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

PYRROLOPYRAZINE DERIVATIVES AS ALPHA V INTEGRIN INHIBITORS (Fri, 17 May 2019)
The disclosure relates to compounds of formula I: Formula I which inhibit αv-containing integrins, and includes pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of αV-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders.
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MULTICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS (Fri, 10 May 2019)
The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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DIAZASPIRO ROCK INHIBITORS (Fri, 10 May 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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ALKENE COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS (Fri, 10 May 2019)
The present invention provides compounds of Formula (I): Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of famesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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SPIROCYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS (Fri, 10 May 2019)
The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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BRIDGED BICYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS (Fri, 10 May 2019)
The present invention provides compounds of Formula (I) or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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ISOFURANONE COMPOUNDS USEFUL AS HPK1 INHIBITORS (Fri, 10 May 2019)
Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is CH or N; Y is CR5 or N; and R1, R2, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds to modulate or inhibit the enzymatic activity of hematopoietic progenitor kinase 1 (HPK1), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
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AMINOIMIDAZOPYRIDINES AS KINASE INHIBITORS (Fri, 10 May 2019)
Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
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ALKENE SPIROCYCLIC COMPOUNDS AS FARNESOID X RECEPTOR MODULATORS (Fri, 10 May 2019)
The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds modulate the activity of farnesoid X receptor (FXR), for example, as agonists. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
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CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS (Fri, 26 Apr 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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SMALL MOLECULE INHIBITORS OF GALECTIN-3 (Fri, 19 Apr 2019)
The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
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CYCLIC DINUCLEOTIDES AS ANTICANCER AGENTS (Fri, 19 Apr 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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INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE (Fri, 19 Apr 2019)
The present invention provides compounds of formula (I), formula (II) or formula (III), wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.
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INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE (Fri, 19 Apr 2019)
The present invention provides compounds of formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.
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IMMUNOMODULATORS (Fri, 12 Apr 2019)
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
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SMALL MOLECULE INHIBITORS OF GALECTIN-3 (Fri, 05 Apr 2019)
The present disclosure relates to compounds of formula I, which inhibit Gal-3, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
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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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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) 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 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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