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1.发明授权
公开(公告)号：EP2978747B1
公开(公告)日：2017-04-19
申请号：EP14712312.9
申请日：2014-03-26
申请人： SANOFI
发明人： RUF, Sven , SADOWSKI, Thorsten , WIRTH, Klaus , SCHREUDER, Herman , BUNING, Christian , KALLUS, Christopher , STROBEL, Hartmut , WEHLAN, Hermut
IPC分类号： C07D263/32 , C07D271/10 , C07D277/30 , C07D413/10 , A61K31/426 , A61P9/00 , A61P11/08 , A61P19/02 , A61P23/00
CPC分类号： C07D263/32 , C07D271/10 , C07D277/30 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14
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公开(公告)号：EP2104497A2
公开(公告)日：2009-09-30
申请号：EP07856207.1
申请日：2007-11-22
申请人： Sanofi-Aventis
发明人： KALLUS, Christopher , BROENSTRUP, Mark , CZECHTIZKY, Werngard , EVERS, Andreas , FOLLMANN, Markus , HALLAND, Nis , SCHREUDER, Herman
IPC分类号： A61K31/17 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4164 , A61K31/4184 , A61K31/4402 , A61K31/4409 , A61P9/10
CPC分类号： A61K31/4164 , A61K31/17 , A61K31/18 , A61K31/198 , A61K31/223 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4184 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4465 , A61K45/06 , C07C307/06 , C07D207/06 , C07D209/20 , C07D211/34 , C07D211/58 , C07D213/40 , C07D213/55 , C07D213/73 , C07D235/14 , C07D261/08 , C07D295/185 , C07D317/58 , C07D333/20 , C07D487/08 , A61K2300/00
摘要： The invention relates to compounds of formula (I) which are inhibitors of activated thrombin-activatable fibrinolysis inhibitor. Said compounds of formula (I) are suitable for producing medicaments used for the prevention, secondary prevention, and treatment of one or several diseases associated with thromboses, embolisms, hypercoagulability, or fibrotic changes.
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公开(公告)号：EP2104497B1
公开(公告)日：2015-02-25
申请号：EP07856207.1
申请日：2007-11-22
申请人： SANOFI
发明人： KALLUS, Christopher , BROENSTRUP, Mark , CZECHTIZKY, Werngard , EVERS, Andreas , FOLLMANN, Markus , HALLAND, Nis , SCHREUDER, Herman
IPC分类号： A61K31/17 , A61K31/381 , A61K31/40 , A61K31/4164 , A61K31/4184 , A61K31/4402 , A61K31/4409 , A61P9/10 , A61P7/02 , A61K31/18 , A61K31/198 , A61K31/223 , A61K31/4406 , A61K31/4453 , A61K31/4465 , C07D213/74 , C07C307/06 , C07D211/34 , C07D295/185 , C07D213/55
CPC分类号： A61K31/4164 , A61K31/17 , A61K31/18 , A61K31/198 , A61K31/223 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/4184 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4453 , A61K31/4465 , A61K45/06 , C07C307/06 , C07D207/06 , C07D209/20 , C07D211/34 , C07D211/58 , C07D213/40 , C07D213/55 , C07D213/73 , C07D235/14 , C07D261/08 , C07D295/185 , C07D317/58 , C07D333/20 , C07D487/08 , A61K2300/00
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公开(公告)号：EP2978754B1
公开(公告)日：2017-05-10
申请号：EP14712667.6
申请日：2014-03-26
申请人： SANOFI
发明人： RUF, Sven , SADOWSKI, Thorsten , WIRTH, Klaus , SCHREUDER, Herman , BUNING, Christian , KALLUS, Christopher , STROBEL, Hartmut , WEHLAN, Hermut
IPC分类号： C07D413/10 , C07D263/32 , C07D271/10 , C07D277/30 , A61K31/426 , A61P9/00 , A61P11/08 , A61P19/02 , A61P23/00
CPC分类号： C07D271/10 , C07D263/32 , C07D277/30 , C07D413/06 , C07D413/10 , C07D413/14
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公开(公告)号：EP2978754A1
公开(公告)日：2016-02-03
申请号：EP14712667.6
申请日：2014-03-26
申请人： SANOFI
发明人： RUF, Sven , SADOWSKI, Thorsten , WIRTH, Klaus , SCHREUDER, Herman , BUNING, Christian , KALLUS, Christopher , STROBEL, Hartmut , WEHLAN, Hermut
IPC分类号： C07D413/10 , C07D263/32 , C07D271/10 , C07D277/30 , A61K31/426 , A61P9/00 , A61P11/08 , A61P19/02 , A61P23/00
CPC分类号： C07D271/10 , C07D263/32 , C07D277/30 , C07D413/06 , C07D413/10 , C07D413/14
摘要： The present invention relates to compounds of the formula (I), wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
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6.发明授权MACROCYCLIC UREA DERIVATIVES AS INHIBITORS OF TAFI A, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 有权大环脲衍生物作为TAFI A的抑制剂，它们的制备及其作为药物的用途
公开(公告)号：EP3027611B1
公开(公告)日：2017-07-26
申请号：EP14729285.8
申请日：2014-06-05
申请人： SANOFI
IPC分类号： C07D413/12 , C07D273/01 , A61K31/553 , A61P7/00 , A61K45/06 , A61K31/395 , A61K31/4427 , C07D213/75
CPC分类号： C07D273/01 , A61K31/395 , A61K31/4427 , A61K45/06 , C07D213/75 , C07D413/12
摘要： The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments.
摘要翻译： 本发明涉及式I（I）的大环化脲衍生物，其中R 1，R 2，R 3，V和Y如下所定义。 式I化合物是酶TAFIa（活化的凝血酶活化纤维蛋白溶解抑制剂）的抑制剂。 本发明进一步涉及制备式I化合物的方法及其作为药物的用途。
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7.发明公开MACROCYCLIC UREA DERIVATIVES AS INHIBITORS OF TAFI A, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS 有权大环脲衍生物作为的TAFIa，生产抑制剂及其用作药物
公开(公告)号：EP3027611A1
公开(公告)日：2016-06-08
申请号：EP14729285.8
申请日：2014-06-05
申请人： SANOFI
IPC分类号： C07D413/12 , C07D273/01 , A61K31/553 , A61P7/00
CPC分类号： C07D273/01 , A61K31/395 , A61K31/4427 , A61K45/06 , C07D213/75 , C07D413/12
摘要： The present invention relates to macrocydic urea derivatives of the formula I (I) in which R1, R2, R3, V and Y are as defined below. The compounds of the formula I are inhibitors of the enzyme TAFIa (activated thrombin-activatable fibrinolysis inhibitor). The invention further relates to the process for the preparation of the compounds of formula I and to the use thereof as medicaments.
摘要翻译： 本发明涉及其中R1，R2，R3，V和Y是如下面所定义的式I（I）的macrocydic脲衍生物。 的式I化合物是酶的TAFIa（活化的凝血酶激活的纤维蛋白溶解抑制剂）的抑制剂。 本发明还涉及到用于制备式I的化合物的制备和涉及其作为药物。
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8.发明授权
公开(公告)号：EP2300462B1
公开(公告)日：2014-05-21
申请号：EP09757185.5
申请日：2009-05-22
申请人： SANOFI
发明人： KALLUS, Christopher , BROENSTRUP, Mark , EVERS, Andreas , GLOBISCH, Anja , SCHREUDER, Herman , WAGNER, Michael
IPC分类号： C07D413/14 , C07D273/01 , A61K31/553 , A61P7/00
CPC分类号： C07D273/01 , A61K31/395 , C07D267/00 , C07D273/02 , C07D413/12 , C07D413/14
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9.发明公开
公开(公告)号：EP2300462A1
公开(公告)日：2011-03-30
申请号：EP09757185.5
申请日：2009-05-22
申请人： Sanofi-Aventis
发明人： KALLUS, Christopher , BROENSTRUP, Mark , EVERS, Andreas , GLOBISCH, Anja , SCHREUDER, Herman , WAGNER, Michael
IPC分类号： C07D413/14 , C07D273/01 , A61K31/553 , A61P7/00
CPC分类号： C07D273/01 , A61K31/395 , C07D267/00 , C07D273/02 , C07D413/12 , C07D413/14
摘要： The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
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公开(公告)号：EP1937673A1
公开(公告)日：2008-07-02
申请号：EP06792327.6
申请日：2006-09-30
申请人： Sanofi-Aventis
IPC分类号： C07D413/06 , C07D417/06 , A61K31/435 , A61K31/41 , A61P7/02
CPC分类号： C07D413/14 , C07D417/14 , C07D495/04
摘要： The invention relates to compounds of formula (I), which act as inhibitors of activated thrombin activatable fibrinolysis inhibitors (TAFI). The compounds of formula (I) are suitable for the production of medicaments for the prophylaxis, secondary prevention and treatment of diseases that are associated with thromboses, embolisms, hypercoagulability or fibrotic changes.
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