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公开(公告)号：US06706715B2
公开(公告)日：2004-03-16
申请号：US10183848
申请日：2002-06-26
申请人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder , Hauke Szillat
发明人： Manfred Schudok , Otmar Klingler , Hans-Peter Nestler , Hans Matter , Herman Schreuder , Hauke Szillat
IPC分类号： A61K314425
CPC分类号： C07C275/42 , C07C2601/14 , C07D333/38
摘要： The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, 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具有所指定的含义 在权利要求中。 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。
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2.发明授权Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途公开(公告)号：US06645992B2
公开(公告)日：2003-11-11
申请号：US09965790
申请日：2001-10-01
IPC分类号： C07D25718
CPC分类号： A61K31/27 , A61K31/167 , A61K31/225 , C07C257/18 , C07C257/20
摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating 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. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译： 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理活性化合物，其表现出很强的抗血栓形成作用，并且适用于例如 治疗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。 还公开了制备式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。
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3.发明授权Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use 有权因子VIIa抑制（硫）脲衍生物，其制备及其应用公开(公告)号：US06743790B2
公开(公告)日：2004-06-01
申请号：US09874318
申请日：2001-06-06
IPC分类号： A61K31535
CPC分类号： C07D213/40 , C07C275/42 , C07C2602/08 , C07C2602/10 , C07C2603/18 , C07D211/96 , C07D319/18
摘要： The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n 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, for example 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 3，R 4，R 5，R 6，A，X，m和n 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。 本发明还涉及制备式I化合物的方法，其用途，例如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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4.发明授权Malonamid and malonamic ester derivatives with antithrombotic activity, their preparation, and their use 有权丙二酰胺和丙二酸酯衍生物具有抗血栓活性，其制备及其用途公开(公告)号：US07153876B2
公开(公告)日：2006-12-26
申请号：US10634827
申请日：2003-08-06
IPC分类号： C07D213/75 , A61K31/44 , A61P7/02 , A61P9/10
CPC分类号： A61K31/27 , A61K31/167 , A61K31/225 , C07C257/18 , C07C257/20
摘要： Compounds of formula I, in which R1, R2, A, and B having the definitions set forth in the claims, are valuable pharmacologically active compounds, which exhibit a strong antithrombotic effect and are suitable, for example, for treating 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. Also disclosed are processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
摘要翻译： 具有权利要求中所述定义的R 1，R 2，A和B的式I化合物是有价值的药理学活性化合物，其表现出强烈的 抗血栓形成作用，并且适用于例如治疗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。 还公开了制备式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。
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公开(公告)号：US07435747B2
公开(公告)日：2008-10-14
申请号：US10886312
申请日：2004-07-07
申请人： Anuschirwan Peyman , David William Will , Uwe Gerlach , Marc Nazaré , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
发明人： Anuschirwan Peyman , David William Will , Uwe Gerlach , Marc Nazaré , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
IPC分类号： A61K31/445 , C07D211/26
CPC分类号： C07D401/12 , C07D211/26 , C07D211/34
摘要： The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V 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是 Q; X; Q'，D，R 10和V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。
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公开(公告)号：US20050143419A1
公开(公告)日：2005-06-30
申请号：US10886312
申请日：2004-07-07
申请人： Anuschirwan Peyman , David Will , Uwe Gerlach , Marc Nazare , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
发明人： Anuschirwan Peyman , David Will , Uwe Gerlach , Marc Nazare , Gerhard Zoller , Hans-Peter Nestler , Hans Matter , Fahad Al-Obeidi
IPC分类号： A61K31/445 , A61K31/4545 , A61P7/02 , A61P43/00 , C07D211/26 , C07D211/34 , C07D401/12 , C07D413/02 , A61K31/4245 , A61K31/4439 , A61K31/454
CPC分类号： C07D401/12 , C07D211/26 , C07D211/34
摘要： The present invention relates to compounds of the formula I, in which R0; Q; X; Q′, D, R10 and V 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是 Q; X; Q'，D，R 10和V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。
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