公开(公告)号：EP1981873A1

公开(公告)日：2008-10-22

申请号：EP07730839.3

申请日：2007-01-22

申请人： Sanofi-Aventis

发明人： DESPEYROUX, Pierre ,  FONTAINE, Evelyne ,  COURTEMANCHE, Gilles ,  ROCHARD, Pierrick ,  SERRADEIL-LE GAL, Claudine

IPC分类号： C07D401/12 ,  C07D207/14 ,  C07D205/04 ,  C07D211/58 ,  A61K31/397 ,  A61K31/4468 ,  A61K31/454 ,  A61P3/04 ,  A61P3/10 ,  A61P25/22 ,  A61P25/18 ,  A61P25/24 ,  A61P25/30 ,  C07C311/44

CPC分类号： C07D403/12 ,  C07C311/29 ,  C07C2601/08 ,  C07D205/04 ,  C07D207/14 ,  C07D211/58 ,  C07D401/14

摘要： The present invention relates to sulphonamide derivatives corresponding to the general formula (I), in which Ar1 represents an aryl optionally substituted with one or more groups, or an optionally substituted heterocyclyl group; T represents a -(CH2)n- or a group (II), Ar2 represents an aryl as optionally substituted with one or more groups, or an optionally substituted heterocyclyl group; Ar3 represents an aryl optionally substituted with one or more groups, or else an optionally substituted heterocyclyl, R1 represents a group of formula (A) or (B): (A) (B) in the form of a base, an addition salt with an acid, a hydrate or a solvate, in the form of enantiomers, diastereoisomers, rotamers or atropoisomers, or mixtures thereof. It also relates to the process for the preparation and also the therapeutic use of the compounds of formula (I).

摘要翻译： 本发明涉及式（I）化合物：其中Ar1，Ar2，Ar3，R1和T如本文所定义，其制备，药物组合物和用作食欲肽2受体拮抗剂。

公开(公告)号：EP1341753B1

公开(公告)日：2007-09-26

申请号：EP01998533.2

申请日：2001-11-30

申请人： Sanofi-Aventis

发明人： BOVY, Philippe, R. ,  CECCHI, Roberto ,  COURTEMANCHE, Gilles ,  OLIVA, Ambrogio ,  VIVIANI, Nunzia ,  CROCI, Tiziano

IPC分类号： C07C311/08 ,  A61K31/195

CPC分类号： C07C311/21 ,  C07C229/46 ,  C07C311/08 ,  C07C317/22 ,  C07C2601/14

摘要： The invention concerns compounds of formula (I), wherein: A is a group of formula (a) or (b), their salts or solvates, pharmaceutical compositions containing them, a method for preparing them and intermediates used in said method. The compounds of formula (I) can be prescribed for treating gastro-intestinal diseases such as inflammatory diseases of the intestine such as irritable colon syndrome (IBS), as modulators of intestinal motricity, as lipolytic agents against obesity, anti-diabetic agents, psychotropic agents, anti-glaucoma agents, healing agents, antidepressants, as uterine contraction inhibitors, as tocolytic agents for preventing or delaying premature deliveries, for treating and/or preventing dysmenorrhea. In addition, the compounds of formula (I) can be used in the treatment of certain diseases of the central nervous system, such as for example depression, and certain disorders of the urinary system such as urinary incontinence.

摘要翻译： 本发明涉及式（I）化合物：其中A是式（a）或（b）的基团，其中R表示氢或卤素原子，-S（O）z（C 1 -C 4） 烷基，-NHSO 2（C 1 -C 4）烷基，-SO 2 NH（C 1 -C 4）烷基，-NHSO 2苯基 - （C 1 -C 4）烷基或-NHSO 2苯基，所述苯基可以被卤素 原子与（C 1 -C 4）烷基或与（C 1 -C 4）烷氧基取代; R1表示氢原子或（C1-C4）烷基，-CO（C1-C4）烷基，苯基 - （C1-C4）烷基或-CO苯基，所述苯基也可以被 卤素原子或与（C1-C4）烷氧基取代; R2是氢原子或-SO2（C1-C4）烷基，-SO2苯基 - （C1-C4）烷基或-SO2苯基; X完成5至8个原子的环，所述环是饱和或不饱和的，可能被一个或两个（C 1 -C 4）烷基取代并带有一个或两个羰基; n，m和z独立地为0,1或2; R3表示氢或卤素原子，（C1-C6）烷基，（C1-C4）烷氧基，-COO（C1-C4）烷基，-CO（C1-C4）烷基， NHSO 2（C 1 -C 4）烷基，-NHSO 2苯基 - （C 1 -C 4）烷基，-NO 2，-CN，-CONR 4 R 5，-COOH或4,5-二氢-1,3-恶唑-2-基 或4,4-二甲基-4,5-二氢-1,3-恶唑-2-基; R 4和R 5独立地表示氢原子，苯基，（C 1 -C 4）烷基或苯基 - （C 1 -C 4）烷基或与其连接的氮原子的R 4和R 5可以形成 总共5至7个原子的环; 以及其盐或溶剂合物，其含有它们的药物组合物，其制备方法和该方法中的中间体。

公开(公告)号：EP1773796A2

公开(公告)日：2007-04-18

申请号：EP05790990.5

申请日：2005-07-20

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  COURTEMANCHE, Gilles ,  CRESPIN, Olivier ,  FETT, Eykmar ,  PASCAL, Cécile

IPC分类号： C07D295/108 ,  C07D451/04 ,  A61K31/445 ,  A61P15/00

CPC分类号： C07D295/104 ,  C07D401/06 ,  C07D405/14 ,  C07D451/04 ,  C07D453/02

摘要： The invention concerns oxopiperidine derivatives of general formula (I) wherein: n = 1; Ra, Ra′, Rb et Rb′ represent hydrogen atoms or alkyl or cycloalkyl groups, or Rb and Rb′ together form a carbon bridge; R1 represents an alkyl or cycloalkyl group; R2 represents a heteroaryl group; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl, -OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR1, -NR-COOR', -NO2, -CN and COOR groups; R5 represents a hydrogen atom or an alkyl group; R4 is selected among the groups of formulae (a), (b) and (c), wherein p = 0, 1, 2 or 3, m = 0, 1 or 2, and X represents a -C(R6)(R7)- or -N(R10)- member. The invention also concerns a method for preparing said derivatives and their therapeutic use.

公开(公告)号：EP1737840A1

公开(公告)日：2007-01-03

申请号：EP05757289.3

申请日：2005-04-13

申请人： Sanofi-Aventis

发明人： AUGEREAU, Jean Michel ,  GESLIN, Michel ,  COURTEMANCHE, Gilles

IPC分类号： C07D401/12 ,  C07D239/32 ,  C07D239/34 ,  C07C65/30 ,  C07C65/32 ,  A61K31/502

CPC分类号： C07D333/22 ,  C07D213/50 ,  C07D237/30 ,  C07D237/32 ,  C07D317/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D451/04

摘要： The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C1-4-alkylene; L = a simple bond or C1-2-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R1 = possibly substituted aryl or heteroaryl; R2, R3 = H, C1-3-alkyl, C1-3-fluoralkyl or R2 et R3 forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R4 = H, C1-5-alkyl, C1-3-fluoralkyl, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-3-alkylene, C1-3-alkyl-O-C1-3-alkylene, HO-C1-3-alkylene, C1-3-alkyl-X-C1-3-alkylene, wherein X = S, SO or S02; or R4 = RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O-, aryl-O-C1-3-alkylene, aryl-C1-3-alkylene-O-C1-3-alkylene, heteroaryl or heteroaryl-C1-3-alkylene; R5 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3-alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R5 = RaRbN-, RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O- or heteroaryl; R6 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, -CN, RaRbN-, RaRbN-C1-3-alkylene, aryl or heteroaryl ; R7 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3--alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R7, = RaRbN-, RaRbN-C1-3--alkylene, ReRbNC(O)-, C1-3-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R8 = H, halogen, C1-5-alkyl, C1-5-alkoxy, C1-3-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.

公开(公告)号：EP1773796B1

公开(公告)日：2010-03-03

申请号：EP05790990.5

申请日：2005-07-20

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  COURTEMANCHE, Gilles ,  CRESPIN, Olivier ,  FETT, Eykmar ,  PASCAL, Cécile

IPC分类号： C07D295/108 ,  C07D451/04 ,  A61K31/445 ,  A61P15/00

CPC分类号： C07D295/104 ,  C07D401/06 ,  C07D405/14 ,  C07D451/04 ,  C07D453/02

摘要： The invention concerns oxopiperidine derivatives of general formula (I) wherein: n = 1; Ra, Ra′, Rb et Rb′ represent hydrogen atoms or alkyl or cycloalkyl groups, or Rb and Rb′ together form a carbon bridge; R1 represents an alkyl or cycloalkyl group; R2 represents a heteroaryl group; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl, -OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR1, -NR-COOR', -NO2, -CN and COOR groups; R5 represents a hydrogen atom or an alkyl group; R4 is selected among the groups of formulae (a), (b) and (c), wherein p = 0, 1, 2 or 3, m = 0, 1 or 2, and X represents a -C(R6)(R7)- or -N(R10)- member. The invention also concerns a method for preparing said derivatives and their therapeutic use.

公开(公告)号：EP1981842A2

公开(公告)日：2008-10-22

申请号：EP07730899.7

申请日：2007-02-01

申请人： sanofi-aventis

发明人： COURTEMANCHE, Gilles ,  DESPEYROUX, Pierre ,  FONTAINE, Evelyne ,  ROCHARD, Pierrick ,  SERRADEIL-LE GAL, Claudine ,  VON ROEDERN, Erich

IPC分类号： C07C311/21 ,  C07C311/29 ,  A61K31/18

CPC分类号： C07C311/29 ,  C07B2200/07 ,  C07D295/13

摘要： The invention concerns sulfonamide derivatives of general formula (I), wherein: Ar1 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl group; T represents a -(CH2)n or a group (A); Ar2 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl group; Ar3 represents an aryl optionally substituted by one or several groups, an optionally substituted heterocyclyl; R represents a hydrogen or a (C1-C4) alkyl; R' represents an optionally substituted (C1-C4) alkyl; a carboxylic acid, a (C1-C4) carboxylate, an optionally substituted carboxamide; in base, acid addition salt, hydrate or solvate form, or in enantiomeric, diastereoisomeric, rotameric, atropoisomeric forms or mixtures thereof. The invention also concerns the preparation method as well as the therapeutic use of the compounds of formula (I).

公开(公告)号：EP1737840B1

公开(公告)日：2007-09-12

申请号：EP05757289.3

申请日：2005-04-13

申请人： Sanofi-Aventis

发明人： AUGEREAU, Jean Michel ,  GESLIN, Michel ,  COURTEMANCHE, Gilles

IPC分类号： C07D401/12 ,  C07D239/32 ,  C07D239/34 ,  C07C65/30 ,  C07C65/32 ,  A61K31/502

CPC分类号： C07D333/22 ,  C07D213/50 ,  C07D237/30 ,  C07D237/32 ,  C07D317/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D451/04

摘要： The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C1-4-alkylene; L = a simple bond or C1-2-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R1 = possibly substituted aryl or heteroaryl; R2, R3 = H, C1-3-alkyl, C1-3-fluoralkyl or R2 et R3 forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R4 = H, C1-5-alkyl, C1-3-fluoralkyl, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-3-alkylene, C1-3-alkyl-O-C1-3-alkylene, HO-C1-3-alkylene, C1-3-alkyl-X-C1-3-alkylene, wherein X = S, SO or S02; or R4 = RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O-, aryl-O-C1-3-alkylene, aryl-C1-3-alkylene-O-C1-3-alkylene, heteroaryl or heteroaryl-C1-3-alkylene; R5 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3-alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R5 = RaRbN-, RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O- or heteroaryl; R6 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, -CN, RaRbN-, RaRbN-C1-3-alkylene, aryl or heteroaryl ; R7 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3--alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R7, = RaRbN-, RaRbN-C1-3--alkylene, ReRbNC(O)-, C1-3-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R8 = H, halogen, C1-5-alkyl, C1-5-alkoxy, C1-3-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.

摘要翻译： 通式（I）的1-氨基 - 酞嗪衍生物，其中取代基如本文所定义。 还公开了制备这种化合物的方法，用于这种方法的中间体和使用式（I）化合物的医疗处理。

公开(公告)号：EP1786809A2

公开(公告)日：2007-05-23

申请号：EP05790800.6

申请日：2005-07-20

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  CORNET, Bruno ,  COURTEMANCHE, Gilles ,  CRESPIN, Olivier ,  FETT, Eykmar ,  PASCAL, Cécile

IPC分类号： C07D451/04 ,  C07D453/02 ,  A61K31/4468 ,  A61K31/439 ,  C07D401/12 ,  C07D405/12 ,  C07D401/14 ,  A61P15/10 ,  C07D211/58

CPC分类号： C07D211/58 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D451/04 ,  C07D453/02

摘要： The invention concerns aminopiperidine derivatives of general formula (I) wherein: Ra, Ra' and R5 represent hydrogen atoms or alkyl groups; R1 represent a hydrogen atom and an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl or NR 11R12 group, Y being other than a hydrogen atom when x = y = 0; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl, -OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and COOR groups; R4 is selected among groups of formula (a), (b) and (c), wherein p = 0, 1, 2 or 3, m = 0, 1 or 2; X represents an oxygen or sulphur atom or a -C(R 6)(R7)- or -N(R10)- member. The invention also concerns a method for preparing said derivatives and their therapeutic use as melanocortin receptor agonists for treating obesity, diabetes, sexual dysfunction.

公开(公告)号：EP1776347A1

公开(公告)日：2007-04-25

申请号：EP05796062.7

申请日：2005-08-02

申请人： Sanofi-Aventis

发明人： COURTEMANCHE, Gilles ,  DESPEYROUX, Pierre ,  FONTAINE, Evelyne ,  ROCHARD, Pierrick ,  SERRADEIL LE GAL, Claudine

IPC分类号： C07D233/66

CPC分类号： C07D213/42 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D217/06 ,  C07D233/64 ,  C07D257/04 ,  C07D271/06 ,  C07D277/28 ,  C07D317/62 ,  C07D319/18 ,  C07D333/20

摘要： The invention concerns sulphonamide derivatives of general formula (I), in base, acid addition salt, hydrate or solvate form, or enantiomeric, diastereoisomeric, atropoisomeric rotameric forms or mixtures thereof. The invention also concerns the method for the preparation and the therapeutic use of the compounds of formula (I).

公开(公告)号：EP1773829B1

公开(公告)日：2008-12-17

申请号：EP05790816.2

申请日：2005-07-20

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  CORNET, Bruno ,  COURTEMANCHE, Gilles ,  CRESPIN, Olivier ,  PASCAL, Cécile

IPC分类号： C07D451/04 ,  A61K31/46 ,  A61K31/55 ,  A61P3/04 ,  A61P3/10 ,  A61P15/00

CPC分类号： C07D451/04

摘要： The invention concerns amino-tropane derivatives of general formula (I), wherein: Ra R a' et R5 represent hydrogen atoms or alkyl groups; R1 represents a hydrogen atom or an alkyl, cycloalkyl, heterocycloalkyl or aryl group; R2 represents a group of formula -(CH2)x-(CO)y-Y or -(CO)y-(CH2)x-Y, wherein Y represents a hydrogen atom or a hydroxy, alkyl, cycloalkyl, alkoxy, aryl, heteroaryl group or NR11R12; R3 represents 1 to 3 groups selected among halogen atoms and alkyl, cycloalkyl OR, -NRR', -CO-NRR', -NR-CO-R', -NR-CO-NRR', -NR-COOR', -NO2, -CN and -COOR groups; R4 is selected among a group of formula (a), (b), (c) or (d): or a group of formula -A-R18, -A-CH=N-R19, -A-N(R20)-A'-R19, -A-CO-N(R2O)-A'-R19, -A-CH(NH2)-R19, -A-N(R20)-COO-A' or -(CH2)r-heteroaryl. The invention also concerns a method for preparing said derivatives and the therapeutic use thereof.