Alkenyl and alkynyl compounds as inhibitors of factor Xa
    5.
    发明授权
    Alkenyl and alkynyl compounds as inhibitors of factor Xa 失效
    烯基和炔基化合物作为因子Xa的抑制剂

    公开(公告)号:US06545054B1

    公开(公告)日:2003-04-08

    申请号:US09501370

    申请日:2000-02-11

    IPC分类号: A61K3118

    摘要: Alkenyl and alkynyl compounds as potent and highly selective inhibitors of factor Xa isolated or assembled in the prothrombinase complex and compositions containing such alkenyl and alkynyl compounds are described. Such compounds show selectivity for factor Xa over other proteases of the coagulation (e.g., thrombin, fvIIa, flXa) or the fibrinolytic cascades (e.g., plasminogen activators, plasmin). Methods for using such alkenyl and alkynyl compounds as diagnostic or therapeutic agents for prevention or treatment of a condition in a mammal characterized by undesired coagulation disorders, such as thrombosis, are also described.

    摘要翻译: 描述了作为在凝血酶原酶复合物中分离或组装的因子Xa的有效和高选择性抑制剂的烯基和炔基化合物以及含有这种烯基和炔基化合物的组合物。 这些化合物显示对凝血因子Xa(例如凝血酶,fvIIa,flXa)或纤维蛋白溶解级联(例如纤溶酶原激活剂,纤溶酶)的其它蛋白酶的选择性。 还描述了使用这种烯基和炔基化合物作为诊断或治疗剂来预防或治疗特征在于不期望的凝血障碍如血栓形成的哺乳动物状况的方法。