公开(公告)号：US20160090364A1

公开(公告)日：2016-03-31

申请号：US14962923

申请日：2015-12-08

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter W. Glunz ,  Yan Zou ,  Mimi L. Quan

IPC: C07D237/32 ,  C07D401/10 ,  C07D413/12 ,  C07D513/04 ,  C07D403/12 ,  C07D417/12 ,  C07D405/12 ,  C07D417/14 ,  C07D403/10 ,  C07D401/12

CPC classification number: C07D237/32 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04 ,  G05B19/418 ,  G05B19/4189 ,  G05B2219/31033 ,  G05B2219/32278 ,  Y02P90/04 ,  Y02P90/28

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.

Abstract translation: 本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性的ROCK抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其治疗心血管，平滑肌，肿瘤学，神经病理学，自身免疫性，纤维化和/或炎症性疾病的方法。

公开(公告)号：US20160002172A1

公开(公告)日：2016-01-07

申请号：US14770489

申请日：2014-02-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Zilun Hu ,  Mimi L. Quan

IPC: C07D231/12 ,  C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D409/12

CPC classification number: C07D231/12 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04

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

Abstract translation: 本发明提供式（I）的化合物：（I）或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性的ROCK抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其治疗心血管，平滑肌，肿瘤学，神经病理学，自身免疫性，纤维化和/或炎症性疾病的方法。

公开(公告)号：US20140243338A1

公开(公告)日：2014-08-28

申请号：US14192955

申请日：2014-02-28

Applicant: Bristol-Myers Squibb Company

Inventor： Mimi L. Quan ,  Zilun Hu ,  Cailan Wang

IPC: C07D231/12 ,  C07D401/12 ,  C07D417/12

CPC classification number: C07D231/12 ,  C07D217/12 ,  C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D513/04

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.

Abstract translation: 本发明提供式（I）的化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中所有变量如本文所定义。 这些化合物是选择性的ROCK抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用其治疗心血管，平滑肌，肿瘤学，神经病理学，自身免疫性，纤维化和/或炎症性疾病的方法。

公开(公告)号：US10385026B2

公开(公告)日：2019-08-20

申请号：US15890436

申请日：2018-02-07

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Peter W. Glunz ,  Yan Zou ,  Mimi L. Quan ,  Vladimir Ladziata

IPC: C07D237/32 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04 ,  C07D405/10 ,  C07D217/24 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048

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：US10081623B2

公开(公告)日：2018-09-25

申请号：US15508122

申请日：2015-09-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jun Shi ,  William R. Ewing ,  Laura Nielsen ,  Zilun Hu ,  Mimi L. Quan

IPC: C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D409/12 ,  C07D401/12

CPC classification number: C07D409/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

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 Factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

公开(公告)号：US20180162823A1

公开(公告)日：2018-06-14

申请号：US15890436

申请日：2018-02-07

Applicant: Bristol-Myers Squibb Company

Inventor： Peter W. Glunz ,  Yan Zou ,  Mimi L. Quan ,  Vladimir Ladziata

IPC: C07D237/32 ,  C07D405/10 ,  C07D217/24 ,  C07D417/14 ,  C07D417/12 ,  C07D413/12 ,  C07D405/12 ,  C07D403/12 ,  C07D403/10 ,  C07D401/12 ,  C07D401/10 ,  C07D491/048 ,  C07D487/04 ,  C07D471/04 ,  C07D417/10 ,  C07D413/10 ,  C07D513/04

CPC classification number: C07D237/32 ,  C07D217/24 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D403/12 ,  C07D405/10 ,  C07D405/12 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D513/04

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：US09828345B2

公开(公告)日：2017-11-28

申请号：US14770489

申请日：2014-02-28

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Zilun Hu ,  Mimi L. Quan

IPC: C07D231/12 ,  C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D409/12 ,  C07D487/04

CPC classification number: C07D231/12 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D471/04 ,  C07D487/04

Abstract: The present invention provides compounds of Formula (I): (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：US20170283403A1

公开(公告)日：2017-10-05

申请号：US15508122

申请日：2015-09-03

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Jun Shi ,  William R. Ewing ,  Laura Nielsen ,  Zilun HU ,  Mimi L. Quan

IPC: C07D409/12 ,  C07D401/06 ,  C07D403/06 ,  C07D403/12 ,  C07D401/12

CPC classification number: C07D409/12 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12

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 Factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

公开(公告)号：US20170226105A1

公开(公告)日：2017-08-10

申请号：US15503419

申请日：2015-08-20

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： Zilun Hu ,  Doree F. Sitkoff ,  Mimi L. Quan

IPC: C07D471/04 ,  C07D403/10 ,  C07D231/12 ,  C07D413/14 ,  C07D401/14 ,  C07D409/14 ,  C07D403/14 ,  C07D401/10 ,  C07D405/14

CPC classification number: C07D401/10 ,  C07D231/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  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：US20170050964A1

公开(公告)日：2017-02-23

申请号：US15345045

申请日：2016-11-07

Applicant: Bristol-Myers Squibb Company

Inventor： Donald J.P. Pinto ,  Mimi L. Quan ,  Michael J. Orwat ,  Yun-Long Li ,  Wei Han ,  Jennifer X. Qiao ,  Patrick Y.S. Lam ,  Stephanie L. Koch

IPC: C07D471/04 ,  A61K31/444 ,  A61K31/55 ,  A61K31/437 ,  A61J1/05 ,  A61K31/454 ,  C07D401/12 ,  C07D213/81 ,  C07D401/14 ,  A61J1/03 ,  A61K31/4545 ,  C07D413/14

CPC classification number: C07D471/04 ,  A61J1/00 ,  A61J1/03 ,  A61J1/05 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/513 ,  A61K31/55 ,  A61K45/06 ,  B65D81/3216 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4  I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract translation: 其中环P（如果存在的话）是5-7元碳环或杂环，并且环M是5-7元碳环或杂环。 本发明的化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是因子Xa。