公开(公告)号：US20180079758A1

公开(公告)日：2018-03-22

申请号：US15809437

申请日：2017-11-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Douglas G. Batt ,  Myra Beaudoin Bertrand ,  George V. Delucca ,  Michael A. Galella ,  Soo Sung Ko ,  Charles M. Langevine ,  Qingjie Liu ,  Qing Shi ,  Anurag S. Srivastava ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D513/04 ,  C07D471/04 ,  C07D403/10 ,  C07D209/88 ,  C07D239/70

CPC classification number: C07D513/04 ,  C07B2200/07 ,  C07B2200/13 ,  C07D209/88 ,  C07D239/70 ,  C07D403/10 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. 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：US20170362176A1

公开(公告)日：2017-12-21

申请号：US15521194

申请日：2015-10-23

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Saleem Ahmad ,  Douglas G. Batt ,  Qingjie Liu ,  John E. Macor ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D209/88 ,  C07D487/04 ,  C07D471/10 ,  C07D403/12 ,  C07D401/04 ,  C07D403/06 ,  C07D403/04 ,  C07D401/06 ,  C07D495/04 ,  C07D471/04

CPC classification number: C07D209/88 ,  A61K31/4523 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D495/04

Abstract: Disclosed are compounds of Formula (I): (I) or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d 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：US20140378475A1

公开(公告)日：2014-12-25

申请号：US14314602

申请日：2014-06-25

Applicant: Bristol-Myers Squibb Company

Inventor： Douglas G. Batt ,  Myra Beaudoin Bertrand ,  George Delucca ,  Michael A. Galella ,  Soo Sung Ko ,  Charles M. Langevine ,  Qingjie Liu ,  Qing Shi ,  Anurag S. Srivastava ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D513/04 ,  C07D471/04 ,  C07D403/10

CPC classification number: C07D513/04 ,  C07B2200/07 ,  C07B2200/13 ,  C07D209/88 ,  C07D239/70 ,  C07D403/10 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. 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，其中：两条虚线表示两个单键或双键; Q是：R1是F，Cl，-CN或-CH3; R2是Cl或-CH3; R3是-C（CH3）2OH或-CH2CH2OH; Ra为H或-CH 3; 每个R b独立地是F，Cl，-CH 3和/或-OCH 3; 并且n为0,1或2.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（例如自身免疫疾病和血管疾病）中的疾病或病症的进展。

公开(公告)号：US20190225583A1

公开(公告)日：2019-07-25

申请号：US16289878

申请日：2019-04-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Saleem Ahmad ,  Douglas G. Batt ,  Qingjie Liu ,  John E. Macor ,  Joseph A. Tino ,  Scott Hunter Watterson ,  Satheesh Kesavan Nair ,  Tarun Kumar Maishal

IPC: C07D209/88 ,  C07D495/04 ,  C07D403/12 ,  C07D471/10 ,  C07D487/04 ,  A61K31/4523 ,  C07D403/06 ,  C07D471/04 ,  C07D403/04 ,  C07D401/04 ,  C07D401/06

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d 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：US20190023719A1

公开(公告)日：2019-01-24

申请号：US16140750

申请日：2018-09-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Douglas G. Batt ,  Myra Beaudoin Bertrand ,  George V. De Lucca ,  Michael A. Galella ,  Soo Sung Ko ,  Charles M. Langevine ,  Qingjie Liu ,  Qing Shi ,  Anurag S. Srivastava ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D513/04 ,  C07D209/88 ,  C07D471/04 ,  C07D403/10 ,  C07D239/70

CPC classification number: C07D513/04 ,  C07B2200/07 ,  C07B2200/13 ,  C07D209/88 ,  C07D239/70 ,  C07D403/10 ,  C07D471/04

Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. 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：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：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：US10106559B2

公开(公告)日：2018-10-23

申请号：US15809437

申请日：2017-11-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Douglas G. Batt ,  Myra Beaudoin Bertrand ,  George V. Delucca ,  Michael A. Galella ,  Soo Sung Ko ,  Charles M. Langevine ,  Qingjie Liu ,  Qing Shi ,  Anurag S. Srivastava ,  Joseph A. Tino ,  Scott Hunter Watterson

IPC: C07D513/04 ,  C07D471/04 ,  C07D403/10 ,  C07D239/70 ,  C07D209/88

Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. 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：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.