公开(公告)号：US11618753B2

公开(公告)日：2023-04-04

申请号：US16963886

申请日：2019-01-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Scott Hunter Watterson ,  Murugaiah Andappan Murugaiah Subbaiah ,  Carolyn Diane Dzierba ,  Hua Gong ,  Jason M. Guernon ,  Junqing Guo ,  Amy C. Hart ,  Guanglin Luo ,  John E. Macor ,  William J. Pitts ,  Jianliang Shi ,  Brian Lee Venables ,  Carolyn A. Weigelt ,  Yong-Jin Wu ,  Zhizhen Barbara Zheng ,  Sing-Yuen Sit ,  Jie Chen

IPC: A61K31/53 ,  C07D253/08 ,  C07D487/04

Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.

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：US20160115126A1

公开(公告)日：2016-04-28

申请号：US14921347

申请日：2015-10-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Qingjie Liu ,  Scott Hunter Watterson ,  Douglas G. Batt ,  Saleem Ahmad ,  Myra Beaudoin Bertrand ,  Hua Gong ,  Weiwei Guo ,  John E. Macor ,  Khehyong Ngu ,  Andrew J. Tebben ,  Joseph A. Tino

IPC: C07D209/08 ,  C07D403/10 ,  C07D403/12 ,  C07D403/04 ,  C07D487/10 ,  C07D487/04 ,  C07D413/04 ,  C07D471/04 ,  C07D401/06 ,  C07D417/04 ,  C07D401/04 ,  C07D401/12

CPC classification number: C07D401/10 ,  C07D209/08 ,  C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Abstract translation: 公开了式（I）的化合物或其盐，其中：X是CR 4或N; R1，R2，R3，R4和A在本文中定义。 还公开了使用这种化合物作为Bruton酪氨酸激酶（Btk）的抑制剂的方法和包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域（例如自身免疫性疾病和血管疾病）中的疾病或病症的进展。

公开(公告)号：US20200347071A1

公开(公告)日：2020-11-05

申请号：US16963886

申请日：2019-01-24

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Scott Hunter Watterson ,  Murugaiah Andappan Murugaiah Subbaiah ,  Carolyn Diane Dzierba ,  Hua Gong ,  Jason M. Guernon ,  Junqing Guo ,  Amy C. Hart ,  Guanglin Luo ,  John E. Macor ,  William J. Pitts ,  Jianliang Shi ,  Brian Lee Venables ,  Carolyn A. Weigelt ,  Yong-Jin Wu ,  Zhizhen Barbara Zheng ,  Sing-Yuen Sit ,  Jie Chen

IPC: C07D487/04

Abstract: The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK 1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.

公开(公告)号：US20160229844A1

公开(公告)日：2016-08-11

申请号：US15022673

申请日：2014-09-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D417/06 ,  C07D401/06 ,  C07D401/12 ,  C07D413/14 ,  C07D215/58 ,  C07D413/06

CPC classification number: C07D417/06 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14

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.

Abstract translation: 描述了式（I）的RORγ调节剂或其药学上可接受的盐，其中所有取代基在本文中定义。 本发明包括式I化合物的立体异构体形式，包括立体异构纯，鳞片和外消旋形式及其互变异构体。 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。

公开(公告)号：US20170260160A1

公开(公告)日：2017-09-14

申请号：US15608340

申请日：2017-05-30

Applicant: Bristol-Myers Squibb Company

Inventor： Qingjie Liu ,  Scott Hunter Watterson ,  Douglas G. Batt ,  Saleem Ahmad ,  Myra Beaudoin Bertrand ,  Hua Gong ,  Weiwei Guo ,  John E. Macor ,  Khehyong Ngu ,  Andrew J. Tebben ,  Joseph A. Tino

IPC: C07D401/10 ,  C07D209/18 ,  C07D401/04 ,  C07D487/04 ,  C07D401/12 ,  C07D471/04 ,  C07D487/10 ,  C07D209/08 ,  C07D401/06

CPC classification number: C07D401/10 ,  C07D209/08 ,  C07D209/18 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/10 ,  C07D403/12 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: X is CR4 or N; R1, R2, R3, R4, and A are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US09593113B2

公开(公告)日：2017-03-14

申请号：US14911485

申请日：2014-08-21

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Weinstein ,  Hua Gong ,  Michael G Yang ,  Zili Xiao

IPC: C07D471/04 ,  C07D311/90 ,  C07D311/80 ,  C07D491/04

CPC classification number: C07D471/04 ,  C07D311/80 ,  C07D311/90 ,  C07D491/04

Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases or disorders associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-KB activity, including metabolic and inflammatory and immune diseases or disorders, having the structure of formula (I): an enantiomer, diastereomer, or tautomer thereof, or a pharmaceutically-acceptable salt thereof, in which the variables are as defined in the specification.

Abstract translation: 提供了新的非甾体化合物，其可用于治疗与调节糖皮质激素受体，AP-1和/或NF-κB活性相关的疾病或病症，所述疾病或病症包括代谢和炎症和免疫疾病或病症，其具有式 （I）：其对映异构体，非对映异构体或其互变异构体或其药学上可接受的盐，其中变量如说明书中所定义。

公开(公告)号：US20160318870A1

公开(公告)日：2016-11-03

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

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.

Abstract translation: 描述了式（I）的RORγ调节剂或其药学上可接受的盐，其中所有取代基在本文中定义。 本发明包括式I化合物的立体异构体形式，包括立体异构纯，鳞片和外消旋形式及其互变异构体。 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。

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：US09725443B2

公开(公告)日：2017-08-08

申请号：US15022673

申请日：2014-09-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: A61K31/47 ,  C07D417/06 ,  C07D401/06 ,  C07D401/12 ,  C07D413/14 ,  C07D215/58 ,  C07D413/06

CPC classification number: C07D417/06 ,  C07D215/58 ,  C07D401/06 ,  C07D401/12 ,  C07D413/06 ,  C07D413/14

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.