公开(公告)号：EP3954681A1

公开(公告)日：2022-02-16

申请号：EP21193297.5

申请日：2017-01-13

Applicant: Bristol-Myers Squibb Company

Inventor： SMITH II, Leon M. ,  LADZIATA, Vladimir ,  DELUCCA, Indawati ,  PINTO, Donald, J. P. ,  ORWAT, Michael J. ,  DILGER, Andrew K. ,  PABBISETTY, Kumar Balashanmuga ,  YANG, Wu ,  SHAW, Scott A. ,  GLUNZ, Peter W. ,  PANDA, Manoranjan

IPC: C07D401/14 ,  A61K31/437 ,  A61K31/4427 ,  C07D231/12 ,  C07D231/18 ,  C07D231/54 ,  C07D401/12 ,  C07D413/12 ,  C07D471/04 ,  C07D471/12 ,  C07D513/04 ,  C07D213/64

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：EP3099687B1

公开(公告)日：2018-07-04

申请号：EP15705860.3

申请日：2015-01-30

Applicant: Bristol-Myers Squibb Company

Inventor： CORTE, James R. ,  DE LUCCA, Indawati ,  FANG, Tianan ,  YANG, Wu ,  WANG, Yufeng ,  DILGER, Andrew K. ,  PABBISETTY, Kumar Balashanmuga ,  EWING, William R. ,  ZHU, Yeheng ,  WEXLER, Ruth R. ,  PINTO, Donald J. P. ,  ORWAT, Michael J. ,  SMITH, Leon M. II

IPC: C07D471/08 ,  C07D487/08 ,  A61K31/529 ,  A61P7/00

CPC classification number: C07D471/08 ,  C07D403/06 ,  C07D403/14 ,  C07D471/18 ,  C07D487/08

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：EP3293186A1

公开(公告)日：2018-03-14

申请号：EP17189935.4

申请日：2015-07-29

Applicant: Bristol-Myers Squibb Company

Inventor： DILGER, Andrew K. ,  CORTE, James R. ,  DE LUCCA, Indawati ,  FANG, Tianan ,  YANG, Wu ,  WANG, Yufeng ,  PABBISETTY, Kumar Balashanmuga ,  EWING, William R. ,  ZHU, Yeheng ,  WEXLER, Ruth R. ,  PINTO, Donald J.P. ,  ORWAT, Michael J. ,  SMITH II, Leon M.

IPC: C07D471/18 ,  A61K31/4162 ,  A61P7/02

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.

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因子XIa抑制剂或FXIa和血浆激肽释放酶的双重抑制剂。 本发明还涉及包含这些化合物的药物组合物以及使用该组合物治疗血栓栓塞性和/或炎症性疾病的方法。

公开(公告)号：EP3089979B1

公开(公告)日：2017-10-18

申请号：EP15747721.7

申请日：2015-07-29

Applicant: Bristol-Myers Squibb Company

Inventor： DILGER, Andrew K. ,  CORTE, James R. ,  DE LUCCA, Indawati ,  FANG, Tianan ,  YANG, Wu ,  WANG, Yufeng ,  PABBISETTY, Kumar Balashanmuga ,  EWING, William R. ,  ZHU, Yeheng ,  WEXLER, Ruth R. ,  PINTO, Donald J.P. ,  ORWAT, Michael J. ,  SMITH II, Leon M.

IPC: C07D471/18 ,  A61K31/4162 ,  A61P7/02

CPC classification number: C07D471/18

公开(公告)号：EP2882734B1

公开(公告)日：2016-10-12

申请号：EP13747624.8

申请日：2013-08-02

Applicant: Bristol-Myers Squibb Company

Inventor： YANG, Wu ,  CORTE, James R. ,  GILLIGAN, Paul J. ,  PINTO, Donald J.P. Pinto ,  EWING, William R. ,  WANG, Yufeng

IPC: C07D401/04 ,  C07D471/08 ,  C07D487/18 ,  A61K31/439 ,  A61P7/00

CPC classification number: C07D487/08 ,  C07D401/04 ,  C07D471/08 ,  C07D487/18

公开(公告)号：EP2739625B1

公开(公告)日：2016-01-20

申请号：EP12766737.6

申请日：2012-08-06

Applicant: Bristol-Myers Squibb Company

Inventor： LAM, Patrick Y.S. ,  CLARK, Charles G. ,  CORTE, James R. ,  EWING, William R. ,  GILLIGAN, Paul J. ,  JEON, Yoon ,  YANG, Wu ,  SMITH, Leon, M., II. ,  WANG, Yufeng

IPC: C07D471/06 ,  C07D487/06 ,  A61K31/505 ,  A61K31/5365 ,  A61K31/4985 ,  A61P7/00 ,  C07D498/06

CPC classification number: C07D498/08 ,  C07D471/06 ,  C07D471/08 ,  C07D487/06 ,  C07D487/08 ,  C07D498/06

公开(公告)号：EP2739625A1

公开(公告)日：2014-06-11

申请号：EP12766737.6

申请日：2012-08-06

Applicant: Bristol-Myers Squibb Company

Inventor： LAM, Patrick Y.S. ,  CLARK, Charles G. ,  CORTE, James R. ,  EWING, William R. ,  GILLIGAN, Paul J. ,  JEON, Yoon ,  YANG, Wu ,  SMITH, Leon, M., II. ,  WANG, Yufeng

IPC: C07D471/06 ,  C07D487/06 ,  A61K31/505 ,  A61K31/5365 ,  A61K31/4985 ,  A61P7/00

CPC classification number: C07D498/08 ,  C07D471/06 ,  C07D471/08 ,  C07D487/06 ,  C07D487/08 ,  C07D498/06

Abstract: The present invention provides compounds of Formula (Ia): 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：EP3548468B1

公开(公告)日：2020-09-16

申请号：EP17811812.1

申请日：2017-11-29

Applicant: Bristol-Myers Squibb Company

Inventor： YANG, Wu ,  GLUNZ, Peter, W. ,  BHIDE, Rajeev, S. ,  THIYAGARAJAN, Kamalraj

IPC: C07D231/54 ,  A61K31/436 ,  C07D403/04 ,  C07D487/04 ,  C07D487/10 ,  C07D491/052 ,  C07D491/147

公开(公告)号：EP3099686B1

公开(公告)日：2020-03-11

申请号：EP15705428.9

申请日：2015-01-30

Applicant: Bristol-Myers Squibb Company

Inventor： CORTE, James R. ,  DE LUCCA, Indawati ,  FANG, Tianan ,  YANG, Wu ,  WANG, Yufeng ,  DILGER, Andrew K. ,  PABBISETTY, Kumar Balashanmuga ,  EWING, William R. ,  ZHU, Yeheng ,  WEXLER, Ruth R. ,  PINTO, Donald J. P. ,  ORWAT, Michael J. ,  SMITH II, Leon M.

IPC: C07D471/08 ,  C07D487/08 ,  A61K31/529 ,  A61P7/00

公开(公告)号：EP2880026B1

公开(公告)日：2017-02-22

申请号：EP13747625.5

申请日：2013-08-02

Applicant: Bristol-Myers Squibb Company

Inventor： YANG, Wu ,  CORTE, James, R. ,  GILLIGAN, Paul, J. ,  PINTO, Donald, J.P., Pinto ,  EWING, William, R. ,  DILGER, Andrew, K. ,  WANG, Yufeng ,  FANG, Tianan ,  PABBISETTY, Kumar, B. ,  SMITH II, Leon, M.

IPC: C07D401/04 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  A61K31/439 ,  A61P7/00

CPC classification number: C07D471/08 ,  C07C53/18 ,  C07D401/04 ,  C07D471/18 ,  C07D487/08 ,  C07D487/18 ,  C07H17/02

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