公开(公告)号：US09334290B2

公开(公告)日：2016-05-10

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: C07D471/04 ,  C07D513/04 ,  C07D403/10 ,  A61P37/06 ,  A61P19/02 ,  A61P25/28

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：US20160200710A1

公开(公告)日：2016-07-14

申请号：US14392355

申请日：2014-06-25

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Soo Sung Ko ,  Douglas G Batt ,  Myra Beaudoin Bertrand ,  George Delucca ,  Charles M. Langevine ,  Qingjie Liu ,  Anurag S. Srivastava ,  Scott Hunter Watterson

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

CPC classification number: C07D403/10 ,  C07D471/04 ,  C07D513/04

Abstract: Disclosed are compounds of Formula (I); and salts thereof, wherein: Formula (II); Q is: R1 is —C(CH3)2OH, —NHC(=0)C(CH3)3, —N(CH3)2, or —CH2Rd; R2 is CI or —CH3; R3 is H, F, or —CH3; Ra is H or —CH3; Rb is H, F, CI, or —OCH3 Rc is H or F; and Rd is —OH, —OCH3, —NHC(=0)CH3, or fORMULA (III), 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; 和其盐，其中：式（II）; Q是：R 1是-C（CH 3）2 OH，-NHC（= O）C（CH 3）3，-N（CH 3）2或-CH 2 R d; R2是Cl或-CH3; R3是H，F或-CH3; Ra为H或-CH 3; R b为H，F，Cl或-OCH 3 R c为H或F; 并且Rd是-OH，-OCH 3，-NHC（= O）CH 3或芳基（III）。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：US20180127368A1

公开(公告)日：2018-05-10

申请号：US15806554

申请日：2017-11-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David Marcoux ,  Myra Beaudoin Bertrand ,  T.G. Murali Dhar ,  Michael G. Yang ,  Zili Xiao ,  Hai-Yun Xiao ,  Yeheng Zhu ,  Carolyn A. Weigelt ,  Douglas G Batt

IPC: C07D211/48 ,  C07D213/40 ,  C07D295/195 ,  C07D213/75 ,  C07D333/48 ,  C07C317/44 ,  C07D335/02 ,  C07D471/04 ,  C07D307/22 ,  C07D241/08 ,  C07D207/10 ,  C07D207/16 ,  C07D231/08 ,  C07D309/10 ,  C07D211/96 ,  C07D471/10 ,  C07D205/04 ,  C07D207/277 ,  C07D257/04 ,  C07D205/08 ,  A61P37/00

CPC classification number: C07D211/48 ,  A61P37/00 ,  C07B2200/05 ,  C07B2200/07 ,  C07C317/20 ,  C07C317/24 ,  C07C317/30 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/38 ,  C07C2602/44 ,  C07C2602/50 ,  C07C2603/08 ,  C07C2603/12 ,  C07C2603/16 ,  C07C2603/90 ,  C07D205/04 ,  C07D205/08 ,  C07D207/09 ,  C07D207/10 ,  C07D207/16 ,  C07D207/277 ,  C07D207/28 ,  C07D211/62 ,  C07D211/78 ,  C07D211/96 ,  C07D213/40 ,  C07D213/56 ,  C07D213/75 ,  C07D213/81 ,  C07D215/36 ,  C07D231/06 ,  C07D231/08 ,  C07D231/18 ,  C07D233/64 ,  C07D233/76 ,  C07D233/78 ,  C07D233/90 ,  C07D241/08 ,  C07D249/12 ,  C07D257/04 ,  C07D261/18 ,  C07D263/20 ,  C07D285/06 ,  C07D295/16 ,  C07D295/195 ,  C07D305/08 ,  C07D307/22 ,  C07D309/10 ,  C07D333/48 ,  C07D335/02 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D471/04 ,  C07D471/10 ,  C07F9/091

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：US09714234B2

公开(公告)日：2017-07-25

申请号：US14392355

申请日：2014-06-25

Applicant: Bristol-Myers Squibb Company

Inventor： Soo Sung Ko ,  Douglas G Batt ,  Myra Beaudoin Bertrand ,  George Delucca ,  Charles M. Langevine ,  Qingjie Liu ,  Anurag S. Srivastava ,  Scott Hunter Watterson

IPC: C07D209/88 ,  C07D209/86 ,  C07D239/91 ,  C07D239/96 ,  A61K31/505 ,  A61K31/407 ,  C07D403/10 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D403/10 ,  C07D471/04 ,  C07D513/04

Abstract: Disclosed are compounds of Formula (I); and salts thereof, wherein: Formula (II); Q is: R1 is —C(CH3)2OH, —NHC(=0)C(CH3)3, —N(CH3)2, or —CH2Rd; R2 is CI or —CH3; R3 is H, F, or —CH3; Ra is H or —CH3; Rb is H, F, CI, or —OCH3 Rc is H or F; and Rd is —OH, —OCH3, —NHC(=0)CH3, or fORMULA (III), 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.