Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    1.
    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

    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
    2.
    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

    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。

    Derivatives of (bridged piperazinyl)-1-alkanone and use thereof as p75 inhibitors
    4.
    发明授权
    Derivatives of (bridged piperazinyl)-1-alkanone and use thereof as p75 inhibitors 有权
    (桥连哌嗪基)-1-烷酮的衍生物及其作为p75抑制剂的用途

    公开(公告)号:US08193190B2

    公开(公告)日:2012-06-05

    申请号:US12966413

    申请日:2010-12-13

    IPC分类号: A61K31/4995

    CPC分类号: C07D471/08

    摘要: The present invention relates to derivatives of ((phenyl)-3,6-dihydropyridin-1-yl)(bridged piperazinyl)-1-alkanone derivatives and ((phenyl)-2,5-dihydropyrrol-1-yl) (bridged piperazinyl)-1-alkanone corresponding to Formula (I): in which the variables are as defined herein, to the preparation thereof and to the therapeutic use thereof.

    摘要翻译: 本发明涉及((苯基)-3,6-二氢吡啶-1-基)(桥连哌嗪基)-1-烷酮衍生物和((苯基)-2,5-二氢吡咯-1-基)(桥接哌嗪基 )-1-烷基酮对应于式(I):其中变量如本文所定义,其制备及其治疗用途。