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1. 发明申请

WO2008155022A1 PYRROLE DERIVATIVES AS P2Y12 ANTAGONISTS 审中-公开
标题翻译： PYRROLE DERIVATIVES作为P2Y12 ANTAGONISTS
公开(公告)号：WO2008155022A1
公开(公告)日：2008-12-24
申请号：PCT/EP2008/004459
申请日：2008-06-04
申请人： SANOFI-AVENTIS , KLINGLER, Otmar , CZECH, Joerg , CZECHTIZKY, Werngard , WEISS, Tilo , JUST, Melitta
发明人： KLINGLER, Otmar , CZECH, Joerg , CZECHTIZKY, Werngard , WEISS, Tilo , JUST, Melitta
IPC分类号： C07D401/06 , C07D403/06 , C07D403/14 , C07D405/14
CPC分类号： C07D401/06 , C07D403/06 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds of the formula (I), in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated 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R 1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; 一个; B，D和E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，因此表现出抗血栓形成的作用，用于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

WO2009080227A3 PYRAZOLE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS 审中-公开
公开(公告)号：WO2009080227A3
公开(公告)日：2009-07-02
申请号：PCT/EP2008/010573
申请日：2008-12-12
申请人： SANOFI-AVENTIS , NAZARÉ, Marc , ZECH, Gernot , GOERLITZER, Jochen , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECHTIZKY, Werngard , RUF, Sven
发明人： NAZARÉ, Marc , ZECH, Gernot , GOERLITZER, Jochen , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECHTIZKY, Werngard , RUF, Sven
IPC分类号： C07D403/12 , A61K31/496 , A61P7/02
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.

3. 发明申请

WO2008128647A1 QUINOLINE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS 审中-公开
标题翻译：喹喔啉羧酰胺衍生物作为P2Y12拮抗剂
公开(公告)号：WO2008128647A1
公开(公告)日：2008-10-30
申请号：PCT/EP2008/002790
申请日：2008-04-09
申请人： SANOFI-AVENTIS , NAZARE, Marc , ZECH, Gernot , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECH, Joerg
发明人： NAZARE, Marc , ZECH, Gernot , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECH, Joerg
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/4709 , A61P9/10 , A61P7/02
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention relates to compounds of the Formula (I), in which R 1 ; R 2 ; R 3 ; R 4 ; R 5 ; R 6 ; Z; A; B; E; X; 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）的化合物，其中R 1， [R ^{2 ; [R ^{3 ; [R ^{4 ; [R ^{5 ; [R ^{6 ; Z者除外; 一个; B; Ë; X; Q; 焦耳; 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，因此表现出抗血栓形成的作用，用于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，特别是药物中的活性成分，以及包含它们的药物制剂。}}}}}

4. 发明公开

EP2238127A2 PYRAZOLE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS 有权
标题翻译：吡唑羧酰胺衍生物作为P2Y12拮抗剂
公开(公告)号：EP2238127A2
公开(公告)日：2010-10-13
申请号：EP08865091.6
申请日：2008-12-12
申请人： Sanofi-Aventis
发明人： NAZARÉ, Marc , ZECH, Gernot , GOERLITZER, Jochen , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECHTIZKY, Werngard , RUF, Sven
IPC分类号： C07D403/12 , A61K31/496 , A61P7/02
CPC分类号： C07D403/12
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.

5. 发明公开

EP2238128A2 HETEROCYCLIC PYRAZOLE-CARBOXAMIDES AS P2Y12 ANTAGONISTS 有权
标题翻译：杂环吡唑 - 甲酰胺作为P2Y12拮抗剂
公开(公告)号：EP2238128A2
公开(公告)日：2010-10-13
申请号：EP08864841.5
申请日：2008-12-12
申请人： Sanofi-Aventis
发明人： NAZARÉ, Marc , ZECH, Gernot , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , KOHLMANN, Markus
IPC分类号： C07D403/14 , A61K31/496 , 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）的化合物，其中R 1， R2; Z者除外; 一个; B; d; Q; 焦耳; V; G和M具有权利要求中所指的含义。式I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聚集作用，因此具有抗血栓形成作用，并且适用于例如血栓形成。用于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，并且通常可以用于存在不希望的血小板ADP受体P2Y12激活的病症或用于治疗或预防血小板ADP受体P2Y12抑制的病症。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。

6. 发明公开

EP2148871A1 QUINOLINE-CARBOXAMIDE DERIVATIVES AS P2Y12 ANTAGONISTS 审中-公开
标题翻译：喹啉甲酰胺衍生物作为P2Y12拮抗剂
公开(公告)号：EP2148871A1
公开(公告)日：2010-02-03
申请号：EP08735104.5
申请日：2008-04-09
申请人： Sanofi-Aventis
发明人： NAZARE, Marc , ZECH, Gernot , JUST, Melitta , WEISS, Tilo , HESSLER, Gerhard , CZECH, Joerg
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , A61K31/4709 , A61P9/10 , A61P7/02
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The present invention relates to compounds of the Formula (I), in which R1; R2; R3; R4; R5; R6; Z; A; B; E; X; 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.

7. 发明公开

EP2167487A1 PYRROLE DERIVATIVES AS P2Y12 ANTAGONISTS 无效
标题翻译：吡咯作为P2Y12拮抗剂
公开(公告)号：EP2167487A1
公开(公告)日：2010-03-31
申请号：EP08759015.4
申请日：2008-06-04
申请人： Sanofi-Aventis
发明人： KLINGLER, Otmar , CZECH, Joerg , CZECHTIZKY, Werngard , WEISS, Tilo , JUST, Melitta
IPC分类号： C07D401/06 , C07D403/06 , C07D403/14 , C07D405/14
CPC分类号： C07D401/06 , C07D403/06 , C07D403/14 , C07D405/14
摘要： The present invention relates to compounds of the formula (I), in which R1; R2; R3; R4; R5; R6; R7; R8; R9; R10; R11; R12; R13; A; B, D and E have the meanings indicated 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.

8. 发明授权

EP1509516B1 INHIBITORS OF THE GPIB -VWF INTERACTION, THEIR PREPARATION AND USE 有权
标题翻译：抑制剂GPIB VWF相互作用
公开(公告)号：EP1509516B1
公开(公告)日：2007-01-31
申请号：EP03740199.9
申请日：2003-06-06
申请人： Sanofi-Aventis Deutschland GmbH
发明人： KLINGLER, Otmar , JUST, Melitta , SAKURAI, Kuniya , Fukuchi, Naoyuki
IPC分类号： C07D401/12 , A61K31/47 , A61P9/00
CPC分类号： C07D401/12 , C07D215/48 , C07D401/14 , C07D417/12
摘要： The present invention relates to compounds of the formula (I); in which R1, R2, A, B, D, E, n, m or o have the meanings indicated below. The compounds of the formula (I) are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases.

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