公开(公告)号：US09663469B2

公开(公告)日：2017-05-30

申请号：US14917420

申请日：2014-09-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： T. G. Murali Dhar ,  Jingwu Duan ,  Hua Gong ,  Bin Jiang ,  Zhonghui Lu ,  David S. Weinstein

IPC: C07D279/16 ,  C07D401/06 ,  C07D417/06 ,  C07D215/58 ,  C07D401/14 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04 ,  C07D491/10 ,  C07D405/14 ,  C07D409/12 ,  C07D471/10 ,  C07D487/10 ,  C07D491/044

CPC classification number: C07D215/58 ,  C07D279/16 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D491/04 ,  C07D491/044 ,  C07D491/10

Abstract: Described are RORγ modulators of the formula (I), or pharmaceutically acceptable salts thereof, wherein all substituents are defined herein. The invention includes stereoisomeric forms of the compounds of formula I, including stereoisomerically-pure, scalemic and racemic form, as well as tautomers thereof. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US20160326115A1

公开(公告)日：2016-11-10

申请号：US15109727

申请日：2015-01-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  T.G. Murali Dhar ,  Bin Jiang ,  Ananta Karmakar ,  Arun Kumar Gupta ,  Zhonghui Lu

IPC: C07D211/54 ,  C07D211/96 ,  C07D405/06 ,  C07D309/08 ,  C07D401/06

CPC classification number: C07D211/54 ,  C07D211/96 ,  C07D309/08 ,  C07D401/06 ,  C07D405/06

Abstract: Described are RORγ modulators of the formula (I), [INSERT CHEMICAL STRUCTURE HERE] or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US11078186B2

公开(公告)日：2021-08-03

申请号：US16348195

申请日：2017-11-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  Bin Jiang ,  T. G. Murali Dhar ,  Zhonghui Lu ,  Arun Kumar Gupta ,  Ananta Karmakar

IPC: C07D401/14 ,  C07D207/06 ,  C07D207/12 ,  C07D207/16 ,  C07D401/06 ,  C07D403/04 ,  C07D405/12 ,  C07D413/06

Abstract: There are described RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US10335392B2

公开(公告)日：2019-07-02

申请号：US15749611

申请日：2016-08-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Hai-Yun Xiao ,  T.G. Murali Dhar ,  Bin Jiang ,  Jingwu Duan

IPC: C07D487/04 ,  C07D487/14 ,  A61K31/4184 ,  A61K31/4188 ,  A61P37/02

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: Ring A is 3- to 6-membered carbocyclic or heterocyclic ring; X is CR1 or N; Y is —(CR5R5)m—; Z is —(CR5R5)n—; and q, R1, R2, R3, R4, R6, R7, R8, R9, and R10 are defined herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US20180222883A1

公开(公告)日：2018-08-09

申请号：US15887214

申请日：2016-08-02

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Hai-Yun XIAO ,  Murali T.G. Dhar ,  Ning Li ,  Jingwu Duan ,  Bin Jiang ,  Zhonghui Lu ,  Khehyong Ngu ,  William J. Pitts ,  Joseph A. Tino

IPC: C07D401/04 ,  C07D215/44 ,  C07D215/42 ,  C07D401/14 ,  C07D401/12 ,  C07D413/14 ,  C07D405/14 ,  C07D417/12 ,  C07D413/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

CPC classification number: C07D401/04 ,  C07D215/42 ,  C07D215/44 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CR1 or N; B is CR3 or N; D is CR4 or N; L1 is —(CR7R7)m—; L2 is —(CR7R7)n—; and X, Z, R1, R2, R3, R4, R5, and R6 are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

公开(公告)号：US09771320B2

公开(公告)日：2017-09-26

申请号：US15109741

申请日：2015-01-05

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  T. G. Murali Dhar ,  Bin Jiang ,  Zhonghui Lu ,  Ananta Karmakar ,  Arun Kumar Gupta ,  Carolyn A. Weigelt

IPC: C07C317/14 ,  C07D213/81 ,  C07D401/04 ,  C07D237/08 ,  C07C317/20 ,  C07C317/30 ,  C07C317/46 ,  C07D471/04 ,  C07D213/30 ,  C07D213/56 ,  C07D309/04 ,  C07D309/14 ,  C07D317/44 ,  C07D231/12 ,  C07D239/38 ,  C07D241/12 ,  C07D471/10 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D211/36 ,  C07D295/16 ,  C07D295/20 ,  C07D303/06 ,  C07D305/14 ,  C07D205/04 ,  C07D211/62 ,  C07D213/40 ,  C07D213/75 ,  C07D295/155 ,  C07D295/108 ,  C07D319/20 ,  C07D285/06 ,  C07D295/18 ,  C07D295/22 ,  C07D303/34 ,  C07C317/22 ,  C07C317/44 ,  C07C317/32 ,  C07C317/50 ,  C07D213/85 ,  C07D295/185

CPC classification number: C07C317/14 ,  C07C317/20 ,  C07C317/22 ,  C07C317/30 ,  C07C317/32 ,  C07C317/44 ,  C07C317/46 ,  C07C317/50 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2602/08 ,  C07D205/04 ,  C07D211/36 ,  C07D211/62 ,  C07D213/30 ,  C07D213/40 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D213/85 ,  C07D231/12 ,  C07D237/08 ,  C07D239/38 ,  C07D241/12 ,  C07D257/04 ,  C07D261/08 ,  C07D263/32 ,  C07D271/06 ,  C07D285/06 ,  C07D295/108 ,  C07D295/155 ,  C07D295/18 ,  C07D295/185 ,  C07D295/20 ,  C07D295/22 ,  C07D303/06 ,  C07D303/34 ,  C07D305/14 ,  C07D309/04 ,  C07D309/14 ,  C07D317/44 ,  C07D319/20 ,  C07D401/04 ,  C07D471/04 ,  C07D471/10

Abstract: Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.