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77 条记录 (耗时 0.045 秒)

    Pyrazole-derivatives as factor Xa inhibitors
    61.
    发明授权
    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：US07910606B2

    公开(公告)日：2011-03-22

    申请号：US12562276

    申请日：2009-09-18

    申请人： Marc Nazare ,  Volkmar Wehner ,  David William Will ,  Hans Matter

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

    IPC分类号： A61K31/454 ,  A61K31/415 ,  A61K31/4245 ,  C07D413/02 ,  C07D419/02 ,  C07D401/04

    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, 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; R1; R2; R3; R4; 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。

    Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use
    64.
    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：US07153876B2

    公开(公告)日：2006-12-26

    申请号：US10634827

    申请日：2003-08-06

    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： C07D213/75 ,  A61K31/44 ,  A61P7/02 ,  A61P9/10

    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学活性化合物，其表现出强烈的 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。

    Guanidine and amidine derivatives as factor Xa inhibitors
    65.
    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。

    Cyclic peptides, their preparation and their use as inhibitors of the platelet adhesion
    67.
    发明授权
    Cyclic peptides, their preparation and their use as inhibitors of the platelet adhesion 有权
    循环肽，它们的制备及其作为血小板粘附抑制剂的用途

    公开(公告)号：US09073975B2

    公开(公告)日：2015-07-07

    申请号：US13818444

    申请日：2011-07-27

    申请人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    发明人： Otmar Klingler ,  Horst Blum ,  Andreas Lindenschmidt ,  Hans Matter

    IPC分类号： C07K7/64 ,  C07K7/06 ,  C07K7/56 ,  A61K38/00

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/06 ,  C07K7/56

    摘要： The present invention relates to compounds of the Formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb), and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式（I）化合物，其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17，R18 X1，X2，X3和X4具有权利要求中所示的含义，并且它们是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间的相互作用的可逆抑制剂，并且适合于例如治疗和预防动脉粥样硬化血栓性疾病 。 本发明还涉及制备式（I）化合物，其用途，特别是作为药物中的活性成分的方法，以及包含它们的药物组合物。

    Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals
    69.
    发明授权
    Cyclic azaindole-3-carboxamides, their preparation and their use as pharmaceuticals 有权
    环状氮杂吲哚-3-甲酰胺，它们的制备及其作为药物的用途

    公开(公告)号：US08580813B2

    公开(公告)日：2013-11-12

    申请号：US12845324

    申请日：2010-07-28

    申请人： Henning Steinhagen ,  Bodo Scheiper ,  Hans Matter ,  Gary Mccort

    发明人： Henning Steinhagen ,  Bodo Scheiper ,  Hans Matter ,  Gary Mccort

    IPC分类号： A61K31/44

    CPC分类号： C07D471/04

    摘要： The present invention relates to cyclic azaindole-3-carboxamides of the formula I, wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

    摘要翻译： 本发明涉及式I的环状氮杂吲哚-3-甲酰胺，其中A，R，R10，R20，R30，R40，Y1，Y2，Y3，Y4，n，p和q具有权利要求中所示的含义， 这是有价值的药物活性化合物。 具体地说，它们抑制酶肾素并调节肾素 - 血管紧张素系统的活性，并且可用于治疗例如高血压等疾病。 本发明还涉及制备式I化合物的方法，其用途和包含它们的药物组合物。