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1. 发明授权

US08426420B2 Heterocyclic pyrazole-carboxamidesas P2Y12 antagonists 有权
标题翻译：杂环吡唑 - 甲酰胺P2Y12拮抗剂
公开(公告)号：US08426420B2
公开(公告)日：2013-04-23
申请号：US12817873
申请日：2010-06-17
申请人： Marc Nazaré , Gernot Zech , Melitta Just , Tilo Weiss , Gerhard Hessler , Markus Kohlmann
发明人： Marc Nazaré , Gernot Zech , Melitta Just , Tilo Weiss , Gerhard Hessler , Markus Kohlmann
IPC分类号： A61K31/496 , A61K31/454 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D403/14
摘要： The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件。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. 发明申请

US20110021537A1 HETEROCYCLIC PYRAZOLE-CARBOXAMIDESAS P2Y12 ANTAGONISTS 有权
标题翻译：杂环磷杂环戊二烯P2Y12拮抗剂
公开(公告)号：US20110021537A1
公开(公告)日：2011-01-27
申请号：US12817873
申请日：2010-06-17
申请人： Marc Nazaré , Gernot Zech , Melitta Just , Tilo Weiss , Gerhard Hessler , Markus Kohlmann
发明人： Marc Nazaré , Gernot Zech , Melitta Just , Tilo Weiss , Gerhard Hessler , Markus Kohlmann
IPC分类号： A61K31/497 , C07D403/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P7/02
CPC分类号： C07D403/14
摘要： The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; 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 anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 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R1; R2; Z; 一个; B; D; Q; J; 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。它们对血小板表现出强烈的抗凝集作用并因此具有抗血栓形成作用，并且适合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。它们是血小板ADP受体P2Y12的可逆拮抗剂，并且通常可用于其中存在血小板ADP受体P2Y12的不期望的活化或用于治疗或预防血小板ADP受体P2Y12的抑制的条件。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。

3. 发明申请

US20100081671A1 Cycloalkylamine substituted isoquinoline derivatives 有权
标题翻译：环烷基胺取代的异喹啉衍生物
公开(公告)号：US20100081671A1
公开(公告)日：2010-04-01
申请号：US12487386
申请日：2009-06-18
申请人： Oliver PLETTENBURG , Armin HOFMEISTER , Dieter KADEREIT , Stefan PEUKERT , Sven RUF , Matthias LÖHN , Peter MONECKE , Alexander SCHIFFER , Aimo KANNT , Markus KOHLMANN
发明人： Oliver PLETTENBURG , Armin HOFMEISTER , Dieter KADEREIT , Stefan PEUKERT , Sven RUF , Matthias LÖHN , Peter MONECKE , Alexander SCHIFFER , Aimo KANNT , Markus KOHLMANN
IPC分类号： A61K31/497 , C07D217/00 , A61K31/47 , A61P9/00 , A61K31/4725 , C07D401/12
CPC分类号： C07D217/24 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The invention relates to 6-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译：本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代的异喹啉衍生物和含有这些化合物的组合物。

4. 发明授权

US08710228B2 Cycloalkylamine substituted isoquinoline derivatives 有权
标题翻译：环烷基胺取代的异喹啉衍生物
公开(公告)号：US08710228B2
公开(公告)日：2014-04-29
申请号：US12487386
申请日：2009-06-18
申请人： Oliver Plettenburg , Armin Hofmeister , Dieter Kadereit , Stefan Peukert , Sven Ruf , Matthias Löhn , Peter Monecke , Alexander Schiffer , Aimo Kannt , Markus Kohlmann
发明人： Oliver Plettenburg , Armin Hofmeister , Dieter Kadereit , Stefan Peukert , Sven Ruf , Matthias Löhn , Peter Monecke , Alexander Schiffer , Aimo Kannt , Markus Kohlmann
IPC分类号： A61K31/47 , C07D217/00
CPC分类号： C07D217/24 , C07D401/04 , C07D401/12 , C07D401/14
摘要： The invention relates to 6-substituted isoquinoline derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.
摘要翻译：本发明涉及可用于治疗和/或预防与肌球蛋白轻链磷酸酶的Rho-激酶和/或Rho-激酶介导的磷酸化有关的疾病的式（I）的6-取代的异喹啉衍生物和含有这些化合物的组合物。

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