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    Heterocyclic pyrazole-carboxamidesas P2Y12 antagonists
    1.
    发明授权
    Heterocyclic pyrazole-carboxamidesas P2Y12 antagonists 有权
    杂环吡唑 - 甲酰胺P2Y12拮抗剂

    公开(公告)号：US08426420B2

    公开(公告)日：2013-04-23

    申请号：US12817873

    申请日：2010-06-17

    申请人： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

    发明人： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

    IPC分类号： A61K31/496 ,  A61K31/454 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    CPC分类号： C07D403/14

    摘要： The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; V; G和M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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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。

    HETEROCYCLIC PYRAZOLE-CARBOXAMIDESAS P2Y12 ANTAGONISTS
    2.
    发明申请
    HETEROCYCLIC PYRAZOLE-CARBOXAMIDESAS P2Y12 ANTAGONISTS 有权
    杂环磷杂环戊二烯P2Y12拮抗剂

    公开(公告)号：US20110021537A1

    公开(公告)日：2011-01-27

    申请号：US12817873

    申请日：2010-06-17

    申请人： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

    发明人： Marc Nazaré ,  Gernot Zech ,  Melitta Just ,  Tilo Weiss ,  Gerhard Hessler ,  Markus Kohlmann

    IPC分类号： A61K31/497 ,  C07D403/14 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P7/02

    CPC分类号： C07D403/14

    摘要： The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; V; G和M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。 它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。 它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件 。 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。