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164 条记录 (耗时 0.071 秒)

    Platelet ADP receptor inhibitors
    44.
    发明授权
    Platelet ADP receptor inhibitors 有权
    血小板ADP受体抑制剂

    公开(公告)号：US06689786B2

    公开(公告)日：2004-02-10

    申请号：US10350883

    申请日：2003-01-23

    申请人： Robert M. Scarborough ,  Wolin Huang

    发明人： Robert M. Scarborough ,  Wolin Huang

    IPC分类号： C07D41712

    CPC分类号： C07D239/22 ,  C07D239/48 ,  C07D239/50 ,  C07D333/34 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D495/04

    摘要： Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

    摘要翻译： 式（I）至（VI）的新型化合物，其更具体地包括作为有效的血小板ADP受体抑制剂的磺酰脲衍生物，磺酰基硫脲衍生物，磺酰基胍衍生物，磺酰基氰胍基衍生物，硫代酰基磺酰胺衍生物和酰基磺酰胺衍生物。 这些衍生物可用于各种药物组合物中，并且对于预防和/或治疗心血管疾病，特别是与血栓形成有关的疾病特别有效。 本发明还涉及一种用于预防或治疗哺乳动物血栓形成的方法，包括施用治疗有效量的式（I） - （VI）化合物或其药学上可接受的盐的步骤。

    Oxindole inhibitors of factor Xa
    45.
    发明授权
    Oxindole inhibitors of factor Xa 失效
    因子Xa的羟吲哚抑制剂

    公开(公告)号：US06548517B2

    公开(公告)日：2003-04-15

    申请号：US09816782

    申请日：2001-03-26

    申请人： Charles K. Marlowe ,  Kim A. Kane-Maguire ,  Bing-Yan Zhu ,  Robert M. Scarborough

    发明人： Charles K. Marlowe ,  Kim A. Kane-Maguire ,  Bing-Yan Zhu ,  Robert M. Scarborough

    IPC分类号： A61K31445

    CPC分类号： C07D401/12

    摘要： Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa is described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

    摘要翻译： 描述了新颖的式I化合物：包括其具有抗哺乳动物因子Xa活性的药学上可接受的异构体，盐，水合物，溶剂合物和前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物可用于体外或体内用于预防或治疗特征在于不希望的血栓形成的哺乳动物的状况。

    Selective factor Xa inhibitors
    48.
    发明授权
    Selective factor Xa inhibitors 失效
    选择因子Xa抑制剂

    公开(公告)号：US06369080B2

    公开(公告)日：2002-04-09

    申请号：US08948664

    申请日：1997-10-10

    申请人： Bing-Yan Zhu ,  Robert M. Scarborough

    发明人： Bing-Yan Zhu ,  Robert M. Scarborough

    IPC分类号： C07D41706

    CPC分类号： C07D213/76 ,  C07D413/12 ,  C07D417/12

    摘要： Novel compounds of formula I: including its pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

    摘要翻译： 描述了新颖的式I化合物：包括其药学上可接受的异构体，盐，水合物，溶剂合物和具有抗哺乳动物因子Xa活性的前药衍生物。 还描述了含有这些化合物的组合物。 化合物和组合物可用于体外或体内用于预防或治疗特征在于不希望的血栓形成的哺乳动物的状况。

    Platelet aggregation inhibitors
    50.
    发明授权
    Platelet aggregation inhibitors 失效
    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。