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11. 发明申请

WO2016001197A1 2-(2-METHYLAMINO-PYRIMIDIN-4-YL)-1H-INDOLE-5-CARBOXYLIC ACID [(S)-1-CARBAMOYL-2-(PHENYL-PYRIMIDIN-2-YL-AMINO)-ETHYL]-AMIDE FOR USE IN THE TREATMENT OF PAIN ASSOCIATED TO OSTEOARTHRITIS 审中-公开
标题翻译： 2-（2-甲基氨基吡啶-4-基）-1H-吲哚-5-羧酸[（S）-1-羧基-2-（苯基 - 嘧啶-2-基 - 氨基） - 乙基] - 酰胺，用于用于治疗与OSTEOARTHRITIS相关的疼痛
公开(公告)号：WO2016001197A1
公开(公告)日：2016-01-07
申请号：PCT/EP2015/064794
申请日：2015-06-30
申请人： SANOFI
发明人： PAEHLER, Tobias , FLECHSENHAR, Klaus , GROTHE, Kirsten , LUNNON, Martin , JAN, Christelle
IPC分类号： A61K31/506 , A61P19/02
CPC分类号： A61K31/506 , C07D403/12 , C07D403/14
摘要： 2-(2-methylamino-pyrimidin-4-yl)-1H-indole-5-carboxylic acid [(S)-1-carbamoyl-2- (phenyl-pyrimidin-2-yl-amino)-ethyl]-amide for use in the treatment of pain associated with osteoarthritis in the knee.
摘要翻译： 2-（2-甲基氨基 - 嘧啶-4-基）-1H-吲哚-5-羧酸[（S）-1-氨基甲酰基-2-（苯基 - 嘧啶-2-基 - 氨基） - 乙基] 用于治疗与膝关节骨性关节炎相关的疼痛。

12. 发明申请

WO2013171317A1 PYRAZOLE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS 审中-公开
标题翻译：吡咯衍生物及其作为LPAR5拮抗剂的用途
公开(公告)号：WO2013171317A1
公开(公告)日：2013-11-21
申请号：PCT/EP2013/060171
申请日：2013-05-16
申请人： SANOFI
发明人： NAZARÉ, Marc , KOZIAN, Detlef , EVERS, Andreas , CZECHTIZKY, Werngard
IPC分类号： C07D231/12 , C07D409/04 , A61K31/415 , A61K31/4155 , A61P7/02
CPC分类号： C07D231/12 , A61K31/415 , C07D231/56 , C07D409/04
摘要： The present invention relates to compounds of the formula (I), wherein theresidues R 1 to R 5 , V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in thetreatmentof diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中残基R1至R5，V，G和M具有权利要求中所示的含义。式（I）的化合物是用于治疗多种疾病，例如心血管疾病如血栓栓塞性疾病或再狭窄的有价值的药理学活性化合物。本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化存在或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5的抑制。本发明还涉及式（I）化合物的制备方法，其用途，特别是作为药物中的活性成分，以及包含它们的药物组合物。

13. 发明申请

WO2013171316A1 PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CONDITIONS ASSOCIATED WITH PATHOLOGICAL THROMBUS FORMATION 审中-公开
标题翻译：吡啶衍生物及其在治疗与病理性血栓形成相关的病症中的用途
公开(公告)号：WO2013171316A1
公开(公告)日：2013-11-21
申请号：PCT/EP2013/060169
申请日：2013-05-16
申请人： SANOFI
发明人： NAZARÉ, Marc , KOZIAN, Detlef , EVERS, Andreas , CZECHTIZKY, Werngard
IPC分类号： C07D213/30 , A61K31/4418 , A61P7/02
CPC分类号： C07D213/30
摘要： The present invention relates to compounds of the formula (I), wherein the residues R 1 to R 6 , V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds for use in the treatment of diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present, or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及式（I）化合物，其中残基R1至R6，V，G和M具有权利要求中所示的含义。式I的化合物是用于治疗多种疾病，例如心血管疾病如血栓栓塞性疾病或再狭窄的有价值的药理活性化合物。本发明的化合物是血小板LPA受体LPAR5（GPR92）的有效拮抗剂，通常可以在血小板LPA受体LPAR5，肥大细胞LPA受体LPAR5或小神经胶质细胞LPA受体LPAR5的不希望的活化或用于治疗或预防血小板，肥大细胞或小胶质细胞LPA受体LPAR5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组合物。

14. 发明申请

WO2010136502A1 PROCESS FOR THE PRODUCTION OF DRONEDARONE INTERMEDIATES 审中-公开
标题翻译：生产干粉碎石中间体的方法
公开(公告)号：WO2010136502A1
公开(公告)日：2010-12-02
申请号：PCT/EP2010/057272
申请日：2010-05-26
申请人： SANOFI-AVENTIS , KRETZSCHMAR, Gerhard , KRAFT, Volker , ROSSEN, Kai , GRÄSER, Joachim
发明人： KRETZSCHMAR, Gerhard , KRAFT, Volker , ROSSEN, Kai , GRÄSER, Joachim
IPC分类号： C07D307/80
CPC分类号： C07D307/80
摘要： A process for the production of Dronedarone intermediates of the formula (I), by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-(4-methoxyphenyl)-ethanone, subsequent treatment of the ester with bases and a zeolite (alumosilicate) catalyst and optional subsequent demethylation. This process can be used for the production of Dronedarone.
摘要翻译：通过2-（2-羟基-5-硝基苯基）-1-（4-甲氧基苯基） - 乙酮的酰化生产式（I）的决奈达隆中间体的方法，随后用碱和沸石处理酯（铝硅酸盐）催化剂和任选的随后的脱甲基化。该方法可用于生产决奈达隆。

15. 发明公开

EP2882715A1 PYRAZOLE DERIVATIVES AND THEIR USE AS LPAR5 ANTAGONISTS 失效
标题翻译：吡唑衍生物及其作为LPAR5拮抗剂
公开(公告)号：EP2882715A1
公开(公告)日：2015-06-17
申请号：EP13723151.0
申请日：2013-05-16
申请人： SANOFI
发明人： NAZARÉ, Marc , KOZIAN, Detlef , EVERS, Andreas , CZECHTIZKY, Werngard
IPC分类号： C07D231/12 , C07D409/04 , A61K31/415 , A61K31/4155 , A61P7/02
CPC分类号： C07D231/12 , A61K31/415 , C07D231/56 , C07D409/04
摘要： The present invention relates to compounds of the formula (I), wherein theresidues R
1 to R
5 , V, G and M have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds for use in thetreatmentof diverse disorders, for example cardiovascular disorders like thromboembolic diseases or restenoses. The compounds of the invention are effective antagonists of the platelet LPA receptor LPAR5 (GPR92) and can in general be applied in conditions in which an undesired activation of the platelet LPA receptor LPAR5, the mast cell LPA receptor LPAR5 or the microglia cell LPA receptor LPAR5 is present or for the cure or prevention of which an inhibition of the platelet, mast cell or microglia cell LPA receptor LPAR5 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 medicaments, and pharmaceutical compositions comprising them.

16. 发明授权

EP2558465B1 TRIZYKLISCHE PYRIDYL-VINYL-PYRROLE ALS PAR1-INHIBITOREN 有权
标题翻译：三环吡啶基乙烯基吡咯AS PAR1抑制剂
公开(公告)号：EP2558465B1
公开(公告)日：2014-12-17
申请号：EP11715496.3
申请日：2011-04-14
申请人： SANOFI
发明人： SCHOENAFINGER, Karl , STEINHAGEN, Henning , SCHEIPER, Bodo , HEINELT, Uwe , WEHNER, Volkmar , HERRMANN, Matthias
IPC分类号： C07D471/14 , C07D487/14 , C07D498/14 , A61K31/407 , A61K31/437 , A61K31/4985 , A61K31/5383 , A61P7/02
CPC分类号： C07D471/14 , C07D487/14 , C07D498/14

17. 发明公开

EP2598157A1 CYCLIC PEPTIDES, THEIR PREPARATION AND THEIR USE AS INHIBITORS OF THE PLATELET ADHESION 有权
标题翻译：环肽，它们的生产及其作为THROMBOZYTENADHÄSIONSHEMMER
公开(公告)号：EP2598157A1
公开(公告)日：2013-06-05
申请号：EP11737951.1
申请日：2011-07-27
申请人： SANOFI
发明人： KLINGLER, Otmar , BLUM, Horst , LINDENSCHMIDT, Andreas , MATTER, Hans
IPC分类号： A61K38/12 , C07K7/50
CPC分类号： C07K7/64 , A61K38/00 , C07K7/06 , C07K7/56
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, R14, R15, R16, R17, R18, X1, X2, X3 and X4 have the meanings indicated in the claims, and which 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),and are suitable, for example, for the therapy and prophylaxis of athero-thrombotic diseases. The invention furthermore relates to processes for the preparation of compounds of the Formula (I), their use, in particular as active ingredients in medicaments, and pharmaceutical compositions comprising them.

18. 发明公开

EP2558465A1 TRIZYKLISCHE PYRIDYL-VINYL-PYRROLE ALS PAR1-INHIBITOREN 有权
标题翻译：三环吡啶基乙烯基吡咯AS PAR1抑制剂
公开(公告)号：EP2558465A1
公开(公告)日：2013-02-20
申请号：EP11715496.3
申请日：2011-04-14
申请人： SANOFI
发明人： SCHOENAFINGER, Karl , STEINHAGEN, Henning , SCHEIPER, Bodo , HEINELT, Uwe , WEHNER, Volkmar , HERRMANN, Matthias
IPC分类号： C07D471/14 , C07D487/14 , C07D498/14 , A61K31/407 , A61K31/437 , A61K31/4985 , A61K31/5383 , A61P7/02
CPC分类号： C07D471/14 , C07D487/14 , C07D498/14
摘要： The invention relates to compounds of formula I, where R1, R2, R3, R4, X and Y have the meanings denoted in the claims. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The invention further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.

19. 发明公开

EP2197550A1 USE OF URATE OXIDASE FOR THE TREATMENT OR PROPHYLAXIS OF DISORDERS OR INDIRECT SEQUELAE OF THE HEART CAUSED BY ISCHEMIC OR REPERFUSION EVENTS 审中-公开
标题翻译：尿酸氧化酶可用于治疗或预防疾病或间接使用FOLLOW缺血或再灌注的心
公开(公告)号：EP2197550A1
公开(公告)日：2010-06-23
申请号：EP08785655.5
申请日：2008-08-20
申请人： Sanofi-Aventis
发明人： LINZ, Wolfgang , SCHAEFER, Matthias
IPC分类号： A61P9/10 , C12N9/06
CPC分类号： C12N9/0046 , A61K31/375 , A61K38/00 , C12Y107/03003 , A61K2300/00 , A61K38/44
摘要： The invention relates to the use of a urate oxidase, preferably recombinant urate oxidase, for example rasburicase, for the treatment or prophylaxis of disorders or indirect sequelae of the heart caused by ischemic or reperfusion events, for example during and after cardiac surgery like CABG (coronary artery bypass graft), PCI (percutaneous coronary intervention), transplantation, post myocardial infarction and for the treatment or prophylaxis of coronary artery disease or heart failure, for example congestive heart failure.

20. 发明公开

EP3318563A1 SUBSTITUTED PYRIDO[3,4-B]INDOLES FOR THE TREATMENT OF CARTILAGE DISORDERS 无效
标题翻译：用于治疗软骨病的替代吡啶[3,4-B]吲哚
公开(公告)号：EP3318563A1
公开(公告)日：2018-05-09
申请号：EP16306452.0
申请日：2016-11-07
申请人： SANOFI
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07D471/04 , C07D519/00 , A61K31/437 , A61P19/02
CPC分类号： C07D471/04 , C07D519/00
摘要： Substituted pyrido[3,4-b]indoles and their use as pharmaceuticals
The present invention relates to 8-aryl-substituted and 8-heteroaryl-substituted 9H-pyrido[3,4-b]indoles of the formula I,

in which A, E, G, R 1 to R 6 and R 10 are as defined in the claims, which stimulate chondrogenesis and cartilage matrix synthesis and can be used in the treatment of cartilage disorders and conditions in which a regeneration of damaged cartilage is desired, for example joint diseases such as osteoarthritis. The invention furthermore relates to processes for the synthesis of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
摘要翻译：取代的吡啶并[3,4-b]吲哚及其作为药物的用途本发明涉及式I的8-芳基取代的和8-杂芳基取代的9H-吡啶并[3,4-b]吲哚，其中A ，E，G，R1至R6和R10如权利要求中所定义，其刺激软骨形成和软骨基质合成并可用于治疗需要受损软骨再生的软骨障碍和病症，例如关节疾病如骨关节炎。本发明还涉及合成式I化合物的方法，其作为药物的用途以及包含它们的药物组合物。

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