公开(公告)号：WO2013022814A1

公开(公告)日：2013-02-14

申请号：PCT/US2012/049698

申请日：2012-08-06

Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  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

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.

Abstract translation: 本发明提供式（Ia）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和使用其制备血栓栓塞和/或炎症性疾病的方法。

公开(公告)号：WO2005009384A3

公开(公告)日：2005-12-08

申请号：PCT/US2004023662

申请日：2004-07-21

Applicant: IMCLONE SYSTEMS INC ,  HADARI YARON ,  SMITH LEON M II

Inventor： HADARI YARON ,  SMITH LEON M II

IPC: A61K20060101 ,  A61K31/55 ,  A61P35/00 ,  C07D498/00 ,  C07D513/00

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: The invention encompasses compounds that inhibit, modulate, or regulate kinases, compositions that contain kinase inhibiting compounds, and methods of treating kinase-dependent diseases and conditions in subjects in need of such treatment. Also, the invention encompasses methods of making compounds that inhibit, modulate or regulate kinases.

Abstract translation: 本发明包括抑制，调节或调节激酶的化合物，含有激酶抑制化合物的组合物，以及在需要这种治疗的受试者中治疗激酶依赖性疾病和病症的方法。 此外，本发明包括制备抑制，调节或调节激酶的化合物的方法。

公开(公告)号：WO2005009384A2

公开(公告)日：2005-02-03

申请号：PCT/US2004/023662

申请日：2004-07-21

Applicant: IMCLONE SYSTEMS INCORPORATED ,  HADARI, Yaron ,  SMITH, Leon, M., II

Inventor： HADARI, Yaron ,  SMITH, Leon, M., II

IPC: A61K

CPC classification number: C07D498/04 ,  C07D513/04

Abstract: The invention encompasses compounds that inhibit, modulate, or regulate kinases, compositions that contain kinase inhibiting compounds, and methods of treating kinase-dependent diseases and conditions in subjects in need of such treatment. Also, the invention encompasses methods of making compounds that inhibit, modulate or regulate kinases.

Abstract translation: 本发明包括抑制，调节或调节激酶的化合物，含有激酶抑制性化合物的组合物，以及治疗需要这种治疗的受试者的激酶依赖性疾病和病症的方法。 而且，本发明包括制备抑制，调节或调节激酶的化合物的方法。