公开(公告)号：US10023576B2

公开(公告)日：2018-07-17

申请号：US15521199

申请日：2015-10-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Zheming Ruan ,  Robert J. Cherney ,  Lyndon A. M. Cornelius ,  T. G. Murali Dhar ,  Hua Gong ,  David Marcoux ,  Michael A. Poss ,  Lan-ying Qin ,  Qing Shi ,  Joseph A. Tino

IPC: C07D487/04

Abstract: Disclosed are compounds of Formula (I); or a salt thereof; wherein Qi is (i) Cl, Br, I, —CN, —CH3, or —CF3; or (ii) pyrazole, triazole, or pyridinyl, each substituted with R1; Q2 is pyridinyl, indazolyl, isoquinolinyl, or benzo[d]imidazolyl substituted with R2 and R3; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

公开(公告)号：US10934286B2

公开(公告)日：2021-03-02

申请号：US16341474

申请日：2017-10-12

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qingjie Liu ,  T. G. Murali Dhar ,  Lan-ying Qin ,  Lyndon A. M. Cornelius ,  Hai-Yun Xiao ,  Jianqing Li ,  Robert J. Cherney

IPC: C07D471/04 ,  C07D491/147

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 Gamma 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 Gamma activity, for example, autoimmune and/or inflammatory disorders.

公开(公告)号：US10538555B2

公开(公告)日：2020-01-21

申请号：US15510138

申请日：2014-09-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Michael Matthew Miller ,  Claudio Mapelli ,  Martin Patrick Allen ,  Michael S. Bowsher ,  Eric P. Gillis ,  David R. Langley ,  Eric Mull ,  Maude A. Poirier ,  Nishith Sanghvi ,  Li-Qiang Sun ,  Daniel J. Tenney ,  Kap-Sun Yeung ,  Juliang Zhu ,  Kevin W. Gillman ,  Qian Zhao ,  Katharine A. Grant-Young ,  Paul Michael Scola ,  Lyndon A. M. Cornelius

IPC: A61K38/12 ,  C07K7/64 ,  C07K7/08 ,  A61K45/06 ,  A61K38/00

Abstract: 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.

公开(公告)号：US10214537B2

公开(公告)日：2019-02-26

申请号：US15521202

申请日：2015-10-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Douglas G. Batt ,  Robert J. Cherney ,  Lyndon A. M. Cornelius ,  Qingjie Liu ,  David Marcoux ,  James Neels ,  Michael A. Poss ,  Zheming Ruan ,  Qing Shi ,  Anurag S. Srivastava ,  Lan-ying Qin ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D487/04 ,  C07D491/08 ,  A61K31/53 ,  A61K31/541 ,  A61P29/00

Abstract: Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Q1 is: (i) Cl, Br, I, —CN, —CH3, or —CF3; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 Ra and zero to 1 Rb; and R1, R2, R3, R4, R5, R6, Ra, and Rb are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.

公开(公告)号：US09815859B2

公开(公告)日：2017-11-14

申请号：US15148209

申请日：2016-05-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jingwu Duan ,  T. G. Murali Dhar ,  David Marcoux ,  Qing Shi ,  Douglas G. Batt ,  Qingjie Liu ,  Robert J. Cherney ,  Lyndon A. M. Cornelius ,  Anurag S. Srivastava ,  Myra Beaudoin Bertrand ,  Carolyn A. Weigelt

IPC: A61K31/437 ,  C07F9/6574 ,  C07D215/36 ,  C07D409/04 ,  C07D417/04 ,  C07D209/30 ,  C07D209/60 ,  C07D209/70 ,  C07D221/10 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D491/107 ,  C07D493/08 ,  C07D495/04 ,  C07D495/08

CPC classification number: C07F9/65742 ,  C07D209/30 ,  C07D209/60 ,  C07D209/70 ,  C07D215/36 ,  C07D221/10 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/06 ,  C07D413/10 ,  C07D413/12 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D491/107 ,  C07D493/08 ,  C07D495/04 ,  C07D495/08

Abstract: There are described RORγ modulators of the formula (I), and formula (II) 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.