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1. 发明申请

WO2007071840A3 COMPOUNDS BASED ON FOUR AROMATIC RINGS, PREPARATION AND USES THEREOF 审中-公开
标题翻译：基于四种芳香环的化合物，其制备和用途
公开(公告)号：WO2007071840A3
公开(公告)日：2007-08-09
申请号：PCT/FR2006002773
申请日：2006-12-18
申请人： CEREP , BOTEZ IULIANA , NICOLAI ERIC , GOURLAOUEN NELLY , DAVID-BASEI CHRISTELLE , BALAVOINE FABRICE , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
发明人： BOTEZ IULIANA , NICOLAI ERIC , GOURLAOUEN NELLY , DAVID-BASEI CHRISTELLE , BALAVOINE FABRICE , SERRADEIL-LE GAL CLAUDINE , VALETTE GERARD
IPC分类号： C07D471/04 , A61K31/431 , A61K31/4439 , A61P3/00 , A61P9/00 , C07D401/06 , C07D401/14 , C07D403/12 , C07D413/06 , C07D413/12 , C07D417/14
CPC分类号： C07D401/06 , C07D207/335 , C07D209/08 , C07D209/14 , C07D211/46 , C07D231/12 , C07D401/14 , C07D403/06 , C07D405/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/113
摘要： The present invention relates to novel compounds, to the preparation thereof and to uses, in particular therapeutic uses, thereof. It relates more particularly to derived compounds which have at least four aromatic rings, to the preparation thereof and to uses thereof, in particular in the field of human or animal health. These compounds have in particular a certain affinity for neuropeptide Y, NPY, biological receptors, and more particularly for NPY Y1 receptors, present in the central and peripheral nervous systems. The compounds according to the invention are preferably NPY antagonists, and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also relates to pharmaceutical compositions comprising such compounds, to the preparation thereof and to uses thereof, and also to methods of treatment using said compounds.
摘要翻译：本发明涉及新化合物，其制备和用途，特别是其治疗用途。本发明更具体地涉及具有至少四个芳香环的衍生化合物，其制备及其用途，特别是在人类或动物健康领域。这些化合物对神经肽Y，NPY，生物受体特别是对中枢和外周神经系统中存在的NPY Y1受体具有特定的亲和力。根据本发明的化合物优选为NPY拮抗剂，因此可以用于任何涉及NPY的病症的治疗或预防性治疗。本发明还涉及包含此类化合物的药物组合物，其制备方法及其用途，以及使用所述化合物的治疗方法。

2. 发明申请

WO2006108965A2 NPY ANTAGONISTS, PREPARATION AND USE 审中-公开
标题翻译： NPY拮抗剂，制备和使用
公开(公告)号：WO2006108965A2
公开(公告)日：2006-10-19
申请号：PCT/FR2006000829
申请日：2006-04-14
申请人： CEREP , BOTEZ IULIANA , DAVID-BASEI CHRISTELLE , GOURLAOUEN NELLY , NICOLAI ERIC , BALAVOINE FABRICE , VALETTE GERARD , SERRADEIL-LE GAL CLAUDINE
发明人： BOTEZ IULIANA , DAVID-BASEI CHRISTELLE , GOURLAOUEN NELLY , NICOLAI ERIC , BALAVOINE FABRICE , VALETTE GERARD , SERRADEIL-LE GAL CLAUDINE
CPC分类号： C07D295/088 , C07D211/42 , C07D211/46 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D453/06 , C07D471/08
摘要： The invention relates to novel compounds, to the preparation and use thereof, in particular therapeutic. Said invention particularly relates to derived compounds comprising at least two aromatic cycles, to the preparation and use thereof, mainly for human and animal health care. Said compounds exhibit an affinity to biological receptors Y and NPY of a neuropeptide Y which are present in the central and peripheral nervous systems. The inventive compounds are preferably embodied in the form NPY antagonists, and more particularly in the form of NPY Y1 subtype antagonists and, whereby are usable in therapeutic or prophylactic treatment all NPY involving disorders. Pharmaceutical compositions comprising said compounds, the preparation and the use thereof and treating methods using said compounds are also disclosed.
摘要翻译：本发明涉及新化合物，其制备和用途，特别是治疗剂。所述发明特别涉及包含至少两个芳族循环的衍生化合物，其制备和用途主要用于人和动物保健。所述化合物对存在于中枢和外周神经系统中的神经肽Y的生物受体Y和NPY表现出亲和力。本发明化合物优选以NPY拮抗剂形式，更具体地以NPY Y1亚型拮抗剂的形式实施，由此可用于治疗或预防性治疗所有涉及疾病的NPY。还公开了包含所述化合物的药物组合物，其制备及其用途和使用所述化合物的治疗方法。

3. 发明申请

WO2007012661A8 HYDANTOIN DERIVED COMPOUNDS AND USE THEREOF AS MCHR-1 ANTAGONISTS 审中-公开
标题翻译： HYDANTOIN衍生化合物及其作为MCHR-1拮抗剂的用途
公开(公告)号：WO2007012661A8
公开(公告)日：2007-03-29
申请号：PCT/EP2006064747
申请日：2006-07-27
申请人： CEREP , BALAVOINE FABRICE , NICOLAI ERIC , SARTORI ERIC
发明人： BALAVOINE FABRICE , NICOLAI ERIC , SARTORI ERIC
IPC分类号： A61P3/04 , A61K31/4164
CPC分类号： C07D233/78 , C07D401/04 , C07D401/12 , C07D403/04 , C07D487/04 , C07D491/10
摘要： The invention concerns compounds of general formula (I) wherein: Ar 1 , L 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , L 2 , Q, and n are such as defined in the claims, as well as the method for preparing same. The invention also concerns the use of the compounds of formula (I) as medicine, and more particularly for preparing a medicine for treating obesity and related diseases, an anorexiant and/or a medicine for losing weight, a medicine for treating depression and/or anxiety, and more generally a medicine for treating a disease associated with MHC (melanin-concentrating hormone ) receptors.
摘要翻译：本发明涉及通式（I）的化合物，其中：Ar 1，L 1，R 1，R 2，，R 3，R 4，R 5，R 6，L 2，...， >，Q和n如权利要求中所定义，以及其制备方法。本发明还涉及式（I）化合物作为药物，特别是制备用于治疗肥胖症和相关疾病的药物，减肥剂和/或减肥药物的用途，用于治疗抑郁症和/或焦虑症，更通常地是用于治疗与MHC（黑色素浓缩激素）受体相关的疾病的药物。

4. 发明申请

WO2007012670A2 COMPOUNDS DERIVED FROM 5-BENZYLIDENE IMIDAZOLIDINE 2,4-DIONE AND THEIR USE AS MCHR-1 ANTAGONISTS 审中-公开
标题翻译：衍生自5-苄氧基咪唑啉2,4-二酮的化合物及其作为MCHR-1拮抗剂的用途
公开(公告)号：WO2007012670A2
公开(公告)日：2007-02-01
申请号：PCT/EP2006064793
申请日：2006-07-28
申请人： CEREP , BALAVOINE FABRICE , NICOLAI ERIC , SARTORI ERIC
发明人： BALAVOINE FABRICE , NICOLAI ERIC , SARTORI ERIC
IPC分类号： C07D233/96 , A61K31/4178 , A61K31/4453 , A61K31/5377 , A61K31/55 , A61P3/00 , C07D403/10
CPC分类号： C07D233/96 , C07D403/10
摘要： The invention concerns the compounds of general formula (I), wherein: Ar 1 , L 1 , R 1 , R 2 , R 3 , R 4 R 5 , R 6 , L 2 , Q, and n are such as defined in the claims, and their preparation method. The invention also concerns the use of the compounds of formula (I) as medicine, and more particularly for preparing a medicine for treating obesity and related diseases, an anorexiant and/or a medicine for losing weight, a medicine for treating depression and/or anxiety, and more generally a medicine for treating a disease associated with MCH (melanin-concentrating hormone) receptors.
摘要翻译：本发明涉及通式（I）的化合物，其中：Ar 1，L 1，R 1，R 2， R 3，R 4，R 4，R 5，R 6，L 2， SUP，Q和n如权利要求书中所定义，及其制备方法。本发明还涉及式（I）化合物作为药物，更具体地涉及制备用于治疗肥胖症和相关疾病的药物，减肥药和/或减肥药物的用途，用于治疗抑郁症和/或焦虑症，更通常地是用于治疗与MCH（黑色素浓缩激素）受体相关的疾病的药物。

5. 发明申请

WO2004018436A3 COMPOUNDS DERIVED FROM ARYL CARBAMATES, PREPARATION THEREOF AND USES OF SAME 审中-公开
标题翻译：衍生自ARYL CARBAMATES的化合物，其制备方法及其用途
公开(公告)号：WO2004018436A3
公开(公告)日：2004-04-15
申请号：PCT/FR0302564
申请日：2003-08-22
申请人： CEREP , MAILLET MAGALI , SANIERE LAURENT , NICOLAI ERIC , POTIN DOMINIQUE , LANGLOIS MICHEL , LAUNAY MICHELE
发明人： MAILLET MAGALI , SANIERE LAURENT , NICOLAI ERIC , POTIN DOMINIQUE , LANGLOIS MICHEL , LAUNAY MICHELE
IPC分类号： A61P1/00 , A61P9/00 , A61P9/06 , A61P13/00 , A61P15/00 , A61P25/00 , C07D207/09 , C07D207/16 , C07D207/34 , C07D207/40 , C07D207/416 , C07D209/18 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/78 , C07D213/69 , C07D213/74 , C07D213/82 , C07D215/48 , C07D215/54 , C07D239/38 , C07D241/20 , C07D241/24 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/215 , C07D307/14 , C07D307/24 , C07D317/66 , C07D317/68 , C07D333/20 , C07D333/38 , C07D401/04 , C07D521/00 , A61K31/445 , A61K31/495 , C07D207/22 , C07D295/12 , C07D295/14 , C07D295/18 , C07D295/20 , C07D307/68 , C07D471/04
CPC分类号： C07D207/416 , C07D207/09 , C07D207/16 , C07D207/34 , C07D209/18 , C07D209/42 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/78 , C07D213/69 , C07D213/74 , C07D213/82 , C07D215/48 , C07D215/54 , C07D231/12 , C07D233/56 , C07D239/38 , C07D241/20 , C07D241/24 , C07D249/08 , C07D295/088 , C07D295/13 , C07D295/135 , C07D295/215 , C07D307/14 , C07D307/24 , C07D317/66 , C07D317/68 , C07D333/20 , C07D333/38 , C07D401/04
摘要： The invention relates to novel compounds, the preparation thereof and the uses, particularly therapeutic, of same. More specifically, the invention relates to compounds derived from aryl carbamates, the preparation thereof and the uses of same, particularly in the human and animal health field. The inventive compounds are preferably 5-HT4 serotoninergic receptor ligands and thus can be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions containing such compounds, the preparation thereof and uses of same as well as to treatment methods using said compounds.
摘要翻译：本发明涉及新化合物，其制备方法及其用途，特别是其治疗用途。更具体地，本发明涉及衍生自芳基氨基甲酸酯的化合物，其制备方法及其用途，特别是在人类和动物健康领域。本发明化合物优选为5-HT4血清素能受体配体，因此可用于治疗或预防性治疗涉及5-HT4受体的任何疾病。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用途以及使用所述化合物的治疗方法。

6. 发明申请

WO02068399B1 ARYL CARBAMATE DERIVATIVES, PREPARATION AND USE THEREOF 审中-公开
标题翻译： ARYL CARBAMATE衍生物，其制备和使用
公开(公告)号：WO02068399B1
公开(公告)日：2003-02-20
申请号：PCT/FR0200668
申请日：2002-02-22
申请人： CEREP , CENTRE NAT RECH SCIENT , INST NAT SANTE RECH MED , NICOLAI ERIC , CURTET SOPHIE , SICSIC JAMES , LEZOUALC H FRANK , FISCHMEISTER RODOLPHE , LANGLOIS MICHEL , MAILLET MAGALI , LAUNAY MICHELE
发明人： NICOLAI ERIC , CURTET SOPHIE , SICSIC JAMES , LEZOUALC H FRANK , FISCHMEISTER RODOLPHE , LANGLOIS MICHEL , MAILLET MAGALI , LAUNAY MICHELE
IPC分类号： C07D295/08 , A61K31/381 , A61K31/404 , A61K31/433 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/519 , A61P1/00 , A61P9/00 , A61P13/00 , A61P25/00 , A61P43/00 , C07D209/08 , C07D213/74 , C07D213/79 , C07D213/84 , C07D213/85 , C07D235/04 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/08 , C07D285/10 , C07D295/088 , C07D333/42 , C07D401/04 , C07D403/04 , C07D487/04 , C07D495/04 , A61K31/445 , C07D295/12 , C07D295/14
CPC分类号： C07D213/74 , C07D213/79 , C07D213/84 , C07D237/20 , C07D239/42 , C07D241/20 , C07D285/10 , C07D295/088 , C07D333/42 , C07D401/04 , C07D403/04
摘要： The invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, the invention relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. According to the invention, the compounds are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.
摘要翻译：本发明涉及新化合物，其制备和用途，特别是其治疗方法。更具体地，本发明涉及衍生自芳基氨基甲酸酯的化合物，其制备和用途，特别是在人和动物健康领域。根据本发明，化合物优选为5-HT4血清素能受体配体，因此可用于治疗或预防性治疗涉及5-HT4受体的任何疾病。本发明还涉及包含这些化合物的药物组合物，其制备和用途以及使用所述化合物的治疗方法。

7. 发明申请

WO2008000951A2 UREA DERIVATIVES OF TROPANE, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION 审中-公开
标题翻译：特罗烷的尿素衍生物，它们的制备和它们的治疗应用
公开(公告)号：WO2008000951A2
公开(公告)日：2008-01-03
申请号：PCT/FR2007001070
申请日：2007-06-26
申请人： SANOFI AVENTIS , ALETRU MICHEL , BRAUN ALAIN , NAMANE CLAUDIE , VENIER OLIVIER , PHILIPPO CHRISTOPHE , MOUGENOT PATRICK , NICOLAI ERIC , GUSSREGEN STEFAN
发明人： ALETRU MICHEL , BRAUN ALAIN , NAMANE CLAUDIE , VENIER OLIVIER , PHILIPPO CHRISTOPHE , MOUGENOT PATRICK , NICOLAI ERIC , GUSSREGEN STEFAN
IPC分类号： C07D471/08 , A61K31/4709 , A61P3/04 , A61P3/10 , A61P9/10 , A61P25/28 , C07D207/09 , C07D211/18 , C07D213/54 , C07D215/08
CPC分类号： C07D471/08
摘要： The invention relates to compounds of the formula (I): in which R 1a , R 1b , R 1c , R 1d , R 2a , R 2b , R 3 , R 4 , p, r and X are as defined in the description. Preparation process and therapeutic application.
摘要翻译：本发明涉及式（I）的化合物：其中R 1a，R 1b，1b，1c，1d，1d， R 2，R 2，R 2，R 3，R 4，p，r和X是如描述中所定义的。制备过程和治疗应用。

8. 发明申请

WO2009112691A3 DERIVATIVES OF TETRAHYDROQUINOXALINE UREA, PREPARATION THEREOF AND THERAPEUTIC APPLICATION THEREOF 审中-公开
标题翻译：四氢喹诺酮尿素衍生物，其制备方法及其应用
公开(公告)号：WO2009112691A3
公开(公告)日：2010-01-07
申请号：PCT/FR2009000083
申请日：2009-01-27
申请人： SANOFI AVENTIS , BRAUN ALAIN , CRESPIN OLIVIER , NAMANE CLAUDIE , NICOLAI ERIC , PACQUET FRANCOIS , PASCAL CECILE , PHILIPPO CHRISTOPHE , VENIER OLIVIER
发明人： BRAUN ALAIN , CRESPIN OLIVIER , NAMANE CLAUDIE , NICOLAI ERIC , PACQUET FRANCOIS , PASCAL CECILE , PHILIPPO CHRISTOPHE , VENIER OLIVIER
IPC分类号： C07D401/12 , A61K31/495 , A61K31/506 , A61P3/00 , A61P9/12 , A61P25/28 , A61P27/06 , C07D401/10 , C07D417/04
CPC分类号： C07D239/26 , C07D241/44 , C07D401/10 , C07D401/12
摘要： The invention relates to compounds of the formula (I) in which: A is a bond, an oxygen atom, or a -0-CH2- group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl or heterocycloalkyl group; R1a,b,c and R2a,b,c are a hydrogen or halogen atom or an alkyl, cycloalkyl, -alkyl-cycloalkyl group optionally substituted by one or more halogen atoms, -OR5 (hydroxy ou alkoxy), hydroxy- alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, -O-halogenoalkyl, oxo, -CO- alkyl, -CO-alkyl-NR6R7, -CO-halogenoalkyl, -COOR5, alkyl-COOR5, -O-alkyl- COOR5, -SO2-alkyl, -SO2-cycloalkyl, -SO2-alkyl-cycloalkyl, -SO2-alkyl-OR5, -SO2- alkyl-COOR5, -SO2-alkyl-NR6R7 -S02-halogenoalkyl, alkyl-S02-alkyl, -SO2-NR6R7, - SO2-alkyl-O-alkyl-OR5, -CONR6R7, -alkyl-CONR6R7 or -O-alkyl-NR6R7, or R1a R 1b, R 1c are respectively bonded to R2a, R2b, R 2c and to the carbon atom bearing them and represent -O-alkyl-0-; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano group, -OR5, hydroxy-alkyl, -COOR5, -NR6R7, -CONR6R7, -SO2-alkyl or -SO2-NR6R7, -NR6- COOR5, -NR6-COR5, -CO-NR6-alkyl-OR5;; R5, R6 and R7 are a hydrogen atom, an alkyl or -alkyl-phenyl group; and R8 is a hydrogen atom, a -SO2-alkyl group or a group of the formula -B-Het in which B can be absent or represents a bond, an oxygen atom or a -CO- ou -SO2- (CH2)n group with n equal to 0, 1 or 2, and Het is a heteroaryl or heterocycloalkyl optionally substituted by alkyl, -SO2-alkyl and - COOR5 groups. The invention also relates to a method for making the same and to the therapeutic application thereof.
摘要翻译：本发明涉及式（I）化合物，其中：A为键，氧原子或-O-CH 2 - 基; Ar1是苯基或杂芳基; Ar 2是苯基，杂芳基或杂环烷基; R1a，b，c和R2a，b，c是氢或卤原子或任选被一个或多个卤素原子取代的烷基，环烷基， - 烷基 - 环烷基，-OR 5（羟基烷氧基），羟基 - 烷基，烷氧基 - 烷基，COOR 5，-O-烷基-COOR 5，-SO 2 - ， - C 1-4烷基，烷基-COOR 5，-SO 2 - 烷基-NR 6 R 7 -SO 2 - 卤代烷基，烷基-SO 2 - 烷基，-SO 2 -NR 6 R 7，-SO 2 - 烷基， -SO 2烷基-O-烷基-OR 5，-CONR 6 R 7， - 烷基-CONR 6 R 7或-O-烷基-NR 6 R 7，或R 1a，R 1b，R 1c分别与R 2a，R 2b，R 2c和带有它们的碳原子键合并代表-O-烷基-O- R3是氢原子或烷基; R4是氢或卤素原子或氰基，-OR5，羟基 - 烷基，-COOR5，-NR6R7，-CONR6R7，-SO2-烷基或-SO2-NR6R7，-NR6-COOR5，-NR6-COR5， - -NR6 - 烷基 - OR5 ;; R5，R6和R7是氢原子，烷基或 - 烷基 - 苯基; 并且R 8是氢原子，-SO 2 - 烷基或式B-Het的基团，其中B可以不存在或表示键，氧原子或-CO- -SO 2 - （CH 2）n n等于0,1或2，Het是任选被烷基，-SO 2 - 烷基和-COOR 5基团取代的杂芳基或杂环烷基。本发明还涉及其制备方法及其治疗应用。

9. 发明申请

WO2008000950A3 DERIVATIVES OF UREAS OF PIPERIDINE OR PYRROLIDINE, THEIR PREPARATION AND THEIR THERAPEUTICAL USE 审中-公开
标题翻译：哌啶或吡咯烷脲的衍生物，它们的制备及其治疗用途
公开(公告)号：WO2008000950A3
公开(公告)日：2008-02-14
申请号：PCT/FR2007001069
申请日：2007-06-26
申请人： SANOFI AVENTIS , BRAUN ALAIN , GUSSREGEN STEFAN , MOUGENOT PATRICK , NAMANE CLAUDIE , NICOLAI ERIC , PACQUET FRANCOIS , PHILIPPO CHRISTOPHE , VENIER OLIVIER , CRESPIN OLIVIER , PASCAL CECILE , ALETRU MICHEL
发明人： BRAUN ALAIN , GUSSREGEN STEFAN , MOUGENOT PATRICK , NAMANE CLAUDIE , NICOLAI ERIC , PACQUET FRANCOIS , PHILIPPO CHRISTOPHE , VENIER OLIVIER , CRESPIN OLIVIER , PASCAL CECILE , ALETRU MICHEL
IPC分类号： C07D401/14 , A61K31/4709 , A61K31/536 , A61P3/00 , C07D401/06 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14 , C07D401/06 , C07D403/06 , C07D403/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/14
摘要： The invention concerns compounds corresponding to formula (I) in which R 1a , R 1b , R 1c , R 1d , R 2a , R 2b , R 2c , R 2d , R 3a , R 3b , R 4 , n, i, j, o, p, q, r and X are as defined in the description. Preparation method and therapeutic use.
摘要翻译：本发明涉及对应于式（I）的化合物，其中R 1a，R 1b，1b，1c，1d R 2，R 2，R 2，R 3，R 3，R 3，R 3，R 3，其中，R，R，R，X，R，R和X如说明书中所定义。制备方法和治疗用途。

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