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1. 发明授权

US5786333A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5786333A
公开(公告)日：1998-07-28
申请号：US484414
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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.
摘要翻译：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，（1-6C）烷基，苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（1- 6C），R3是H，（1-6C）烷基，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R 5独立地为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。

2. 发明授权

US5770564A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5770564A
公开(公告)日：1998-06-23
申请号：US465178
申请日：1995-06-05
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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* 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(1-6 C) or at most one R.sup.1 is R.sup.2 --C.dbd.NR.sup.3 wherein R.sup.2 is H, alkyl(1-6 C), phenyl or benzyl, or is NR.sup.4.sub.2 in which each R.sup.4 is independently H or alkyl(1-6 C) and R.sup.3 is H, alkyl(1-6 C), 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(1-6 C); 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.
摘要翻译：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- 6 C），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，以及每个R 5独立地为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。

3. 发明授权

US5807825A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5807825A
公开(公告)日：1998-09-15
申请号：US482278
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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 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.
摘要翻译：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 ），R为H，烷基（1-6C），苯基或苄基，或R2-C = NR3为选自下列的基团：R5独立地为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。

4. 发明授权

US5686571A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5686571A
公开(公告)日：1997-11-11
申请号：US484779
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A16K38/00 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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.sup.* -(G/Sar)-D wherein K.sup.* 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.
摘要翻译：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 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），R3是H，（1-6C）烷基，苯基或苄基，或R2-C = NR3是选自下组的基团：其中m是2-3的整数，并且每个R 5 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。

5. 发明授权

US5935926A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5935926A
公开(公告)日：1999-08-10
申请号：US482275
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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 formulaR.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 heteroatomare prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
摘要翻译：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。

6. 发明授权

US5759999A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5759999A
公开(公告)日：1998-06-02
申请号：US482280
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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.
摘要翻译：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是选自下组的基团：A 5 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。

7. 发明授权

US5968902A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5968902A
公开(公告)日：1999-10-19
申请号：US482263
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
摘要： The isolated and purified PAI from several 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 formulaR.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 heteroatomare prepared and shown to specifically inhibit the binding of fibrinogen or von Willebrand Factor to GP IIb-IIIa.
摘要翻译：描述和表征了来自几种活性蛇毒液的分离和纯化的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R 12 N（CH 2）4 CHNHCO-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，（1-6C）烷基，苯基或苄基，或是NR42，其中每个R4独立地是H或烷基（ 1-6C），R3为H，（1-6C）烷基，苯基或苄基，或R2-C = NR3为选自下组的基团：其中m为2-3的整数，每个R 5为独立地是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。

8. 发明授权

US5756451A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5756451A
公开(公告)日：1998-05-26
申请号：US472808
申请日：1995-06-07
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , A61K38/02 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
摘要： This invention relates to a group of peptides which are, or are related to, platelet aggregation inhibitors isolated and purified from various snake venoms. The instant platelet aggregation inhibitors inhibit (a) binding of Fg or vWF to GPIIb-IIIa more than (b) binding of vitronectin to vitronectin receptor or fibronectin to fibronectin receptor. The peptides are useful as therapeutic agents for the treatment of, and prevention of, platelet-associated ischemic disorders.
摘要翻译：本发明涉及与各种蛇毒分离和纯化的血小板聚集抑制剂有关或与其相关的一组肽。瞬时血小板聚集抑制剂抑制（a）超过（b）玻连蛋白与玻连蛋白受体或纤连蛋白与纤连蛋白受体结合的Fg或vWF与GPIIb-IIIa的结合。肽可用作治疗和预防血小板相关缺血性疾病的治疗剂。

9. 发明授权

US5686570A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5686570A
公开(公告)日：1997-11-11
申请号：US463765
申请日：1995-06-05
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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.
摘要翻译：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。

10. 发明授权

US5686569A Platelet aggregation inhibitors 失效
标题翻译：血小板聚集抑制剂
公开(公告)号：US5686569A
公开(公告)日：1997-11-11
申请号：US463870
申请日：1995-06-05
申请人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
发明人： Robert M. Scarborough , David Lawrence Wolf , Israel F. Charo
IPC分类号： A61K38/00 , A61K38/12 , A61K38/17 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78 , C07K5/00 , C07K7/00
CPC分类号： A61K38/12 , A61K38/1703 , A61K38/57 , C07K14/46 , C07K14/75 , C07K14/755 , C07K14/78
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 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.
摘要翻译：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。

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