发明授权
- 专利标题: Thromboresistant materials incorporating pyrazinone protease inhibitors
- 专利标题(中): 结合吡嗪酮蛋白酶抑制剂的抗栓材料
-
申请号: US09773730申请日: 2001-02-02
-
公开(公告)号: US06514978B2公开(公告)日: 2003-02-04
- 发明人: Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan
- 申请人: Tianbao Lu , Bruce E. Tomczuk , Thomas P. Markotan
- 主分类号: A61K314965
- IPC分类号: A61K314965
摘要:
Thromboresistant materials are described which incorporate pyrazinone compounds of the Formula I: wherein X is O, NR11 or CH═N, R3-R11, Ra, Rb, Rc, W, m, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. 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.
公开/授权文献
信息查询