发明授权
US06900231B2 Aminopyridyl-substituted phenyl acetamides as protease inhibitors
有权
氨基吡啶基取代的苯基乙酰胺作为蛋白酶抑制剂
- 专利标题: Aminopyridyl-substituted phenyl acetamides as protease inhibitors
- 专利标题(中): 氨基吡啶基取代的苯基乙酰胺作为蛋白酶抑制剂
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申请号: US10262871申请日: 2002-10-03
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公开(公告)号: US06900231B2公开(公告)日: 2005-05-31
- 发明人: Wenxi Pan , Tianbao Lu , Thomas P. Markotan , Bruce E. Tomczuk
- 申请人: Wenxi Pan , Tianbao Lu , Thomas P. Markotan , Bruce E. Tomczuk
- 申请人地址: US PA Exton
- 专利权人: 3-Dimensional Pharmaceuticals, Inc.
- 当前专利权人: 3-Dimensional Pharmaceuticals, Inc.
- 当前专利权人地址: US PA Exton
- 代理机构: Woodcock Washburn LLP
- 主分类号: A61K31/155
- IPC分类号: A61K31/155 ; A61K31/165 ; A61K31/18 ; A61K31/255 ; A61K31/44 ; A61K45/00 ; A61L31/00 ; A61P7/02 ; A61P9/08 ; A61P9/10 ; A61P29/00 ; A61P43/00 ; C07C279/00 ; C07C279/04 ; C07C291/02 ; C07C309/67 ; C07C309/73 ; C07C311/13 ; C07C311/21 ; C07D213/73 ; C07D213/75 ; C07D213/64 ; C07D213/74
摘要:
Phenyl acetamide compounds are described, including compounds of or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.
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