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    • 8. 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。
    • 9. 发明授权
    • Indole derivatives as inhibitors or factor Xa
    • 吲哚衍生物作为抑制剂或因子Xa
    • US06337344B1
    • 2002-01-08
    • US09582344
    • 2000-08-14
    • Elisabeth DefossaUwe HeineltOtmar KlinglerGerhard ZollerFahad A. Al-ObeidiArmin WalserPeter WildgooseHans Matter
    • Elisabeth DefossaUwe HeineltOtmar KlinglerGerhard ZollerFahad A. Al-ObeidiArmin WalserPeter WildgooseHans Matter
    • A61K3144
    • C07D401/06C07D209/42C07D401/12C07D403/10C07D471/04
    • The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (I) in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (I) together with pharmaceutically acceptable carrier substances and/or auxiliary substances.
    • 本发明涉及抑制血液凝固蛋白质,更具体地说,涉及式(I)的吲哚衍生物,其中R1a,R1b,R1c R1d,R2,R3,R4和A如权利要求中所示定义。 式(I)的化合物是凝血酶因子Xa的抑制剂。 本发明还涉及制备式(I)化合物的方法,抑制因子Xa活性和抑制血液凝固的方法,使用式(I)化合物治疗和预防可以 通过抑制诸如血栓栓塞性疾病的因子Xa活性而被治愈或预防,以及式(I)化合物在制备用于这些疾病的药物中的用途。 本发明还涉及包含与惰性载体混合或以其它方式结合的式(I)化合物的组合物,特别是含有式(I)化合物与药学上可接受的载体物质和/或辅助物质的药物组合物。