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10 条记录 (耗时 0.03 秒)

    Guanidine and amidine derivatives as factor Xa inhibitors
    1.
    发明授权
    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：US07435747B2

    公开(公告)日：2008-10-14

    申请号：US10886312

    申请日：2004-07-07

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

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

    IPC分类号： A61K31/445 ,  C07D211/26

    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。

    Guanidine and amidine derivatives as factor Xa inhibitors
    5.
    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。

    Linear analogs of alpha-msh fragments
    10.
    发明授权
    Linear analogs of alpha-msh fragments 失效
    α-msh片段的线性类似物

    公开(公告)号：US5714576A

    公开(公告)日：1998-02-03

    申请号：US826676

    申请日：1997-04-07

    申请人： Victor J. Hruby ,  Mac E. Hadley ,  Fahad Al-Obeidi

    发明人： Victor J. Hruby ,  Mac E. Hadley ,  Fahad Al-Obeidi

    IPC分类号： A61K38/00 ,  C07K14/685 ,  C07K5/00 ,  C07K7/00

    CPC分类号： C07K14/685 ,  A61K38/00

    摘要： Linear and Cyclic Alpha-MSH fragment analogues of Ac-Nle.sup.4 -Glu.sup.5 -His.sup.6 -D-Phe.sup.7 -Arg.sup.8 -Try.sup.9 -Gly.sup.10 -NH.sub.2. The method of stimulating melanocytes by the transdermal application of these biologically-active analogues and compositions comprising these analogues for use in the method are disclosed.

    摘要翻译： Ac-Nle4-Glu5-His6-D-Phe7-Arg8-Try9-Gly10-NH2的线性和环状α-MSH片段类似物。 公开了通过透皮施用这些生物活性类似物和包含这些类似物的组合物刺激黑素细胞的方法用于该方法。