PATENTSCOPE: EN_ALL:nmr AND PA:Bristol-Myers Squibb

CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS (Fri, 08 Mar 2019)
The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS (Fri, 08 Mar 2019)
The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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6-AMINO-7,9-DIHYDRO-8H-PURIN-8-ONE DERIVATIVES AS IMMUNOSTIMULANT TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS (Fri, 22 Feb 2019)
Compounds having a structure according to formula (I) where R1, R2, and R3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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2-(1,1 '-BIPHENYL)-1 H-BENZO[D]IMIDAZOLE DERIVATIVES AND RELATED COMPOUNDS AS APELIN AND APJ AGONISTS FOR TREATING CARDIOVASCULAR DISEASES (Fri, 22 Feb 2019)
The present invention provides compounds of Formula (I): wherein all variables are as defined in the specification. The compounds are apelin and APJ agonists for treating cardiovascular diseases. Preferred compounds are 2-(l,l'-biphe -lH-benzo[d]imidazole derivatives. The invention further provides compositions comprising the compounds and the compounds for use in methods of medical treatment.
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6-AMINO-7,9-DIHYDRO-8H-PURIN-8-ONE DERIVATIVES AS TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS AS IMMUNOSTIMULANTS (Fri, 22 Feb 2019)
Compounds having a structure according to formula (I). where R1 and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS HAVING A TRICYCLIC MOIETY, CONJUGATES THEREOF, AND METHODS AND USES THEREFOR (Fri, 22 Feb 2019)
Compounds having a structure according to formula (I), (II), or (III) where R1, R2, R3, R5 X1, X2, and X3 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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6-AMINO-7,9-DIHYDRO-8H-PURIN-8-ONE DERIVATIVES AS IMMUNOSTIMULANT TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS (Fri, 22 Feb 2019)
Compounds having a structure according to formula (I) or (II), where R1, R2, and Ar are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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6-AMINO-7,9-DIHYDRO-8H-PURIN-8-ONE DERIVATIVES AS IMMUNOSTIMULANT TOLL-LIKE RECEPTOR 7 (TLR7) AGONISTS (Fri, 22 Feb 2019)
Compounds having a structure according to formula (I) or (II) where R1, R2, R3, R4, Ar and X1 are as defined herein, are agonists for the Toll-like receptor 7 (TLR7) and can be used as adjuvants for stimulating the immune system. Some such compounds can be used in conjugates for targeted delivery to the organ or tissue of intended action.
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ALKYLPHENYL COMPOUNDS (Fri, 15 Feb 2019)
Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is -CH2- or -C(O)-; R1 is -OH or -OP(O)(OH)2; L is a bond, -CH2-, or -C(O)-; R2 is n-C6-8 alkyl; each R3 is independently selected from Cl and -CH3; and n is zero, 1, or 2; provided that if X is -CH2-, then L is -CH2- or -C(O)-. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor SlP1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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OXIME ETHER COMPOUNDS (Fri, 15 Feb 2019)
Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein: X is CH or N; Y is CH or N; R1 is -OH or -OP(O)(OH)2; L1 is -CR3=N-O-CRaRa- or CRaR-O-N=CR3; L2 is a bond, -C(O)-, or S(O)2-;and R2, R3, Ra, m, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
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SUBSTITUTED INDOLE COMPOUNDS USEFUL AS INHIBITORS OF TLR7/8/9 (Fri, 08 Feb 2019)
Disclosed are compounds of Formula (I) or a salt thereof, wherein: Y is Formula (II), or Formula (III); R1, R2, R2a, R2b, R2c, R3, R4,R5, m, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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[1,2,4]TRIAZOLO[4,3-a]PYRIDINYL SUBSTITUTED INDOLE COMPOUNDS (Fri, 08 Feb 2019)
Disclosed are compounds of Formula (I) or a salt thereof, wherein R1, R2, R3, R4a, R4b, R4c, R4d, R5, n, and p are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS (Fri, 01 Feb 2019)
The present invention is directed to compounds of the formulae I, II and III as shown below (I) (II) (III) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and said compositions for use in the treatment of various disorders.
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PROCESS FOR THE PREPARATION OF N-((1R,2S,5R)-5-(TERT-BUTYLAMINO)-2-((S)-3-(7-TERT-BUTYLPYRAZOLO[1,5-A][1,3,5]TRIAZIN-4-YLAMINO)-2-OXOPYRROLIDIN-1-YL)CYCLOHEXYL)ACETAMIDE (Fri, 25 Jan 2019)
The invention generally relates to an improved process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, as well as novel intermediates employed in the process, which may be useful for the treatment of cancer.
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PHENYLACETAMIDES AS INHIBITORS OF ROCK (Fri, 18 Jan 2019)
The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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FIVE MEMBERED-AMINOHETEROCYCLIC AND 5,6-OR 6,6-MEMBERED BICYCLIC AMINOHETEROCYCLIC INHIBITORS OF ROCK FOR THE TREATMENT OF HEART FAILURE (Fri, 18 Jan 2019)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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SPIROHEPTANYL HYDANTOINS AS ROCK INHIBITORS (Fri, 18 Jan 2019)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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5-MEMBERED AND BICYCLIC HETEROCYCLIC AMIDES AS INHIBITORS OF ROCK (Fri, 18 Jan 2019)
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
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AMORPHOUS AND CRYSTALLINE FORMS OF IDO INHIBITORS (Fri, 04 Jan 2019)
The present disclosure relates to amorphous and crystalline forms of (R)-N-(4- chlorophenyl)-2-((lS,4S)-4-(6-fluoroquinolin-4-yl) cyclohexyl)propanamide and its salts and hydrates, processes for their production, pharmaceutical compositions comprising them, and methods of treatment using them.
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SUBSTITUTED QUINOLINYCYCLOHEXYLPROPANAMIDE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION (Fri, 04 Jan 2019)
The disclosure is directed to improved methods for preparing substituted quinolinylcyclohexylpropanamide compounds.
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