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    • 9. 发明公开
    • 신규 아미디노 유도체 및 트롬빈 억제제로서의 그의 용도
    • 新型氨基酸衍生物及其作为抑制剂的使用
    • KR1020000022437A
    • 2000-04-25
    • KR1019980710870
    • 1997-06-26
    • 아스트라제네카 아베
    • 안톤쏜,토마스
    • C07C311/21C07C309/71C07D333/34A61K31/18
    • C07D333/34C07C309/73C07C311/21C07C311/29C07C323/60C07D233/84C07D261/16C07F9/5304
    • PURPOSE: Novel amidino derivatives are provided which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants. CONSTITUTION: Amino derivatives which exhibit competitive inhibitory activity towards thrombin are useful as anticoagulants and in the treatment or prophylaxis of thrombosis and hypercoagulability in blood and tissues of animals including man. The compounds are orally bio available and selective in inhibiting thrombin over other serine proteases. The method for treatment or prophylaxis consists in administration of a therapeutically effective amount of the compounds or a pharmaceutically acceptable salt thereof, to a person suffering from, or susceptible to such a condition.
    • 目的:提供新的脒基衍生物,其可用作胰蛋白酶样蛋白酶(例如凝血酶)的竞争性抑制剂,特别是用于治疗需要凝血酶抑制(例如血栓形成)或作为抗凝剂的条件。 构成:对凝血酶具有竞争性抑制活性的氨基衍生物可用作抗凝剂,也可用于治疗或预防包括人在内的动物的血液和组织中的血栓形成和高凝状态。 这些化合物是口服生物获得的,并且与其它丝氨酸蛋白酶相比抑制凝血酶具有选择性。 用于治疗或预防的方法包括向患有或易患这种病症的人施用治疗有效量的化合物或其药学上可接受的盐。