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1. 发明申请

WO2009007015A1 MALONAMIDE DERIVATIVES WITH ANTITHROMBOTIC ACTIVITY 审中-公开
标题翻译：具有抗血栓活性的马来酰胺衍生物
公开(公告)号：WO2009007015A1
公开(公告)日：2009-01-15
申请号：PCT/EP2008/005187
申请日：2008-06-26
申请人： SANOFI-AVENTIS , STEINHAGEN, Henning , SZILLAT, Hauke , FOLLMANN, Markus , KIRSCH, Reinhard , WEHNER, Volkmar , MATTER, Hans , LORENZ, Martin , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
发明人： STEINHAGEN, Henning , SZILLAT, Hauke , FOLLMANN, Markus , KIRSCH, Reinhard , WEHNER, Volkmar , MATTER, Hans , LORENZ, Martin , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
IPC分类号： C07D213/30 , C07D213/80 , C07C15/00 , C07D211/42 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12 , A61K31/44 , A61P7/00
CPC分类号： C07D213/80 , C07C257/18 , C07C311/08 , C07C311/46 , C07C317/22 , C07C317/32 , C07C2601/14 , C07D211/42 , C07D213/30 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds of the formula (I). The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIla and can in general be applied in conditions in which an undesired activity of factor VIla is present or for the cure or prevention of which an inhibition of factor VIla 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。式（I）的化合物是有价值的药理活性化合物。它们表现出强烈的抗血栓形成作用，并且适用于治疗和预防心血管疾病如血栓栓塞性疾病或再狭窄。它们是血液凝固酶的抑制剂，特别是因子VIla，并且通常可用于其中存在不需要的因子VIla的活性或用于治疗或预防因子VIla的抑制的病症。本发明还涉及式（I）化合物的制备方法，其用途，特别是药物中的活性成分，以及包含它们的药物制剂。

2. 发明公开

EP2176223A1 MALONAMIDE DERIVATIVES WITH ANTITHROMBOTIC ACTIVITY 有权
标题翻译：马来酸氨基甲酸酯麻黄酯抗生素治疗WIRKUNG
公开(公告)号：EP2176223A1
公开(公告)日：2010-04-21
申请号：EP08773673.2
申请日：2008-06-26
申请人： Sanofi-Aventis
发明人： STEINHAGEN, Henning , SZILLAT, Hauke , FOLLMANN, Markus , KIRSCH, Reinhard , WEHNER, Volkmar , MATTER, Hans , LORENZ, Martin , NEUENSCHWANDER, Kent, W. , SCOTESE, Anthony, C.
IPC分类号： C07D213/30 , C07D213/80 , C07C15/00 , C07D211/42 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12 , A61K31/44 , A61P7/00
CPC分类号： C07D213/80 , C07C257/18 , C07C311/08 , C07C311/46 , C07C317/22 , C07C317/32 , C07C2601/14 , C07D211/42 , C07D213/30 , C07D213/34 , C07D309/08 , C07D409/12 , C07D413/12
摘要： The present invention relates to compounds of the formula (I). The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIla and can in general be applied in conditions in which an undesired activity of factor VIla is present or for the cure or prevention of which an inhibition of factor VIla 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。式I化合物是有价值的药理活性化合物。它们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。它们是血液凝固酶，特别是因子VIIa的抑制剂，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。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。

3. 发明授权

EP1423357B1 UREA DERIVATIVES WITH ANTIPROTEOLYTIC ACTIVITY 失效转让
标题翻译： HARNSTOFFVERBINDUNGEN MIT ANTIPROTEOLYTISCHER WIRKUNG
公开(公告)号：EP1423357B1
公开(公告)日：2006-09-06
申请号：EP02758230.3
申请日：2002-06-12
申请人： Sanofi-Aventis Deutschland GmbH
发明人： SCHUDOK, Manfred , KLINGLER, Otmar , NESTLER, Hans-Peter , MATTER, Hans , SCHREUDER, Herman , SZILLAT, Hauke
IPC分类号： C07C275/42 , C07D333/38 , A61K31/17 , A61P7/00
CPC分类号： C07C275/42 , C07C2601/14 , C07D333/38
摘要： The present invention relates to compounds of the formula I, in which R?1, R2, R4, R5, D¿1, D2, X1, X2, X3, A and B 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 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. 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 1，R 2，R 4，R 5，D 1，D 2，X 1，X 2，X 3，A和B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。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。

4. 发明授权

EP1740569B1 IMIDAZOL-DERIVATE ALS TAFIA-INHIBITOREN 有权
标题翻译：咪唑衍生物作为抑制剂的TAFIa
公开(公告)号：EP1740569B1
公开(公告)日：2008-02-20
申请号：EP05731221.7
申请日：2005-04-07
申请人： Sanofi-Aventis Deutschland GmbH
发明人： KALLUS, Christopher , HEITSCH, Holger , LINDENSCHMIDT, Andreas , GRUENEBERG, Sven , SZILLAT, Hauke
IPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/06 , A61K31/435 , A61K31/41 , A61P7/00
CPC分类号： C07D401/06 , C07D401/14 , C07D409/14 , C07D417/06
摘要： The invention relates to compounds of formula (I), which are inhibitors of the activated thrombin-activatable fibrinolysis inhibitor. The compounds of formula (I) are suited for producing medicaments for the prevention and treatment of diseases accompanied by thromboses, embolisms, hypercoagulability or fibrotic changes.

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