US Pat. No. 9,321,761

PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING

CURIS, INC., Lexington, ...

1. A process for preparing a compound of formula I
wherein
A is substituted benzene;
X is NR4C(O) or NR4C(S);

Y is absent;
R1 is aryl or heteroaryl, each of which is optionally substituted;

R2 is halogen, or alkyl substituted with halogen and an R2 is in the o-position on said A benzene relative to pyridyl;

R3 is halogen, hydroxyl, carboxyl, alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, a carbocycle
or a heterocycle wherein each alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, carbocycle
and heterocycle is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, sulfonyl or alkoxy;

R4 is H or alkyl;

m is 0-3;
n is 1-3;or a salt or solvate thereof, comprising,
reacting a compound of formula (d)

with a compound of formula (e)
wherein R14, m and n are as defined above;
Z is O or S, and
Q? is halogen, OH or OR wherein R is an activating group, to yield said compound of formula I, and, optionally, forming a
salt or solvate thereof.

US Pat. No. 9,278,961

PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING

GENENTECH, INC., South S...

1. A method of treating cancer in a mammal, comprising administering a compound of formula I:

wherein
A is a carbocycle or heterocycle;
X is alkylene, NR4C(O), NR4C(S), N(C(O)R1)C(O), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, NR4PO or NR4PO(OH);

Y is absent, CHR4, O, S, SO, SO2 or NR4;

R1 is selected from the group consisting of alkyl, a carbocycle or a heterocycle each of which is optionally substituted with
hydroxyl, halogen, amino, carboxyl, amidino, guanidino, carbonyl, nitro, cyano, acyl, alkyl, haloalkyl, sulfonyl, sulfinyl,
alkoxy, alkylthio, carbamoyl, acylamino, sulfamoyl, sulfonamide, a carbocycle or a heterocycle; wherein said amino, amidino,
alkyl, acyl, sulfonyl, sulfinyl, alkoxy, alkylthio, carbamoyl, acylamino, sulfamoyl, sulfonamide, carbocycle and heterocycle
substituent is optionally substituted with, halogen, haloakyl, hydroxyl, carboxyl, carbonyl, or an amino, alkyl, alkoxy, acyl,
sulfonyl, sulfinyl, phosphinate, carbocycle or heterocycle that is optionally substituted with hydroxyl, carboxyl, carbonyl,
amino, halogen, haloalkyl, alkyl, alkoxy, alkylthio, sulfonyl, sulfinyl, acyl, a carbocycle or a heterocycle;

R2 is halogen, hydroxyl, alkyl, acyl or alkoxy, wherein each alkyl, acyl and alkoxy is optionally substituted with hydroxyl,
halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy;

R3 is halogen, hydroxyl, carboxyl, alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, a carbocycle
or a heterocycle wherein each alkyl, acyl, alkoxy, alkoxycarbonyl, carbamoyl, alkylsulfide, sulfinyl, sulfonyl, carbocycle
and heterocycle is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, sulfonyl or alkoxy;

R4 is H or alkyl;

m is 0-3;
n is 0-3;
or a salt or solvate thereof.

US Pat. No. 9,133,165

SULFONIC ACID SALTS OF HETEROCYCLYLAMIDE-SUBSTITUTED IMIDAZOLES

1. A salt of a compound of formula (I)

in which
R1 stands for methyl, ethyl, butyl, or cyclopropylmethyl,

R2 stands for phenyl, which phenyl is substituted with a substituent that is selected from the group consisting of trifluoromethoxy
and difluoromethoxy, and

R3 stands for hydrogen, methyl, chlorine, methoxy, or trifluoromethyl,

with methanesulfonic acid
or a hydrate thereof.
US Pat. No. 9,096,686

E518A/K MUTANT SMOOTHENED AND METHODS OF USING THE SAME

Genentech, Inc., South S...

1. A recombinant mutant SMO protein comprising the amino acid sequence of SEQ ID NO: 2, wherein said amino acid sequence comprises
alanine (A) or lysine (K) at amino acid 518.
US Pat. No. 9,321,823

MUTANT SMOOTHENED AND METHODS OF USING THE SAME

Genentech, Inc., South S...

1. A method of
(a) detecting a mutant SMO protein in a sample comprising contacting protein from said sample with a monoclonal antibody that
binds to a mutant SMO protein consisting of SEQ ID NO: 2 and having an amino acid other than aspartic acid at the amino acid
position corresponding to amino acid 473 of SEQ ID NO: 2 with a higher affinity than to a wildtype SMO protein consisting
of SEQ ID NO: 2 and having an aspartic acid at the amino acid position corresponding to amino acid 473 of SEQ ID NO: 2; or

(b) identifying at least one SMO mutation in a sample comprising contacting nucleic acid from said sample with a nucleic acid
probe that differentially binds a mutant SMO nucleic acid sequence as compared to a wildtype SMO nucleic acid sequence, wherein
the wildtype SMO nucleic acid sequence encodes a SMO protein consisting of SEQ ID NO: 2 and having an aspartic acid at the
amino acid position corresponding to amino acid 473 of SEQ ID NO: 2, and wherein the mutant SMO nucleic acid sequence encodes
a mutant SMO protein consisting of SEQ ID NO: 2 and having an amino acid other than aspartic acid at the amino acid position
corresponding to amino acid 473 of SEQ ID NO: 2.

US Pat. No. 9,340,535

N-[5-(AMINOSULFONY1)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MESYLATE MONOHYDRATE

1. A crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide methanesulfonic
acid monohydrate having a purity above 96 weight-%.

US Pat. No. 9,288,671

DEVICE AUTHENTICATION METHOD AND DEVICES

ACCURIS TECHNOLOGIES LIMI...

1. A wireless network access method performed by a subscriber device subscribed to a home mobile network, a WLAN, and an authentication
system, the method comprising the steps and sequence of:
in a once-off registration phase:
sending, by the device, registration data in a mobile originating short message via a mobile network to the authentication
system,

performing a query to said home mobile network of a subscriber by the authentication system to validate the subscriber and
resolve subscriber and device identifiers, and

receiving network access information from the authentication system at the device, said network access information allowing
the device to generate network access credentials for a subsequent network access; and

in a network access phase:
generating network access credentials by the device, using said network access information previously received from the authentication
system during the once-off registration phase; wherein

the authentication system generates and signs a unique subscriber certificate during the once-off registration phase, and
the device downloads the unique subscriber certificate as part of said network access information;

the device uses said unique subscriber certificate to generate and encrypt the network access credentials during the network
access phase; and

including the step of the device sending a token to the authentication system, the authentication system using the token to
sign the unique subscriber certificate, and the device using the token to subsequently retrieve the signed unique subscriber
certificate; and wherein the token is a nonce with a globally unique identifier (GUID) unique reference number.

US Pat. No. 9,119,786

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHAR

1. A unit dosage of a composition comprising crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide
mono methanesulfonic acid monohydrate particles of the following formula

having a purity of >99%,
wherein said particles in the composition have a particle size range from 1 to 500 ?m, a particle size distribution which
is defined by d(0.1) from 2 to 100 ?m, d(0.5) from 30 to 210 ?m and d(0.9) from 70 to 400 ?m and a specific surface area of
less than 1.0 m2/g,

and wherein said unit dosage contains 5 to 29% by weight of said crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide
mono methanesulfonic acid monohydrate particles measured as the free base equivalent dosage.

US Pat. No. 9,814,853

AIRWAY STABILIZATION SYSTEM

Securisyn Medical, LLC, ...

1. An airway stabilization system for maintaining an airway device in a patient's trachea, the patient having a head, a face,
a mouth, lips, an oral cavity, vocal cords, a neck, a chest and a chin, the system comprising:
an s-shaped tubular airway device adapted to conform anatomically to the patient's trachea, the airway device including an
elongate body portion having internal and external diameters extending along a central axis, a proximal end, a distal end
and a continuous sidewall extending between the proximal and distal ends;

a respiratory connector adapted to connect the s-shaped tubular airway device to an external source of ventilatory air;
a central connector adapted to connect the respiratory connector to the s-shaped tubular airway device;
a retention member positioned on the s-shaped tubular airway device and extending circumferentially about and coaxially along
the elongate body portion of the s-shaped tubular airway device the retention member having a length and including a plurality
of substantially uniformly spaced-apart ribs positioned axially along the length of the retention member and extending radially
outwardly therefrom, the retention member further including a plurality of structural recesses positioned axially along the
length of the retention member, each of the plurality of structural recesses being positioned intermediate an adjacent two
of the plurality of substantially uniformly spaced-apart ribs;

a securing device being a single continuous piece of material adapted to be secured to the patient, the securing device including
a stabilizer having an upper or top surface, a lower or bottom surface, and a generally cylindrically-shaped bite block extending
in a substantially perpendicular direction from the bottom surface coaxially with the central axis, the generally cylindrically-shaped
bite block a body portion having a length, an outer surface and an inner surface defining a cylindrically shaped cavity about
the central axis, a plurality of substantially uniformly spaced-apart annular flanges positioned axially along the inner surface
of the body portion of the generally cylindrically-shaped bite block and extending substantially inwardly therefrom, a plurality
of structural recesses positioned axially along the inner surface of the body portion of the generally cylindrically-shaped
bite block intermediate an adjacent two of the plurality of substantially uniformly spaced-apart annular flanges, respectively,
each one of the plurality of substantially uniformly spaced-apart annular flanges cooperating with an adjacent one of the
plurality of the plurality of substantially uniformly spaced-apart annular flanges to define one of the plurality of structural
recesses of the generally cylindrically-shaped bite block, respectively, each of the plurality the plurality of substantially
uniformly spaced-apart annular flanges defining an aperture, each aperture being of the same configuration, alignment and
orientation, each aperture being adapted to receive the s-shaped tubular airway device;

a strap adapted to be releaseably secured about the patient's head and to releaseably secure the securing device to the patient.

US Pat. No. 9,454,659

SOFTWARE VULNERABILITIES DETECTION SYSTEM AND METHODS

SECURISEA, INC., Atlanta...

1. A software vulnerabilities detection system comprising:
a memory device storing computer-readable instructions;
a microprocessor, coupled to the memory device for executing instructions stored thereon, comprising a set of concurrent worker
threads;

the microprocessor is configured to:
a) receive compiled code and source code that resulted in said compiled code, wherein each of said concurrent worker threads
processes an instruction from said compiled code where an external input is supplied;

b) create an instruction model for each instruction of said compiled code comprising location, debug information, instruction
type, operands, existing memory state requirements, bytecode metadata, potential security attributes, basic block membership,
function/method membership, and class membership of each said instructions;

c) create a control flow graph for each said instructions comprising all potential control flow paths, and a bidirectional
list of predecessor instructions for each said instruction;

d) create a data flow model comprising recorded flow of unsafe data as observed during execution of said compiled code;
e) analyze said instruction model, said control graph and said data flow model to create a security finding for each said
instruction that calls an unsafe function on said unsafe data; and

f) generate a security report comprising each said security finding with corresponding said debug information and said source
code information, and an execution trace of said unsafe data corresponding to each said security finding, wherein said execution
trace comprising information from the origin to the termination of said unsafe data, and the associated line numbers from
said source code information.

US Pat. No. 9,296,720

CARBOXAMIDE-SUBSTITUTED HETEROARYL-PYRAZOLES AND THE USE THEREOF

1. A compound of Formula (I):

in which
R1 stands for phenyl or pyridyl,

whereby phenyl is substituted with 1 to 3, substituents, whereby the substituents are selected independently of one another
from: halogen, hydroxy, amino, cyano, nitro, (C1-C4)-alkyl, (C3-C6)-cycloalkyl, (C1-C4)-alkylamino and (C1-C4)-alkoxy,

in which
the alkyl, cycloalkyl, alkylamino and alkoxy groups are optionally substituted in one to three places, in the same way or
differently, with radicals selected from: halogen, cyano, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C3-C7)-cycloalkyl, and 4- to 7-membered heterocyclyl,

and
whereby pyridyl is optionally substituted with 1 or 2 substituents, whereby the substituents, independently of one another,
are selected from halogen, hydroxy, amino, cyano, nitro, (C1-C4)-alkyl, (C3-C6)-cycloalkyl, and (C1-C4)-alkoxy, and whereby the nitrogen atom of the pyridyl can optionally form an N-oxide,

in which
the alkyl, cycloalkyl and alkoxy groups are optionally substituted in one to three places, in the same way or differently,
with radicals selected from the series halogen, cyano, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C3-C7)-cycloalkyl, and 4- to 7-membered heterocyclyl,

R2 stands for phenyl or pyridyl,

whereby phenyl is substituted with 1 to 3 substituents, whereby the substituents, independently of one another, are selected
from: halogen, hydroxy, amino, cyano, nitro, (C1-C4)-alkyl, (C3-C6)-cycloalkyl, (C1-C4)-alkylamino, and (C1-C4)-alkoxy,

in which
the alkyl, cycloalkyl, alkylamino and alkoxy groups are optionally substituted in one to three places, in the same way or
differently, with radicals selected from the series halogen, cyano, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C3-C7)-cycloalkyl, and 4- to 7-membered heterocyclyl,

and
whereby pyridyl is optionally substituted with 1 or 2 substituents, whereby the substituents, independently of one another,
are selected from: halogen, hydroxy, amino, cyano, nitro, (C1-C4)-alkyl, (C3-C6)-cycloalkyl, and (C1-C4)-alkoxy, and whereby the nitrogen atom of pyridyl can form an N-oxide

in which
the alkyl, cycloalkyl, and alkoxy groups are optionally substituted in one to three places, in the same way or differently,
with radicals selected from: halogen, cyano, hydroxy, (C1-C4)-alkoxy, amino, mono-(C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C3-C7)-cycloalkyl, and 4- to 7-membered heterocyclyl, and

A stands for imidazolidine-1-yl, morpholin-4-yl, thiomorpholin-4-yl, 1,3-thiazolidin-3-yl, piperidin-1-yl, piperazin-1-yl
or 1,4-oxazepan-4-yl, each bonded via nitrogen,

each of which is substituted with 1 to 3 substituents, whereby the substituents, independently of one another, are selected
from: halogen, hydroxy, hydroxymethyl, formyl, amino, oxo, trifluoromethyl, trifluoromethoxy, (C1-C4)-alkyl, (C1-C4)-alkoxy, and (C1-C4)-alkoxycarbonyl, provided that there is at least one oxo substituent,

whereby R2 stands for pyridyl, when R1 stands for phenyl,

whereby R2 stands for phenyl, when R1 stands for pyridyl, and

whereby when R1 stands for 3-pyridyl, the latter cannot be substituted with unsubstituted alkoxy,
or a salt, solvate or solvate of a salt thereof.

US Pat. No. 9,249,156

PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A salt of a compound represented by the formula:
wherein said salt is a benzenesulfonate salt or a methanesulfonate salt.

US Pat. No. 9,150,571

CRYSTALLINE FORMS OF FUSED AMINO PYRIDINES AS HSP90 INHIBITORS

Curis, Inc., Lexington, ...

1. A polymorphic form of Compound 1 characterized by an X-ray powder diffraction with a characteristic peak at 7.1° 2Theta:

US Pat. No. 9,173,869

MEDIATORS OF HEDGEHOG SIGNALING PATHWAYS, COMPOSITIONS AND USES RELATED THERETO

CURIS, INC., Cambridge, ...

1. A compound of the formula (II):

wherein, as valence and stability permit,
R1 and R2, independently for each occurrence, are H, lower alkyl, substituted or unsubstituted —(CH2)naryl or substituted or unsubstituted —(CH2)nheteroaryl, wherein the optional substitutions are by halogen, cyano, unsubstituted alkyl, unsubstituted alkenyl, unsubstituted
alkynyl, aryl, hydroxyl, unbranched alkyl-O—, silyloxy, amino, nitro, thiol, imino, amido, carboxyl, silyl, thioether, alkylsulfonyl,
arylsulfonyl, sulfoxido, selenoether or ester, provided that, when R1 is substituted or unsubstituted —(CH2)naryl, n is 0;

L adjacent to X is —(CH2)n?—where n? is an integer of 1-10, -alkenyl-, -alkynyl-, —(CH2)nalkenyl-, —(CH2)nalkynyl-, —(CH2)nO(CH2)p—, —(CH2)nNR2(CH2)p—, —(CH2)nS(CH2)p—, —(CH2)nalkenyl(CH2)p—, —(CH2)nalkynyl(CH2)p—, —O(CH2)n—, —NR2(CH2)n—, or —S(CH2)n—;

L, adjacent to R1 is absent,

L adjacent to R2 is —(CH2)n—, -alkenyl-, -alkynyl-, —(CH2)nalkenyl-, —(CH2)nalkynyl-, —(CH2)nO(CH2)p—, —(CH2)nNR2(CH2)p—, —(CH2)nS(CH2)p—, —(CH2)nalkenyl(CH2)p—, —(CH2)nalkynyl(CH2)p—,—O(CH2)n—, —NR2(CH2)n—, or —S(CH2)n—;

X—Y—Z together is —N(R12)—C(?O)—N(R8)—or —N(R 12)—C(?O)—, where R12 is lower alkyl;

R8 is H, lower alkyl, substituted or unsubstituted —(CH2)naryl, or substituted or unsubstituted —(CH2)nheteroaryl;

W is a substituted or unsubstituted benzene ring fused to the pyrimidone ring;
p is, independently for each occurrence, an integer from 0 to 10; and
n, independently for each occurrence, is an integer from 0 to 10;
or a pharmaceutically acceptable salt thereof.

US Pat. No. 9,402,832

FUSED AMINO PYRIDINE AS HSP90 INHIBITORS

Curis, Inc., Lexington, ...

1. A method of producing a compound represented by the formula
comprising the step of reacting a compound represented by the formula
with a compound represented by the formula
in the presence of sodium t-butoxide, neocuproine and cuprous iodide, wherein R is vinyl, ethyl, —CN, —N(CH3)2, —NO2, or —CH2—N(CH3)2.

US Pat. No. 9,108,929

QUINAZOLINE BASED EGFR INHIBITORS

Curis, Inc., Lexington, ...

1. A method of inhibiting epidermal growth factor tyrosine kinase activity in a subject in need thereof, comprising administering
to the subject a therapeutically effective amount of a compound represented by formula (I):

or a pharmaceutically acceptable salt or ester thereof, wherein
X is O, S, CH2, or CONH;

B is an unsubstituted C3 to C9 alkylene;

R1 is selected from hydrogen, hydroxy, and C1 to C4 alkoxy;

each R2 is independently selected from halogen, hydroxy, C1 to C4 alkyl, C2 to C4 alkenyl, and C2 to C4 alkynyl; and

n is 1, 2 or 3.

US Pat. No. 9,592,225

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARM

AICURIS ANTI-INFECTIVE CU...

1. A composition of crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide
mono methanesulfonic acid monohydrate particles of the following formula

having a purity of >99%,
wherein said particles in the composition have a particle size range from 1 to 500 ?m, a particle size distribution which
is defined by d(0.1) from 2 to 100 ?m, d(0.5) from 30 to 210 ?m and d(0.9) from 70 to 400 ?m and a specific surface area of
less than 1.0 m2/g.

US Pat. No. 9,512,085

SALTS OF A DIHYDROQUINAZOLINE DERIVATIVE

1. A salt of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl) phenyl]-3,4-dihydroquinazoline-4-yl}acetic
acid or a solvate thereof that is the crystalline besylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-
dihydroquinazoline 4-yl}acetic acid, the crystalline tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic
acid or solvates thereof.
US Pat. No. 9,458,433

PRODUCTION OF DENSE BODIES (DB) FROM HCMV-INFECTED CELLS

1. A method for preparing dense bodies, comprising
(1) preparing isolated biological cells that are infected with human cytomegalovirus (HCMV) in a medium, and
(2) incubating the infected biological cells with one of the following substances (A), (B), (C) or (D) at a concentration
of the substance (A), (B), (C) or (D) of approximately 1 nmol/l to approximately 1 ?mol/l:

substance (A), which is (4S)-{8-fluoro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)-phenyl]-3,4-dihydro-4-quinazolinyl}acetic
acid;

substance (B), which is N-{1-methyl-2-[(4-(5-methyl-pyridin-2-yl)-piperazin-1-yl)carbonyl]-1H-imidazol-4-yl}-N?-[4-(trifluoromethoxy)phenyl]urea;
substance (C), which is 1-[6-fluoro-8-methoxy-3-({[2-methyl-4-(trifluoromethoxy)benzyl]amino}carbonyl)-4-oxo-1-(2,2,2-trifluoroethyl)-1,4-dihydroquinolin-7-yl]piperidine-4-carboxylic
acid; or

substance (D), which is N-{3-[({4-[5-(6-aminopyridin-2yl)-1,2,4-oxadiazol-3-yl]phenyl}sulfonyl)amino]-5-fluorophenyl}-1-cyanocyclopropane
carboxamide, and then

(3) isolating the resultant dense bodies from the cell supernatant without lysing the cells.

US Pat. No. 9,715,593

SOFTWARE VULNERABILITIES DETECTION SYSTEM AND METHODS

SECURISEA, INC., Atlanta...

1. A software vulnerabilities detection system comprising:
(a) a non-transitory storage medium storing computer-readable program instructions;
(b) a microprocessor, coupled to said non-transitory storage medium for executing said program instructions;
(c) said microprocessor configured to:
(d) receive compiled code;
(e) create an instruction model for each instruction of said compiled code, said instruction model comprising instruction
location, debug information, instruction type, operands, existing memory state requirements, basic block membership, function/method
membership of said each instruction;

(f) create a control flow graph for each said instruction, said control flow graph comprising all potential control flow paths
and a bidirectional list of predecessor instructions for each said instruction;

(g) create a data flow model comprising recorded flow of unsafe data as observed during the execution of said compiled code;
(h) analyze said instruction model, said control flow graph and said data flow model to create a security finding for each
said instruction that calls an unsafe function on said unsafe data; and

(i) generate a security report comprising each said security finding, wherein said security report further comprises an execution
trace of said unsafe data corresponding to each said security finding, said execution trace comprising information from the
origin to the termination of said unsafe data.

US Pat. No. 9,249,148

TRIS(HETERO)ARYLPYRAZOLES AND USE THEREOF

1. A compound of the formula

wherein
A stands for a group of the formula

wherein
U stands for NH, CH2 or C?O,

V stands for N or CH,
W stands for CH or CMe, wherein CMe stands for C—CH3,

X stands for N or CH, and
* is the point of attachment to the carbon atom,
R1 stands for phenyl or pyridyl,

whereby phenyl is substituted with 1 to 2 substituents, the substituents being selected independently of one another from
the group consisting of halogen, cyano, methyl, trifluoromethyl, methoxy and trifluoromethoxy,

whereby pyridyl can be substituted with 1 or 2 substituents, the substituents being selected independently of one another
from the group consisting of halogen, methyl and trifluoromethyl, and whereby the nitrogen atom of the pyridyl can form an
N oxide,

and
R2 stands for phenyl or pyridyl,

whereby phenyl is substituted with 1 to 2 substituents, the substituents being selected independently of one another from
the group consisting of halogen, cyano, (C1-C4)-alkyl and (C1-C4)-alkoxy,

wherein alkyl and alkoxy in turn may be substituted with 1 to 3 fluorine atoms,
whereby pyridyl can be substituted with 1 or 2 substituents, the substituents being selected independently of one another
from the group consisting of halogen, cyano, (C1-C4)-alkyl, and (C1-C4)-alkoxy, and whereby the nitrogen atom of the pyridyl can form an N oxide,

wherein alkyl and alkoxy in turn may be substituted with 1 to 3 fluorine atoms,
or a salt thereof.
US Pat. No. 9,714,272

RECOMBINANT PROTEINS OF PARAPDXVIRUS OVIS AND PHARMACEUTICAL COMPOSITIONS THEREFROM

1. A method for down-regulating cross-presentation of an antigen with a MHC Class I molecule on a cell in a subject, comprising
administering to the subject a recombinant protein encoded by a polynucleotide selected from the group consisting of:
a polynucleotide comprising the sequence of nucleotide residues 122616 to 136025 of SEQ ID NO:1 (PPVO insert of VVOV 82),
or a complementary sequence thereof; and

a polynucleotide comprising the sequence of nucleotide residues 10264 to 20003 of SEQ ID NO:1 (PPVO insert of VVOV 215), or
a complementary sequence thereof,

thereby down-regulating MHC Class I cross-presentation of an antigen on a cell in the subject,
wherein the subject has hepatitis, papillomatosis, herpes virus infection, liver fibrosis, HIV infection, AIDS, or influenza.

US Pat. No. 9,169,244

TYROSINE KINASE INHIBITORS CONTAINING A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A method of treating a cancer which is susceptible to inhibition of one or more of Src, Bcr-Abl and HDAC, 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 or solvate thereof, wherein
Cz is pyrimidine or substituted pyrimidine;
Ar is phenyl or substituted phenyl;
X3 is NH;

Z2 is S;

Y2 is N;

R21 is hydrogen;

B is a direct bond or straight- or branched-, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted
or unsubstituted alkynyl, arylalkyl, arylalkenyl, arylalkynyl, heteroarylalkyl, heteroarylalkenyl, heteroarylalkynyl, heterocyclylalkyl,
heterocyclylalkenyl, heterocyclylalkynyl, aryl, heteroaryl, heterocyclyl, cycloalkyl, cycloalkenyl, alkylarylalkyl, alkylarylalkenyl,
alkylarylalkynyl, alkenylarylalkyl, alkenylarylalkenyl, alkenylarylalkynyl, alkynylarylalkyl, alkynylarylalkenyl, alkynylarylalkynyl,
alkylheteroarylalkyl, alkylheteroarylalkenyl, alkylheteroarylalkynyl, alkenylheteroarylalkyl, alkenylheteroarylalkenyl, alkenylheteroarylalkynyl,
alkynylheteroarylalkyl, alkynylheteroarylalkenyl, alkynylheteroarylalkynyl, alkylheterocyclylalkyl, alkylheterocyclylalkenyl,
alkylheterocycloalkynyl, alkenylheterocyclylalkyl, alkenylheterocyclylalkenyl, alkenylheterocyclylalkynyl, alkynylheterocyclylalkyl,
alkynylheterocyclylalkenyl, alkynylheterocyclylalkynyl, alkylaryl, alkenylaryl, alkynylaryl, alkylheteroaryl, alkenylheteroaryl,
or alkynylhereroaryl, in 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;

R8 is hydrogen, acyl, aliphatic or substituted aliphatic;

C is
where W is O; Y is absent; Z is N; R7 is absent; and R9 is OR?, wherein R? is hydrogen.

US Pat. No. 10,111,864

PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A method of producing Compound 1,
comprising the step of reacting Compound 108,

wherein R is methyl or ethyl, with hydroxylamine, thereby producing Compound 1.

US Pat. No. 9,824,214

HIGH PERFORMANCE SOFTWARE VULNERABILITIES DETECTION SYSTEM AND METHODS

SECURISEA, INC., Atlanta...

1. A software vulnerabilities detection system comprising:
a memory device storing computer-readable instructions;
a microprocessor, coupled to the memory device for executing instructions thereon, wherein the microprocessor is configured
to:

a) receive compiled code and source code that resulted in said compiled code;
b) create an instruction model for each instruction of said compiled code comprising instruction location, debug information,
instruction type and operands of each said instruction;

c) create a control flow graph for each said instruction comprising all potential control flow paths for each said instruction;
d) create a data flow model comprising recorded flow of unsafe data as observed during the execution of said compiled code,
said data flow model utilizing a precomputation of data flow inputs and outputs associated with a basic block of said compiled
code and said source code, wherein said precomputation results in an identification of at least one data location referenced
by an instruction of said basic block, said at least one data location selected from the group consisting of a register, a
local variable, a pointer reference and a stack entry;

e) analyze said instruction model, said control flow graph and said data flow model to obtain a security finding for each
said instruction that calls an unsafe function on said unsafe data; and

f) generate a security report comprising each said security finding, said security report comprising said debug information
and said source code information.

US Pat. No. 9,782,390

AMIDINE SUBSTITUTED ?-LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS

1. A method for prophylactically treating a bacterial infection in a human or animal comprising administering an antibacterially
effective amount of a compound of formula (I):
in which

R1 and R2 independently of one another represent hydrogen, aminocarbonyl or (C1-C4)-alkyl, or

R1 and R2 together with the carbon atom to which they are bonded form a (C3-C8)-cycloalkyl,

R3 represents —(CH2)m—(SO2)OH or —O—(CH2)o—(SO2)OH,

wherein m and o independently of one another represent an integer 0, 1, 2 or 3, and
wherein any CH2-group contained in the residues which R3 represents may be substituted with one or two (C1-C4)-alkyl-residues,

X represents CR4 or N,

R4 represents hydrogen or halogen,

Z represents a bond or an alkyl-chain having one, two, three or four carbon atoms,
whereby the alkyl-chain may be substituted with one, two, three or four substituents, selected independently of one another
from the group consisting of carboxy, aminocarbonyl and (C1-C4)-alkyl,

whereby alkyl in turn may be substituted with a substituent selected from the group consisting of hydroxy, carboxy and aminocarbonyl,
Y represents a bond, O, NH or S,
A represents (C6-C10)-aryl or 5- to 10-membered heteroaryl,

whereby aryl and heteroaryl are substituted with a substituent of the following formula
wherein

R1b, R2b and R3b independently of one another represent hydrogen, amino, hydroxy, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C3-C6)-cycloalkyl, 4-, 5-6- or 7-membered heterocyclyl or 5- or 6-membered heteroaryl,

whereby amino and hydroxy may be substituted with one or two substituents selected independently of one another from the group
consisting of carbonyl, (C1-C4)-alkylcarbonyl, mono- or di-(C1-C4)-alkylaminocarbonyl, and (C1-C4)-alkyl,

whereby alkoxy, heterocyclyl and heteroaryl may be substituted with one, two or three substituents selected independently
of one another from the group consisting of halogen, hydroxy, amino, carbonyl, carboxy, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxy, mono- or di-(C1-C4)-alkylamino, mono- or di-(C1-C4)-alkylaminocarbonyl, —NH—CH(?NH), —NH—C(?NH)(NH2), —C(?NH)CH3 and (C1-C4)-alkyl, and

whereby alkyl and cycloalkyl may be substituted with one, two or three substituents selected independently of one another
from the group consisting of halogen, hydroxy, amino, carbonyl, carboxy, carbonyloxy, aminocarbonyl, carbonylamino, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxy, mono- or di-(C1-C4)-alkylamino, mono- or di-(C1-C4)-alkylaminocarbonyl, —NH—CH(?NH), —NH—C(?NH)(NH2), —CH(?NH)CH3, (C6-C10)-aryl, 5- or 6-membered heteroaryl and 5- or 6-membered heterocyclyl,

whereby heteroaryl and heterocyclyl in turn may be substituted with (C1-C4)-alkyl, and

whereby amino in turn may be substituted with 5- or 6-membered heteroaryl, or
R2b and R3b together with the nitrogen atom to which they are bonded form a 5- to 7-membered heterocycle including one, two or three further
heteroatoms selected from the series N, O and S and R1b is as defined above,

R4b represents hydrogen, amino, hydroxy, (C1-C4)-alkyl or (C1-C4)-alkoxy,

whereby amino and hydroxy may be substituted with one or two substituents selected independently of one another from the group
consisting of (C1-C4)-alkylcarbonyl, mono- or di-(C1-C4)-alkylaminocarbonyl and (C1-C4)-alkyl,

whereby alkoxy may be substituted with one, two or three substituents selected independently of one another from the group
consisting of halogen, hydroxy, amino, carbonyl, carboxy, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxy, mono- or di-(C1-C4)-alkylamino, mono- or di-(C1-C4)-alkylaminocarbonyl, —NH—CH(?NH), —NH—C(?NH)(NH2), —CH(?NH)CH3 and (C1-C4)-alkyl, and

whereby alkyl may be substituted with one, two or three substituents selected independently of one another from the group
consisting of halogen, hydroxy, amino, carbonyl, carboxy, aminocarbonyl, (C1-C4)-alkylcarbonyl, (C1-C4)-alkoxy, mono- or di-(C1-C4)-alkylamino, mono- or di-(C1-C4)-alkylaminocarbonyl, —NH—CH(?NH), —NH—C(?NH)—(NH2), —CH(?NH)CH3, (C1-C4)-alkyl, (C6-C10)-aryl and 5- or 6-membered heteroaryl,

R5b represents hydrogen or (C1-C4)-alkyl,

Q represents a bond, CH2 or NH,

k represents an integer 1 or 2, and
* is the linkage site to the residue represented by A, and
whereby aryl and heteroaryl further may be substituted with one or two substituents selected independently of one another
from the group consisting of halogen, cyano, amino, hydroxy, (C1-C4)-alkyl, (C1-C4)-alkoxy, mono- or di-(C1-C4)-alkylamino, amino-(C1-C4)-alkyl, hydroxy-(C1-C4)-alkyl or carboxy,

whereby alkyl, alkoxy, alkylamino, aminoalkyl, hydroxyalkyl and carboxy in turn may be substituted with a substituent selected
from the group consisting of halogen, (C1-C4)-alkyl and carbonyl, and

l represents an integer 0, 1, 2 or 3,
or a salt thereof, or a hydrate thereof or a hydrate of a salt thereof.

US Pat. No. 9,657,032

PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A method of treating a disease selected from hematological cancers and hematological precancerous conditions in a subject
in need thereof, the method comprising orally administering to the subject a therapeutically effective amount of a compound
of the formula
or a pharmaceutically acceptable salt thereof.
US Pat. No. 9,616,105

AGENT FOR THE TREATMENT AND/OR PROPHYLAXIS OF AN AUTOIMMUNE DISEASE AND FOR THE FORMATION OF REGULATORY T CELLS

1. A method for the treatment and/or prevention of the worsening of an autoimmune disease in an organism, the method comprising:
(a) administering a mutein of human interleukin-2 (hIL-2 mutein) to the organism, wherein said hIL-2 mutein has an amino acid
substitution in at least one of the positions 20, 88 or 126, numbered in accordance with the hIL-2 wild type sequence as set
forth in SEQ ID NO: 1; and

(b) if necessary, repeating step (a),
wherein the autoimmune disease is type I diabetes, multiple sclerosis, or systemic lupus erythematosus, and wherein the administration
induces regulatory T cells in the organism.

US Pat. No. 10,086,046

AGENT FOR THE TREATMENT AND OR PROPHYLAXIS OF AN AUTOIMMUNE DISEASE AND FOR THE FORMATION OF REGULATORY T CELLS

1. A method for the treatment of an autoimmune disease in an organism, the method comprising:(a) contacting peripheral mononuclear blood cells (PBMCs) derived from a first organism with a mutein of human interleukin-2 (hIL-2 mutein), wherein said hIL-2 mutein has an amino acid substitution in at least one of the positions 20, 88, or 126, numbered in accordance with the hIL-2 wild type sequence as set forth in SEQ ID NO: 1, to obtain a cell population which comprises regulatory T cells, and
(b) introducing the cell population into a second organism for the treatment of the autoimmune disease in the second organism, wherein the autoimmune disease is selected from the group consisting of type I diabetes, multiple sclerosis, and systemic lupus erythematosus (SLE).
US Pat. No. 9,910,050

MUTANT SMOOTHENED AND METHODS OF USING THE SAME

Genentech, Inc., South S...

1. A method of screening for compounds that inhibit signaling of a mutant SMO protein that comprises an amino acid substitution
at amino acid 473 of SEQ ID NO:2, wherein amino acid 473 of SEQ ID NO:2 is an amino acid other than aspartic acid, comprising
a. contacting said mutant SMO protein with a test compound and detecting binding of said compound to said mutant SMO protein,
whereby binding of said test compound to said mutant SMO protein indicates that said test compound is potentially an inhibitor
of mutant SMO protein, and

b. contacting a cell that expresses said mutant SMO protein with a test compound determined in step a. to potentially be an
inhibitor of said mutant SMO protein, and detecting activity of Gli in the cell, whereby the reduction or inhibition of Gli
activity indicates that said test compound is an inhibitor of mutant SMO protein.

US Pat. No. 9,890,128

PROCESS FOR MAKING SUBSTITUTED QUINAZOLINE COMPOUNDS

AICURIS ANTI-INFECTIVE CU...

1. A process for making a compound of Formula (I):

wherein said process comprises contacting a compound of formula (viii):

or a salt thereof,
with a phase-transfer catalyst and a base, in a mixture of water and organic solvent A, for a time sufficient to form a compound
of formula (I), wherein:

R1 represents 0 to 3 phenyl group substituents, each independently selected from C1-C6 alkyl, C1-C6haloalkyl, halo, —CN, —OH and C1-C6 alkoxy;

R2 represents 0 to 3 phenyl group substituents, each independently selected from C1-C6 alkyl, C1-C6haloalkyl, halo, —CN, —OH and C1-C6 alkoxy;

R3 represents 0 to 3 phenyl group substituents, each independently selected from C1-C6 alkyl, C1-C6haloalkyl, halo, —CN, —OH and C1-C6 alkoxy; and

R4 is C1-C6 alkyl or C3-C7 cycloalkyl,

wherein:
organic solvent A is selected from toluene, DCM, MTBE, 2-methyltetrahydrofuran, xylenes, ethyl acetate, isopropyl acetate,
acetonitrile and mixtures thereof;

the base is selected from an alkali metal carbonate, an alkali metal hydrogen carbonate, an alkali metal bicarbonate, an alkali
metal phosphate, an alkali metal hydrogen phosphate, an alkali metal hydroxide, a trialkylamine and an aromatic amine;

organic solvent A is selected from toluene, DCM, MTBE, 2-methyltetrahydrofuran, xylenes and mixtures thereof; and
the phase-transfer catalyst is a compound of formula (PT1) or (PT2):

wherein:
Ra is selected from ethyl and vinyl,

Rb is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, aryl, 5 or 6-membered monocyclic heteroaryl, 9 or 10-membered bicyclic heteroaryl, —C1-4alkyl-aryl, —C1-4alkyl-(5 or 6-membered monocyclic heteroaryl) and C1-4alkyl-(9 or 10-membered bicyclic heteroaryl), wherein C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, aryl, heteroaryl and the aryl and heteroaryl portions of —C1-4alkyl-aryl, —C1-4alkyl-(5 or 6-membered monocyclic heteroaryl), and C1-4alkyl-(9 or 10-membered bicyclic heteroaryl), are optionally substituted with one to five substituents independently selected
from Rf,

Rc is selected from hydrogen, methoxy, halo, —CN, —NO2 and —CF3;

Rd is selected from the group consisting of hydrogen, C(O)R, C(O)OR, CONRR?, and C1-6alkyl,

Re is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, aryl, 5 or 6-membered monocyclic heteroaryl, 9 or 10-membered bicyclic heteroaryl, —C1-4alkyl-aryl, —C1-4alkyl-(5 or 6-membered monocyclic heteroaryl) and C1-4alkyl-(9 or 10-membered bicyclic heteroaryl), wherein C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl, aryl, heteroaryl and the aryl and heteroaryl portions of —C1-4alkyl-aryl, —C1-4alkyl-(5 or 6-membered monocyclic heteroaryl), and C1-4alkyl-(9 or 10-membered bicyclic heteroaryl), are optionally substituted with one to five substituents independently selected
from Rf,

each occurrence of Rf is independently selected from the group consisting of C1-4 alkyl, C1-4 haloalkyl, aryl, C1-4 alkoxy, hydroxy, CN, CO2R, CONRR?, SR, SO2R, SO3R, PR2, PO(OR)2, PO(OR) (NRR?), PO(NRR?)2, P(OR)2, P(OR)(NRR?), P(NRR?)2, SiRR?R?, B(OR)2, C(O)R, NRR?, NO2, and halogen,

each R, R? and R? is independently selected from the group consisting of, H, C1-6alkyl, hydroxyl, C1-6alkoxy, aryl, 5 or 6-membered monocyclic heteroaryl, 9 or 10-membered bicyclic heteroaryl, —CH2-aryl, —CH2-heteroaryl, and

each X and Y are independently anions selected from halide, OH, HSO4, SO4, BF4, SbF6, carboxylate, carbonate, hydrogen carbonate, NO3, sulfonate, hexafluorophosphate, phosphate, hydrogen phosphate and perchlorate.

US Pat. No. 9,637,459

SODIUM AND CALCIUM SALTS OF DIHYDROQUINAZOLINE DERIVATIVE AND USE THEREOF AS ANTIVIRAL AGENTS

1. A salt of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5 (trifluoromethyl) phenyl]-3,4-dihydroquinazoline-4-yl}acetic
acid or a solvate thereof selected from the group consisting of crystalline sodium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic
acid, crystalline calcium salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic
acid and solvates thereof.

US Pat. No. 9,889,124

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARM

AICURIS ANTI-INFECTIVE CU...

1. A method of treatment or suppression of the incidence of a herpes simplex virus subtype 1 or 2 infection, or suppression
of transmission of a herpes simplex virus subtype 1 or 2 infection, comprising administering to a subject in need thereof
an effective amount of a composition of crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide
mono methanesulfonic acid monohydrate particles of the following formula
having a purity of >99%,wherein said particles in the composition have a particle size range from 1 to 500 ?m, a particle size distribution which
is defined by d(0.1) from 2 to 100 ?m, d(0.5) from 30 to 210 ?m and d(0.9) from 70 to 400 ?m and a specific surface area of
less than 1.0 m2/g.

US Pat. No. 9,725,461

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A compound represented by formula (XIV),
or a pharmaceutically acceptable salt or prodrug thereof, wherein
n is 0, 1, 2, 3 or 4;
p is 0, 1 or 2;
G1 is CR1, S, O, NR10 or NS(O)2R10,

G2 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocyclic;

R8 is independently hydrogen, acyl, aliphatic or substituted aliphatic;

each R1 and R2 is independently selected from absent, hydrogen, hydroxy, amino, halogen, alkoxy, alkylamino, dialkylamino, CF3, CN, NO2, sulfonyl, acyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic,
and substituted heterocyclic;

R10 is selected from hydrogen, hydroxy, amino, alkoxy, alkylamino, dialkylamino, sulfonyl, acyl, aliphatic, substituted aliphatic,
aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, and substituted heterocyclic;

B is selected from the group consisting of

d and e are independently 0, 1, 2, 3, 4, 5, 6, 7 or 8;
R100 is hydrogen, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or C3-C8 cycloalkyl; and

C is
where R33 is selected from hydrogen and C1-C8-alkyl.

US Pat. No. 9,630,965

FUSED AMINO PYRIDINE AS HSP90 INHIBITORS

Curis, Inc., Lexington, ...

1. A compound represented by the formula

wherein
X is chloro and Y is hydrogen; or
X is chloro or amino and Y is neopentyl.

US Pat. No. 9,708,299

HEDGEHOG ANTAGONISTS HAVING ZINC BINDING MOIETIES

Genentech, Inc., South S...

1. A compound represented by Formula XI:

or a pharmaceutically acceptable salt or prodrug thereof;
wherein
one of W1-W5 is C(X—B-D) and the others are each independently N or CR3, provided that no more than three of W1-W5 are N;

each R3 is independently selected from hydrogen, hydroxy, amino, halogen, alkoxy, alkylamino, dialkylamino, CF3, CN, NO2, sulfonyl, acyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic,
and substituted heterocyclic;

E is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl or substituted or unsubstituted saturated
or partially unsaturated heterocyclyl;

X is absent, —O—, —N(R2)—, —S—, —S(O)—, —S(O)2—, —C(O)—, —C(O)O—, —OC(O)—, —C(O)N(R2)—, —N(R2)C(O)—, —S(O)2N(R2)—, or —N(R2)S(O)2—;

R2 is hydrogen or aliphatic;

B is C2-C10-alkyl, aryl, heteroaryl, C2-C10-alkenyl, aryl-C2-C10-alkyl, aryl-C2-C10-alkenyl, aryloxy-C1-C10-alkyl, heterocyclylheteroaryl, C1-C10-alkylheterocyclylheteroaryl, or C1-C10-alkylaminoheteroaryl;

provided that when B is C1-C10-alkyl, X is not absent; and

D is
where W is O; Y2 and R32 are absent Z is N; R34 is hydroxy; and
R33 is hydrogen.

US Pat. No. 10,035,797

FUSED AMINO PYRIDINE AS HSP90 INHIBITORS

Curis, Inc., Lexington, ...

1. A method of treating a neurodegenerative disease 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 thereof, wherein;
U is N;
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 R8 is 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 is optionally 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 R8 is hydrogen, acyl, aliphatic or substituted aliphatic;
wherein said neurodegenerative disease is selected from the group consisting of Alzheimer's disease; Senile dementia of the Alzheimer type; Pick's disease;
Huntington's disease, Multiple system atrophy combining dementia with ataxia and/or manifestations of Parkinson's disease, Progressive supranuclear palsy, diffuse Lewy body disease, corticodentatonigral degeneration, Hallervorden-Spatz disease, progressive familial myoclonic epilepsy; Parkinson's disease, striatonigral degeneration, progressive supranuclear palsy, torsion dystonia, spasmodic torticollis, familial tremor, Gilles de la Tourette syndrome; cerebellar cortical degeneration, olivopontocerebellar atrophy, spinocerebellar degeneration; Shy-Drager syndrome;
amyotrophic lateral sclerosis, spinal muscular atrophy, primary lateral sclerosis, hereditary spastic paraplegia; neural muscular atrophy; chronic familial polyneuropathies, peroneal muscular atrophy; hypertrophic interstitial polyneuropathy;
retinitis pigmentosa; and hereditary optic atrophy.

US Pat. No. 9,556,165

AMIDINE SUBSTITUTED ?-LACTAM COMPOUNDS, THEIR PREPARATION AND USE AS ANTIBACTERIAL AGENTS

12. A composition comprising at least one compound according to claim 1 in combination with at least one further active compound.

US Pat. No. 10,214,514

HEDGEHOG ANTAGONISTS HAVING ZINC BINDING MOIETIES

Curis, Inc., Lexington, ...

1. A compound of Formula (VI):
or a pharmaceutically acceptable salt or prodrug thereof;
wherein
Q is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;
G is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;
K is halogen;
X is absent, —O—, —N(R2)—, —S—, —S(O)—, —S(O)2—, —C(O)—, —C(O)O—, —OC(O)—, —C(O)N(R2)—, —N(R2)C(O)—, —S(O)2N(R2)—, or —N(R2)S(O)2—;
R2 is hydrogen or C1-C6-alkyl;
B is a direct bond, 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, aryloxyC1-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 and heteroaryloxyC1-C10alkoxy, in each of which one or more methylenes is optionally interrupted or terminated by —O—, —N(R2)—, —C(O)—, —C(O)N(R2)—, or —C(O)O—; and
D is

where Y2 and R32 are absent, Z is N, W is O, R33 is H and R34 is hydroxyl.

US Pat. No. 10,137,117

CRYSTALLINE N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MONO MESYLATE MONOHYDRATE HAVING A SPECIFIC PARTICLE SIZE DISTRIBUTION RANGE AND A SPECIFIC SURFACE AREA RANGE FOR USE IN PHARMACEUTICAL FORMULATIONS

AiCuris Anti-Infective Cu...

1. A composition of crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide mono methanesulfonic acid monohydrate particles of the following formula
having a purity of >99%,
wherein said particles in the composition have a particle size range from 2 ?m to 500 ?m, a particle size distribution which is defined by d(0.1) from 2 to 100 ?m, d(0.5) from 30 to 210 ?m and d(0.9) from 70 to 400 ?m and a specific surface area of less than 1.0 m2/g.

US Pat. No. 10,336,770

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A compound represented by formula (II);or a pharmaceutically acceptable salt thereof,wherein represents a single or double bond;
X and Y are independently CR1, N(R8), S or O , wherein when one of X and Y is CR1, the other is N(R8), S or O;
R1 is selected from hydrogen, hydroxy, amino, halogen, alkoxy, alkylamino, dialkylamino, CF3, CN, NO2, sulfonyl, acyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, and substituted heterocyclic;
G1 is O;
G2 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or, substituted or unsubstituted heterocyclic;
each R8 is independently hydrogen, acyl, aliphatic or substituted aliphatic;
B is a linker; and
C is

 wherein R33 is hydrogen.
US Pat. No. 10,330,683

MUTANT SMOOTHENED AND METHODS OF USING THE SAME

Genentech, Inc., South S...

1. A method of screening for compounds that inhibit signaling of a mutant SMO (Smoothened) protein having an amino acid sequence of SEQ ID NO: 6, wherein said amino acid sequence has an amino acid other than threonine at amino acid 241, comprising contacting said mutant SMO with a test compound, and detecting binding of said compound to said mutant SMO, whereby binding of said test compound to mutant SMO indicates that said test compound is an inhibitor of mutant SMO.
US Pat. No. 10,287,254

SALTS OF A DIHYDROQUINAZOLINE DERIVATIVE

1. A method for purifying {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid using the following steps:1.) Reacting {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid in a solvent with benzenesulfonic acid or toluenesulfonic acid to obtain a crystalline salt,
2.) Isolating the salt obtained in step 1.),
3.) Treating the isolated salt obtained in step 2.) with a buffer solution at a pH in the range of 5 to 7 to release a zwitterionic form of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid, and
4). Isolating the zwitterionic form of {8-fluoro-2-[4-(3-methoxyphenyl)piperazine-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazoline-4-yl}acetic acid obtained in step 3.).

US Pat. No. 10,442,773

AMORPHOUS LETERMOVIR AND SOLID PHARMACEUTICAL FORMULATIONS THEREOF FOR ORAL ADMINISTRATION

AICURIS ANTI-INFECTIVE CU...

1. Letermovir according to Formula (I),which is amorphous Letermovir, the pure chemical entity with (S)-configuration, obtained by a precipitation process for isolating amorphous Letermovir, wherein the process comprises:precipitating said amorphous Letermovir from the water miscible solvents acetone or acetonitrile into excess stirred water,
followed by isolating the amorphous Letermovir via filtration or centrifugation,
wherein said process for isolating the amorphous Letermovir does not include precipitation using alcohols or precipitation using tetrahydrofuran or methylethylketone.

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. 10,463,822

AIRWAY STABILIZATION SYSTEM

Securisyn Medical, LLC, ...

1. An airway stabilization system for maintaining an airway in a patient's trachea, the patient having a head, a face, cheeks, a mouth, an oral cavity, a chin, vocal cords, and a carina, the system comprising: an airway device adapted to be maintained in a preselected position in the patient's trachea and including a flexible body portion extending along an axis and having a preselected length and preselected internal and external diameters, a distal end portion adapted to be positioned a preselected distance from the patient's carina, and a proximal end portion adapted to be positioned outside of the patient's oral cavity; a retention structure secured to the proximal end portion of the airway device and adapted to be positioned outside of the patient's oral cavity, the retention structure having a preselected length; a securing apparatus adapted to be secured to the patient, the securing apparatus including a restraining device having a length and being adapted to releaseably engage the retention structure outside the patient's oral cavity whereby the risk of oral and dental injury to the patient is minimized, the securing apparatus and the retention structure cooperating with one another and being adapted to form a barrier to movement of the airway device in the patient's trachea in response to the application of multidirectional forces to the airway device; the retention structure and securing apparatus further cooperating to encapsulate a portion of the airway device circumferentially along the length of the restraining device whereby the encapsulated portion of the airway device is isolated from any constricting, pinching or crushing forces which would constrict the internal diameter of the airway device, wherein the retention structure includes a plurality of ribs formed thereon, each of the plurality of ribs extending radially outwardly therefrom in the form of an annular flange, the plurality of ribs being positioned axially along the length of the retention structure having a uniform or substantially uniform spacing distance therebetween, forming a plurality of spaces or structural recesses positioned axially along the length of the retention structure, wherein at least one of the plurality of ribs formed on the retention structure is marked to distinguish the at least one of the plurality of ribs from the other of the plurality of ribs formed thereon, wherein the securing apparatus includes a faceplate adapted to be secured to the patient and defining a plane, wherein the restraining device includes a pair of oppositely disposed, pivotally interconnected, c-shaped collars respectively extending generally symmetrically about and along an axis in a direction substantially perpendicular to the plane defined by the faceplate and adapted to be away from the patient's face, and wherein at least one of the pair of c-shaped collars includes a plurality of insertion depth guides affixed thereto.