公开(公告)号：US20210155618A1

公开(公告)日：2021-05-27

申请号：US16629784

申请日：2018-07-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Benjamin P. Vokits ,  Scott A. Shaw

IPC: C07D471/04 ,  C07D401/12 ,  C07D401/14 ,  C07D487/04 ,  C07D405/14

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：US20240092755A1

公开(公告)日：2024-03-21

申请号：US17888600

申请日：2022-08-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Benjamin P. Vokits ,  Scott A. Shaw

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

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：US11447487B2

公开(公告)日：2022-09-20

申请号：US16629784

申请日：2018-07-11

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Benjamin P. Vokits ,  Scott A. Shaw

IPC: C07D401/12 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04

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：US20180282320A1

公开(公告)日：2018-10-04

申请号：US15756378

申请日：2016-08-30

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Scott A. Shaw ,  Joanne M. Smallheer

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

公开(公告)号：US20250011288A1

公开(公告)日：2025-01-09

申请号：US18701270

申请日：2022-10-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Adam James Clarke ,  Todd J. Friends ,  Arvind Mathur ,  Michael C. Myers ,  Jianqing Li ,  Donald J. P. Pinto ,  Kumar Balashanmuga Pabbisetty ,  Shun Su ,  Benjamin P. Vokits ,  Durga Buchi Raju Barre ,  Leon M. Smith, II ,  Michael J. Orwat ,  Scott A. Shaw ,  Sreekantha Ratna Kumar ,  Hima Kiran Potturi

IPC: C07D213/82 ,  A61K31/343 ,  A61K31/353 ,  A61K31/381 ,  A61K31/415 ,  A61K31/416 ,  A61K31/42 ,  A61K31/423 ,  A61K31/424 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4427 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4704 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/50 ,  A61K31/505 ,  A61K31/5383 ,  A61K31/541 ,  C07D215/54 ,  C07D217/02 ,  C07D217/04 ,  C07D217/08 ,  C07D231/18 ,  C07D231/22 ,  C07D231/54 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D261/04 ,  C07D307/00 ,  C07D311/24 ,  C07D333/38 ,  C07D401/06 ,  C07D405/12 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D491/107 ,  C07D498/04

Abstract: The disclosure relates to compounds of Formula (I), which arm RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension). Formula (I)

公开(公告)号：US12060341B2

公开(公告)日：2024-08-13

申请号：US17888600

申请日：2022-08-16

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Benjamin P. Vokits ,  Scott A. Shaw

IPC: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D471/04

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：US20200291015A1

公开(公告)日：2020-09-17

申请号：US16083951

申请日：2017-03-10

Applicant: Bristol-Myers Squibb Company

Inventor： Joanne M. Smallheer ,  Carol Hui HU ,  Meriah Neissel Valente ,  Scott A. Shaw ,  Benjamin P. Vokits ,  Oz Scott Halpern

IPC: C07D471/04

Abstract: The present invention provides compounds of Formula (I). wherein A and Z are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.

公开(公告)号：US20200131200A1

公开(公告)日：2020-04-30

申请号：US16739363

申请日：2020-01-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Leon M. Smith, II ,  Vladimir Ladziata ,  Indawati De Lucca ,  Donald J.P. Pinto ,  Michael J. Orwat ,  Andrew K. Dilger ,  Kumar Balashnmuga Pabbisetty ,  Wu Yang ,  Scott A. Shaw ,  Peter W. Glunz ,  Manoranjan Panda

IPC: C07D513/04 ,  A61P9/10 ,  A61P15/10 ,  C07D213/64 ,  C07D231/12 ,  C07D401/14 ,  C07D231/54 ,  C07D401/12 ,  C07D413/12 ,  C07D471/12 ,  C07D471/04 ,  C07D231/18

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：US20240417369A1

公开(公告)日：2024-12-19

申请号：US18700868

申请日：2022-10-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Donald J. P. Pinto ,  Shun Su ,  Arvind Mathur ,  Michael C. Myers ,  Jianqing Li ,  Kumar Balashanmuga Pabbisetty ,  Scott A. Shaw

IPC: C07C235/14 ,  A61K31/167 ,  A61K31/17 ,  A61K31/192 ,  A61K31/424 ,  C07C235/74 ,  C07C235/84 ,  C07C275/34 ,  C07D498/04

Abstract: The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).

公开(公告)号：US11059818B2

公开(公告)日：2021-07-13

申请号：US16083951

申请日：2017-03-10

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Joanne M. Smallheer ,  Carol Hui Hu ,  Meriah Neissel Valente ,  Scott A. Shaw ,  Benjamin P. Vokits ,  Oz Scott Halpern

IPC: C07D471/04

Abstract: The present invention provides compounds of Formula (I). wherein A and Z are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and may be useful for the treatment and/or prophylaxis of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.