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    • 2. 发明申请
    • PYRROLE DERIVATIVES AS P2Y12 ANTAGONISTS
    • PYRROLE DERIVATIVES作为P2Y12 ANTAGONISTS
    • WO2008155022A1
    • 2008-12-24
    • PCT/EP2008/004459
    • 2008-06-04
    • SANOFI-AVENTISKLINGLER, OtmarCZECH, JoergCZECHTIZKY, WerngardWEISS, TiloJUST, Melitta
    • KLINGLER, OtmarCZECH, JoergCZECHTIZKY, WerngardWEISS, TiloJUST, Melitta
    • C07D401/06C07D403/06C07D403/14C07D405/14
    • C07D401/06C07D403/06C07D403/14C07D405/14
    • 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; A; B, D and E have the meanings indicated 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.
    • 本发明涉及式(I)化合物,其中R 1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; 一个; B,D和E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,因此表现出抗血栓形成的作用, 用于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。