the hydrocarbon chain of said derivative are replaced with substituent groups selected from hydroxyl, amino, carboxyl, aryl, or heteroaryl groups

US Pat. No. 10,428,100

SUBSTITUTED LEAD HALIDE PEROVSKITE INTERMEDIATE BAND ABSORBERS

UChicago Argonne, LLC, C...

1. A substituted perovskite comprising:a material having the formula:
APb1-xBxBr3-yCly,
where A is a cation, B is Fe or Co, X is greater than 0 and less than 1 and y is 0-3).

US Pat. No. 10,428,099

PHARMACEUTICAL CO-CRYSTAL COMPOSITION AND USE THEREOF

SYN-NAT PRODUCTS ENTERPRI...

1. A co-crystal comprising a platinum analogue and a diacid,wherein the platinum analogue is selected from the group consisting of:
andthe diacid is selected from the group consisting of:

provided that when the platinum analogue is carboplatin (Pt-01), the diacid is not CF-01, CF-04, CF-10A, CF-10B, CF-10C, or CF-10D.

US Pat. No. 10,428,097

PROCESS FOR PREPARATION OF FOSAPREPITANT DIMEGLUMINE AND AN INTERMEDIATE THEREOF

Piramal Enterprises Limit...

1. A process for the in-situ preparation of 1-deoxy-1-(methylamino)-D-Glucitol[3-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl) phenyl] ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-2,5-dihydro-5-oxo-1H-1,2,4-triazol-1-yl] phosphonate (2:1) salt (fosaprepitant dimeglumine) of formula I,
comprising the steps of,
(i) treating aprepitant of formula III,

with tetrabenzyl pyrophosphate using a base in the presence of a solvent at a temperature of ?35° C. to 0° C. for 1 h to 4 h to obtain fosaprepitant dibenzyl ester of formula II,

(ii) adding at least one solvent or a mixture of solvents to the reaction mass obtained in step (i),
(iii) adding an inorganic acid to the reaction mass obtained in step (ii),
(iv) concentrating the reaction mass obtained in step (iii),
(v) adding at least one solvent or a mixture of solvents thereof to the reaction mass obtained in step (iv),
(vi) filtering the reaction mass obtained in step (v) to obtain a residue, Residue-A,
(vii) adding at least one solvent or a mixture of solvents thereof to the residue obtained in step (vi),
(viii) filtering the reaction mass obtained in step (vii) to obtain a residue, Residue-B,
(ix) adding at least one solvent or a mixture of solvents thereof to the residue obtained in step (viii),
(x) filtering the reaction mass obtained in step (ix) and concentrating the filtrate to yield fosaprepitant dibenzyl ester of purity >96% as an oil,
(xi) dissolving the oil obtained in step (x) in at least one solvent or a mixture of solvents thereof,
(xii) adding N-methyl-D-glucamine and Pd/C to the reaction mass obtained in step (xi) and hydrogenating the reaction mass for 8 h to 14 h at 2 kg to 8 kg pressure,
(xiii) filtering the reaction mass obtained in step (xii),
(xiv) adding metal scavenger to the reaction mass obtained in step (xiii) and stirring for 8 h to 14 h, and
(xv) obtaining fosaprepitant dimeglumine of purity >99% from the resulting reaction mass of step (xiv) on further work-up.

US Pat. No. 10,428,096

POLYKETONE POLYMERIZATION CATALYST

HYOSUNG CHEMICAL CORPORAT...

1. A polyketone polymerization catalyst, consisting of:(A) a metal ion;
(B) ((2,2-dimethyl-1,3-dioxane-5,5-diyl)bis(methylene))bis(bis(2-methoxyphenyl)phosphine) represented by following Formula 1 as a ligand; and
(C) an acid, wherein a molar ratio of component (A) and component (B) to component (C) is 1:7 to 1:20

US Pat. No. 10,428,094

AMIDE COMPOUNDS FOR TREATMENT OF COMPLEMENT MEDIATED DISORDERS

Achillion Pharmaceuticals...

1. A pharmaceutical composition comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable carrier:wherein:Q1 is C(R1R1?);
Q2 is C(R2R2?);
Q3 is C(R3R3?);
X1 is N and X2 is CH;
R1, R1?, R2, R2?, R3, and R3? are independently chosen from hydrogen, halogen, hydroxyl, nitro, cyano, amino, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C1-C6alkoxy, C2-C6alkynyl, C2-C6alkanoyl, C1-C6thioalkyl, hydroxyC1-C6alkyl, aminoC1-C6alkyl, —C0-C4alkylNR9R10, —C(O)OR9, —OC(O)R9, —NR9C(O)R10, —C(O)NR9R10, —OC(O)NR9R10, —NR9C(O)OR10, C1-C2haloalkyl, and C1-C2haloalkoxy, where R9 and R10 are independently chosen at each occurrence from hydrogen, C1-C6alkyl, (C3-C7cycloalkyl)C0-C4alkyl, —C0-C4alkyl(C3-C7cycloalkyl), and —O—C0-C4alkyl(C3-C7cycloalkyl);
or R1 and R2 are linked to form a 3- to 6-membered carbocyclic or aryl ring;
or R2 and R3 are linked to form a 3- to 6-membered carbocyclic ring;
or R1 and R1?, or R2 and R2?, or R3 and R3? are linked to form a 3- to 6-membered carbocyclic spiro ring;
or R2 and R2? or R3 and R3? are linked to form a 3- to 6-membered heterocyclic spiro ring;
each of which ring is unsubstituted or substituted with 1 or more substituents independently chosen from halogen, hydroxyl, cyano, —COOH, C1-C4alkyl, C2-C4alkenyl, C2-C4alkynyl, C1-C4alkoxy, C2-C4alkanoyl, hydroxyC1-C4alkyl, (mono- and di-C1-C4alkylamino)C0-C4alkyl, —C0-C4alkyl(C3-C7cycloalkyl), —O—C0-C4alkyl(C3-C7cycloalkyl), C1-C2haloalkyl, and C1-C2haloalkoxy;
or R1 and R1? or R2 and R2? are linked to form a carbonyl group;
A is a group selected from:

R5 and R6 are independently selected from —CHO, —C(O)NH2, —C(O)NH(CH3), C2-C6alkanoyl, hydrogen, hydroxyl, halogen, cyano, nitro, —COOH, —SO2NH2, vinyl, C1-C6alkyl, C2-C6alkenyl, C1-C6alkoxy, —C0-C4alkyl(C3-C7cycloalkyl), —C(O)C0-C4alkyl(C3-C7cycloalkyl), —P(O)(OR9)2, —OC(O)R9, —C(O)OR9, —C(O)N(CH2CH2R9)(R10), —NR9C(O)R10, phenyl, and 5- to 6-membered heteroaryl;
R8 and R8? are independently chosen from hydrogen, halogen, hydroxyl, C1-C6alkyl, —C0-C4alkyl(C3-C7cycloalkyl), C1-C6alkoxy, and (C1-C4alkylamino)C0-C2alkyl; or R8 and R8? are linked to form an oxo group; or R8 and R8? taken together with the carbon that they are bonded to form a 3-membered carbocyclic ring;
X11 is N or CR11;
X12 is CR12;
X13 is CR13;
X14 is N or CR14;
one of R12 and R13 is chosen from R31 and the other of R12 and R13 is chosen from R32:
R31 is chosen from hydrogen, halogen, hydroxyl, nitro, cyano, amino, —COOH, C1-C2haloalkyl, C1-C2haloalkoxy, C1-C6alkyl, —C0-C4alkyl(C3-C7cycloalkyl), C2-C6alkenyl, C2-C6alkanoyl, C1-C6alkoxy, C2-C6alkenyloxy, —C(O)OR9, C1-C6thioalkyl, —C0-C4alkylNR9R10, —C(O)NR9R10, —SO2R9, —SO2NR9R10, —OC(O)R9, and —C(NR9)NR9R10, each of which R31 other than hydrogen, halogen, hydroxyl, nitro, cyano, C1-C2haloalkyl, and C1-C2haloalkoxy is unsubstituted or substituted with one or more substituents independently selected from halogen, hydroxyl, nitro, cyano, amino, —COOH, —CONH2 C1-C2haloalkyl, and C1-C2haloalkoxy, and each of which R31 is also optionally substituted with one substituent chosen from phenyl and 4- to 7-membered heterocycle containing 1, 2, or 3 heteroatoms independently chosen from N, O, and S; which phenyl or 4- to 7-membered heterocycle is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkanoyl, C1-C6alkoxy, (mono- and di-C1-C6alkylamino)C0-C4alkyl, C1-C6alkylester, —C0-C4alkyl)(C3-C7cycloalkyl), C1-C2haloalkyl, and C1-C2haloalkoxy;
R32 is —C(O)NR21SO2R22, —NR9C(O)OR10, —NR9C(O)OR23, —NR9C(O)R21, —NR9C(O)NR9R10, —NR9C(O)NR10R23, or —NR9C(O)NR24R25;
R11 and R14, are independently chosen at each occurrence from hydrogen, halogen, hydroxyl, nitro, cyano, —O(PO)(OR9)2, —(PO)(OR9)2, C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C2-C6alkanoyl, C1-C6alkoxy, C1-C6thioalkyl, —C0-C4alkyl(mono- and di-C1-C6alkylamino), —C0-C4alkyl(C3-C7cycloalkyl), —C0-C4alkoxy(C3-C7cycloalkyl), C1-C2haloalkyl, and C1-C2haloalkoxy;
R21 and R22 are independently chosen at each occurrence from hydrogen, hydroxyl, cyano, amino, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, (C3-C7cycloalkyl)C0-C4alkyl, (phenyl)C0-C4alkyl, —C1-C4alkylOC(O)OC1-C6alkyl, —C1-C4alkylOC(O)C1-C6alkyl, —C1-C4alkylC(O)OC1-C6alkyl, (4- to 7-membered heterocycloalkyl)C0-C4alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and (5- or 6- membered unsaturated or aromatic heterocycle)C0-C4alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S;
R23 is independently chosen at each occurrence from C1-C6alkyl, C1-C6haloalkyl, (aryl)C0-C4alkyl, (C3-C7cycloalkyl)C0-C4alkyl, (phenyl)C0-C4alkyl, (4- to 7-membered heterocycloalkyl)C0-C4alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and (5- or 6- membered unsaturated or aromatic heterocycle)C0-C4alkyl having 1, 2, or 3 heteroatoms independently chosen from N, O, and S;
R24 and R25 are taken together with the nitrogen to which they are attached to form a 4- to 7-membered monocyclic heterocycloalkyl group, or a 6- to 10- membered bicyclic heterocyclic group having fused, spiro, or bridged rings;
L is

R17 is hydrogen, C1-C6alkyl, or —C0-C4alkyl(C3-C7cycloalkyl);
R18 and R18? are independently chosen from hydrogen, halogen, hydroxymethyl, and methyl;
m is 0, 1, 2, or 3;
B is monocyclic or bicyclic carbocyclic; a monocyclic or bicyclic carbocyclic-oxy group; a monocyclic, bicyclic, or tricyclic heterocyclic group having 1, 2, 3, or 4 heteroatoms independently selected from N, O, and S and from 4 to 7 ring atoms per ring; C2-C6alkenyl; C2-C6alkynyl; —(C0-C4alkyl)(aryl); —(C0-C4alkyl)(heteroaryl); or —(C0-C4alkyl)(biphenyl) each of which B is unsubstituted or substituted with one or more substituents independently chosen from R33 and R34, and 0 or 1 substituents chosen from R35 and R36;
R33 is independently chosen from halogen, hydroxyl, —COOH, cyano, C1-C6alkyl, C2-C6alkanoyl, C1-C6alkoxy, —C0-C4alkylNR9R10, —SO2R9, —C1-C2 haloalkyl, and C1-C2 haloalkoxy;
R34 is independently chosen from nitro, C2-C6alkenyl, C2-C6alkynyl, C1-C6thioalkyl, -JC3-C7cycloalkyl, —B(OH)2, -JC(O)NR9R23, -JOSO2OR21, —C(O)(CH2)1-4S(O)R21, —O(CH2)1-4S(O)NR21R22, -JOP(O)(OR21)(OR22), -JP(O)(OR21)(OR22), -JOP(O)(OR21)R22, -JP(O)(OR21)R22, -JOP(O)R21R22, -JP(O)R21R22, -JSP(O)(OR21)(OR22), -JSP(O)(OR21)(R22), -JSP(O)(R21)(R22), -JNR9P(O)(NHR21)(NHR22), -JNR9P(O)(OR21)(NHR22), -JNR9P(O)(OR21)(OR22), -JC(S)R21, -JNR21SO2R22, -JNR9S(O)NR10R22, -JNR9SO2NR10R22, -JSO2NR9COR22, -JSO2NR9CONR21R22, -JNR21SO2R22, -JC(O)NR21SO2R22, -JC(NH2)NR22, -JC(NH2)NR9S(O)2R22, -JOC(O)NR21R22, -JNR21C(O)OR22, -JNR21OC(O)R22, —(CH2)1-4C(O)NR21R22, -JNR9C(O)R21, -JC(O)R21, -JNR9C(O)NR10R22, —CCR21, —(CH2)1-4OC(O)R21, and -JC(O)OR23; each of which R34 is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, amino, oxo, —B(OH)2, —Si(CH3)3, —COOH, —CONH2, —P(O)(OH)2, C1-C6alkyl, —C0-C4alkyl(C3-C7cycloalkyl), C1-C6alkoxy, —C0-C2alkyl(mono- and di-C1-C4alkylamino), C1-C6alkylester, C1-C4alkylamino, C1-C4hydroxylalkyl, C1-C2haloalkyl, and C1-C2haloalkoxy;
R35 is independently chosen from naphthyl, naphthyloxy, indanyl, (4- to 7-membered heterocycloalkyl)C0-C4alkyl containing 1 or 2 heteroatoms chosen from N, O, and S, and bicyclic heterocycle containing 1, 2, or 3 heteroatoms independently chosen from N, O, and S, and containing 4- to 7- ring atoms in each ring; each of which R35 is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkanoyl, C1-C6alkoxy, (mono- and di-C1-C6alkylamino)C0-C4alkyl, C1-C6alkylester, —C0-C4alkyl(C3-C7cycloalkyl), —SO2R9, C1-C2haloalkyl, and C1-C2haloalkoxy; and
R36 is independently chosen from tetrazolyl, (phenyl)C0-C2alkyl, (phenyl)C1-C2alkoxy, phenoxy, and 5- or 6-membered heteroaryl containing 1, 2, or 3 heteroatoms independently chosen from N, O, B, and S, each of which R36 is unsubstituted or substituted with one or more substituents independently chosen from halogen, hydroxyl, nitro, cyano, C1-C6alkyl, C2-C6alkenyl, C2-C6alkanoyl, C1-C6alkoxy, (mono- and di-C1-C6alkylamino)C0-C4alkyl, C1-C6alkylester, —C0-C4alkyl(C3-C7cycloalkyl), —SO2R9, —OSi(CH3)2C(CH3)3, —Si(CH3)2C(CH3)3, C1-C2haloalkyl, and C1-C2haloalkoxy; and
J is independently selected at each occurrence from a covalent bond, C1-C4alkylene, —OC1-C4alkylene, C2-C4alkenylene, and C2-C4alkynylene.

US Pat. No. 10,428,091

CATALYST SYSTEMS CONTAINING LOW VALENT TITANIUM-ALUMINUM COMPLEXES AND POLYMERS PRODUCED THEREFROM

Chevron Phillips Chemical...

1. A method of making a titanium-aluminum complex having the formula:the method comprising:contacting a half-metallocene titanium compound having the formula:
with an alkylaluminum compound having the formula Al(RX)(RY)(RZ) to form a mixture comprising the titanium-aluminum complex having formula (A); wherein:X1 and X2 independently are a halide;
R1, R2, and R3 independently are H or a halide, C1 to C36 hydrocarbyl group, C1 to C36 halogenated hydrocarbyl group, C1 to C36 hydrocarboxy group, or C1 to C36 hydrocarbylsilyl group;
Cp is a substituted or unsubstituted cyclopentadienyl, indenyl, or fluorenyl group; and
RX, RY, and RZ independently are a C1 to C10 alkyl group.

US Pat. No. 10,428,090

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE COMPRISING THE SAME

Samsung Display Co., Ltd....

1. A condensed-cyclic compound represented by Formula 1:
wherein, in Formula 1,
ring A, ring B, and ring C are each independently selected from a C5-C30 carbocyclic group and a C1-C30 heterocyclic group,
each of L1 to L9 is independently selected from a substituted or unsubstituted C3-C10 cycloalkylene group, a substituted or unsubstituted C1-C10 heterocycloalkylene group, a substituted or unsubstituted C3-C10 cycloalkenylene group, a substituted or unsubstituted C1-C10 heterocycloalkenylene group, a substituted or unsubstituted C6-C60 arylene group, a substituted or unsubstituted C1-C60 heteroarylene group, a substituted or unsubstituted divalent non-aromatic condensed polycyclic group, and a substituted or unsubstituted divalent non-aromatic condensed heteropolycyclic group,
each of a1 to a9 is independently an integer from 0 to 5,
each of Ar1 to Ar6, R11, and R12 is independently selected from a substituted or unsubstituted C1-C60 alkyl group, a substituted or unsubstituted C2-C60 alkenyl group, a substituted or unsubstituted C2-C60 alkynyl group, a substituted or unsubstituted C1-C60 alkoxy group, a substituted or unsubstituted C3-C10 cycloalkyl group, a substituted or unsubstituted C1-C10 heterocycloalkyl group, a substituted or unsubstituted C3-C10 cycloalkenyl group, a substituted or unsubstituted C1-C10 heterocycloalkenyl group, a substituted or unsubstituted C6-C60 aryl group, a substituted or unsubstituted C1-C60 heteroaryl group, a substituted or unsubstituted monovalent non-aromatic condensed polycyclic group, and a substituted or unsubstituted monovalent non-aromatic condensed heteropolycyclic group,
each of b1 to b6 is independently an integer from 1 to 5,
each of n1 to n3 is independently selected from 0, 1, 2, and 3, provided that the sum of n1, n2, and n3 is 2 or greater,
each of R1 to R3 is independently selected from hydrogen, deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a nitro group, an amidino group, a hydrazino group, a hydrazono group, a substituted or unsubstituted C1-C60 alkyl group, a substituted or unsubstituted C2-C60 alkenyl group, a substituted or unsubstituted C2-C60 alkynyl group, a substituted or unsubstituted C1-C60 alkoxy group, a substituted or unsubstituted C3-C10 cycloalkyl group, a substituted or unsubstituted C1-C10 heterocycloalkyl group, a substituted or unsubstituted C3-10 cycloalkenyl group, a substituted or unsubstituted C1-C10 heterocycloalkenyl group, a substituted or unsubstituted C6-C60 aryl group, a substituted or unsubstituted C6-C60 aryloxy group, a substituted or unsubstituted C6-C60 arylthio group, a substituted or unsubstituted C1-C60 heteroaryl group, a substituted or unsubstituted monovalent non-aromatic condensed polycyclic group, a substituted or unsubstituted monovalent non-aromatic condensed heteropolycyclic group, Si(Q1)(Q2)(Q3), —N(Q1)(Q2), —B(Q1)(Q2), —C(?O)(Q1), —S(?O)2(Q1), and —P(?O)(Q1)(Q2),
each of c1 to c3 is independently an integer from 0 to 8, and
at least one substituent of the substituted C3-10 cycloalkylene group, substituted C1-C10 heterocycloalkylene group, substituted C3-C10 cycloalkenylene group, substituted C1-C10 heterocycloalkenylene group, substituted C6-C60 arylene group, substituted C1-C60 heteroarylene group, a substituted divalent non-aromatic condensed polycyclic group, a substituted divalent non-aromatic condensed heteropolycyclic group, substituted C1-C60 alkyl group, substituted C2-C60 alkenyl group, substituted C2-C60 alkynyl group, substituted C1-C60 alkoxy group, substituted C3-C10 cycloalkyl group, substituted C1-C10 heterocycloalkyl group, substituted C3-C10 cycloalkenyl group, substituted C1-C10 heterocycloalkenyl group, substituted C6-C60 aryl group, substituted C6-C60 aryloxy group, substituted C6-C60 arylthio group, substituted C1-C60 heteroaryl group, substituted monovalent non-aromatic condensed polycyclic group, and substituted monovalent non-aromatic condensed heteropolycyclic group is selected from:
deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a nitro group, an amidino group, a hydrazino group, a hydrazono group, a C1-C60 alkyl group, a C2-C60 alkenyl group, a C2-C60 alkynyl group, and a C1-C60 alkoxy group;
a C1-C60 alkyl group, a C2-C60 alkenyl group, a C2-C60 alkynyl group, and a C1-C60 alkoxy group, each substituted with at least one selected from deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a nitro group, an amidino group, a hydrazino group, a hydrazono group, a C3-C10 cycloalkyl group, a C1-C10 heterocycloalkyl group, a C3-C10 cycloalkenyl group, a C1-C10 heterocycloalkenyl group, a C6-C60 aryl group, a C6-C60 aryloxy group, a C6-C60 arylthio group, a C1-C60 heteroaryl group, a monovalent non-aromatic condensed polycyclic group, a monovalent non-aromatic condensed heteropolycyclic group, —Si(Q11)(Q12)(Q13), —N(Q11)(Q12), —B(Q11)(Q12), —C(?O)(Q11), —S(?O)2(Q11), and —P(?O)(Q11)(Q12);
a C3-C10 cycloalkyl group, a C1-C10 heterocycloalkyl group, a C3-10 cycloalkenyl group, a C1-C10 heterocycloalkenyl group, a C6-C60 aryl group, a C6-C60 aryloxy group, a C6-C60 arylthio group, a C1-C60 heteroaryl group, a monovalent non-aromatic condensed polycyclic group, a monovalent non-aromatic condensed heteropolycyclic group, a biphenyl group, and a terphenyl group;
a C3-C10 cycloalkyl group, a C1-C10 heterocycloalkyl group, a C3-C10 cycloalkenyl group, a C1-C10 heterocycloalkenyl group, a C6-C60 aryl group, a C6-C60 aryloxy group, a C6-C60 arylthio group, a C1-C60 heteroaryl group, a monovalent non-aromatic condensed polycyclic group, and a monovalent non-aromatic condensed heteropolycyclic group, each substituted with at least one selected from deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a nitro group, an amidino group, a hydrazino group, a hydrazono group, a C1-C60 alkyl group, a C2-C60 alkenyl group, a C2-C60 alkynyl group, a C1-C60 alkoxy group, a C3-10 cycloalkyl group, a C1-C10 heterocycloalkyl group, a C3-C10 cycloalkenyl group, a C1-C10 heterocycloalkenyl group, a C6-C60 aryl group, a C6-C60 aryloxy group, a C6-C60 arylthio group, a C1-C60 heteroaryl group, a monovalent non-aromatic condensed polycyclic group, a monovalent non-aromatic condensed heteropolycyclic group, —Si(Q21)(Q22)(Q23), —N(Q21)(Q22), —B(Q21)(Q22), —C(?O)(Q21), —S(?O)2(Q21), and —P(?O)(Q21)(Q22); and
—Si(Q31)(Q32)(Q33), —N(Q31)(Q32), —B(Q31)(Q32), —C(?O)(Q31), —S(?O)2(Q31), and —P(?O)(Q31)(Q32),
wherein each of Q1 to Q3, Q11 to Q13, Q21 to Q23, and Q31 to Q33 is independently selected from hydrogen, deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a nitro group, an amidino group, a hydrazino group, a hydrazono group, a C1-C60 alkyl group, a C2-C60 alkenyl group, a C2-C60 alkynyl group, a C1-C60 alkoxy group, a C3-C10 cycloalkyl group, a C1-C10 heterocycloalkyl group, a C3-C10 cycloalkenyl group, a C1-C10 heterocycloalkenyl group, a C6-C60 aryl group, a C1-C60 heteroaryl group, a monovalent non-aromatic condensed polycyclic group, a monovalent non-aromatic condensed heteropolycyclic group, a phenyl group, a biphenyl group, and a terphenyl group.

US Pat. No. 10,428,088

MUSCARINIC RECEPTOR AGONISTS

Heptares Therapeutics Lim...

1. A compound of the formula (1a):
or a salt thereof, wherein:
m is 1;
p is 0;
q is 0;
W is C;
Z is CH2;
Y is O;
X1 and X2 are saturated hydrocarbon groups which together contain a total of five to nine carbon atoms and which link together such that the moiety:

is selected from ring systems BA to BH below:

R1 can be H, optionally substituted C1-6 alkyl or CH2-aryl;
R2 is H;
R3 is H, OH, or an optionally substituted C1-6 non-aromatic hydrocarbon group;
R4 can be H, optionally substituted C1-5 alkyl or optionally substituted C2-5 alkynyl.

US Pat. No. 10,428,085

ASYMMETRIC BENZOTRICHALCOGENOPHENE COMPOUND AND POLYMER

NATIONAL CHIAO TUNG UNIVE...

1. An asymmetric benzotrichalcogenophene compound, having a structure of chemical formula (1):
wherein
R1 is hydrogen, —CpH2p+1, —COCqH2q+1 or —COOCrH2r+1, p is an integer of 1-20, q is an integer of 1-12, r is an integer of 1-12,
X is selected from the group consisting of sulfur, selenium, tellurium, and a combination thereof,
Y is selected from the group consisting of oxygen, sulfur, selenium, tellurium, and a combination thereof, and when X is sulfur, Y is not sulfur.

US Pat. No. 10,428,084

COMPOUND FOR ORGANIC ELECTRIC ELEMENT, ORGANIC ELECTRIC ELEMENT COMPRISING THE SAME AND ELECTRONIC DEVICE THEREOF

DUK SAN NEOLUX CO., LTD.,...

1. A compound of Formula 1 below:
wherein
X and Y are each independently O or S,
a and b are each an integer of 0 or 1, and at least one of a and b is 1,
Ar1 to Ar3 are each independently selected from the group consisting of a C6-C60 aryl group, a fluorenyl group, a C2-C60 heterocyclic group containing at least one heteroatom selected from the group consisting of O, N, S, Si, and P, C1-C60 alkyl group, a fused ring group of a C6-C60 aromatic ring and a C3-C60 aliphatic ring, and -L-N(R?)(R?),
R1 to R3 are each independently selected from the group consisting of deuterium, tritium, halogen, a C6-C60 aryl group, a fluorenyl group, a C2-C60 heterocyclic group containing at least one heteroatom selected from the group consisting of O, N, S, Si, and P, a fused ring group of a C6-C60 aromatic ring and a C3-C60 aliphatic ring, a C1-C50 alkyl group, a C2-C20 alkenyl group, a C2-C20 alkynyl group, a C1-C30 alkoxyl group, a C6-C30 aryloxyl group, and -L?-N(R?)(R?), and neighboring groups of R1, neighboring groups of R2 or neighboring groups of R3 may be optionally linked each other to form a ring when a plurality of neighboring R1 to R3 exist, l and n are each an integer of 0-4, and m is an integer of 0 or 1,
L1, L2 and L? are each independently selected from the group consisting of a single bond, a C6-C60 arylene group, a fluorenylene group, a C2-C60 heterocyclic group containing at least one heteroatom selected from O, N, S, Si, and P, a fused ring group of a C6-C60 aromatic ring and a C3-C60 aliphatic ring, and a aliphatic hydrocarbon group,
R? and R? are each independently selected from the group consisting of a C6-C60 aryl group, a fluorenyl group, a C2-C60 heterocyclic group containing at least one heteroatom selected from the group consisting of O, N, S, Si, and P, a fused ring group of a C6-C60 aromatic ring and a C3-C60 aliphatic ring, and
when Ar1 to Ar3, R1 to R3, R? and R? are each the aryl group, fluorenyl group, heterocyclic group, or fused ring group, when Ar1 to Ar3 are each the alkyl group, when R1 to R3 are each the alkyl group, alkenyl group, alkynyl group, alkoxyl group or aryloxy group, or when L1, L2 and L? are each the arylene group, fluorenylene group, heterocyclic group, or fused ring group, each of them may be optionally further substituted with one or more substituents selected from the group consisting of deuterium, halogen, a silane group substituted or unsubstituted with a C1-C20 alkyl group or a C6-C20 aryl group, a siloxane group, a boron group, a germanium group, a cyano group, a nitro group, a C1-C20 alkylthio group, a C1-C20 alkoxyl group, a C1-C20 alkyl group, a C2-C20 alkenyl group, a C2-C20 alkynyl group, a C6-C20 aryl group, a C6-C20 aryl group substituted with deuterium, a fluorenyl group, a C2-C20 heterocyclic group containing at least one heteroatom selected from the group consisting of O, N, S, Si, and P, a C3-C20 cycloalkyl group, a C7-C20 arylalkyl group, and a C8-C20 arylalkenyl group.

US Pat. No. 10,428,083

HETEROCYCLYLMETHYL-THIENOURACILE AS ANTAGONISTS OF THE ADENOSINE-A2B-RECEPTOR

BAYER PHARMA AKTIENGESELL...

1. Compound of the formula (I)
in which
the ring A is an azaheterocycle of the formula

in which * marks the bond to the adjoining CH(R1) group,
R5 is hydrogen, (C1-C4)-alkyl, hydroxyl, (C1-C4)-alkoxy, amino, (C1-C5)-alkanoylamino or (C1-C4)-alkoxycarbonylamino,
R6 is hydrogen, methyl or ethyl,
R7A and R7B are the same or different and are independently hydrogen or (C1-C4)-alkyl,
R8 is hydrogen, (C1-C4)-alkyl, (C2-C4)-alkenyl, (C1-C5)-alkanoyl or (C1-C4)-alkoxycarbonyl,
where (C1-C4)-alkyl may be up to disubstituted by hydroxyl,
R9A and R9B are the same or different and are independently hydrogen or (C1-C4)-alkyl
and
X is O, N(R10) or S, in which
R10 is hydrogen, cyano or (C1-C4)-alkoxycarbonyl,
R1 is hydrogen or methyl,
R2 is hydrogen, methyl or ethyl, where methyl and ethyl may be up to trisubstituted by fluorine,
R3 is (C2-C6)-alkyl, (C2-C6)-alkenyl or (C2-C6)-alkynyl,
where (C2-C6)-alkyl may be substituted by a radical selected from the group of hydroxyl, methoxy, ethoxy, trifluoromethoxy, cyclopropyl, cyclobutyl, oxetanyl and phenyl, and up to trisubstituted by fluorine,
and
(C2-C6)-alkenyl may be up to trisubstituted by fluorine,
where the cyclopropyl and cyclobutyl groups mentioned may in turn be up to disubstituted, identically or differently, by a radical selected from fluorine and methyl,
or
R3 is a group of the formula —CH2—R14 in which
R14 is cyclopropyl, cyclobutyl, oxetanyl or tetrahydrofuranyl, where cyclopropyl, cyclobutyl and oxetanyl may be up to disubstituted, identically or differently, by a radical selected from fluorine and methyl,
and
R4 is (C1-C6)-alkyl or (C2-C6)-alkenyl,
where (C1-C6)-alkyl may be up to pentasubstituted and (C2-C6)-alkenyl up to trisubstituted by fluorine
and
where one CH2 group in (C1-C6)-alkyl may be exchanged for —O—, —S— or —S(O)2—, with the proviso that there are at least two carbon atoms between such a heteroatom and the uracil N1 atom,
or
R4 is a group of the formula —(CH2)m—CN, —(CH2)n—R11 or —(CH2)p—R12, in which
m is the number 1, 2, 3 or 4,
n is the number 2 or 3,
p is the number 1 or 2,
R11 is dimethylamino, diethylamino or azetidino
and
R12 is (C3-C6)-cycloalkyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl or 5-membered azaheteroaryl,
where (C3-C6)-cycloalkyl may be up to disubstituted, identically or differently, by a radical selected from fluorine and methyl
and
azaheteroaryl may be up to disubstituted, identically or differently, by a radical selected from methyl and trifluoromethyl,
or
R4 is a group of the formula —(CH2)2—O—R13 in which
R13 is (C3-C6)-cycloalkyl,
and a salt, a solvate, and a solvate of the salt thereof.

US Pat. No. 10,428,081

EGFR INHIBITOR, PREPARATION METHOD AND USE THEREOF

SHANGHAI HANSOH BIOMEDICA...

1. A compound selected from the group consisting of a compound of formula (IIIA1-7), a compound of formula (IIIA1-8), a compound of formula (IIIA1-9), a compound of formula (IVA1-4), a compound of formula (IVA-5), a compound of formula (IVA1-6), and a compound of formula (IVA1-7), or a stereoisomer or a pharmaceutically acceptable salt thereof:
wherein
R is selected from the group consisting of hydrogen and bis-C1-8 alkylaminomethyl;
R1 is selected from the group consisting of:

wherein the three R6 in
are optionally the same or different substituents;R2 is selected from the group consisting of C1-8 alkyl and C3-8 cycloalkyl, wherein the C1-8 alkyl and C3-8 cycloalkyl are each optionally substituted by one or more groups selected from the group consisting of halogen, hydroxy, C1-8 alkyl, C1-8 alkoxy, haloC1-8 alkoxy, C3-8 cycloalkyl and C3-8 cycloalkoxy;
R3 is selected from the group consisting of hydrogen, deuterium, halogen, cyano, nitro, C1-8 alkyl, C1-8 alkoxy, C3-8 cycloalkyl, trifluoromethyl, trifluoromethoxy, SO2R9, C(O)R10, C(O)OR10 and P(O)R11R12;
each R4 is independently selected from the group consisting of hydrogen, deuterium, halogen, hydroxy, sulfhydryl, cyano, nitro, azido, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, 3- to 8-membered heterocyclyloxy, 3- to 8-membered heterocyclylthio, C5-10 aryl, C5-10 aryloxy, C5-10 arylthio, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, —C0-8—P(O)R11R12, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8, —C0-8—C(O)NR7R8, —N(R7)—C(O)R10 and —N(R7)—C(O)OR10;
wherein the C1-8 alkyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, C5-10 aryl, 5- to 10-membered heteroaryl, 5- to 7-membered carbocycle, 5- to 7-membered heterocycle, C5-7 aryl and 5- to 7-membered heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, hydroxy, sulfhydryl, cyano, nitro, azido, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, 3- to 8-membered heterocyclyloxy, 3- to 8-membered heterocyclylthio, C5-10 aryl, C5-10 aryloxy, C5-10 arylthio, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8, —C0-8—C(O)NR7R8, —N(R7)—C(O)R10 and —N(R7)—C(O)OR10;
R6 is selected from the group consisting of hydrogen, deuterium, C1-8 alkyl, haloC1-8 alkyl and C(O)R10;
R7 is selected from the group consisting of hydrogen, deuterium, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, C5-10 aryl, 5- to 10-membered heteroaryl, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8 and —C0-8—C(O)NR7R8,
wherein the C1-8 alkyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, C5-10 aryl and 5- to 10-membered heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, hydroxy, sulfhydryl, cyano, nitro, azido, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, 3- to 8-membered heterocyclyloxy, 3- to 8-membered heterocyclylthio, C5-10 aryl, C5-10 aryloxy, C5-10 arylthio, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8, —C0-8—C(O)NR7R8, —N(R7)—C(O)R10 and —N(R7)—C(O)OR10;
R8 is selected from the group consisting of hydrogen, deuterium, halogen, hydroxy, sulfhydryl, cyano, nitro, azido, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, 3- to 8-membered heterocyclyloxy, 3- to 8-membered heterocyclylthio, C5-10 aryl, C5-10 aryloxy, C5-10 arylthio, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8, —C0-8—C(O)NR7R8, —N(R7)—C(O)R10 and —N(R7)—C(O)OR10,
wherein the C1-8 alkyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, C5-10 aryl and 5- to 10-membered heteroaryl are each optionally substituted by one or more groups selected from the group consisting of halogen, hydroxy, sulfhydryl, cyano, nitro, azido, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclyl, 3- to 8-membered heterocyclyloxy, 3- to 8-membered heterocyclylthio, C5-10 aryl, C5-10 aryloxy, C5-10 arylthio, 5- to 10-membered heteroaryl, 5- to 10-membered heteroaryloxy, 5- to 10-membered heteroarylthio, —C0-8—S(O)rR9, —C0-8—O—R10, —C0-8—C(O)R10, —C0-8—C(O)OR10, —C0-8—O—C(O)R10, —C0-8—NR7R8, —C0-8—C(O)NR7R8, —N(R7)—C(O)R10 and —N(R7)—C(O)OR10;
R9 is selected from the group consisting of hydrogen, deuterium, C1-8 alkyl, C3-8 cycloalkyl, haloC1-8 alkyl, bis-C1-8 alkylamino, phenyl and p-methylphenyl;
R10, R11 and R12 are each independently selected from the group consisting of hydrogen, deuterium, C1-8 alkyl, C3-8 cycloalkyl, haloC1-8 alkyl and hydroxyC1-8 alkyl,
provided that when the compound is a compound of formula (IIIA1-9), each R10 is independently selected from the group consisting of hydrogen, deuterium, C3-8 cycloalkyl, haloC1-8 alkyl and hydroxy C1-8 alkyl;
m is 0, 1, 2, 3 or 4;
r is 0, 1 or 2;
q is 0, 1, 2, 3 or 4; and
“” means that substituent R can have a Z or E configuration.

US Pat. No. 10,428,080

TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF

Merck Patent GmbH, Darms...

1. A compound of formula I,
or pharmaceutically acceptable derivatives, solvates, salts, hydrates, or stereoisomers thereof, wherein:
R1 is hydrogen, optionally substituted C1-6 aliphatic, optionally substituted 3-8 membered saturated or partially unsaturated carbocyclic ring, —OR, or halogen;
ring Z is pyridine, or pyrimidine;
each R2 is independently —R, halogen, —OR, —SR, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
each R3 is independently —R, halogen, —OR, —SR, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
ring A is phenyl or a 5-6-membered heteroaryl having 1, 2, or 3 nitrogens;
R4 is halogen, —SR, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2 or —NRSO2R;
each R5 is independently —R, halogen, —OR, —SR, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
each R is independently hydrogen, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or a 6-12 membered spiro, fused, or bridged bicyclic carbocyclic or heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted; or
two R groups on the same atom are taken together with the atom to which they are attached to form a C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; each of which is optionally substituted;
n is 1 or 2;
p is 0, 1, or 2; and
q is 0, 1, or 2;
wherein the following compounds are excluded:
4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-fluoro-N-(2-hydroxy-ethyl)-N-methyl-benzamide;
5-{2-[2-fluoro-4-(piperazine-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile;
5-{2-[2-fluoro-4-(5-oxo-[1,4]diazepane-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile;
5-{2-[2-fluoro-4-(4-hydroxy-piperidine-1-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile;
5-{2-[2-fluoro-4-(morpholine-4-carbonyl)-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile;
4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-N-(2-hydroxy-ethyl)-3-methoxy-N-methyl-benzamide;
5-{2-[4-(4-hydroxy-piperidine-1-carbonyl)-2-methoxy-phenyl]-furo[3,2-b]pyridin-7-yl}-2-(tetrahydro-pyran-4-yloxy)-benzonitrile;
4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N,N-dimethyl-benzamide;
4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N—(S)-piperidin-3-yl-benzamide; and
4-{7-[3-cyano-4-(tetrahydro-pyran-4-yloxy)-phenyl]-furo[3,2-b]pyridin-2-yl}-3-methoxy-N—(R)-piperidin-3-yl-benzamide.

US Pat. No. 10,428,079

PROCESS FOR IMPROVED OXYCODONE SYNTHESIS

RHODES TECHNOLOGIES, Cov...

1. A process for preparing oxycodone or a salt or solvate thereof from thebaine, the process comprising or consisting of the steps
(a) oxidizing the thebaine to 14-hydroxycodeinone;
(b) adding an acid H+nXn? to the reaction mixture of step (a) before, during and/or after the oxidation reaction;
(c) optionally precipitating the resulting 14-hydroxycodeinone as 14-hydroxycodeinone salt or a solvate thereof;
(d) optionally isolating the precipitated 14-hydroxycodeinone salt or solvate thereof;
(e) providing a solution or suspension of the 14-hydroxycodeinone salt or solvate thereof;
(f) adding trifluoroacetic acid and/or a glycol to the solution or suspension obtained in step (e);
(g) after step (f), reducing the 14-hydroxycodeinone present in the solution or suspension to the oxycodone by hydrogenation; and
(h) optionally adding a base, thus raising the pH to a pH where the oxycodone precipitates as its free base, and isolating the oxycodone as its free base or a solvate thereof,
wherein
Xn? is an anion selected from the group consisting of Cl?, HSO4?, SO42?, methanesulfonate, tosylate, trifluoroacetate, H2PO4?, HPO42?, PO43?, oxalate, perchlorate, and any mixtures thereof; and
n is 1, 2, or 3.

US Pat. No. 10,428,078

COMPOUNDS

GlaxoSmithKline Intellect...

1. A compound of Formula (I-3) or a pharmaceutically acceptable salt thereof:whereinR1 is selected from the group consisting of H, C1-3alkyl and —C(O)—C1-3alkyl; and
R2 and R3 together with the carbon to which they are attached form a 4, 5 or 6 membered saturated ring, which ring
optionally contains one heteroatom ring member selected from N or O, and
is optionally substituted with one substituent of -L-K, wherein
L is selected from the group consisting of C(O), CH2, and S(O)2, and
K is selected from the group consisting of C1-3alkyl, phenyl, and C3-6cycloalkyl;
or R1 and R2 together with the nitrogen and carbon to which they are attached form a 5-membered saturated heterocyclic ring, which ring
optionally contains one or two additional heteroatom ring member independently selected from the group consisting of N, O, C(O), S, S(O), and S(O)2, and
is optionally substituted with one or more substituents independently selected from the group consisting of OH, halo, NR1aR1b, COOH, and —Y—Rc, wherein
Y is absent or is selected from the group consisting of C(O), S(O)2, —C(O)—C(O)—, and CH2, and
Rc is selected from the group consisting of
C1-5alkyl optionally substituted with one or more substituents independently selected from the group consisting of NR2aR2b, C3-6 cycloalkyl, and —COOH,
C1-3haloalkyl,
C1-3alkoxyl,
NR3aR3b,
—(CH2)p—C(O)—O—C1-3alkyl, wherein p is 1, 2, or 3 and the —(CH2)p— is optionally substituted by one or more methyl,
—(CH2)q—C3-6 cycloalkyl wherein q is 1, 2, or 3, the cycloalkyl is optionally substituted with NR4aR4b, and the —(CH2)q— is optionally substituted by one or more methyl, and
heterocyclyl optionally substituted with one or more substituents independently selected from the group consisting of halo and NR5aR5b,
wherein R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, R5a, and R5b are independently H or C1-3alkyl; and
R3 is H;
each occurrence of R4 is independently H or D;
X is absent or is selected from the group consisting of
—O—,
—NH—, and
—N (C1-3 alkyl)-,
n is 1 or 2; or
X is —O—CH2— bicyclo[1.1.1]pentanyl-CH2—O— and n is 0;
A is

wherein
R5 and R9 are independently H or halo,
Z? is N or CR6,
Z is N or CR8,
wherein R6 and R8 are independently selected from the group consisting of H, CN, halo, C1-3alkyl, C1-3haloalkyl, —S(O)2—C1-3alkyl and —S(O)—C1-3alkyl, and
V is CR7, wherein R7 is -Q-(CH2)m—W, wherein
Q is O, N, or CH2,
m is 0 or 1, and
W is 6 membered heteroaryl, wherein the 6 membered heteroaryl is selected from the group consisting of pyridazinyl, pyrimidinyl, pyrazinyl, and triaziny, and
wherein said heteroaryl is optionally substituted with one or more substituents independently selected from the group consisting of C1-3haloalkyl, CN, halo and C1-5alkyl.

US Pat. No. 10,428,077

IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION

Bristol-Myers Squibb Comp...

1. A compound of Formula I:
or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein:

W is O or S;
R1 is —CH3;
R8 and R9 are H;
R2 is H;
X1 is CH;
X2 and X4 are each CH;
X3 is CR3;
R3 is OCH3;
R4 and R5 are independently selected from H and C1-C6 alkyl, or R4 and R5 can be taken together with the carbon to which they are attached to form a C3-C7 cycloalkyl ring;

R6 is selected from the group consisting of:
a) phenyl substituted by 0 to 3 groups independently selected from the group consisting of chloro, —CF3, cyano, —OCH3, —OCF3, —SO2CH3 and (C?O)N(CH3)2;
b) pyridinyl or pyrimidinyl substituted by 0 to 3 groups independently selected from the group consisting of fluoro, chloro, —CH3 and —OCH3; and
c) piperidinyl, morpholinyl or thiomorpholinyl substituted by 0 to 3 groups independently selected from the group consisting of fluoro, OH, —CH3 and —NH2; and
R7 is selected from the group consisting of H, and —CH3.

US Pat. No. 10,428,076

SOLUBLE GUANYLATE CYCLASE STIMULATORS

1. A method for treating a condition selected from cardiovascular disease, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, heart failure, pulmonary hypertension, angina pectoris, thrombosis, restenosis, myocardial infarction, stroke, cardiac insufficiency, fibrosis, pulmonary hypertonia, erectile dysfunction, asthma, acute respiratory distress syndrome (ARDS), chronic kidney disease, cystic fibrosis, sickle cell anemia, scleroderma, Raynaud's Syndrome, diabetes, diabetic retinopathy, cirrhosis of the liver, chronic obstructive pulmonary disease (COPD), acute lung injury, pulmonary fibrosis, or interstitial lung disease, comprising administering a therapeutically effective amount of a compound of the Formula (I)
wherein:
X is C(H) or N;
each R1 is independently halo, hydroxy, C1-C3 alkyl, C3-C6 cycloalkyl or —O—C1-C3 alkyl;
R2 is:
(a.) C1-C6 alkyl, wherein said C1-C6 alkyl of R2 is unsubstituted or substituted by 1 to 6 moieties independently selected from fluoro or —O—C1-C3 alkyl;
(b.) ring C2, wherein ring C2 is:
(i.) C3-C12 cycloalkyl;
(ii.) phenyl;
(iii.) a 5- or 6-membered monocyclic heteroaryl containing 1 to 2 heteroatoms selected from N, O, or S; or
(iv.) a 5- or 6-membered monocyclic heterocyclyl containing 1 to 2 heteroatoms selected from N, O, or S:
wherein ring C2 is unsubstituted or substituted by 1 to 3 moieties independently selected from halo, cyano, C1-C3 alkyl, —O—C1-C3 alkyl, or oxo;
R4 is C1-C6 alkyl, CF3, or C3-C6 cycloalkyl;
ring C3 is:
(a.) phenyl;
(b.) a 5- or 6-membered monocyclic heteroaryl or a 9- to 10-membered bicyclic heteroaryl containing 1 to 3 heteroatoms selected from N, O, or S;
(c.) a 5- or 6-membered monocyclic heterocyclyl containing 1 to 3 heteroatoms selected from N, O, or S; or
(d.) C3-C6 cycloalkyl;
each Ra is independently selected from halo, cyano, C1-C3 alkyl, —O—C1-C3 alkyl, oxo, or hydroxy;
Y is:
(a.) a bond;
(b.) a group of the formula

wherein RY1 and RY2 are independently H, C1-C3 alkyl, hydroxy, fluoro, C1-C3 hydroxyalkyl, or amino; or alternatively RY1 and RY2, together with the carbon atom to which they are attached form a C3-C6 cycloalkyl;
RY3 and RY4 are independently H, C1-C3 alkyl, hydroxy, fluoro, or C1-C3 hydroxyalkyl; or alternatively RY3 and RY4, together with the carbon atom to which they are attached form a C3-C6 cycloalkyl;
(c.) a group of the formula

(d.) ring AH, wherein ring AH is C3-C6 cycloalkyl or phenyl, wherein ring AH is unsubstituted or substituted by 1 to 3 moieties independently selected from halo or C1-C3alkyl;
(e.) a group —CH?CH—; or
(f.) a group

Z is:
(a.) —CO2H; (b.) —C(O)N(H)OH;

 (f.) —SO3H; (g.) —P(?O)(OH)2; or (h.) —C(O)N(H)S(O)2CH3;
the subscript m is 0, 1, or 2;
the subscript p is 0, 1, 2, or 3;
the subscript q is 0 or 1;
the subscript r1 is 0, 1, 2, 3, or 4; and
the subscript r2 is 0 or 1,or a pharmaceutically acceptable salt thereof, to a patient in need thereof.

US Pat. No. 10,428,075

COELENTERAZINE ANALOGUES

PROMEGA CORPORATION, Mad...

1. A method for in vivo bioluminescent imaging, the method comprising:contacting a live cell with a compound of Formula I or Formula II:

wherein R5 and R5a are hydrogen;
R6 and R6a are aryl optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from the group consisting of halogen, hydroxy, cyano, nitro, amino, alkylamino, dialkylamino, acyl amino, aminoalkyl, alkyl, fluoroalkyl, alkoxyfluoroalkyl, fluoroalkoxy, alkenyl, alkynyl, haloalkyl, haloalkoxy, heteroalkyl, alkoxy, sulfonylamino, sulfonyl, alkylsulfonyl, amide, carbamate, silyl, substituted silyl, acyl, or aminosulfonyl;
R8 and R8a are optionally substituted aryl, heteroaryl, alkyl substituted with aryl, or alkyl substituted with heteroaryl;
Rx is halogen, hydroxy, cyano, nitro, amino, alkylamino, dialkylamino, alkyl, alkenyl, alkynyl, alkoxy, or heteroalkyl; and
p is 0, 1, 2, 3, 4, or 5;
provided that the following compounds are excluded from formula (I): 8-benzyl-2-(furan-2-ylmethyl)-6-phenylimidazo[1,2-a]pyrazin-3(7H)-one; and
8-benzyl-2-(furan-2-ylmethyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one; and
Rx is not 4-hydroxy when p is 1, R5a is not hydrogen, or R8a is not benzyl, or any combination thereof;
and
detecting luminescence; wherein the live cell expresses a coelenterazine-utilizing luciferase.

US Pat. No. 10,428,074

PYRROLE HETEROARYL RING DERIVATIVE AND METHOD OF USE THEREOF

Jiangsu Hengrui Medicine ...

4. A process for preparing (3aR,5S,6aS)-N-(3-methoxyl- 1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide:or a tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or a pharmaceutically acceptable salt thereof according to claim 1, the process comprising reacting a compound of formula (I), or a pharmaceutically acceptable salt thereof, with compound 34c to obtain (3aR,5S,6aS)-N-(3-methoxyl-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)hexahydrocyclopenta[c]pyrrole-2(1H)-carboxamide:or the tautomer, mesomer, racemate, enantiomer, diastereomer, or mixture thereof, or the pharmaceutically acceptable salt thereof,wherein:
R2 is methyl;
A is nitrogen;
L is a bond;
each of R, R1, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 is hydrogen; and
each of p, q, s, and t is 1.

US Pat. No. 10,428,073

SALT TYPE AND CRYSTAL TYPE OF 4H-PYRAZOLO [1, 5-ALPHA] BENZIMIDAZOLE COMPOUND AND PREPARATION METHOD AND INTERMEDIATE THEREOF

Hubei Bio-Pharmaceutical ...

5. Crystal type A of compound 3, characterized by an XRPD pattern as shown in FIG. 1,

US Pat. No. 10,428,072

INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL

Eli Lilly and Company, I...

1. A compound of the Formula (I) or a pharmaceutically acceptable salt thereof:
wherein:
R1 is H, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl;
R2 is H, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl, optionally substituted with one or more R5 groups;
R3 is H, C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl;
R4 is halo, hydroxy, alkoxy, thiol, alkylthio, amino, alkylamino, dialkylamino, cyano, nitro, amido, alkylamido, dialkylamido, thioyl, sulfonyl, cyclyl, heterocyclyl, aryl, or heteroaryl, optionally substituted at one or more positions with 1-4 R6 groups;
R5 is independently H, halogen, alkyl, aralkyl, alkenyl, alkynyl, hydroxy, amino, amido, phosphonate, carboxyl, ether, alkylthio, haloalkyl, and cyano; and
R6 is independently H, halogen, alkyl, aralkyl, alkenyl, alkynyl, cycloalkyl, hydroxy, amino, nitro, sulfhydryl, imino, amido, phosphate, phosphonate, phosphinate, carbonyl, carboxyl, silyl, ether, alkylthio, sulfonyl, ketone, aldehyde, ester, heterocycle, an aromatic or heteroaromatic ring, haloalkyl, and cyano.

US Pat. No. 10,428,071

CARBOLINE DERIVATIVE SERVING AS BROMODOMAIN INHIBITOR

NINGBO WENDA PHARMA TECHN...

1. A carboline derivative selected from the group consisting ofor a salt thereof.

US Pat. No. 10,428,070

HEPATITIS B ANTIVIRAL AGENTS

Enanta Pharmaceuticals, I...

1. A compound represented by Formula (I):or a pharmaceutically acceptable salt thereof, wherein:A is optionally substituted aryl or optionally substituted heteroaryl;
B is selected from the group consisting of hydrogen, halo, CN, optionally substituted —C1-C6 alkyl, and optionally substituted C3-C6 cycloalkyl;
X is optionally substituted aryl or optionally substituted heteroaryl;
Y is —C(O)NR1R2, —C(O)OR1, optionally substituted aryl or optionally substituted heteroaryl;
R1 and R2 are each independently selected from the group consisting of hydrogen, optionally substituted —C1-C6 alkyl, optionally substituted —C2-C8 alkenyl, optionally substituted —C2-C8 alkynyl, optionally substituted —C3-C8 cycloalkyl, optionally substituted 3- to 8-membered heterocyclic, optionally substituted aryl, and optionally substituted heteroaryl; alternatively, R1 and R2 are taken together with the nitrogen atom to which they are attached to form an optionally substituted 3- to 8-membered heterocyclic; and
R and Z are taken together with the carbon atom to which they are attached to form an optionally substituted 3- to 8-membered cycloalkyl, 3- to 8-membered cycloalkenyl, or 3- to 8-membered heterocyclic;
provided that when Y is optionally substituted aryl or optionally substituted heteroaryl, R and Z taken together with carbon atom to which they are attached do not form
where R5 is hydrogen, optionally substituted —C1-C8 alkyl, optionally substituted —C2-C8 alkenyl, optionally substituted —C2-C8 alkynyl, optionally substituted —C3-C8 cycloalkyl, optionally substituted 3- to 8-membered heterocyclic, optionally substituted aryl, optionally substituted heteroaryl, —C(O)R13, —C(O)OR13, —C(O)NR13R14, —S(O)2R13, or —S(O)2NR13R14; and R13 and R14 at each occurrence are independently hydrogen, optionally substituted —C1-C8 alkyl, optionally substituted —C2-C8 alkenyl, optionally substituted —C2-C8 alkynyl, optionally substituted —C3-C8 cycloalkyl, optionally substituted 3- to 8-membered heterocyclic, optionally substituted aryl or optionally substituted heteroaryl.

US Pat. No. 10,428,069

6-FUSED HETEROARYLDIHYDROPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

Hoffmann-La Roche Inc., ...

1. A compound of formula (I)whereinR1 is hydrogen, halogen or C1-6alkyl;
R2 is hydrogen or halogen;
R3 is hydrogen or halogen;
R4 is C1-6alkyl;
R5 is hydrogen or carboxy;
R6 is hydrogen, C1-6alkoxycarbonyl or carboxy-CmH2m—;
X is carbonyl or sulfonyl;
Y is —CH2—, —O— or —N(R7)—, wherein R7 is hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkoxycarbonyl-CmH2m—, —CmH2m—COOH, —(C1-6alkoxy)C1-6alkyl-COOH, —C1-6alkyl-O—C1-6alkyl-COOH, —C3-7cycloalkyl-CmH2m—COOH, —CmH2m—C3-7cycloalkyl-COOH, hydroxy-CmH2m—, carboxyspiro[3.3]heptyl or carboxyphenyl-CmH2m—;
W is —CH2—, —C(C1-6alkyl)2-, —O— or carbonyl;
n is 0 or 1; and
m is 0-7;
or a pharmaceutically acceptable salts or enantiomer thereof.

US Pat. No. 10,428,068

FUSED AMINO PYRIDINE AS HSP90 INHIBITORS

Curis, Inc., Lexington, ...

1. A method of treating an inflammatory disease or immune system disorder in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of a compound represented by formula I:or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein;U is CH;
W is hydrogen, halogen, amino, hydroxy, thiol, alkyl, substituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamino, substituted or unsubstituted dialkylamino, substituted or unsubstituted alkylthio, substituted or unsubstituted alkylsulfonyl, CF3, NO2, CN, N3, sulfonyl, acyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, cycloalkyl, or substituted cycloalkyl;
X is absent, O, S, S(O), S(O)2, N(R8), C(O), CF2, C(R8) or C2-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl in which one or more methylene can be interrupted or terminated by O, S, SO, SO2, N(R8), C(O), where R8is hydrogen, acyl, aliphatic or substituted aliphatic;
Y is independently hydrogen, halogen, NO2, CN, or lower alkyl;
Z is amino, substituted or unsubstituted alkylamino, substituted or unsubstituted dialkylamino, substituted or unsubstituted alkylcarbonylamino;
Q is aryl, substituted aryl, heteroaryl, substituted heteroaryl, cycloalkyl, or heterocycloalkyl;V is hydrogen, straight- or branched-, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, which one or more methylenes can be interrupted or terminated by O, S, S(O), SO2, N(R8), C(O), substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic; substituted or unsubstituted cycloalkyl; where R8is hydrogen, acyl, aliphatic or substituted aliphatic, wherein said inflammatory disease or immune system disorder is selected from rheumatoid arthritis, osteoarthritis, juvenile chronic arthritis, graft versus host disease, psoriasis, asthma, spondyloarthropathy, Crohn's Disease, inflammatory bowel disease, colitis ulcerosa, alcoholic hepatitis, Sjoeqrens's syndrome, multiple sclerosis, ankylosing spondylitis, membranous qlomerulopathy, discogenic pain and systemic lupus erythematosus.

US Pat. No. 10,428,067

COMPOUNDS AND METHODS FOR KINASE MODULATION

Plexxikon Inc., Berkeley...

1. A compound having Formula I:or a pharmaceutically acceptable salt, a solvate, a tautomer, a stereoisomer, or a deuterated analog thereof, wherein:A is N or —C(Z3)?;
W is —C(R2)? or N;
Z3 is hydrogen or halo;
Z2 is:

L is —SO2—NR6R7, —NHC(O)R4, or —C(O)NR3R4;
R1 is C1-6alkyl, halo, or halo-C1-6alkyl;
R2 is hydrogen, —CH3, —CH2F, —CHF2, —CF3, or halo;
R3 is hydrogen or C1-6alkyl;
R4 is C3-6cycloalkyl, C3-6cycloalkyl-C1-3alkylene, cyano-C3-6 cycloalkyl, cyano-C3-6 cycloalkyl-C1-3alkylene, cyano-C1-6alkylene, heterocycloalkyl, heteroaryl, or —(CH2)—[(CR10)]2-OH, wherein the C3-6cycloalkyl, C3-6cycloalkyl-C1-3alkylene, cyano-C3-6 cycloalkyl, cyano-C3-6 cycloalkyl-C1-3alkyl, cyano-C1-6alkylene, heterocycloalkyl, and heteroaryl are optionally substituted with 1-2 G groups;
or R3 and R4, together with the N atom to which they are attached, join to form a 4-6 membered heterocycloalkyl moiety substituted with 1-2 G groups;
R6 is hydrogen, C1-6alkyl, cyano-C1-6alkylene optionally substituted with 1-2 G groups, or C3-6cycloalkyl optionally substituted with 1-2 G2 groups;
R7 is hydrogen or C1-6alkyl;
or R6 and R7, together with the N atom to which they are attached, join to form a heterocycloalkyl moiety substituted with 1-2 G groups;
R8 is C1-3alkyl, hydroxy-C1-6alkyl, halo-C1-6alkyl, cyano-C1-6alkylene, —[C(R9)2]1-2—C3-6cycloalkyl, —[C(R9)2]1-2-heterocycloalkyl, —[C(R9)2]1-2-heteroaryl, —[C(R9)2]1-2—SO2—C1-3alkyl, —[C(R9)2]1-2—C(O)—C1-3alkyl, —[C(R9)2]1-2—C(O)—N(C1-3alkyl)2, —[C(R9)2]1-2—C(O)—NH2, —[C(R9)2]1-2—C(O)—C3-6cycloalkyl, or —[C(R9)2]1-2—C(O)-heterocycloalkyl, or —CH2—C(O)-pyridyl;
each R9 is independently selected from hydrogen, C1-6alkyl, C3-6cycloalkyl, halo, and halo-C1-6alkyl;
each R10 is C1-3alkyl or two R10, together with the C atom to which they are attached, join to form a C3-6 cycloalkyl;
each G is independently hydroxyl, C1-6alkyl, C3-6 cycloalkyl, or heterocycloalkyl;
each G2 is independently C1-6alkyl, halogen, or cyano;
m is 0, 1, or 2; and
n is 0 or 2;
provided that the compound is not
N-(2-cyano-2-methyl-propyl)-6-[2-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
N-(2-cyano-2-methyl-propyl)-6-[2-[1-(difluoromethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
N-(1-cyano-1-methyl-ethyl)-6-[2-[1-(difluoromethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
N-(1-cyano-1-methyl-ethyl)-6-[2-(2-isopropyl-4-methyl-thiazol-5-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
6-[2-[1-(2-cyanoethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-N-(1-cyano-1-methyl-ethyl)pyridine-2-carboxamide,
N-(1-cyano-1-methyl-ethyl)-6-[2-[1-(2-morpholinoethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
N-(1-cyano-1-methyl-ethyl)-6-[2-(1-isopropyl-3-methyl-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
6-[3-chloro-2-[1-(difluoromethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]-N-(1-cyano-1-methyl-ethyl)pyridine-2-carboxamide,
6-[3-chloro-2-(1-isopropyl-3-methyl-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl]-N-(1-cyano-1-methyl-ethyl)pyridine-2-carboxamide,
N-(1-cyano-1-methyl-ethyl)-6-[2-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]-1H-pyrrolo[2,3-b]pyridin-5-yl]pyridine-2-carboxamide,
N-(2-cyanopropan-2-yl)-6-(2-(1-(2-hydroxy-2-methylpropyl)-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)picolinamide,
N-(2-cyanopropan-2-yl)-6-(2-(1-(2,2-difluoroethyl)-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)picolinamide,
N-(2-cyanopropan-2-yl)-6-(2-(1-(oxetan-3-ylmethyl)-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)picolinamide, and
N-(2-cyanopropan-2-yl)-6-(2-(1-((methylsulfonyl)methyl)-1H-pyrazol-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)picolinamide.

US Pat. No. 10,428,065

ISOXAZOLYL SUBSTITUTED IMIDAZOPYRIDINES

CELLCENTRIC LTD, Cambrid...

1. A compound which is an isoxazolyl imidazopyridine of formula (I):wherein:R0 and R, which are the same or different, are each H or C1-6 alkyl;
R9? and R9?, which are the same or different, are each H or F;
R2 and R2?, which are the same or different, are each H or C1-6 alkyl; or R2 and R2? form, together with the C atom to which they are attached, a C3-6 cycloalkyl group;
R3 and R3?, which are the same or different, are each H, C1-6 alkyl, OH or F;
R4 is phenyl or a 5- to 12-membered N-containing heteroaryl group and is unsubstituted or substituted;
alk is C1-6 alkylene;
R? is C1-6 alkyl;
n is 0 or 1; and
X—R1 is selected from the following structures:













or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,064

FUSED-TRICYCLIC INHIBITORS OF KRAS AND METHODS OF USE THEREOF

Araxes Pharma LLC, San D...

1. A compound having the following structure (I?a):or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein:A is a carbocyclic, heterocyclic or heteroaryl ring;
G1 and G2 are each independently N or CH;
L1 is a bond or NR5;
L2 is a bond or alkylene;
R1 is aryl or heteroaryl;
R2a, R2b and R2c are each independently H, amino, halo, hydroxyl, cyano, C1-C6 alkyl, C1-C6 alkylaminyl, C1-C6 haloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy; C3-C8 cycloalkyl, heterocyclylalkyl, C2-C6 alkynyl, C2-C6 alkenyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl, aminylcarbonyl, heteroaryl or aryl;
R3a and R3b are, at each occurrence, independently H, —OH, —NH2, —CO2H, halo, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C3-C8 cycloalkyl, heterocyclylalkyl, C2-C6 alkynyl, hydroxylalkyl, alkoxyalkyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl; or R3a and R3b join to form a carbocyclic or heterocyclic ring; or R3a is H, —OH, —NH2, —CO2H, halo, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C3-C8 cycloalkyl, heterocyclylalkyl, C2-C6 alkynyl, hydroxylalkyl, alkoxyalkyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl, and R3b joins with R4b to form a carbocyclic or heterocyclic ring;
R4a and R4b are, at each occurrence, independently H, —OH, —NH2, —CO2H, halo, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C3-C8 cycloalkyl, heterocyclylalkyl, C2-C6 alkynyl, hydroxylalkyl, alkoxyalkyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl; or R4a and R4b join to form a carbocyclic or heterocyclic ring; or R4a is H, —OH, —NH2, —CO2H, halo, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C3-C8 cycloalkyl, heterocyclylalkyl, C2-C6 alkynyl, hydroxylalkyl, alkoxyalkyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl or aminylcarbonyl, and R4b joins with R3b to form a carbocyclic or heterocyclic ring;
R5 is, at each occurrence, independently H, C1-C6 alkyl, C3-C8 cycloalkyl or heterocycloalkyl;
m1 and m2 are each independently 1, 2 or 3;
represents a double or triple bond;
Q is —C(?O)—, —C(?NR8?)—, NR8C(?O)—, —S(?O)2— or NR8S(?O)2;
R8 is H, C1-C6 alkyl, hydroxylalkyl aminoalkyl, alkoxyalkyl, aminylalkyl, alkylaminylalkyl, cyanoalkyl, carboxyalkyl, aminylcarbonylalkyl, C3-C8 cycloalkyl or heterocycloalkyl;
R8? is H, —OH, —CN or C1-C6 alkyl;
when is a double bond then R9 and R10 are each independently H, halo, cyano, carboxyl, C1-C6 alkyl, alkoxycarbonyl, aminylalkyl, alkylaminylalkyl, aryl, heterocyclyl, heterocyclylalkyl, heteroaryl or hydroxylalkyl, or R9 and R10 join to form a carbocyclic, heterocyclic or heteroaryl ring; and
when is a triple bond then R9 is absent and R10 is H, C1-C6, alkyl, aminylalkyl, alkylaminylalkyl or hydroxylalkyl.

US Pat. No. 10,428,063

4H-PYRROLO[3,2-C]PYRIDIN-4-ONE DERIVATIVES

Bayer Pharma Aktiengesell...

1. A compound of formula (I)
wherein:
R1 is hydrogen, C1-C6-alkyl or C1-C6-haloalkyl;
R2 is hydrogen, C1-C6-alkyl or C1-C6-haloalkyl;
or
R1 and R2 are taken together with the carbon atom to which they are attached to form a 3- to 6-membered cycloalkyl ring;
R3 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, R11—C(O)—, R11O—C(O)— or phenyl-C1-C3-alkyl-,
wherein said phenyl group is optionally independently substituted, one or more times, with R5;
R4 is hydrogen, C1-C4-alkyl or C1-C4-alkoxy-C2-C4-alkyl-;
RA is hydrogen, hydroxy or C1-C4-alkyl;
RB is hydrogen;
or
RB and R2 are taken together to form an additional bond;
A is a group selected from the group consisting of:

wherein * indicates the point of attachment of said group with the rest of the molecule, and said group is optionally independently substituted, one or more times, with R5;
R5 is hydroxy, halogen, cyano, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy;
E is a group selected from the group consisting of:

wherein * indicates the point of attachment of said group with the rest of the molecule;
R6 and R7 are independently hydrogen, halogen, hydroxy, cyano, C1-C4-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, or C3-C6-halocycloalkyl,
wherein said C1-C6-alkoxy is optionally independently substituted one, two or three times, with halogen or is optionally substituted one time with hydroxy, C1-C4-alkoxy, R9R10N—, C3-C6-cycloalkyl, 5- to 6-membered heterocycloalkyl or phenyl, which is optionally independently substituted, one or more times, with R5;
each R8 is independently halogen, hydroxy, nitro, cyano, C1-C4-alkyl, C1-C4-haloalkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, or C3-C6-halocycloalkyl,
wherein said C1-C6-alkoxy is optionally independently substituted one, two or three times, with halogen and is optionally substituted one time with hydroxy, C1-C4-alkoxy, R9R10N—, C3-C6-cycloalkyl, 4- to 7-membered heterocycloalkyl or phenyl, which is optionally independently substituted one or more times, with R5;
each R9 and R10is independently hydrogen, C1-C4-alkyl, C3-C6-cycloalkyl, C1-C4-haloalkyl, C3-C6-halocycloalkyl or phenyl,
wherein said phenyl group is optionally independently substituted, one or more times, with R5;
or
R9 and R10are taken together with the nitrogen atom to which they are attached to form a 3- to 6-membered nitrogen containing heterocyclic ring, optionally containing one additional heteroatom or heteroatom containing group selected from the group consisting of O, NH, and S, and which is optionally independently substituted, one or more times, with R5;
each R11 is independently C1-C4-alkyl, C3-C6-cycloalkyl, C1-C4-haloalkyl or C3-C6-halocycloalkyl;
m is 0, 1, 2, or 3; and
n is 0, 1, or 2,
or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer.

US Pat. No. 10,428,062

GEMINAL SUBSTITUTED AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF ?7-NICOTINIC ACETYLCHOLINE RECEPTORS

Axovant Sciences GmbH, B...

1. A compound represented by Formula (Ia) or Formula (Ib):wherein:R1 and R2 independently represent an unbranched C1-C4-alkyl radical or a branched C3-C4-alkyl radical; or the C(R1)(R2) moiety forms a (3-4 membered)-carbocycle, wherein R1 and R2 taken together represent a C2-C3-alkyl di-radical; wherein the unbranched C1-C4-alkyl radical, the branched C3-C4-alkyl radical, and the C2-C3-alkyl di-radical may be independently substituted with up to 4 radical substituents selected from the group consisting of: -D, —F, —Cl, —CN, —CH3, —CH2CH3, ?O, and —OR3;
R3 independently represents —H; an unbranched C1-C4-alkyl radical; a branched C3-C4-alkyl radical; or a C3-C4-cycloalkyl radical; wherein the unbranched C1-C4-alkyl radical, the branched C3-C4-alkyl radical, and the C3-C4-cycloalkyl radical may be independently substituted with up to 4 radical substituents selected from the group consisting of: -D, —F, —Cl, —CN, ?O, —OH, —OC1-C4-alkyl, and —OCF3,
R4 and R5 independently represent —H, -D, or halogen radical;
R6 independently represents —F, —Cl, —Br, —CN, —CH3, —CH2CH3, cyclopropyl radical, —CHF2, —CH2F, —CF3, —CH2CF3, —OCH3, —OCH2CH3, —OCH(CH3)2, —O-cyclopropyl, or —OCF3; and
R7 independently represents —H, -D, —F, —Cl, —CN, —CH3, —CH(CH3)2, cyclopropyl radical, cyclobutyl radical, —CH2F, —CHF2, —CF3, —CH2CF3, —OCH3, —OH3, —OCH2CH3, —OCH(CH3)2, —O-cyclopropyl, —OCF3, or —OCH2CF3;or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,061

AUTOTAXIN INHIBITORS

Cancer Research Technolog...

1. A method of treating a cancer selected from lung, colon, breast, ovarian, prostate, liver, pancreas, brain, bladder, kidney, bone, nerve and skin cancer in a patient in need of such treatment, said method comprising administering to said patient a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, having the structural formula (I) shown below:
wherein:
R1 and R2 are independently selected from H, (1-8C)alkyl, (4-7C)cycloalkyl, 4-7 membered heterocyclyl, 5-6 membered heteroaryl, —S(O)yRa or C(O)Ra, wherein Ra is selected from H, (1-4C)alkyl or (1-4C)alkoxy, y is 0, 1 or 2, and wherein any (1-8C)alkyl, (4-7C)cycloalkyl, 4-7 membered heterocyclyl or 5-6 membered heteroaryl is optionally substituted by one or more substituents selected from oxo, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, sulphamoyl, NRbRc, ORb, C(O)Rb, C(O)ORb, OC(O)Rb, C(O)N(Rb)Rc, N(Rb)C(O)Rc, S(O)yRb (where y is 0, 1 or 2), SO2N(Rb)Rc, N(Rb)SO2Rc or (CH2)zNRbRc (where z is 1, 2 or 3), (4-6C)heterocycyl, 6 membered aryl or 5 or 6 membered heteroaryl, wherein Rb and Rc are each independently selected from H or (1-4C)alkyl; or
R1 and R2 are linked such that, together with the nitrogen atom to which they are attached, they form a 4 to 10 membered mono or bicyclic heterocyclic ring which is optionally substituted by one or more substituents selected from oxo, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, sulphamoyl, NRdRe, ORd, C(O)Rd, C(O)ORd, OC(O)Rd, C(O)N(Re)Rd, N(Re)C(O)Rd, S(O)yRd (where y is 0, 1 or 2), SO2N(Re)Rd, N(Re)SO2Rd or (CH2)zNRdRe (where z is 1, 2 or 3), (4-6C)heterocycyl, 6 membered aryl or 5 or 6 membered heteroaryl, wherein Rd and Re are each independently selected from H or (1-4C)alkyl;
L is a (1-3C)alkylene optionally substituted by fluoro, (1-2C)alkyl or oxo;
R4a, R4b, R4c and R4d are each independently selected from H, halo, (1-2C)alkyl, cyano, nitro, hydroxyl, amino, (1-2C)haloalkyl, (1-2C)alkoxy, or (1-2C)haloalkoxy;
A is C(?X) or CRfRg;
wherein X is O, NH or S; and
Rf and Rg are independently selected from H or (1-2C)alkyl;
Q is selected from —NH—S(O)y—, —S(O)y—NH—, —C(O)NRh—, —NRhC(O)—, —NRh—S(O)(NH)—, —S(O)(NH)—NRh—, —C(O)O—, —OC(O)—, —CH2CH2—, —CH2NRh— or —NRhCH2—, wherein y is 0, 1 or 2 and Rh is selected from H or (1-2C)alkyl;
HET is a 5 or 6 membered nitrogen containing heteroaryl optionally substituted with one or more substituents selected from H, (1-4C)alkyl, halo, cyano, nitro, hydroxyl, amino, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, carboxyl, carbamoyl, amido or sulphamoyl;
W is either a group of the formula:
-Q1-Ri—
wherein:
Q1 is attached to HET and is —C(O)— or —CH2—; and
Ri is attached to R3 and is selected from —CHRj—, —NRj—, or —O—, wherein Rj is selected from H or (1-2C)alkyl;
or W is a group of the formula:
—Rk-Q2-
wherein:
Q2 is attached to R3 and is selected from —C(O)— or —CH2—; and
Rk is attached to HET and is selected from CHR1, NR1, O or S(O)y, wherein y is 0, 1 or 2 and R1 is H or (1-4C)alkyl;
R3 is selected from (1-6C)alkyl, phenyl, (4-8C)carbocyclyl, heteroaryl or heterocyclyl, each of which is optionally substituted with one or more substituents selected from (1-4C)alkyl, halo, (1-4C)haloalkyl, (1-4C)alkoxy, (1-4C)haloalkoxy, (3-6C)cycloalkyl, (3-6C)cycloalkyl(1-2C)alkyl, (2-4C)alkenyl or (2-4C)alkynyl.

US Pat. No. 10,428,060

PI-KINASE INHIBITORS WITH ANTI-INFECTIVE ACTIVITY

The Board of Trustees of ...

1. A compound of the formula (XXI)
wherein:
R2 is alkoxy or substituted alkoxy;
R3 is hydrogen, lower alkyl or substituted lower alkyl;
Y3 is CH;
Z2 is absent;
R1 is aryl, substituted aryl, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocycle or substituted heterocycle; and
R4 is selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, alkyl-cycloalkyl, substituted alkyl-cycloalkyl, alkyl-aryl, substituted alkyl-aryl, aryl, substituted aryl, heterocycle, substituted heterocycle, alkyl-heterocycle and substituted alkyl-heterocycle, wherein the substituted alkyl, the substituted cycloalkyl, and the substituted alkyl-cycloalkyl are not substituted with an oxo or a thioketo;
or a prodrug thereof, or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,059

COMPOUNDS AND METHODS OF TREATING OR AMELIORATING AN IL-1R-MEDIATED DISEASE OR DISORDER USING SAME

Drexel University, Phila...

1. A method of relieving or improving an IL-1R-mediated disease or disorder in a mammal, wherein the IL-1R-mediated disease or disorder is scleroderma or systemic lupus erythematosus (lupus), the method comprising administering to the mammal a therapeutically effective amount of at least one compound, or a salt, tautomer or solvate thereof, wherein the at least one compound is a compound of formula (XI):
wherein in (XI):
each occurrence of R1 is independently selected from the group consisting of H and methyl;
R2 is O or —NH; and
R3 is optionally substituted phenyl or naphthyl.

US Pat. No. 10,428,058

PRODRUGS OF NH-ACIDIC COMPOUNDS

ALKERMES PHARMA IRELAND L...

1. A compound of Formula XIH:
or a pharmaceutically acceptable salt thereof;wherein:X is —O—;
each G3 and G4 is independently selected from the group consisting of —N— and —C(R10)—[C(R10)(R11)]a—, wherein a is 0;
A is selected from the group consisting of absent, alkyl, alkenyl, alkynyl, —S—, —O—, —S(O)—, —S(O)2—, —S[C(R30)(R31)]u—, —S(O)[C(R30)(R31)]u—, —S(O)2[C(R30)(R31)]u—, —O[C(R30)(R31)]u—, —N(R30)—, —N(R30)[C(R31)(R32)]u—, —[C(R30)(R31)]u, —C(O)[C(R30)(R31)]u—;
B is absent, or a linker, wherein the linker is selected from the group consisting of a bond, a straight chain C1-C10 alkyl, C1-C10 alkenyl, C1-C10 alkynyl, C1-C10 alkoxy, alkoxyC1-C10alkoxy, C1-C10 alkylamino, alkoxyC1-C10alkylamino, C1-C10 alkylcarbonylamino, C1-C10 alkylaminocarbonyl, aryloxyC1-C10alkoxy, aryloxyC1-C10alkylamino, aryloxvC1-C10alkylamino carbonyl, C1-C10-alkylaminoalkylaminocarbonyl, C1-C10 alkyl(N-alkyl)aminoalkyl-aminocarbonyl, alkylaminoalkylamino, alkylcarbonylaminoalkylamino, alkyl(N-alkyl)aminoalkylamino, (N-alkyl)alkylcarbonylaminoalkylamino, alkylaminoalkyl, alkylaminoalkylaminoalkyl, alkylpiperazinoalkyl, piperazinoalkyl, alkylpiperazino, alkenylaryloxyC1-C10alkoxy, alkenylarylaminoC1-C10alkoxy, alkenylaryllalkylaminoC1-C10alkoxy, alkenylaryloxyC1-C10alkylamino, alkenylaryloxyC1-C10alkylaminocarbonyl, piperazinoalkylaryl, heteroarylC1-C10alkyl, heteroarylC2-C10alkenyl, heteroarylC2-C10alkynyl, heteroarylC1-C10alkylamino, heteroarylC1-C10alkoxy, heteroaryloxyC1-C10alkyl, heteroaryloxyC2-C10alkenyl, heteroaryloxyC2-C10alkynyl, heteroaryloxyC1-C10alkylamino or heteroaryloxyC1-C10alkoxy;
D is selected from the group consisting of absent, —O—, —NR33, —C(R34)(R35)—, —S—, —S(O)—, —S(O)2—, —C(O)—;
R1 is selected from the group consisting of —C(RA)(RB)—OC(O)OR20, —C(RA)(RB)—OC(O)R20, and —C(RA)(RB)—OC(O)NR20R21;
each R2, R30, R31, R32 R33, R34, and R35 is independently selected from the group consisting of absent, hydrogen, halogen, —OR10, —SR10, —NR10R11—, —C(O)R10, aliphatic, aryl, or heterocyclyl;
each RA and RB is independently selected from the group consisting of hydrogen, halogen, aliphatic, and aryl;
each R10 and R11 is independently hydrogen, halogen, aliphatic, or aryl; alternatively two R10 and R11 together with the atoms to which they are attached and any intervening atoms may form an additional 3, 4, 5, 6 or 7 membered ring;
each R20 and R21 is independently selected from hydrogen, aliphatic, or aryl;
R5 is selected from absent, hydrogen, halogen, —OR10, —SR10, —NR10R11—, —C(O)R10, aliphatic, and heterocyclyl;
or is selected from:

R100 and R101 each represent 1 to 4 substituents independently selected from hydrogen, halogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, C1-C8 alkoxy, C1-C8 alkylamino and aryl;
R103 is selected from hydrogen, halogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, C1-C8 alkoxy, C1-C8 alkylamino and aryl;
p is 0, 1, 2, or 3; and
u is independently 1, 2, 3, 4, 5, 6 or 7.

US Pat. No. 10,428,057

BICYCLO[1.1.1]PENTANE INHIBITORS OF DUAL LEUCINE ZIPPER (DLK) KINASE FOR THE TREATMENT OF DISEASE

Board of Regents, The Uni...

1. A method of treating a disease selected from the group consisting ofchemotherapy-induced cognitive deficits (CICD),
chemotherapy-induced cognitive impairment (CICI),
chemotherapy-induced peripheral neuropathy (CIPN),
diabetic neuropathy,
Alzheimer's disease,
amyotrophic lateral sclerosis,
frontotemporal dementia,
Huntington's disease,
Kennedy's disease,
Lewy body disease,
Parkinson's disease,
progressive supranuclear palsy,
spinocerebellar ataxia,
traumatic brain injury (TBI), and
traumatic injury to the central nervous system or peripheral nervous system neurons,
the method comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I:

or a pharmaceutically acceptable salt thereof,
wherein:
X1 is selected from C or N;
X2 is selected from C or N;
exactly one of X1 and X2 is N;
X3 is N;
X4 and X5 are C;
X1, X2, X3, X4, and X5 form a five membered heteroaryl;
R1 is selected from alkyl, cycloalkyl, or heterocycloalkyl, any of which is optionally substituted with one to three R5 groups;
R2 is H or is selected from alkyl, amino, aryl, cycloalkyl, haloalkyl, heteroalkyl, heteroaryl, heterocycloalkyl, or sulfonylalkyl, any of which is optionally substituted with one to three R6 groups;
R3 is selected from H, alkyl, (alkoxy)alkyl, (arylalkoxy)alkyl, (heteroarylalkoxy)alkyl, cyano, cycloalkyl, halo, haloalkoxy, or haloalkyl;
R4 is (NR4a)2, wherein each R4a is independently selected from hydrogen, C1-4alkyl, or C1-4haloalkyl;
or R3 and R4 together with the atoms to which they are attached form a 5- or 6-membered heteroaryl or heteroalkyl ring, optionally substituted with one to three R7 groups;
each R5 and R6 is independently selected from C1-4alkyl, C1-4haloalkyl, C1-4alkoxy, C1-4haloalkoxy, C1-4-alkylthio, C1-4haloalkylthio, aryl, heteroaryl, C3-7cycloalkyl, C3-7heterocycloalkyl, (aryl)C1-4alkyl, (heteroaryl)C1-4alkyl, (C3-7cycloalkyl)C1-4alkyl, (C3-7heterocycloalkyl)C1-4alkyl, (ethenyl)C1-4alkyl, (ethynyl)C1-4alkyl, (aryl)C1-4alkoxy, (heteroaryl)C1-4alkoxy, (C3-7cycloalkyl)C1-4alkoxy, (C3-7heterocycloalkyl)C1-4alkoxy, (aryl)C1-4alkylthio, (heteroaryl)C1-4alkylthio, (C3-7cycloalkyl)C1-4alkylthio, (C3-7heterocycloalkyl)C1-4alkylthio, amino, halo, hydroxy, cyano, or oxo; and
each R7 is independently selected from C1-4alkyl, C1-4haloalkyl, C1-4alkoxy, C1-4haloalkoxy, aryl, heteroaryl, C3-7cycloalkyl, C3-7heterocycloalkyl, (aryl)C1-4alkyl, (heteroaryl)C1-4alkyl, (C3-7cycloalkyl)C1-4alkyl, (C3-7heterocycloalkyl)C1-4alkyl, halo, hydroxy, cyano, or oxo.

US Pat. No. 10,428,055

SUBSTITUTED PIPERIDINES HAVING GPR119 AGONISTIC ACTIVITY

DONG-A ST CO., LTD., (KR...

9. A pharmaceutical composition comprising as an effective component the compound of claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically acceptable carrier or excipient.

US Pat. No. 10,428,054

KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

CHDI Foundation, Inc., N...

1. A method of treating a condition or disorder mediated by Kynurenine 3-mono-oxygenase activity in a subject in need of such a treatment, wherein the method comprises administering to the subject a therapeutically effective amount of at least one compound of formula:or a pharmaceutically acceptable salt thereof, whereinR1 is 1,3-benzothiazol-2-yl, 2-methyl-1,3-benzothiazol-6-yl, 8-chloroquinoxalin-6-yl, 8-chloroquinolin-6-yl, 7-chloro-2-methyl-1-benzofuran-5-yl, 7-chloro-1-benzofuran-5-yl, 8-chloroisoquinolin-6-yl, 5-chloroquinazolin-7-yl, 8-chloroquinazolin-6-yl, 8-chlorocinnolin-6-yl, 4-chlorobenzo[d]oxazol-6-yl, 4-chloro-2-methylbenzo[d]oxazol-6-yl, 4-chloro-1H-benzo[d]imidazol-6-yl, 7-chlorobenzo[d]oxazol-5-yl, 7-chloro-2-methylbenzo[d]oxazol-5-yl, 7-chlorobenzo[d]thiazol-5-yl, 7-chloro-2-methylbenzo[d]thiazol-5-yl, 7-chloro-1H-indol-5-yl, 7-chloro-1H-indazol-5-yl, 7-chloro-1-methyl-1H-indazol-5-yl, 7-chlorobenzo[d]isoxazol-5-yl, 7-chloro-1-methyl-1H-indol-5-yl, or 7-chlorobenzofuran-5-yl;
X is —CR2R3—;
R2 and R3 are independently chosen from hydrogen, optionally substituted amino, hydroxyl, lower alkoxy, and optionally substituted lower alkyl;
L is —C(O)O—;
R5 is hydrogen; and
R6 and R7 are independently chosen from hydrogen, halo, optionally substituted amino, hydroxyl, lower alkoxy, and optionally substituted lower alkyl; and
wherein the condition or disorder is Huntington's Disease, Alzheimer's disease, Parkinson's disease, dystonia, multiple sclerosis, stroke, cerebral ischemia, AIDS-dementia complex, or AIDS-induced encephalopathy.

US Pat. No. 10,428,052

PROCESS FOR PREPARING LIFITEGRAST AND INTERMEDIATES THEREOF

ScinoPharm Taiwan, Ltd., ...

1. A process for preparing the compound of Formula I:
or a pharmaceutically acceptable salt thereof; the process comprising:
a) contacting the compound of Formula II

with a first activating reagent in a first activating solvent to provide an activated intermediate of Formula IIa
andcontacting the activated intermediate of Formula IIa with a compound of Formula III or III?

in a first coupling solvent to provide a compound of Formula IV
andb) contacting the compound of Formula IV with a second activating reagent in a second activating solvent to provide an activated intermediate of Formula IVa
andcontacting the activated intermediate of Formula IVa with a compound of Formula V or V?

in a second coupling solvent to provide a compound of Formula I;wherein AG1 and AG2 are each independently Cl or an activated hydroxyl moiety and X? is Cl? Br?, I? or CF3C(O)O?.

US Pat. No. 10,428,051

SUBSTITUTED AMIDE DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN

ESTEVE PHARMACEUTICALS, S...

1. A compound of general Formula (I):
wherein
m is 1 or 2;
n is 0, 1 or 2;
p is 0, 1 or 2;
W is nitrogen or carbon;
X is a bond, —C(RxRx?)—, C?O, —C(O)O— or —O—;
wherein Rx is selected from the group consisting of halogen, —OR15, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
Rx?is selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
R15 is selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
R1 is selected from the group consisting of substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
wherein the cycloalkyl, aryl or heterocyclyl in R1 if substituted, is substituted with one or more substituent/s selected from the group consisting of halogen, —R11, —OR11, —NO2, —NR11R11??, NR11C(O)R11?, —NR11S(O)2R11?, —S(O)2NR11R11?, —NR11C(O)NR11?R11?, —SR11, —S(O)R11, S(O)2R11, —CN, haloalkyl, haloalkoxy, —C(O)OR11, —C(O)NR11R11?, —NR11S(O)2NR11?R11? and C(CH3)2OR11;
and wherein the cycloalkyl or non-aromatic heterocyclyl in R1, if substituted, may also be substituted with

 or ?O;
wherein the alkyl, alkenyl or alkynyl in R1, if substituted, is substituted with one or more substituent/s selected from the group consisting of —OR11, halogen, —CN, haloalkyl, haloalkoxy, —SR11, —S(O)R11, and —S(O)2R11;
wherein R11, R11? and R11? are independently selected from the group consisting of hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl and unsubstituted C2-6 alkynyl;
and wherein R11?? is selected from the group consisting of hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl and -Boc;
R2 is selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
wherein the cycloalkyl, aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituent/s selected from the group consisting of halogen, —R12, —OR12, —NO2, —NR12R12??, NR12C(O)R12?, —NR12S(O)2R12?, —S(O)2NR12R12?, —NR12C(O)NR12?R12?, —SR12, —S(O)R12, S(O)2R12, —CN, haloalkyl, haloalkoxy, —C(O)OR12, —C(O)NR12R12?, —NR12S(O)2NR12?R12? and C(CH3)2OR12;
and wherein the cycloalkyl or non-aromatic heterocyclyl in R2, if substituted, may also be substituted with

 or ?O;
wherein the alkyl, alkenyl or alkynyl in R2, if substituted, is substituted with one or more substituent/s selected from the group consisting of —OR12, halogen, —CN, haloalkyl, haloalkoxy, —SR12, —S(O)R12, and —S(O)2R12;
wherein R12, R12? and R12? are independently selected from the group consisting of hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl and unsubstituted C2-6 alkynyl;
and wherein R12?? is selected from the group consisting of hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl and -Boc;
R3 is selected from the group consisting of substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, —NR9R9? and —CH2OR9;
wherein R9 and R9? are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
R4 and R4? are independently selected from the group consisting of substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl,
or R4 and R4? together with the carbon atom to which they are attached, form a cycle of Formula (A) (with “?” marking the carbon atom to which R4 and R4? are attached):

wherein
q is 0 or 1;
r is 0, 1 or 2;
Y is —CH2—, —N(Ry)—, —S— or —O—;
R8 and R8? are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
or R8 and R8? together with the carbon atom to which they are attached, form a C3-6 cycloalkyl;
Ry is selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
R5 and R5? are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, —CH2OR10 and —C(O)OR10;
wherein R10 is selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
R6 and R6? are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
R7 and R7? are independently selected from the group consisting of hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
and wherein

 is selected from

wherein
the alkyl, alkenyl or alkynyl, other than those defined in R1 or R2, if substituted, is substituted with one or more substituent/s selected from the group consisting of —OR13, halogen, —CN, haloalkyl, haloalkoxy, —SR13, —S(O)R13, and —S(O)2R13;
wherein R13 is selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, and unsubstituted C2-6 alkynyl;
the aryl, heterocyclyl or cycloalkyl other than those defined in R1 or R2, if substituted, is substituted with one or more substituent/s selected from the group consisting of halogen, —R14, —OR14, —NO2, —NR14R14??, NR14C(O)R14?, —NR14S(O)2R14?, —S(O)2NR14R14?, —NR14C(O)NR14?R14?, —SR14, —S(O)R14, S(O)2R14, —CN, haloalkyl, haloalkoxy, —C(O)OR14, —C(O)NR14R14?, —NR14S(O)2NR14?R14? and C(CH3)2OR14;
and wherein the cycloalkyl or non-aromatic heterocyclyl, other than those defined in R1 or R2, if substituted, may also be substituted with

 or ?O;
wherein R14, R14? and R14? are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;
and wherein R14?? is selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl and -Boc;
optionally as a stereoisomer, a racemate or a mixture of at least two stereoisomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof;
with the provisos that:
—[CR5R5?]m—X—(CR6R6?)n—R2 is not unsubstituted methyl;
or
R1 is neither an unsubstituted nor an N-alkyl-substituted compound of the following formula:

US Pat. No. 10,428,050

SUBSTITUTED REVERSE PYRIMIDINE BMI-1 INHIBITORS

PTC THERAPEUTICS, INC., ...

1. A compound of Formula (I):
or a form thereof, wherein
R1 is bicyclic heteroaryl or bicyclic heterocyclyl substituted on a carbon atom ring member with one, two, three or four R5 substituents, or on a nitrogen atom ring member with an oxygen atom substituent to form an N-oxide;
X is N or N substituted with an oxygen atom substituent to form an N-oxide;
R2 is amino;
R3 is hydrogen, cyano, halo, C1-8alkyl, amino, C1-8alkyl-amino or (C1-8alkyl)2-amino;
R4 is phenyl, optionally substituted with one, two, three or four R6 substituents;
R5 is independently selected from the group consisting of cyano, halo, hydroxyl, nitro, oxo, C1-8alkyl, cyano-C1-8alkyl, halo-C1-8alkyl, hydroxyl-C1-8alkyl, C1-8alkoxy, C1-8alkoxy-C1-8alkyl, halo-C1-8alkoxy, C2-8alkenyl, C1-8alkoxy-C2-8alkenyl, C2-8alkynyl, C1-8alkoxy-C2-8alkynyl, carboxyl, amino, C1-8alkyl-amino, (C1-8alkyl)2-amino, amino-C1-8alkyl, C1-8alkyl-amino-C1-8alkyl, (C1-8alkyl)2-amino-C1-8alkyl, hydroxyl-C1-8alkyl-amino, hydroxyl-C1-8alkyl-amino-C1-8alkyl, hydroxyl-C1-8alkyl-amino-C1-8alkyl-amino, C1-8alkyl-thio, C1-8alkyl-carbonyl, C1-8alkyl-carbonyl-amino, C1-8alkyl-carbonyl-oxy, C1-8alkyl-carbonyl-oxy-C1-8alkyl, C1-8alkoxy-carbonyl, C1-8alkoxy-carbonyl-C1-8alkyl, C1-8alkoxy-carbonyl-amino, C1-8alkyl-sulfonyl, C3-14cycloalkyl, aryl, aryl-C1-8alkyl, aryl-amino, aryl-C1-8alkyl-amino, heteroaryl, heteroaryl-C1-8alkyl and heterocyclyl, wherein C3-14cycloalkyl, aryl, heteroaryl or heterocyclyl and the aryl and heteroaryl portions of aryl-C1-8alkyl, aryl-amino, aryl-C1-8alky-amino and heteroaryl-C1-8alkyl are each optionally substituted with one, two, three or four halo, C1-8alkyl, halo-C1-8alkyl, hydroxyl-C1-8alkyl, C1-8alkoxy, halo-C1-8alkoxy, hydroxyl-C1-8alkoxy or carboxyl substituents;
R6 is independently selected from the group consisting of cyano, halo, nitro, C1-8alkyl, halo-C1-8alkyl, hydroxyl-C1-8alkyl, C1-8alkoxy, halo-C1-8alkoxy, C2-8alkenyl, C1-8alkoxy-C2-8alkenyl, C2-8alkynyl, C1-8alkoxy-C2-8alkynyl, carboxyl, formyl, formyl-oxy, C1-8alkyl-carbonyl, halo-C1-8alkyl-carbonyl, C1-8alkyl-thio, halo-C1-8alkyl-thio, amino, C1-8alkyl-amino, (C1-8alkyl)2-amino, C1-8alkyl-carbonyl, C1-8alkyl-carbonyl-oxy, C1-8alkyl-carbonyl-oxy-C1-8alkyl, C1-8alkoxy-carbonyl, halo-C1-8alkoxy-carbonyl, C1-8alkoxy-carbonyl-C1-8alkyl, C1-8alkoxy-carbonyl-amino, C1-8alkoxy-carbonyl-amino-C1-8alkyl, amino-carbonyl, C1-8alkyl-amino-carbonyl, (C1-8alkyl)2-amino-carbonyl, C1-8alkyl-carbonyl-amino, C1-8alkyl-carbonyl-amino-C1-8alkyl, amino-C1-8alkyl, C1-8alkyl-amino-C1-8alkyl, (C1-8alkyl)2-amino-C1-8alkyl, amino-C1-8alkyl-amino, C1-8alkyl-amino-C1-8alkyl-amino, (C1-8alkyl)2-amino-C1-8alkyl-amino, hydroxyl-C1-8alkyl-amino, hydroxyl-C1-8alkyl-amino-C1-8alkyl, hydroxyl-C1-8alkyl-amino-C1-8alkyl-amino, imino-C1-8alkyl, hydroxyl-imino-C1-8alkyl, C1-8alkoxy-imino-C1-8alkyl, C1-8alkyl-sulfonyl, halo-C1-8alkyl-sulfonyl, amino-sulfonyl, C1-8alkyl-amino-sulfonyl, (C1-8alkyl)2-amino-sulfonyl, B(OR8)2, C3-14cycloalkyl, heterocyclyl, aryl and heteroaryl, wherein C3-14cycloalkyl, heterocyclyl, aryl, and heteroaryl are each optionally substituted with one, two, three or four halo or C1-8alkyl substituents;
R8 is independently hydrogen or C1-8alkyl;
wherein the form of the compound is selected from the group consisting of a free acid, free base, salt, ester, hydrate, solvate, chelate, clathrate, isotopologue, stereoisomer, racemate, enantiomer, diastereomer and tautomer thereof.

US Pat. No. 10,428,048

ANDROGEN RECEPTOR ANTAGONISTS

City of Hope, Duarte, CA...

1. A compound, or a pharmaceutically acceptable salt thereof, having the formula:
wherein
R1 is hydrogen or substituted or unsubstituted pyrid-2-yl;
R2 is independently a hydrogen, halogen, —CX23, —CHX22, —CH2X2, —CN, —SOn2R10, —SOv2NR7R8, —NHNR7R8, —ONR7R8, —NHC?(O)NHNR7R8, —NHC?(O)NR7R8, —N(O)m2, —NR7R8, —C(O)R9, —C(O)—OR9, —C(O)NR7R8, —OR10, —NR7SO2R10, —NR7C?(O)R9, —NR7C(O)—OR9, —NR7OR9, —OCX23, —OCHX22, —OCH2X2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R3 is independently a hydrogen, halogen, —CX33, —CHX32, —CH2X3, —CN, —SOn3R14, —SOv3NR11R12, —NHNH2, —ONR11R12, —NHC?(O)NHNH2, —NHC?(O)NR11R12, —N(O)m3, —NR11R12, —C(O)R13, —C(O)—OR13, —C(O)NR11R12, —OR14, —NR11SO2R14, —NR11C?(O)R13, —NR11C(O)—OR13, —NR11OR13, —OCX33, —OCHX32, —OCH2X3, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R7, R8, R9, R10, R11, R12, R13 and R14 are independently hydrogen, halogen, —CX3, —CHX2, —CH2X, —OCX3, —OCHX2, —OCH2X, —CN, —OH, —NH2, —COOH, —CONH2, —NO2, —SH, —SO3H, —SO4H, —SO2NH2, —NHNH2, —ONH2, —NHC?(O)NHNH2, —NHC?(O)NH2, —NHSO2H, —NHC?(O)H, —NHC(O)—OH, —NHOH, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl; and R8 substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl; R11 and R12 substituents bonded to the same nitrogen atom may optionally be joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;
R4 is independently hydrogen, a —CX43, —CHX42, —CH2X4, —CN, —C(O)H, —C(O)OH, —C(O)NH2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R5 is independently a hydrogen, halogen, —CX53, —CHX52, —CH2X5, —CN, —C(O)H, —C(O)OH, —C(O)NH2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
R6 is independently a hydrogen, halogen, —CX63, —CHX62, —CH2X6—CN, —C(O)H, —C(O)OH, —C(O)NH2, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
L1 is independently a bond, substituted or unsubstituted alkylene, substituted or unsubstituted alkenylene, substituted or unsubstituted alkynylene, substituted or unsubstituted heteroalkylene, substituted or unsubstituted heteroalkenylene, or substituted or unsubstituted heteroalkynylene;
m2, m3, v2, and v3 are independently 1 or 2;
n2 and n3 are independently an integer from 0 to 4;
X1, X2, X3, X4, X5, and X6 are independently —Cl, —Br, —I, or —F.

US Pat. No. 10,428,047

MAP KINASE MODULATORS AND USES THEREOF

The Trustees of Columbia ...

1. A method of treating a tauopathy in a subject comprising administration of a therapeutically effective amount of a compound of formula (I), or a composition comprising a compound of formula (I),whereinX1 is N and X2 is CH, or X1 is CH and X2 is N;
R1 is —N(R4)2, cyclopropyl, or R5-piperidin-4-yl;
R2 is independently D or halogen;
R3 is naphthyl, quinolinyl, or isoquinolinyl, wherein said naphthyl, quinolinyl, or isoquinolinyl is optionally independently substituted with at least one D, halogen, (C1-C3)-alkoxy, or (C1-C3)-alkoxy substituted with at least one D;
R4 is independently H, (C1-C4)-alkyl, (C1-C4)-alkyl substituted with at least one D, (C3-C5)-cycloalkyl, or each R4 together with the nitrogen to which they are attached form a 3-7 membered heterocyclic ring, wherein one of the carbon atoms is optionally replaced with NR6, O or S, and wherein the 3-7 membered heterocyclic ring is optionally substituted with a (C1-C3)-alkyl;
R5 is H or (C1-C3)-alkyl, or (C1-C3)-alkyl substituted with at least one D;
R6 is H, (C1-C3)-alkyl, (C1-C3)-alkyl substituted with at least one D, or pyrimidin-2-yl; and
n is an integer from 0-4; or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,428,045

BENZAZEPINE COMPOUNDS, CONJUGATES, AND USES THEREOF

Silverback Therapeutics, ...

1. A conjugate represented by the formula:wherein Antibody is an antibody construct, L3 is a linker moiety, and D is a compound represented by the structure of Formula (IIB):or a pharmaceutically acceptable salt thereof, wherein:L10 is selected from —C(O)—, and —C(O)N(R10)—*, wherein * represents where L10 is bound to R5—;
L2 is selected from —C(O)— and —C(O)N(R10)—;
R1 and R2 are independently selected from hydrogen; and C1-10 alkyl, C2-10 alkenyl, and C2-10 alkynyl, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)2, —S(O)R10, —S(O)2R10, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), and —CN;
R4 is selected from:
OR10, —N(R10)2, —C(O)N(R10)2, —C(O)R10, —C(O)OR10, —S(O)R10, and —S(O)2R10; and
C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C3-12 carbocycle, and 3- to 12-membered heterocycle; and
C3-12 carbocycle, and 3- to 12-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl;
R5 is selected from unsaturated C4-8 carbocycle; bicyclic carbocycle; and fused 5-5, fused 5-6, and fused 6-6 bicyclic heterocycle, wherein R5 is optionally substituted and wherein substituents are independently selected at each occurrence from:
halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), and —CN; and
C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C3-12 carbocycle, and 3- to 12-membered heterocycle; and
C3-12 carbocycle, and 3- to 12-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from halogen, —OR10, —SR10, —C(O)N(R10)2, —N(R10)C(O)R10, —N(R10)C(O)N(R10)2, —N(R10)2, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl;
R10 is independently selected at each occurrence from:
hydrogen, —NH2, and—C(O)OCH2C6H5; and
C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocycle, and 3- to 12-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from halogen, —OH, —CN, —NO2, —NH2, ?O, ?S, —C(O)OCH2C6H5, —NHC(O)OCH2C6H5, C1-10 alkyl, —C1-10 haloalkyl, —O—C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-12 carbocycle, and 3- to 12-membered heterocycle;
R20, R21, R22, and R23 are independently selected from hydrogen, halogen, —OR10, —SR10, —N(R10)2, —S(O)R10, —S(O)2R10, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C1-10 alkyl, C2-10 alkenyl, and C2-10 alkynyl; and
R24 and R25 are independently selected from hydrogen, halogen, —OR10, —SR10, —N(R10)2, —S(O)R10, —S(O)2R10, —C(O)R10, —C(O)OR10, —OC(O)R10, —NO2, ?O, ?S, ?N(R10), —CN, C1-10 alkyl, C2-10 alkenyl, and C2-10 alkynyl; or R24 and R25 taken together form an optionally substituted saturated C3-7 carbocycle.

US Pat. No. 10,428,044

3-AMINO-1,5,6,7-TETRAHYDRO-4H-INDOL-4-ONES

Bayer Pharma Aktiengesell...

1. A compound of formula (I)
wherein:
R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, or phenyl,
wherein said phenyl is optionally independently substituted, one or more times, with R3, and
wherein said C3-C6-cycloalkyl is optionally independently substituted, one or more times, with halogen;
R2 is hydrogen, C1-C4-alkyl or C1-C4-haloalkyl;
or
R1 and R2 are taken together with the carbon atom to which they are attached to form a 3- to 7-membered cycloalkyl ring;
ring A is a group selected from the group consisting of:

wherein * indicates the point of attachment of said group with the rest of the molecule and said group is optionally independently substituted, one or more times, with R3;
G1 is O, S, or NR21;
G2 and G3 are independently CR21 or N;
R3 is hydrogen, halogen, hydroxy, amino, nitro, cyano, C3-C6-cycloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl-, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-alkyl-C(O)—, R18—O—C(O)—, R7R8N—C(O)—, C1-C4-alkyl-C(O)—NH—, R7R8N—, R7R8N—SO2—,
or a group selected from the group consisting of

wherein * indicates the point of attachment of said group with the rest of the molecule, and
wherein said C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy groups are optionally substituted with one or two hydroxy groups;
G4 is O, S, or NR21;
G5 and G6 are independently CR21 or N;
each R6 is independently halogen, hydroxy, amino, nitro, cyano, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy;
ring B is a group selected from the group consisting of:

wherein * indicates the point of attachment of said group with the rest of the molecule;
X is CR4 or N;
Y is CR4 or N,
wherein when one of X and Y is N, the other is CR4;
each R4 is independently hydrogen, halogen, hydroxy, cyano, C1-C4-alkyl, C3-C4-cycloalkyl, C1-C4-alkoxy, C1-C4-alkyl-S—, C1-C4-alkyl-SO—, C1-C4-alkyl-SO2—, R9R10N—, R11—C(O)—(NR7)—, (R11—C(O)—)(R12—C(O)—)N—, R9R10N—C(O)—(NR7)—, R9R10N—C(S)-(NR7)—, R18—O—C(O)—(NR7)—, R9R10N—SO2— or C1-C4-alkyl-SO2—NH—,
wherein said C1-C4-alkyl is optionally independently substituted, one or more times, with a substituent selected from hydroxy and halogen,
wherein said C1-C4-alkoxy is optionally independently substituted, one or more times, with a substituent selected from hydroxy, halogen, C1-C4-alkoxy, C3-C6-cycloalkyl and phenyl,
wherein said phenyl is optionally independently substituted, one or more times, with R3, and
wherein said C3-C4-cycloalkyl is optionally independently substituted, one or more times, with halogen;
each R5 is independently halogen, hydroxy, amino, nitro, cyano, C1-C4-alkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy or phenyl-C1-C4-alkyl,
wherein said phenyl group is optionally independently substituted, one or more times, with a substituent selected from halogen, hydroxy, C1-C3-alkyl, C1-C3-haloalkyl and C1-C3-alkoxy, and
wherein said C3-C6-cycloalkyl group is optionally independently substituted, one or more times, with halogen;
J is hydrogen or hydroxy;
E is hydrogen, C1-C4-alkyl, C1-C4-alkoxy-C2-C4-alkyl, R17aR17bR17cSi—O—C2-C4-alkyl, C1-C4-alkyl-SO2—C1-C4-alkyl, R18—O—C(O)—C1-C4-alkyl, R7R8N—C2-C4-alkyl, R7R8N—C(O)—C1-C4-alkyl or phenyl-C1-C4-alkyl,
wherein said C1-C4-alkyl is optionally independently substituted, one or more times, with a substituent selected from hydroxy and halogen, and
wherein said phenyl group is optionally independently substituted, one or more times, with R5;
Q is O or N—OR16;
R7 and R8 are independently hydrogen, C1-C1-alkyl or tert-butyl-O—C(O)—;
R9 and R10 are independently hydrogen, C1-C1-alkyl, C3-C6-cyclo-alkyl-, C1-C4-haloalkyl-, phenyl or heteroaryl,
wherein said phenyl or heteroaryl group is optionally independently substituted, one or more times, with R5, and
wherein said C1-C4-alkyl is optionally independently substituted, one or more times, with a substituent selected from the group consisting of hydroxy, C1-C4-alkoxy, C1-C4-alkyl-S—, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl, heteroaryl and R18—O—C(O)—,
wherein said C3-C6-cycloalkyl or 4- to 6-membered heterocycloalkyl is optionally independently substituted, one or more times, with a substituent selected from the group consisting of halogen, C1-C4-alkyl and tert-butyl-O—C(O)—, and
wherein said phenyl or heteroaryl group is optionally independently substituted, one or more times, with R5;
or
R9 and R10 are taken together with the nitrogen atom to which they are attached to form a 3- to 7-membered nitrogen containing heterocyclic ring, optionally containing one additional heteroatom selected from the group consisting of O, NH and S, and which is optionally independently substituted, one or more times, with R5;
R11 and R12 are independently C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl, heteroaryl, or R13—(C1-C4-alkyl)-O—CH2—,
wherein said C1-C4-alkyl is optionally independently substituted, one or more times, with a substituent selected from the group consisting of halogen, hydroxy, cyano, C1-C4-alkoxy, R7R8N—, R14, R15, —O—, and phenyl optionally independently substituted, one or more times, with R5,
wherein said C3-C6-cycloalkyl is optionally independently substituted, one or more times, with a substituent selected from the group consisting of halogen, cyano, C1-C4-alkyl, C1-C4-haloalkyl and phenyl optionally independently substituted, one or more times, with R5,
wherein said 4- to 6-membered heterocycloalkyl is optionally independently substituted, one or more times, with a substituent selected from the group consisting of hydroxy, C1-C4-alkyl, C1-C4-alkoxy, R7R8N— and R18—O—C(O)—, and
wherein said phenyl or heteroaryl is optionally independently substituted, one or more times, with R5;
R13 is branched C3-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl or heteroaryl,
wherein said phenyl or heteroaryl is optionally independently substituted, one or more times, with R5;
R14 is C1-C4-alkyl-S—, C1-C4-alkyl-SO2—, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl or heteroaryl,
wherein said phenyl or heteroaryl is optionally independently substituted, one or more times, with R5;
R15 is phenyl or heteroaryl,
wherein said phenyl or heteroaryl is optionally independently substituted, one or more times, with R5;
R16 is hydrogen, C1-C6-alkyl, phenyl or C1-C4-alkyl-C(O)—,
wherein said phenyl group is optionally independently substituted, one or more times, with R5;
R17a, R17b, and R17c are independently C1-C4-alkyl;
R18 is hydrogen or C1-C6-alkyl;
R21 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, or C1-C6-cycloalkyl optionally independently substituted, one or more times, with halogen;
R22 is hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, or C1-C6-cycloalkyl optionally independently substituted, one or more times, with halogen;
m is 0, 1 or 2; and
n is 0, 1, 2 or 3,
or an N-oxide, a salt, a tautomer or a stereoisomer thereof, or a salt of said N-oxide, tautomer or stereoisomer.