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。