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    • 9. 发明授权
    • Factor VIIa inhibitors
    • 因子VIIa抑制剂
    • US06500803B1
    • 2002-12-31
    • US09588651
    • 2000-06-07
    • Otmar KlinglerManfred SchudokGerhard ZollerUwe HeineltElisabeth DefossaHans MatterPavel Safar
    • Otmar KlinglerManfred SchudokGerhard ZollerUwe HeineltElisabeth DefossaHans MatterPavel Safar
    • A61K3805
    • C07K5/06086A61K38/00
    • The present invention relates to compounds of formula I, in which R1, R2, R91, R92, R93, R94, R95, R96, R97, r, s, and t have the meanings indicated in the claims. Compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    • 本发明涉及式Ⅰ化合物,其中R1,R2,R91,R92,R93,R94,R95,R96,R97,r,s和t具有权利要求中所示的含义。 式I化合物是有价值的药理活性化合物。 它们具有强烈的抗血栓形成作用,并且适用于例如治疗和预防血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子VIIa的可逆抑制剂,并且通常可以在其中存在不需要的因子VIIa活性的条件下或用于治疗或预防预期因子VIIa的抑制的病症。 本发明还涉及制备式I化合物的方法,其用途,特别是作为药物中的活性成分,以及包含它们的药物制剂。