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    • 1. 发明申请
    • 1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES
    • 1,2,5,6-四氢吡啶氧化衍生物
    • WO1992006959A1
    • 1992-04-30
    • PCT/GB1991001751
    • 1991-10-09
    • BEECHAM GROUP PLCBROMIDGE, Steven, MarkORLEK, Barry, SidneyDABBS, Steven
    • BEECHAM GROUP PLC
    • C07D211/70
    • C07D213/89C07D211/70C07D211/78C07D211/94
    • 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.
    • 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。
    • 2. 发明申请
    • 1,2,5,6-TETRAHYDROPYRIDINE OXIME DERIVATIVES
    • 1,2,5,6-四氢吡啶氧化衍生物
    • WO1992004323A1
    • 1992-03-19
    • PCT/GB1991001456
    • 1991-08-29
    • BEECHAM GROUP PLCBROMIDGE, Steven, MarkORLEK, Bary, SidneyDABBS, Steven
    • BEECHAM GROUP PLC
    • C07D211/70
    • C07D211/70C07D211/78C07D213/57
    • 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.
    • 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。