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INHIBITEURS DE PROTEASE A BASE DE PYRAZINONE
专利权人:
3-DIMENSIONAL PHARMACEUTICALS; INC.
发明人:
LU, TIANBAO,TOMCZUK, BRUCE E.,MARKOTAN, THOMAS P.
申请号:
CA2334679
公开号:
CA2334679C
申请日:
1999.06.11
申请国别(地区):
CA
年份:
2012
代理人:
摘要:
Pyrazinone compounds are described, including compounds of Formula (I),wherein X is O, NR11 or CH=N, R3-R11, Ra, Rb, Rc, W, m and n are set forth inthe specification, as well as hydrates, solvates or pharmaceuticallyacceptable salts thereof. The compounds of the invention are potent inhibitorsof proteases, especially trypsin-like serine proteases, such as chymotrypsin,trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibitantithrombotic activity via direct, selective inhibition of thrombin.Compositions for inhibiting loss of blood platelets, inhibiting formation ofblood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombusformation, and inhibiting embolus formation are described. Other uses ofcompounds of the invention are as anticoagulants either embedded in orphysically linked to materials used in the manufacture of devices used inblood collection, blood circulation, and blood storage, such as catheters,blood dialysis machines, blood collection syringes and tubes, blood lines andstents. Additionally, the compounds can be detectably labeled and employed forin vivo imaging of thrombi.
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中国工程科技知识中心
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http://www.ckcest.cn/home/

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