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1. 发明申请

WO2004101554A1 NEW INDOLE DERIVATIVES AS FACTOR XA INHIBITORS 审中-公开
标题翻译：作为因子XA抑制剂的新型吲哚衍生物
公开(公告)号：WO2004101554A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004751
申请日：2004-05-05
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , NAZARE, Marc , WEHNER, Volkmar , RITTER, Kurt , LAUX, Volker
发明人： NAZARE, Marc , WEHNER, Volkmar , RITTER, Kurt , LAUX, Volker
IPC分类号： C07D413/14
CPC分类号： C07D413/14
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 ; R 7 ; 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 Vila (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor Vila is present or for the cure or prevention of which an inhibition of factor Xa and/or 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）的化合物，其中R 0; R 1; R 2; R 3; R 4; R 5; R 6; R 7; 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。

2. 发明申请

WO2004101556A1 INDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：吲哚衍生物作为因子Xa抑制剂
公开(公告)号：WO2004101556A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004753
申请日：2004-05-05
申请人： AVENTIS PHARMA DEUTSCHLAND GmbH , NAZARE, Marc , WEHNER, Volkmar , LAUX, Volker , URMANN, Matthias , BAUER, Armin , MATTER, Hans
发明人： NAZARE, Marc , WEHNER, Volkmar , LAUX, Volker , URMANN, Matthias , BAUER, Armin , MATTER, Hans
IPC分类号： C07D413/14
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，其中R 0为 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）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。

3. 发明申请

WO2004101553A1 BENZIMIDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物作为因子Xa抑制剂
公开(公告)号：WO2004101553A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004750
申请日：2004-05-05
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , NAZARE, Marc , WAGNER, Michael , WEHNER, Volkmar , MATTER, Hans , URMANN, Matthias , RITTER, Kurt
发明人： NAZARE, Marc , WAGNER, Michael , WEHNER, Volkmar , MATTER, Hans , URMANN, Matthias , RITTER, Kurt
IPC分类号： C07D413/14
CPC分类号： C07D235/24 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/08 , C07D495/04
摘要： The present invention relates to compounds of the formula (I), 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 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，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。

4. 发明申请

WO2004101563A1 AZAINDOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：作为XA抑制剂的因子衍生物
公开(公告)号：WO2004101563A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004754
申请日：2004-05-05
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , NAZARE, Marc , WEHNER, Volkmar , WILL, David, William , RITTER, Kurt , URMANN, Matthias , MATTER, Hans
发明人： NAZARE, Marc , WEHNER, Volkmar , WILL, David, William , RITTER, Kurt , URMANN, Matthias , MATTER, Hans
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Indazole-derivatives as factor Xa inhibitors. The present invention relates to compounds of the formula (I), wherein R 0 , R 1 , R 2 , R 3 , 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：吲唑衍生物作为因子Xa抑制剂。本发明涉及式（I）化合物，其中R 0，R 1，R 2，R 3，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，特别是药物中的活性成分，以及包含它们的药物制剂。

5. 发明申请

WO2005085239A2 PYRROLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：吡咯衍生物作为因子Xa抑制剂
公开(公告)号：WO2005085239A2
公开(公告)日：2005-09-15
申请号：PCT/EP2005/001423
申请日：2005-02-12
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , BAUER, Armin , WAGNER, Michael , NAZARÉ, Marc , WEHNER, Volkmar , URMANN, Matthias , MATTER, Hans
发明人： BAUER, Armin , WAGNER, Michael , NAZARÉ, Marc , WEHNER, Volkmar , URMANN, Matthias , MATTER, Hans
IPC分类号： C07D413/14
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The present invention relates to compounds of the formulae (I) and (Ia), wherein R 0 ; R 1 ; R3; R4; R22, Q; V, G and M have the meanings indicated in the claims. The compounds of the formulae (I) and (Ia) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable 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 (Ia), 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（Ia）的化合物，其中R为0; [R ^{1 ; R3; R4; R22，Q; V，G和M具有权利要求中所表示的含义。式（I）和（Ia）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作用，适用于心血管疾病如血栓栓塞性疾病或再狭窄的治疗和预防。它们是凝血酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以用于其中存在不想要的因子Xa和/或因子VIIa活性的条件或用于治疗或预防因子Xa和/或因子VIIa的抑制。本发明还涉及制备式（I）和（Ia）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。}

6. 发明申请

WO2005095440A1 BETA-AMINOACID-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译： β-氨基酸衍生物作为因子Xa抑制剂
公开(公告)号：WO2005095440A1
公开(公告)日：2005-10-13
申请号：PCT/EP2005/001736
申请日：2005-02-19
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , URMANN, Matthias , NAZARÉ, Marc , WEHNER, Volkmar , MATTER, Hans , BAUER, Armin , WAGNER, Michael
发明人： URMANN, Matthias , NAZARÉ, Marc , WEHNER, Volkmar , MATTER, Hans , BAUER, Armin , WAGNER, Michael
IPC分类号： C07K5/02
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 ° ; 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）的化合物，其中R 1， [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。

7. 发明申请

WO2004050636A2 IMIDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：咪唑衍生物作为因子Xa抑制剂
公开(公告)号：WO2004050636A2
公开(公告)日：2004-06-17
申请号：PCT/EP2003/012996
申请日：2003-11-20
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： NAZARÉ, Marc , BAUER, Armin , WEHNER, Volkmar , WILL, David, William , MATTER, Hans , WAGNER, Michael , SCHREUDER, Herman
IPC分类号： C07D233/70
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）的化合物，其中R为0; R ^{1 ; R ^{2 ; R ^{3 ; [R ^{4 ; Q; V，G和M具有权利要求中所表示的含义。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。它们是凝血酶因子Xa（FXa）和/或因子VIIa（FVIIa）的可逆抑制剂，并且通常可以用于其中存在不想要的因子Xa和/或因子VIIa活性的条件或用于治疗或预防因子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。}}}}

8. 发明申请

WO2003011288A1 NOVEL IMIDAZOLIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS VLA-4 ANTAGONISTS 审中-公开
标题翻译：新的咪唑啉衍生物，其制备及其作为VLA-4拮抗剂的用途
公开(公告)号：WO2003011288A1
公开(公告)日：2003-02-13
申请号：PCT/EP2002/008106
申请日：2002-07-20
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： WEHNER, Volkmar , FLOHR, Stefanie , BLUM, Horst , RÜTTEN, Hartmut , STILZ, Hans, Ulrich
IPC分类号： A61K31/4166
CPC分类号： C07D405/12 , C07D233/74
摘要： The present invention relates to novel imidazolidine derivatives of the formula (I), in which B, E, W, Y, R, R 2 , R 3 , R 30 , e and h have the meanings given in the claims. The compounds of the formula (I) are valuable pharmaceutical active compounds which are suitable, for example, for treating inflammatory disease, for example rheumatoid arthritis, or allergic diseases. The compounds of the formula (I) are inhibitors of the adhesion and migration of leukocytes and/or antagonists of the adhesion receptor VLA-4, which belongs to the integrin group. They are generally suitable for treating diseases which are caused by, or associated with, an undesirable degree of leukocyte adhesion and/or leukocyte migration or in which cell-cell or cell-matrix interactions, which are based on the interactions of VLA-4 receptors with their ligands, play a role. The invention furthermore relates to processes for preparing the compounds of the formula (I), to their use and topharmaceutical preparations which comprise compounds of the formula (I).
摘要翻译：本发明涉及式（I）的新型咪唑烷衍生物，其中B，E，W，Y，R，R 2，R 3，R 30，e和h具有索赔。式（I）的化合物是有价值的药物活性化合物，其适用于例如治疗炎性疾病，例如类风湿性关节炎或过敏性疾病。式（I）的化合物是属于整联蛋白基团的粘附受体VLA-4的白细胞和/或拮抗剂的粘附和迁移的抑制剂。它们通常适用于治疗由不利程度的白细胞粘附和/或白细胞迁移引起的或与之相关的疾病，或其中基于VLA-4受体的相互作用的细胞 - 细胞或细胞 - 基质相互作用与他们的配体，发挥作用。本发明还涉及制备式（I）化合物及其用途和包含式（I）化合物的药物制剂的方法。

9. 发明申请

WO2002072557A1 BIS(TRIFLUOROMETHYL)HYDANTOINS AS INTERMEDIATES FOR PHARMACEUTICALLY ACTIVE INGREDIENTS 审中-公开
标题翻译：作为药物活性成分的中间体的BIS（三氟甲基）HYDANTOINS
公开(公告)号：WO2002072557A1
公开(公告)日：2002-09-19
申请号：PCT/EP2002/001918
申请日：2002-02-23
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： WEHNER, Volkmar , STILZ, Hans, Ulrich , BURGER, Klaus , GOLUBEV, Alexander , OSSIPOV, Sergej
IPC分类号： C07D233/76
CPC分类号： C07D233/76
摘要： The present invention relates to hydantoins of formula (I), in which R is the residue of an amino carboxylic acid or of an amino carboxylic acid derivative which is obtained formally by removing an NH 2 group from an amino carboxylic acid or an amino carboxylic acid or an amino carboxylic acid derivative, to the preparation thereof and to the use thereof as intermediates, in particular for preparing pharmaceutically active ingredients.
摘要翻译：本发明涉及式（I）的乙内酰脲，其中R是氨基羧酸或氨基羧酸衍生物的残基，其通过从氨基羧酸或氨基羧酸除去NH 2基而正式获得，或氨基羧酸衍生物，其制备方法及其作为中间体的用途，特别是用于制备药物活性成分。

10. 发明申请

WO2004060874A1 IMINOSÄUREDERIVATE ALS INHIBITOREN VON MATRIX-METALLOPROTEINASEN 审中-公开
标题翻译： IMINOSÄUREDERIVATEAS基质金属蛋白酶的抑制剂
公开(公告)号：WO2004060874A1
公开(公告)日：2004-07-22
申请号：PCT/EP2003/014611
申请日：2003-12-19
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH
发明人： SCHUDOK, Manfred , RUF, Sven , MATTER, Hans , WEHNER, Volkmar , KIRSCH, Reinhard , STAHL, Petra
IPC分类号： C07D209/42
CPC分类号： C07D403/12 , C07D209/42 , C07D209/52 , C07D405/12 , C07D409/12 , C07D417/14 , C07D495/04
摘要： Verbindungen der Formel (I) eignen sich zur Herstellung von Arzneimitteln zur Prophylaxe und Therapie von Erkrankungen, an deren Verlauf eine verstärkte Aktivität von Matrix-Metalloproteinasen beteiligt sind. Dazu gehören Erkrankungen wie eine degenerative Gelenkerkrankung beispielsweise Osteoarthrosen, Spondylosen, Knorpelschwund nach Gelenktrauma oder längerer Gelenksruhigstellung nach Meniskus-oder Patellaverletzungen oder Bänderrissen, oder eine Erkrankung des Bindegewebes wie Kollagenosen, Periodontalerkrankungen, Wundheilungsstörungen, oder eine chronische Erkrankung des Bewegungsapparates wie entzündliche, immunologisch oder stoffwechselbedingte akute oder chronische Arthritiden, Arthropathien, Myalgien oder Störungen des Knochenstoffwechsels oder eine Ulceration Atherosklerose oder Stenose oder eine entzündliche Erkrankung oder eine Krebserkrankung, Tumormetastasenbildung, Kachexie, Anorexie oder spetischer Schock.
摘要翻译：式（I）的化合物是适用于制备用于预防和在其当然基质金属蛋白酶的活性增加参与疾病的治疗药物。这些包括疾病，如退行性关节病，例如，骨关节炎，病，软骨损失以下后弯月面或髌骨损伤或韧带撕裂或结缔组织疾病如结缔组织疾病，牙周，伤口愈合，或运动系统的慢性疾病如炎性疾病，免疫或代谢关节创伤或长期关节固定急性或慢性关节炎，关节病，肌痛和骨代谢或溃疡，动脉粥样硬化或狭窄或炎性疾病或癌症，肿瘤转移，恶病质，厌食或spetischer休克的干扰。

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