公开(公告)号：US07294628B2

公开(公告)日：2007-11-13

申请号：US10516808

申请日：2003-06-05

申请人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

发明人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

IPC分类号： A61K31/497 ,  A61K31/4965 ,  C07D241/04 ,  C07D295/00

CPC分类号： C07D417/14 ,  C07D401/14

摘要： The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.

摘要翻译： 本发明涉及通式（I）的取代的1-哌嗪基酰基哌啶衍生物，其中n为1或2; R 1表示卤素原子; 三氟甲基; （C 1 -C 4 -C 4）烷基; （C 1 -C 4 -C 4）烷氧基; 三氟甲氧基; R 2表示氢原子或卤素原子; R 3代表氢原子; 一个基团-OR 5; 基团-CH 2或OR 5; 基团-NR 6 R 7; 基团-NR 8 COR 9; 基团-NR 8 CONR 10 R 11; 基团-CH 2 NR 12 R 13; 基团-CH 2 NR 8 CONR 14 R 15 15; （C 1 -C 4 -C 4）烷氧基羰基; 基团-CONR 16 R 17 R 17; 或者R 3 3在其所连接的碳原子和哌啶环的相邻碳原子之间构成双键; R 4代表下式的芳族基团1,3-噻唑-2-基：制备方法和治疗应用。

公开(公告)号：US07468368B2

公开(公告)日：2008-12-23

申请号：US10516704

申请日：2003-06-05

申请人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

发明人： Françoise Bono ,  Michaël Bosch ,  Victor Dos Santos ,  Jean-Marc Herbert ,  Dino Nisato ,  Bernard Tonnerre ,  Jean Wagnon

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D241/04 ,  C07D401/00 ,  C07D403/00

CPC分类号： C07D417/14 ,  C07D401/14

摘要： The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.

摘要翻译： 本发明涉及通式（I）的取代的1-哌嗪基酰基哌啶衍生物，其中n为1或2; p为1或2; R1表示卤素原子; 三氟甲基; （C1-C4）烷基; （C 1 -C 4）烷氧基; 三氟甲氧基; R2表示氢原子或卤素原子; R3表示氢原子; 一组-OR5; 基团-CH 2 OR 5; 基团-NR 6 R 7; 一个-NR8COR9基团; 一组-NR8CONR10R11; 基团-CH 2 NR 12 R 13; 基团-CH2NR8CONR14R15; （C1-C4）烷氧基羰基; 一组-CONR16R17; 或者R 3构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; R 4表示选自以下的芳族基团：所述芳族基团是未取代的或被独立地选自卤素原子的取代基单取代或二取代; （C1-C4）烷基; （C 1 -C 4）烷氧基; 三氟甲基; 制备工艺及治疗应用。