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    1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES
    1.
    发明申请
    1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES 审中-公开
    1,2,5,6-四氢吡啶氧化衍生物

    公开(公告)号：WO1992006959A1

    公开(公告)日：1992-04-30

    申请号：PCT/GB1991001751

    申请日：1991-10-09

    Applicant: BEECHAM GROUP PLC ,  BROMIDGE, Steven, Mark ,  ORLEK, Barry, Sidney ,  DABBS, Steven

    Inventor： BEECHAM GROUP PLC

    IPC: C07D211/70

    CPC classification number: C07D213/89 ,  C07D211/70 ,  C07D211/78 ,  C07D211/94

    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein R1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R10 wherein R10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C1-8 alkoxy; C2-8 alkenyloxy; C2-8 alkynyloxy; C3-8 cycloalkyloxy; or COR13 wherein R13 represents hydrogen, C1-8 alkyl, phenyl or phenyl C1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C1-6 alkoxy, C1-6 alkyl, halo, C1-6 alkoxycarbonyl, cyano, C1-6 alkylthio or C1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.

    Abstract translation: 式（I）化合物或其药学上可接受的盐，其中R 1表示被R 10取代的1,2,5,6-四氢吡啶-3-基，其中R 10表示OH; 可在体内水解成OH或氢的基团; C 1-8烷氧基 C2-8烯氧基; C2-8炔氧基; C3-8环烷基氧基; 或COR 13，其中R 13表示氢，C 1-8烷基，苯基或苯基C 1-4烷基; 其中任何苯基部分任选被至多3个独立地选自C 1-6烷氧基，C 1-6烷基，卤素，C 1-6烷氧基羰基，氰基，C 1-6烷硫基或C 1-6烷基磺酰基的取代基取代; 通过中枢神经系统内毒蕈碱受体的作用增强乙酰胆碱的功能，因此在哺乳动物的治疗和/或预防痴呆中具有潜在的用途。

    1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES
    2.
    发明申请
    1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES 审中-公开
    1,2,5,6-四氢吡啶氧化衍生物

    公开(公告)号：WO1992004323A1

    公开(公告)日：1992-03-19

    申请号：PCT/GB1991001456

    申请日：1991-08-29

    Applicant: BEECHAM GROUP PLC ,  BROMIDGE, Steven, Mark ,  ORLEK, Bary, Sidney ,  DABBS, Steven

    Inventor： BEECHAM GROUP PLC

    IPC: C07D211/70

    CPC classification number: C07D211/70 ,  C07D211/78 ,  C07D213/57

    Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R10 wherein R10 represents hydrogen, C1-2 alkyl, prop-2-enyl, prop-2-ynyl or cyclopropyl; R2 is a group OR4, where R4 is C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, a group OCOR5 where R5 is hydrogen or R4, or a group NHR6, or NR7R8 where R6, R7 and R8 are independently C1-2 alkyl; and R3 is chloro, fluoro, bromo, methoxy, C1-3 alkyl substituted by one, two or three halogen atoms, or R3 is a group (CH2)nR9 where R9 is -CN, -SH or -SCH3 and n is 0 or 1, with the proviso that when n is 0, R9 is not -SH; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.

    Abstract translation: 式（I）化合物或其药学上可接受的盐，其中R 1表示被R 10取代的1,2,5,6-四氢吡啶-3-基，其中R 10表示氢，C 1-2烷基，丙-2-醇， 丙炔基，丙-2-炔基或环丙基; R2是OR4基团，其中R4是C1-4烷基，C2-4烯基，C2-4炔基，其中R5是氢或R4的基团OCOR5，或者NHR6或NR7R8，其中R6，R7和R8独立地是C1 -2烷基; 并且R 3是氯，氟，溴，甲氧基，被一个，两个或三个卤素原子取代的C 1-3烷基，或者R 3是基团（CH 2）n R 9，其中R 9是-CN，-SH或-SCH 3，n是0或 1，条件是当n为0时，R 9不是-SH; 通过中枢神经系统内毒蕈碱受体的作用增强乙酰胆碱的功能，因此在哺乳动物的治疗和/或预防痴呆中具有潜在的用途。

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