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40 条记录 (耗时 0.023 秒)

    Guanidine and amidine derivatives as factor Xa inhibitors
    1.
    发明申请
    Guanidine and amidine derivatives as factor Xa inhibitors 失效
    胍和脒衍生物作为因子Xa抑制剂

    公开(公告)号：US20050143419A1

    公开(公告)日：2005-06-30

    申请号：US10886312

    申请日：2004-07-07

    申请人： Anuschirwan Peyman ,  David Will ,  Uwe Gerlach ,  Marc Nazare ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    发明人： Anuschirwan Peyman ,  David Will ,  Uwe Gerlach ,  Marc Nazare ,  Gerhard Zoller ,  Hans-Peter Nestler ,  Hans Matter ,  Fahad Al-Obeidi

    IPC分类号： A61K31/445 ,  A61K31/4545 ,  A61P7/02 ,  A61P43/00 ,  C07D211/26 ,  C07D211/34 ,  C07D401/12 ,  C07D413/02 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454

    CPC分类号： C07D401/12 ,  C07D211/26 ,  C07D211/34

    摘要： The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V have the meanings indicated in the claims. 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R 0是 Q; X; Q'，D，R 10和V具有权利要求中所示的含义。 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。 本发明还涉及式I化合物的制备方法，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。

    Sulfonamide-substituted fused 7-membered ring compounds, their use as a medicament, and pharmaceutical preparations comprising them
    7.
    发明授权
    Sulfonamide-substituted fused 7-membered ring compounds, their use as a medicament, and pharmaceutical preparations comprising them 失效
    磺酰胺取代的稠合的7-元环化合物，它们作为药物的用途，以及包含它们的药物制剂

    公开(公告)号：US06908947B2

    公开(公告)日：2005-06-21

    申请号：US09983670

    申请日：2001-10-25

    申请人： Joachim Brendel ,  Hans Jochen Lang ,  Uwe Gerlach

    发明人： Joachim Brendel ,  Hans Jochen Lang ,  Uwe Gerlach

    IPC分类号： A61P9/00 ,  C07C311/07 ,  C07D313/08 ,  A61K31/16 ,  A61K31/18 ,  C07C303/00 ,  C07C381/00

    CPC分类号： C07D313/08 ,  C07C311/07 ,  C07C2602/12

    摘要： The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.

    摘要翻译： 本发明涉及式Ⅰ化合物，其中X1，X2，X3，X4，Y1，Y2，Y3，Y4，R（3），R（4）和R（5） 他们的准备和使用，特别是在药物。 这些化合物影响由环磷酸腺苷（cAMP）打开的钾通道或IκS通道，并且非常适合作为药物活性化合物，例如用于预防和治疗心血管疾病，特别是心律失常， 用于治疗胃肠道区域的溃疡或用于治疗腹泻病症。