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    Pyrazole-derivatives as factor Xa inhibitors
    1.
    发明申请
    Pyrazole-derivatives as factor Xa inhibitors 有权
    吡唑衍生物作为因子Xa抑制剂

    公开(公告)号：US20040204406A1

    公开(公告)日：2004-10-14

    申请号：US10744744

    申请日：2003-12-23

    申请人： AVENTIS PHARMA DEUTSCHLAND GMBH

    发明人： Marc Nazare ,  Volkmar Wehner ,  David W. Will ,  Hans Matter

    IPC分类号： A61K031/541 ,  A61K031/5377 ,  A61K031/496 ,  A61K031/454 ,  A61K031/415

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D417/14

    摘要： The present invention is directed to a compound of formula I, 1 in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.

    摘要翻译： 本发明涉及式I化合物，其中R 0; R 1; R 2; R 3; R 4; Q; V，G和M具有以下含义。 式I化合物是药理活性化合物。 它表现出强烈的抗血栓形成作用，并且适用于例如治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。 它是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以在其中存在因子Xa和/或因子VIIa的不希望的活性或对于 治疗或预防因素Xa和/或因子VIIa的抑制。 本发明还涉及制备式I化合物的方法和包含其的药物制剂。

    Indazole-derivatives as factor Xa inhibitors
    2.
    发明申请
    Indazole-derivatives as factor Xa inhibitors 有权
    吲唑衍生物作为因子Xa抑制剂

    公开(公告)号：US20040235824A1

    公开(公告)日：2004-11-25

    申请号：US10849088

    申请日：2004-05-19

    申请人： Aventis Pharma Deutschland GmbH

    发明人： Marc Nazare ,  Volkmar Wehner ,  Volker Laux ,  Matthias Urmann ,  Armin Bauer ,  Hans Matter

    IPC分类号： A61K031/55 ,  A61K031/541 ,  A61K031/5377 ,  A61K031/501

    CPC分类号： C07D413/14 ,  C07D401/12 ,  C07D401/14

    摘要： The present invention relates to a compound of the formula I 1 wherein J1, J2, R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

    摘要翻译： 本发明涉及式I化合物，其中J 1，J 2，R 0，R 1，R 2，Q，V，G和M如本文所定义。 式I的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心血管疾病如血栓栓塞性疾病或再狭窄。 它们是血液凝固酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可用于存在因子Xa和/或因子VIIa的不期望活性或用于治愈 或预防因子Xa和/或因子VIIa的抑制。 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。

    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use
    4.
    发明申请
    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：US20040034027A1

    公开(公告)日：2004-02-19

    申请号：US10634827

    申请日：2003-08-06

    申请人： Aventis Pharma Deutschland GmbH

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

    IPC分类号： A61K031/44 ,  A61K031/50

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

    摘要： Compounds of formula I, 1 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。