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1. 发明申请

WO2005085230A1 4-BENZIMIDAZOL-2-YL-PYRIDAZIN-3-ON-DERIVATIVE, IHRE HERSTELLUNG UND VERWENDUNG IN ARZNEIMITTELN 审中-公开
标题翻译： 4-苯并咪唑-2-基 - 哒嗪-3-酮衍生物，它们的制备和在药物中使用
公开(公告)号：WO2005085230A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/002179
申请日：2005-03-02
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , SCHOENAFINGER, Karl , HOELDER, Swen , WILL, David, William , MATTER, Hans , MUELLER, Guenther , BOSSART, Martin
发明人： SCHOENAFINGER, Karl , HOELDER, Swen , WILL, David, William , MATTER, Hans , MUELLER, Guenther , BOSSART, Martin
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D417/14 , C07D471/04
摘要： Die Erfindung betrifft Verbindungen gemäß der allgemeinen Formel (I), wobei die Definition der Substituenten A, B, D, E, R l und R 2 in der Beschreibung aufgeführt sind, sowie deren physiologisch verträglichen Salze, Verfahren zur Herstellung dieser Verbindungen und deren Verwendung als Arzneimittel. Diese Verbindungen sind Kinaseinhibitoren, insbesondere Inhibitoren der Kinase GSK-3ß (Glykogensynthasekinase-3ß).
摘要翻译：本发明涉及的化合物根据结构通式（I），其中，所述取代基A的定义中，B，D，E，R 和R如说明书中所<2>中列出，以及它们的生理学可接受的盐，用于制备这些方法化合物和它们作为药物的用途。这些化合物是激酶抑制剂，在激酶GSK-3SS的特定抑制剂（糖原合酶激酶3SS）。

2. 发明申请

WO2005111018A1 PYRIDAZINONE DERIVATIVES, METHODS FOR PRODUCING THEM AND THEIR USE AS PHARMACEUTICALS 审中-公开
标题翻译：吡咯烷酮衍生物，其生产方法及其作为药物的用途
公开(公告)号：WO2005111018A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/005346
申请日：2005-05-17
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , HOELDER, Swen , MUELLER, Guenter , SCHOENAFINGER, Karl , WILL, David, William , MATTER, Hans , BOSSART, Martin
发明人： HOELDER, Swen , MUELLER, Guenter , SCHOENAFINGER, Karl , WILL, David, William , MATTER, Hans , BOSSART, Martin
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R 1 and R 2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. Formula (I) These compounds are kinase inhibitors, in particular inhibitors of the kinase GSK15 30 (glycogen synthase kinase-3ß).
摘要翻译：本发明涉及根据通式（I）的化合物，其定义如下文中给出的取代基X，R 1和R 2以及它们的生理上可接受的盐，制备这些的方法化合物及其作为药物的用途。式（I）这些化合物是激酶抑制剂，特别是激酶GSK1530（糖原合成酶激酶-3β）的抑制剂。

3. 发明申请

WO2005085231A1 NOVEL 4-BENZIMIDAZOL-2-YLPYRIDAZIN-3-ONE DERIVATIVES 审中-公开
标题翻译：新的4-苯并咪唑-2-基吡啶-3-酮衍生物
公开(公告)号：WO2005085231A1
公开(公告)日：2005-09-15
申请号：PCT/EP2005/002569
申请日：2005-02-18
申请人： AVENTIS PHARMA S.A. , HOELDER, Swen , SCHOENAFINGER, Karl , WILL, David, William , MATTER, Hans , MUELLER, Guenther , COMBEAU, Cécile , DELAISI, Christine , STEINMETZ, Anke , SASSOON, Ingrid
发明人： HOELDER, Swen , SCHOENAFINGER, Karl , WILL, David, William , MATTER, Hans , MUELLER, Guenther , COMBEAU, Cécile , DELAISI, Christine , STEINMETZ, Anke , SASSOON, Ingrid
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04
摘要： The invention relates to compounds of the general formula (I), where the definition of the substituents A, B, D, E, R 1 and R 2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
摘要翻译：本发明涉及通式（I）的化合物，其中取代基A，B，D，E，R 1和R 2的定义在说明书中详细描述，其生理上可耐受的盐，这些化合物的制备方法及其作为药物的用途。这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。

4. 发明申请

WO2005111019A1 NOVEL PYRIDAZINONE DERIVATIVES AS INHIBITORS OF CDK2 审中-公开
标题翻译：作为CDK2的抑制剂的新型吡咯烷酮衍生物
公开(公告)号：WO2005111019A1
公开(公告)日：2005-11-24
申请号：PCT/EP2005/006046
申请日：2005-05-17
申请人： AVENTIS PHARMA S.A. , HOELDER, Swen , MUELLER, Guenter , SCHOENAFINGER, Karl , WILL, David William , MATTER, Hans
发明人： HOELDER, Swen , MUELLER, Guenter , SCHOENAFINGER, Karl , WILL, David William , MATTER, Hans
IPC分类号： C07D401/14
CPC分类号： C07D403/04 , C07D401/14
摘要： The present invention relates to compounds according to the general formula (I), with the definitions of the substituents X, R1 and R2 given below in the text, as well as their physiologically acceptable salts, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).
摘要翻译：本发明涉及根据通式（I）的化合物，其定义如下文中给出的取代基X，R 1和R 2及其生理上可接受的盐，制备这些化合物的方法及其作为药物的用途。这些化合物是激酶抑制剂，特别是激酶CDK2（细胞周期蛋白依赖性激酶2）的抑制剂。

5. 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。

6. 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。

7. 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。}

8. 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。

9. 发明申请

WO2005073236A2 THIENO-IMINOSÄURE-DERIVATE ALS INHIBITOREN VON MATRIX-METALLOPROTEINASEN 审中-公开
标题翻译：噻吩并 - 亚氨基衍生物作为基质金属蛋白酶抑制剂
公开(公告)号：WO2005073236A2
公开(公告)日：2005-08-11
申请号：PCT/EP2005/000417
申请日：2005-01-18
申请人： AVENTIS PHARMA DEUTSCHLAND GMBH , SCHUDOK, Manfred , MATTER, Hans , HOFMEISTER, Armin
发明人： SCHUDOK, Manfred , MATTER, Hans , HOFMEISTER, Armin
IPC分类号： C07D495/00
CPC分类号： C07D495/04
摘要： Verbindungen der Formel (I) eignen sich zur Herstellung von Arzneimitteln zur Prophylaxe und Therapie von Erkrankungen, an deren Verlauf eine verstärke 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 Bänderrisen, 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. Weiterhin eignen sich die Verbindungen der Formel (I) zur Behandlung von Entzündungen, Krebserkrankungen, Tumormetastasenbildung, Kachexie, Anorexie, Herzversagen und septischem Schock und zur Prophylaxe von Myocard- und Cerebral-Infarkten.
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强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Bänderrisen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的干扰。此外，式（I）的化合物是用于治疗炎症，癌症疾病，肿瘤转移的形成，恶病质，厌食，心脏衰竭和脓毒性休克的治疗和心肌和脑梗塞的预防。

10. 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。

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