公开(公告)号：EP2364311A1

公开(公告)日：2011-09-14

申请号：EP09760218.9

申请日：2009-10-27

申请人： SANOFI

发明人： BRAUN, Alain, Jean ,  CRESPIN, Olivier ,  NICOLAI, Eric ,  PASCAL, Cécile ,  VENIER, Olivier

IPC分类号： C07D451/02 ,  C07D451/06 ,  C07D471/08 ,  A61K31/496 ,  A61P3/00 ,  A61P9/00 ,  A61P19/00 ,  A61P25/00

CPC分类号： C07D451/06 ,  C07D451/02 ,  C07D471/08 ,  C07D487/08

摘要： The invention relates to tropane urea derivatives of general formula (I) and to the application thereof as modulators of the activity of 11β-hodroxysteroid dehydrogenose type 1 (11βHSD1).

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.

公开(公告)号：EP2238126B1

公开(公告)日：2014-11-05

申请号：EP09720707.0

申请日：2009-01-27

申请人： SANOFI

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

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：EP2459548B1

公开(公告)日：2014-11-19

申请号：EP10752089.2

申请日：2010-07-23

申请人： SANOFI

发明人： CRESPIN, Olivier ,  NICOLAI, Eric ,  VENIER, Olivier

IPC分类号： C07D401/10 ,  C07D401/12 ,  A61K31/495 ,  A61P3/00

CPC分类号： C07D401/12 ,  C07D401/10

公开(公告)号：EP2459548A1

公开(公告)日：2012-06-06

申请号：EP10752089.2

申请日：2010-07-23

申请人： SANOFI

发明人： CRESPIN, Olivier ,  NICOLAI, Eric ,  VENIER, Olivier

IPC分类号： C07D401/10 ,  C07D401/12 ,  A61K31/495 ,  A61P3/00

CPC分类号： C07D401/12 ,  C07D401/10

摘要： The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, or an –O-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
R2a,b,c are a hydrogen or halogen atom, or an alkyl, cycloalkyl, or –alkyl-cycloalkyl group optionally substituted by one or more halogen atoms, or an -OR
5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, -O-halogenoalkyl, oxo, -CO-alkyl, -CO-alkyl-NR
6 R
7 , -CO-halogenoalkyl, -COOR
5 , alkyl-COOR
5 , -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 , -SO
2 -halogenoalkyl, alkyl-SO
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 group, or further R
1a , R
1b , and R
1c are bonded to R
2a , R
2b , R
2c , respectively, as well as to the carbon atom having same, and are –O-alkyl-O-; R
3 is a hydrogen atom or an alkyl group; R
4 is a –CONR
6 R
7 group, a hydroxyalkyl group substituted by a halogenoalkyl group, or an –alkyl-NH-SO
2 -alkyl, NH-SO
2 -alkyl, -O-SO
2 -NR
6 R
7 , -alkyl-CO-NR
6 R
7 , -O-alkyl-CO-NR
6 R
7 , -alkyl-NR
6 R
7 , -O-CO-NR
6 R
7 , -alkyl-heteroaryl, a heteroaryl group optionally substituted by an alkyl, alkoxy-imino, or –CO-NH-NH-CO-alkyl group, with the proviso that R
4 is in the cis position when it is the –CONR
6 R
7 group and that R
6 and R
7 are each hydrogen, or an –alkyl or –alkyl-phenyl group; R
5 is hydrogen, an –alkyl group, or –alkyl-phenyl; R
6 and R
7 , identical or different, are each a hydrogen atom, an alkyl group, alkoxy, or an alkyl-phenyl group; and R
8 is a hydrogen atom or an –SO
2 -alkyl group, or a group of formula –B-Het, where B can be absent or be a bond, an oxygen atom, or a –CO- or –SO
2 -(CH
2 )
n group, with n being equal to 0, 1, or 2, and where Het is a heteroaryl or heterocycloaryl optionally substituted by the alkyl, -SO
2 -alkyl, and -COOR
5 groups. The invention also relates to a method for preparing same to the therapeutic use thereof.

摘要翻译： 本发明涉及式（I）的化合物，其中：A是键，氧原子或α-O-CH 2 - 基团; Ar 1是苯基或杂芳基; Ar 2是苯基，杂芳基或杂环烷基; R 1a，b，c和R 2a，b，c是氢或卤素原子，或任选被一个或多个卤素原子取代的烷基，环烷基或C 1-6烷基 - 环烷基，或-OR 5（羟基或烷氧基 ），羟烷基，烷氧基烷基，烷氧基烷氧基，卤代烷基，-O-卤代烷基，氧代，-CO-烷基，-CO-烷基-NR 6 R 7，-CO-卤代烷基，-COOR 5，烷基-COOR 5 ，-O-烷基-COOR 5，-SO 2 - 烷基，-SO 2 - 环烷基，-SO 2 - 烷基 - 环烷基，-SO 2 - 烷基-OR 5，-SO 2 - 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-O-烷基-OR 5，-CONR 6 R 7， - 烷基-CORR 6R 7或α-O-烷基-NR 6 R 7基团，或进一步R 1a，R 1b和R 1c分别与R 2a，R 2b，R 2c以及具有相同的碳原子键合， 并且是-O-烷基-O-; R 3是氢原子或烷基; R 4是被一个卤代烷基取代的羟基烷基或一个卤素烷基-NH-SO 2 - 烷基，NH-SO 2 - 烷基，-O-SO 2 -NR 6 R 7， - 烷基-CO-NR 6 R 7，-O-烷基-CO-NR 6 R 7， - 烷基-NR 6 R 7，-O-CO-NR 6 R 7， - 烷基 - 杂芳基， 烷氧基 - 亚氨基或α-CO-NH-NH-CO-烷基，条件是当R 4为“CONR 6R 7”基团时R 4处于顺式位置，且R 6和R 7各自为氢， 或者是一个??烷基或??烷基 - 苯基基团; R 5是氢，一个“烷基”或“烷基 - 苯基”。 R 6和R 7相同或不同，分别为氢原子，烷基，烷氧基或烷基 - 苯基; 和R 8是氢原子或-SO 2 2-烷基或式B 14 -Het的基团，其中B可以不存在或是一个键，氧原子或α1 -CO-或α-CO- SO 2 - （CH 2）n基团，其中n等于0,1或2，并且其中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芳基。 本发明还涉及用于制备其治疗用途的方法。

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：EP1150972A1

公开(公告)日：2001-11-07

申请号：EP00900674.3

申请日：2000-01-28

申请人： SANOFI-SYNTHELABO

发明人： BERTIN, Jean ,  BOVY, Philippe, R. ,  COURTEMANCHE, Gilles ,  CRESPIN, Olivier ,  DEFOSSE, Gérard ,  FETT, Eykmar

IPC分类号： C07D401/12 ,  A61K31/445 ,  C07D249/12 ,  C07D249/10 ,  C07D401/14

CPC分类号： C07D401/12 ,  C07D249/10 ,  C07D249/12 ,  C07D401/14

摘要： The invention concerns compounds of formula (I) wherein: the pair (A, B) represents (N, N), (N, C) or (C, N); n = 0 if A represents a nitrogen atom, if not, n = 1; m = 0 if B represents a nitrogen atom, if not m = 1; R1 and R2 independently of each other, represent a hydrogen atom, a C1-C6 alkyl, a C2-C6 alkenyl, or a cyclo C3-C6 alkyl group; Ar1 represents a phenyl radical or a pyridyl radical substituted by the groups R3, R'3 and R''3; Ar2 represents a phenyl radical substituted by the groups R4 and R' 4', wherein R3, R'3, R''3, R4 and R'4, independently of one another, represent a hydrogen atom, a halogen atom, a C1-C4 alkyl, hydroxy, a C1-C4 alkoxy, a cyano, a nitro, a perfluoro C1-C2 alkyl, an amino, a C1-C4 alkylamino, a di-(C1-C4 alkyl)-amino, a C1-C4 alkoxycarbonyl amino, a (C1-C4 alkoxycarbonyl) (C1-C4 alkyl)-amino, aminosulphonyl, a C1-C4 alkyl-aminosulphonyl or a di(C1-C4 alkyl)-aminosulphonyl group; and their salts, N-oxides and hydrates. Said compounds have therapeutic applications.