发明申请
US20110028446A1 ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
有权
芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂
- 专利标题： ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
- 专利标题（中）： 芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂
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申请号： US12900542申请日： 2010-10-08
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公开(公告)号： US20110028446A1公开(公告)日： 2011-02-03
- 发明人: Donald J.P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
- 申请人： Donald J.P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith, II
- 专利权人： Bristol-Myers Squibb Company
- 当前专利权人： Bristol-Myers Squibb Company
- 主分类号： A61K31/4178
- IPC分类号： A61K31/4178 ; C07D403/10 ; C07D401/14 ; C07D403/14 ; C07D233/68 ; C07D409/12 ; C07D403/12 ; C07D401/10 ; C07D413/14 ; C07D417/14 ; C07D487/08 ; A61K31/4439 ; A61K31/4174 ; A61K31/4709 ; A61K31/5377 ; A61K31/497 ; A61P7/00 ; A61P9/00 ; A61P9/10
摘要：
The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that 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.