公开(公告)号：EP1773829A1

公开(公告)日：2007-04-18

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.

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：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：EP2238126A2

公开(公告)日：2010-10-13

申请号：EP09720707.0

申请日：2009-01-27

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  CRESPIN, Olivier ,  NAMANE, Claudie ,  NICOLAI, Eric ,  PACQUET, François ,  PASCAL, Cécile ,  PHILIPPO, Christophe ,  VENIER, Olivier

IPC分类号： C07D401/12 ,  C07D401/10 ,  C07D417/04 ,  A61K31/495 ,  A61K31/506 ,  A61P3/00 ,  A61P9/12 ,  A61P25/28 ,  A61P27/06

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-CH
2 - group; Ar
1 is a phenyl or heteroaryl group; Ar
2 is a phenyl, heteroaryl or heterocycloalkyl group; R
1a,b,c and R
2a,b,c are a hydrogen or halogen atom or an alkyl, cycloalkyl, -alkyl-cycloalkyl group optionally substituted by one or more halogen atoms, -OR
5 (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- COOR
5, -SO
2 -alkyl, -SO
2 -cycloalkyl, -SO
2 -alkyl-cycloalkyl, -SO
2 -alkyl-OR
5 , -SO
2 - alkyl-COOR
5, -SO
2 -alkyl-NR
6 R
7 -S0
2 -halogenoalkyl, alkyl-S0
2 -alkyl, -SO
2 -NR
6 R
7, - SO
2 -alkyl-O-alkyl-OR
5 , -CONR
6 R
7 , -alkyl-CONR
6 R
7 or -O-alkyl-NR
6 R
7 , or R
1a R
1b , R
1c are respectively bonded to R
2a, R
2b, R
2c and to the carbon atom bearing them and represent -O-alkyl-0-; R
3 is a hydrogen atom or an alkyl group; R
4 is a hydrogen or halogen atom or a cyano group, -OR
5, hydroxy-alkyl, -COOR
5 , -NR
6 R
7 , -CONR
6 R
7, -SO
2 -alkyl or -SO
2 -NR
6 R
7 , -NR
6 - COOR
5 , -NR
6 -COR
5, -CO-NR
6 -alkyl-OR
5 ;; R
5 , R
6 and R
7 are a hydrogen atom, an alkyl or –alkyl-phenyl group; and R
8 is a hydrogen atom, a -SO
2 -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 -SO
2 - (CH
2 )n group with n equal to 0, 1 or 2, and Het is a heteroaryl or heterocycloalkyl optionally substituted by alkyl, -SO
2 -alkyl and - COOR
5 groups. The invention also relates to a method for making the same and to the therapeutic application thereof.

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：EP2044057A2

公开(公告)日：2009-04-08

申请号：EP07803781.9

申请日：2007-06-26

申请人： Sanofi-Aventis

发明人： BRAUN, Alain ,  GUSSREGEN Stefan ,  MOUGENOT, Patrick ,  NAMANE, Claudie ,  NICOLAI, Eric ,  PACQUET, François ,  PHILIPPO, Christophe ,  VENIER, Olivier ,  CRESPIN, Olivier ,  PASCAL, Cécile ,  ALETRU, Michel

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D401/06 ,  C07D417/14 ,  A61K31/4709 ,  A61K31/536 ,  A61P3/00

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 R1a, R1b, R1c, R1d, R2a, R2b, R2c, R2d, R3a, R3b, R4, n, i, j, o, p, q, r and X are as defined in the description. Preparation method and therapeutic use.

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.