[EN] 5-MEMBERED AND BICYCLIC HETEROCYCLIC AMIDES AS INHIBITORS OF ROCK<br/>[FR] AMIDES HÉTÉROCYCLIQUES À 5 CHAÎNONS ET BICYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE ROCK
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2019014308A1
公开(公告)日:2019-01-17
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.
N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
申请人:Rodgers James D.
公开号:US20100298334A1
公开(公告)日:2010-11-25
The present invention relates to N-(hetero)aryl-pyrrolidine derivatives of Formula I:
which are JAK inhibitors, such as selective JAK1 inhibitors, useful in the treatment of JAK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
[EN] THIENOPYRIDINES AND BENZOTHIOPHENES USEFUL AS IRAK4 INHIBITORS<br/>[FR] THIÉNOPYRIDINES ET BENZOTHIOPHÈNES UTILES EN TANT QU'INHIBITEURS D'IRAK4
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2018209012A1
公开(公告)日:2018-11-15
Disclosed are compounds of Formula (I) or a salt or prodrug thereof, wherein: X is CR4 or N; Y is CR5 or N; provided that only one of X and Y is N; (R1) is: or; wherein R1, R1a, R1b, R1c, R2, and R3 are define herein. Also disclosed are methods of using such compounds as modulators of IRAK4, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases, or in the treatment of cancer.
(1H-Tetrazol-5-yl)tetrazolo[1,5-a]thienopyridines and related compounds which are useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate halocyano-quinoline with ammonium chloride and an azide such as sodium azide in an inert solvent such as dimethylformamide.
(1H-Tetrazol-5-yl)thienopyridinones and related compounds which are useful as antiallergic agents are described herein. The compounds are prepared by the reaction of an appropriate cyanoketone with ammonium chloride and an azide such as sodium azide in an inert solvent such as dimethylformamide.