公开(公告)号：US08901305B2

公开(公告)日：2014-12-02

申请号：US13946344

申请日：2013-07-19

Applicant: Bristol-Myers Squibb Company

Inventor： Vivekananda M. Vrudhula ,  Senliang Pan ,  Ramkumar Rajamani ,  Susheel Jethanand Nara ,  Maheswaran Sivasamban Karatholuvhu ,  Tarun Kumar Maishal ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Joanne J. Bronson ,  John E. Macor

IPC: A61K31/44 ,  C07D471/00 ,  C07D471/04

CPC classification number: C07D471/04

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

Abstract translation: 本公开一般涉及可抑制AAK1（衔接子相关激酶1），包含这些化合物的组合物和抑制AAK1的方法的化合物。

公开(公告)号：US20180346440A1

公开(公告)日：2018-12-06

申请号：US15763280

申请日：2016-09-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC: C07D401/04 ,  C07D413/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/02

Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

公开(公告)号：US11673886B2

公开(公告)日：2023-06-13

申请号：US17349980

申请日：2021-06-17

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter W. Glunz ,  Vladimir Ladziata ,  Indawati De Lucca ,  George O. Tora ,  Tarun Kumar Maishal ,  Raghuram Tangirala ,  Kamalraj Thiyagarajan

IPC: C07D417/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  C07D491/052

CPC classification number: C07D417/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I):




or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US11078197B2

公开(公告)日：2021-08-03

申请号：US16629717

申请日：2018-07-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter W. Glunz ,  Vladimir Ladziata ,  Indawati De Lucca ,  George O. Tora ,  Tarun Kumar Maishal ,  Raghuram Tangirala ,  Kamalraj Thiyagarajan

IPC: C07D417/12 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically-acceptable salts thereof wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US11053197B2

公开(公告)日：2021-07-06

申请号：US16859103

申请日：2020-04-27

Applicant: BRISTOL-MYERS SQUIBB COMPANY

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

IPC: C07D401/04 ,  C07D403/04 ,  C07D487/04 ,  C07D487/10 ,  C07D209/88 ,  A61K31/4523 ,  C07D471/04 ,  A61K31/403 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D471/10 ,  C07D495/04

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：US20180141956A1

公开(公告)日：2018-05-24

申请号：US15563697

申请日：2016-04-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Susheel Jethanand Nara ,  Carolyn Diane Dzierba ,  John E. Macor ,  Joanne J. Bronson ,  Rajamani Ramkumar ,  Tarun Kumar Maishal ,  Maheswaran Sivasamban Karatholuvhu ,  Soodamani Thangavel ,  Kamalraj Thiyagarajan

IPC: C07D491/052 ,  C07D471/04 ,  C07B59/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P25/04 ,  A61P25/02

CPC classification number: C07D491/052 ,  A61P25/02 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07B59/002 ,  C07B2200/05 ,  C07D471/04 ,  C07D491/04

Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.

公开(公告)号：US10787450B2

公开(公告)日：2020-09-29

申请号：US16315679

申请日：2017-07-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Mandar Shrikrishna Bodas ,  Pravin Sudhakar Shirude ,  Sharanabasappa Patil ,  Tarun Kumar Maishal ,  Kamalraj Thiyagarajan ,  Kumaresan Chinnakotti ,  Peter W. Glunz

IPC: C07D471/10 ,  C07D403/10 ,  C07D487/10 ,  C07D491/10

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

公开(公告)号：US10544120B2

公开(公告)日：2020-01-28

申请号：US15763280

申请日：2016-09-29

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne J. Bronson ,  Ling Chen ,  Jonathan L. Ditta ,  Carolyn Diane Dzierba ,  Prasada Rao Jalagam ,  Guanglin Luo ,  John E. Macor ,  Tarun Kumar Maishal ,  Susheel Jethanand Nara ,  Ramkumar Rajamani ,  Ramesh Kumar Sistla ,  Soodamani Thangavel

IPC: C07D401/04 ,  C07D413/14 ,  A61P25/16 ,  A61P25/28 ,  A61P25/18 ,  A61P25/02

Abstract: The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

公开(公告)号：US20190300528A1

公开(公告)日：2019-10-03

申请号：US16315679

申请日：2017-07-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Rajeev S. Bhide ,  Mandar Shrikrishna Bodas ,  Pravin Sudhakar Shirude ,  Sharanabasappa Patil ,  Tarun Kumar Maishal ,  Kamalraj Thiyagarajan ,  Kumaresan Chinnakotti ,  Peter W. Glunz

IPC: C07D471/10 ,  C07D491/10 ,  C07D403/10 ,  C07D487/10

Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.

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.