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1. 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。}}}}}

2. 发明申请

WO2009000412A1 A REGIOSELECTIVE METAL CATALYZED SYNTHESIS OF ANNELATED BENZIMIDAZOLES AND AZABENZIMIDAZOLES 审中-公开
标题翻译：邻苯二甲酸二甲酯和亚氨基半乳糖的选择性金属催化合成
公开(公告)号：WO2009000412A1
公开(公告)日：2008-12-31
申请号：PCT/EP2008/004638
申请日：2008-06-11
申请人： SANOFI AVENTIS , ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARE, Marc , R'KYEN, Omar , URMANN, Mathias , HALLAND, Nis
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARE, Marc , R'KYEN, Omar , URMANN, Mathias , HALLAND, Nis
IPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D491/14
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D491/14
摘要： A regioselective metal catalyzed synthesis of benzimidazoles and azabenzimidazoles The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N- substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo- nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
摘要翻译：苯并咪唑和氮杂苯并咪唑的区域选择性金属催化合成本发明涉及用于区域选择性合成式（I）化合物的方法，其中R1; R2; R3; R4; J1; J2; J3; J4和G具有权利要求中所示的含义。本发明提供直接金属，例如，钯或铜，催化的区域选择性方法，用于从用于制备药物，诊断剂，液体的2-卤代 - 硝基芳烃和N-取代的酰胺开始的多种不对称，多官能的式（I）的N-取代的苯并咪唑或氮杂苯并咪唑晶体，聚合物，除草剂，杀真菌剂，杀线虫剂，杀寄生虫剂，杀虫剂，杀螨剂和节肢动物杀虫剂。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2004101555A1 TRIAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 审中-公开
标题翻译：三唑衍生物作为因子Xa抑制剂
公开(公告)号：WO2004101555A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004752
申请日：2004-05-05
申请人： AVENTIS PHARMA DEUTSCHLAND GmbH , NAZARE, Marc , LAUX, Volker , BAUER, Armin , WAGNER, Michael
发明人： NAZARE, Marc , LAUX, Volker , BAUER, Armin , WAGNER, Michael
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to compounds of the formulae (I) and (II), in which R O ; R 1 ; R 3 ; Q; J 1 ; J 2 ; J 3 ; J 4 ; J 5 ; V; G and M have the meanings indicated in the claims. The compounds of the formulae (I) and (II) 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 (II), 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（II）的化合物，其中R 0; [R <1>; [R <3>; Q; Ĵ<1>; Ĵ<2>; Ĵ<3>; Ĵ<4>; Ĵ<5>; V; G和M具有权利要求中所示的含义。式（I）和（II）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（II）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. 发明公开

EP1636216A1 BENZIMIDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 有权
标题翻译：苯并咪唑Xa因子抑制剂
公开(公告)号：EP1636216A1
公开(公告)日：2006-03-22
申请号：EP04731162.6
申请日：2004-05-05
申请人： Sanofi-Aventis Deutschland GmbH
发明人： NAZARE, Marc , WAGNER, Michael , WEHNER, Volkmar , MATTER, Hans , URMANN, Matthias , RITTER, Kurt
IPC分类号： C07D413/14 , C07D401/14 , C07D417/14
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 R0,, R1 , R2, 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.

9. 发明公开

EP2173747A1 A REGIOSELECTIVE METAL CATALYZED SYNTHESIS OF ANNELATED BENZIMIDAZOLES AND AZABENZIMIDAZOLES 有权
标题翻译： REGIO选择性合成金属熔融苯并咪唑和氮杂
公开(公告)号：EP2173747A1
公开(公告)日：2010-04-14
申请号：EP08759157.4
申请日：2008-06-11
申请人： Sanofi-Aventis
发明人： ALONSO, Jorge , LINDENSCHMIDT, Andreas , NAZARE, Marc , R'KYEN, Omar , URMANN, Mathias , HALLAND, Nis
IPC分类号： C07D471/04 , C07D471/14 , C07D487/04 , C07D491/14
CPC分类号： C07D487/04 , C07D471/04 , C07D471/14 , C07D491/14
摘要： A regioselective metal catalyzed synthesis of benzimidazoles and azabenzimidazoles The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N- substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo- nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.

10. 发明公开

EP1628971A1 TRIAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS 有权
标题翻译：三唑Xa因子抑制剂
公开(公告)号：EP1628971A1
公开(公告)日：2006-03-01
申请号：EP04731152.7
申请日：2004-05-05
申请人： Sanofi-Aventis Deutschland GmbH
发明人： NAZARE, Marc , LAUX, Volker , BAUER, Armin , WAGNER, Michael
IPC分类号： C07D413/14 , A61K31/4196 , A61P7/02
CPC分类号： C07D413/14
摘要： The present invention relates to compounds of the formulae (I) and (II), in which RO; R1; R3; Q; J1; J2; J3; J4; J5; V; G and M have the meanings indicated in the claims. The compounds of the formulae (I) and (II) 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 (II), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

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