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    • 86. 发明授权
    • Platelet aggregation inhibitors
    • 血小板聚集抑制剂
    • US5686570A
    • 1997-11-11
    • US463765
    • 1995-06-05
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • A61K38/00A61K38/12A61K38/17A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78C07K5/00C07K7/00
    • A61K38/12A61K38/1703A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78
    • 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.
    • 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂(PAI)的测定法。 使用该测定,完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 另外,缺乏Arg-Gly-Asp(RGD)粘附序列但含有K * - (G / Sar)-D的PAI,其中K *是式R 12 N(CH 2)4 CHNHCO-的修饰的赖氨酰残基,其中每个R 1独立地为H ,烷基(1-6C)或至多一个R1是R2-C = NR3,其中R2是H,烷基(1-6C),苯基或苄基,或是NR42,其中每个R4独立地是H或烷基(1-6C )和R 3是H,烷基(1-6C),苯基或苄基,或者R 2 -C = NR 3是选自下列的基团:依赖性地是H或烷基(1-6C); 并且其中一个或两个(CH 2)可以被O或S替代,条件是所述O或S不与另一个杂原子相邻,并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。
    • 87. 发明授权
    • Platelet aggregation inhibitors
    • 血小板聚集抑制剂
    • US5686569A
    • 1997-11-11
    • US463870
    • 1995-06-05
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • A61K38/00A61K38/12A61K38/17A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78C07K5/00C07K7/00
    • A61K38/12A61K38/1703A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78
    • 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 in which each R.sup.4 is independently H or alkyl(1-6C) and R.sup.3.spsp.2 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.
    • 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂(PAI)的测定法。 使用该测定,完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 另外,缺少Arg-Gly-Asp(RGD)粘附序列但含有K * - (G / Sar)-D的PAI,其中K *是式R12N(CH2)4CHNHCO-的修饰的赖氨酰残基,其中每个R 1是 独立地是H,烷基(1-6C)或至多一个R1是R2-C = NR3,其中R2是H,烷基(1-6C),苯基或苄基,或是NR4,其中每个R4独立地是H或烷基(1 -6C),R32是H,烷基(1-6C),苯基或苄基,或R2-C = NR3是选自以下的基团:其中m是2-3的整数,并且每个 R5独立地是H或(1-6C)烷基; 并且其中一个或两个(CH 2)可以被O或S替代,条件是所述O或S不与另一个杂原子相邻,并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。
    • 88. 发明授权
    • Platelet aggregation inhibitors
    • 血小板聚集抑制剂
    • US5686567A
    • 1997-11-11
    • US462698
    • 1995-06-05
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • Robert M. ScarboroughDavid Lawrence WolfIsrael F. Charo
    • A61K38/00A61K38/12A61K38/17A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78C07K5/00C07K7/00
    • A61K38/12A61K38/1703A61K38/57C07K14/46C07K14/75C07K14/755C07K14/78
    • 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.
    • 描述了基于特异性受体结合筛选蛇毒用于存在或不存在血小板聚集抑制剂(PAI)的测定法。 使用该测定,完成了广泛的蛇毒样品中PAIs的鉴定和表征。 描述和表征了来自这些活性蛇毒中的几种的分离和纯化的PAI。 此外,缺少Arg-Gly-Asp(RGD)粘附序列但含有K * - (G / Sar)-D的PAI,其中K是式​​R 12 N(CH 2)4 CHNHCO-的修饰的赖氨酰残基,其中每个R 1独立地为H, 烷基(1-6C)或至多一个R1是R2-C = NR3,其中R2是H,烷基(1-6C),苯基或苄基,或是NR42,其中每个R4独立地是H或烷基(1-6C) 并且R 3是H,烷基(1-6C),苯基或苄基,或者R 2 -C = NR 3是选自以下的基团:其中m是2-3的整数,并且每个R 5独立地是 H或烷基(1-6C); 并且其中一个或两个(CH 2)可以被O或S替代,条件是所述O或S不与另一个杂原子相邻,并且显示出特异性抑制纤维蛋白原或血管性血友病因子与GP IIb-IIIa的结合。