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    • 2. 发明申请
    • TETRACYCLIC COMPOUNDS
    • 四环化合物
    • WO8402704A2
    • 1984-07-19
    • PCT/GB8300353
    • 1983-12-29
    • BEECHAM GROUP PLC
    • CONNELL ANTHONY CHRISTOPHER
    • A61K31/55C07C233/07C07D223/00C07D223/20C07D235/00C07D243/00C07D243/38C07D267/00C07D267/20C07D281/00C07D281/14C07D281/16C07D487/00C07D487/04C07D498/00C07D498/04C07D513/00C07D513/04
    • C07D487/04C07C233/07C07D223/20C07D243/38C07D267/20C07D281/16C07D513/04
    • Compounds of formula (I) or a pharmaceutically acceptable salt thereof wherein: X is CH2, O, S, or NR where R is C1-4 alkyl; R1 and R2 are independently selected from hydrogen, hydroxy, C1-4 alkyl, C1-4 alkoxy, halogen or CF3; R3 is C1-7 alkyl, C2-5 alkynyl, C3-7 cycloalkyl, C4-7 cycloalkenyl or C1-6 alkyl substituted by C2-7 alkenyl, C2-7alkynyl, C3-7 cycloalkyl, hydroxy, thiol, C1-6 alkoxy, C1-6 alkylthio, carboxy, C1-6 alkoxycarbonyl, C2-7 alkanoyl, amino optionally substituted by one or two C1-4 alkyl or by C4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C1-6 alkyl groups, or benzoyl or phenyl either being optionally ring-substituted by one or two C1-4 alkyl, C1-4 alkoxy, halogen or trifluoromethyl; and one of R4, R5 and R6 is C1-6 alkyl and the other two are independently hydrogen or C1-6 alkyl, having anti-depressant and/or anxiolytic activity, a process for their preparation and their use.
    • 式(I)化合物或其药学上可接受的盐,其中:X为CH 2,O,S或NR,其中R为C 1-4烷基; R 1和R 2独立地选自氢,羟基,C 1-4烷基,C 1-4烷氧基,卤素或CF 3; R3是C1-7烷基,C2-5炔基,C3-7环烷基,C4-7环烯基或被C2-7烯基取代的C1-6烷基,C2-7炔基,C3-7环烷基,羟基,硫醇,C1-6烷氧基 C 1-6烷硫基,羧基,C 1-6烷氧基羰基,C 2-7烷酰基,任选被一个或两个C 1-4烷基取代的氨基或任选地含有氧或氮原子的C 4-6二聚亚甲基,任选地被一个或多个N取代的氨基羰基 或两个C 1-6烷基,或任选被一个或两个C 1-4烷基,C 1-4烷氧基,卤素或三氟甲基环取代的苯甲酰基或苯基; R 4,R 5和R 6中的一个是C 1-6烷基,另外两个独立地是氢或具有抗抑郁和/或抗焦虑活性的C 1-6烷基,其制备方法和用途。