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77 条记录 (耗时 0.046 秒)

    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them
    51.
    发明授权
    Malonic acid derivatives, processes for their preparation, for their use and pharmaceutical compositions containing them 有权
    丙二酸衍生物，其制备方法，用途及含有它们的药物组合物

    公开(公告)号：US06395737B1

    公开(公告)日：2002-05-28

    申请号：US09473053

    申请日：1999-12-28

    申请人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    发明人： Elisabeth Defossa ,  Uwe Heinelt ,  Otmar Klingler ,  Gerhard Zoller ,  Hans Matter ,  Fahad A. Al-Obeidi ,  Armin Walser ,  Peter Wildgoose

    IPC分类号： A61K31165

    CPC分类号： C07C257/18 ,  C07C279/14

    摘要： New compounds for the inhibition of blood clotting proteins, and more particularly, to malonic acid derivatives of the formula I, wherein R(1), R(2), R(3), R(4), R(5), and R(6) have the meanings indicated in the claims. The compounds of formula I are inhibitors of the blood clotting enzyme factor Xa. Processes for the preparation of the compounds of formula I, methods of inhibiting factor Xa activity and of inhibiting blood clotting, use of the compounds of formula I in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and use of the compounds of formula I in the preparation of medicaments to be applied in such diseases. 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 auxiliary substances.

    摘要翻译： 用于抑制血液凝固蛋白质的新化合物，更具体地，涉及式I的丙二酸衍生物，其中R（1），R（2），R（3），R（4），R（5）和 R（6）具有权利要求中所示的含义。 式I化合物是凝血酶因子Xa的抑制剂。 用于制备式I化合物的方法，抑制因子Xa活性和抑制血液凝固的方法，式I化合物在治疗和预防疾病中的用途，其可以通过抑制因子Xa来治疗或预防 活性如血栓栓塞性疾病，以及式I化合物在制备用于这些疾病的药物中的应用。 含有式I化合物的组合物与惰性载体混合或以其它方式结合，特别是含有式I化合物的药物组合物以及药学上可接受的载体物质和辅助物质。

    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use
    59.
    发明授权
    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权
    丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途

    公开(公告)号：US06645992B2

    公开(公告)日：2003-11-11

    申请号：US09965790

    申请日：2001-10-01

    申请人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    发明人： Manfred Schudok ,  Otmar Klingler ,  Hans-Peter Nestler ,  Hans Matter ,  Herman Schreuder

    IPC分类号： C07D25718

    CPC分类号： A61K31/27 ,  A61K31/167 ,  A61K31/225 ,  C07C257/18 ,  C07C257/20

    摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating thromboembolic diseases and 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 which an inhibition of factor VIIa is intended. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理活性化合物，其表现出很强的抗血栓形成作用，并且适用于例如 治疗血栓栓塞性疾病和再狭窄。 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的活性或用于治疗或预防因子VIIa的抑制的条件下使用。 还公开了制备式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。