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    Indol-2-one derivatives
    8.
    发明授权
    Indol-2-one derivatives 失效
    吲哚-2-酮衍生物

    公开(公告)号：US5773612A

    公开(公告)日：1998-06-30

    申请号：US640080

    申请日：1996-04-30

    申请人： Jean Wagnon ,  Bernard Tonnerre ,  Alain Di Malta ,  Richard Roux ,  Marie-Sophie Amiel ,  Claudine Serradeil-Legal

    发明人： Jean Wagnon ,  Bernard Tonnerre ,  Alain Di Malta ,  Richard Roux ,  Marie-Sophie Amiel ,  Claudine Serradeil-Legal

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61K31/54 ,  A61K31/541 ,  A61P1/00 ,  A61P7/04 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/24 ,  A61P25/26 ,  A61P43/00 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D209/30

    CPC分类号： C07D401/04 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  Y02P20/55

    摘要： A compound of formula II' ##STR1## in which R.sub.I is an ethoxy group or a chlorine atom; R.sub.II is hydrogen, a chlorine atom or a methyl group; R.sub.III is a chlorophenyl group or a methoxyphenyl group; R.sub.IV is an amino group, a group NR.sub.9 R.sub.10 or NR.sub.9 R.sub.XI, or a piperazin-1-yl radical substituted in the 4-position by a (C.sub.2 -C.sub.10)alkylene group substituted by an amino group which is free or carries a protective group; R.sub.10 is (CH.sub.2).sub.p R.sub.35 or a (C.sub.2 -C.sub.10)alkylene group substituted by R.sub.21 ; R.sub.XI is a (C.sub.1 -C.sub.12)alkyl group or a group .omega.-R.sub.32 R.sub.33 N(C.sub.1 -C.sub.4)-alkylcarbonyl; and R.sub.21 is R.sub.36 ; a group OR.sub.37 ; a group NR.sub.32 R.sub.33 ; a cyano group; a group S(C.sub.1 -C.sub.7)alkyl; a group SO(C.sub.1 -C.sub.7)alkyl; or a group SO.sub.2 (C.sub.1 -C.sub.7)alkyl; R.sub.35 is a piperid-4-yl group which is unsubstituted or substituted in the 1-position by a (C.sub.1 -C.sub.7)alkoxycarbonyl group or by a (C.sub.1 -C.sub.7)alkyl group; or a pyrid-2-yl group; R.sub.37 is R.sub.13 ; a (C.sub.3 -C.sub.7)cycloalkyl group; a (C.sub.1 -C.sub.6)alkylene group substituted by R.sub.24 ; a (C.sub.2 -C.sub.6)alkylene group substituted by a hydroxyl or a (C.sub.1 -C.sub.7)alkoxy group; or a (C.sub.2 -C.sub.6)alkylene group substituted by an amino group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups or by a protective group; R.sub.24 is a carboxyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl group; a benzyloxycarbonyl group; or a carbamoyl group which is free or substituted by one or two (C.sub.1 -C.sub.7)alkyl groups.

    摘要翻译： 其中RI是乙氧基或氯原子的式II'化合物（II'）; RII是氢，氯原子或甲基; RIII是氯苯基或甲氧基苯基; RIV是被无取代或携带保护基团的氨基取代的（C2-C10）亚烷基在4-位取代的氨基，NR9R10或NR9RXI基团或哌嗪-1-基; R 10为被R 21取代的（CH 2）p R 35或（C 2 -C 10）亚烷基; RXI是（C 1 -C 12）烷基或ω-R 32 R 33 N（C 1 -C 4） - 烷基羰基; R21为R36; 一组OR37; 一组NR32R33; 氰基; S（C 1 -C 7）烷基; SO（C 1 -C 7）烷基; 或基团SO 2（C 1 -C 7）烷基; R35是未被取代的或被（C1-C7）烷氧基羰基或（C1-C7）烷基取代在1位的哌啶-4-基; 或吡啶-2-基; R37是R13; （C 3 -C 7）环烷基; 被R24取代的（C1-C6）亚烷基; 被羟基或（C 1 -C 7）烷氧基取代的（C 2 -C 6）亚烷基; 或被一个或两个（C 1 -C 7）烷基或保护基取代的氨基取代的（C 2 -C 6）亚烷基; R24是羧基; （C1-C7）烷氧基羰基; 苄氧基羰基; 或不含或被一个或两个（C 1 -C 7）烷基取代的氨基甲酰基。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    9.
    发明授权
    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof 有权
    哌嗪酰基哌啶衍生物，其制备和治疗用途

    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。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    10.
    发明授权
    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof 有权
    哌嗪酰基哌啶衍生物，其制备和治疗用途

    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。