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1. 发明公开

EP1571154A1 Beta-aminoacid-derivatives as factor Xa inhibitors 审中-公开
标题翻译：衍生出β-Alanins als Hemmer des Faktors Xa
公开(公告)号：EP1571154A1
公开(公告)日：2005-09-07
申请号：EP04004904.1
申请日：2004-03-03
申请人： Aventis Pharma Deutschland GmbH
发明人： Urmann, Matthias, Dr. , Nazaré, Marc, Dr. , Wehner, Volkmar, Dr. , Matter, Hans, Dr. , Bauer, Armin, Dr. , Wagner, Michael, Dr.
IPC分类号： C07K5/02 , C07D413/12 , C07D409/12 , C07D295/104 , C07D419/12 , A61K31/381 , A61K31/5377 , A61K31/4965 , A61K31/4178 , A61K31/54
CPC分类号： C07K5/0202 , C07D265/32 , C07D265/33 , C07D291/06 , C07D295/112 , C07D409/12 , C07D409/14 , C07D413/12 , C07D419/12
摘要： The present invention relates to compounds of the formula I,
in which R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; R 5 , R 6 , Q; 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 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为CHEM; R 1; R 2; R 3; [R <4>; R 5，R 6，Q; 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，并且通常可以在其中存在因子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。

2. 发明公开

EP1479679A1 Triazole-derivatives as factor Xa inhibitors 审中-公开
标题翻译： Triazolderivate als Faktor-Xa-Inhibitoren
公开(公告)号：EP1479679A1
公开(公告)日：2004-11-24
申请号：EP03011309.6
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Laux, Volker, Dr. , Bauer, Armin, Dr. , Wagner, Michael, Dr.
IPC分类号： C07D413/14 , A61K31/4196 , A61P7/02
CPC分类号： C07D413/14
摘要： The present invention relates to compounds of the formulae I and II,

in which R 0 ; R 1 ; R 2 ; R 3 ; Q; J 1 ; J 2 ; J 3 ; J 4 ; J 5 ; V; G and M have the meanings indicated in the claims. The compounds of the formulae I and II 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 formulae I and II, 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和II化合物，其中R 0为CHEM> CHEM; [R <1>; [R <2>; [R <3>; Q; Ĵ<1>; Ĵ<2>; Ĵ<3>; Ĵ<4>; Ĵ<5>; V; G和M具有权利要求中所示的含义。式I和II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，并且通常可以在其中存在因子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和II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. 发明公开

EP1479674A1 Imidiazole-derivatives as factor xa inhibitors 审中-公开
标题翻译： Imidazolderivate als Faktor-Xa-Inhibitoren
公开(公告)号：EP1479674A1
公开(公告)日：2004-11-24
申请号：EP03011307.0
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Bauer, Armin, Dr. , Wehner, Volkmar, Dr. , Will, David William, Dr. , Matter, Hans, Dr. , Wagner, Michael, Dr. , Schreuder, Herman, Dr.
IPC分类号： C07D401/12 , C07D413/14 , C07D401/14 , C07D417/14 , A61K31/4178 , A61P7/02
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to compounds of the formula I,
wherein R 0 ; R 1 ; R 2 ; R 3 ; R 4 ; Q; 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 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为CHEM; R 1; R 2; R 3; [R <4>; Q; 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，并且通常可以在其中存在因子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。

4. 发明公开

EP1479675A1 Indazole-derivatives as factor Xa inhibitors 审中-公开
标题翻译： Indazolderivate als Faktor Xa-Inhibitoren
公开(公告)号：EP1479675A1
公开(公告)日：2004-11-24
申请号：EP03011303.9
申请日：2003-05-19
申请人： Aventis Pharma Deutschland GmbH
发明人： Nazaré, Marc, Dr. , Wehner, Volkmar, Dr. , Laux, Volker, Dr. , Urmann, Matthias, Dr. , Bauer, Armin, Dr. , Matter, Hans, Dr.
IPC分类号： C07D413/14 , C07D401/14 , C07D401/12 , C07D413/04 , A61K31/416 , A61P7/02
CPC分类号： C07D413/14 , C07D401/12 , C07D401/14
摘要： The present invention relates to compounds of the formulae I and Ib

wherein R 0 ; R 1 ; R 2 ;Q; 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 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 formulae I and Ib, 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和Ib化合物 CHEM>其中R 0; R 1; R 2; Q; 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，并且通常可以在其中存在因子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和Ib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。

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