公开(公告)号：US20190300523A1

公开(公告)日：2019-10-03

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：US20170260237A1

公开(公告)日：2017-09-14

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: C07K7/64 ,  A61K45/06 ,  A61K38/12

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：US20170355698A1

公开(公告)日：2017-12-14

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

CPC classification number: 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：US20130178444A1

公开(公告)日：2013-07-11

申请号：US13785039

申请日：2013-03-05

Applicant: Bristol-Myers Squibb Company

Inventor： John Hynes ,  Percy H. Carter ,  Lyndon A.M. Cornelius ,  T.G. Murali Dhar ,  John V. Duncia ,  Satheesh K. Nair ,  Joseph B. Santella ,  Jayakumar S. Warrier ,  Hong Wu

IPC: C07D211/60 ,  C07F9/59

CPC classification number: C07D211/60 ,  C07D211/52 ,  C07F9/59

Abstract: The present application describes prodrugs of the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis using the prodrug compounds of the invention are disclosed.

Abstract translation: 本申请描述了式（I）化合物的前药或其立体异构体或其药学上可接受的盐。 此外，公开了使用本发明的前药化合物治疗和预防炎症性疾病如哮喘和过敏性疾病以及自身免疫性病症如类风湿性关节炎的方法。

公开(公告)号：US20180002358A1

公开(公告)日：2018-01-04

申请号：US15701818

申请日：2017-09-12

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

公开(公告)号：US20170355707A1

公开(公告)日：2017-12-14

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: C07D491/08 ,  C07D487/04

CPC classification number: C07D491/08 ,  C07D487/04

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：US20160326195A1

公开(公告)日：2016-11-10

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

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.

Abstract translation: 或其立体异构体，互变异构体，其药学上可接受的盐，溶剂合物或前药，其中所有取代基均在本文中定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于调节细胞中RORγ活性的方法和用于治疗受试者治疗受益于RORγ活性（例如自身免疫和/或炎症性疾病）的疾病或病症的受试者的方法。