发明授权
- 专利标题: Platelet aggregation inhibitors
- 专利标题(中): 血小板聚集抑制剂
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申请号: US462698申请日: 1995-06-05
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公开(公告)号: US5686567A公开(公告)日: 1997-11-11
- 发明人: Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
- 申请人: Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
- 申请人地址: CA San Francisco
- 专利权人: COR Therapeutics, Inc.
- 当前专利权人: COR Therapeutics, Inc.
- 当前专利权人地址: CA San Francisco
- 主分类号: A61K38/00
- IPC分类号: A61K38/00 ; A61K38/12 ; A61K38/17 ; A61K38/57 ; C07K14/46 ; C07K14/75 ; C07K14/755 ; C07K14/78 ; C07K5/00 ; C07K7/00
摘要:
An assay for screening snake venom for the presence or absence of platelet aggregation inhibitors (PAIs) based on specific receptor binding is described. Using this assay, the identification and characterization of PAIs in a wide range of snake venom samples was accomplished. The isolated and purified PAI from several of these active snake venoms is described and characterized. In addition, PAIs lacking the Arg-Gly-Asp (RGD) adhesion sequence but containing K*-(G/Sar)-D wherein K is a modified lysyl residue of the formula R.sup.1.sub.2 N(CH.sub.2).sub.4 CHNHCO-- wherein each R.sup.1 is independently H, alkyl(1-6C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3 is H, alkyl(1-6C), phenyl or benzyl, or R.sup.2 --C.dbd.NR.sup.3 is a radical selected from the group consisting of: ##STR1## where m is an integer of 2-3, and each R.sup.5 is independently H or alkyl(1-6C); and wherein one or two (CH.sub.2) may be replaced by O or S provided said O or S is not adjacent to another heteroatom are prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
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