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    • 2. 发明授权
    • 1-Phenylthiopropyl-4-hydroxy-4-phenyl piperidines
    • 1-苯基硫丙基-4-羟基-4-苯基哌啶
    • US3960873A
    • 1976-06-01
    • US481796
    • 1974-06-21
    • Isamu MaruyamaHisao YamamotoMasaru NakaoShigeru SakaiKikuo SasajimaSumio KitagawaShigeho Inaba
    • Isamu MaruyamaHisao YamamotoMasaru NakaoShigeru SakaiKikuo SasajimaSumio KitagawaShigeho Inaba
    • C07D295/092C07D211/52
    • C07D295/088
    • Novel N-substituted heterocyclic derivatives represented by the formula, ##SPC1##Wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkoxy, nitro, halogen or trifluoromethyl group; R.sub.2 is hydrogen atom or lower alkyl group; X is sulfur atom, sulfinyl or sulfonyl group; Y is ##EQU1## group (wherein R.sub.3 is phenyl or substituted phenyl group; R.sub.4 is hydrogen atom, hydroxy, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, carbamoyl, N-(lower alkyl)-carbamoyl or N,N-di(lower akyl)-carbamoyl group; R.sub.5 is hydrogen atom, morpholino, pyrrolidinyl, piperidinyl, hexamethylenimino, lower alkyl, cyclo(lower alkyl), cyclo(lower alkyl)-(lower alkyl), hydroxy-(lower alkyl), (lower alkoxy)-(lower alkyl), phenyl or substituted phenyl group; k is 0 or 1 and m is 0, 1 or 2); and n is 3 or 4, and pharmaceutically acceptable salts thereof, which have excellent tranquillizing, anti-psychotonic, anti-emotional, anti-convulsive, anti-psychosis, sedative, analgesic or anti-hypertensive activities.
    • 由式WHEREIN R1表示的新型N-取代的杂环衍生物是氢原子,低级烷基,低级烷氧基,硝基,卤素或三氟甲基; R2是氢原子或低级烷基; X是硫原子,亚磺酰基或磺酰基; Y是|| - (CH2)kN-(CH2)m-R3, - (CH2)kC-(CH2)m-R5或| R4 | -CH = C-(CH2)m-R5基(其中R3是苯基 或取代的苯基; R 4是氢原子,羟基,低级烷基,低级烷氧基,低级烷酰基,低级烷酰氧基,氨基甲酰基,N-(低级烷基) - 氨基甲酰基或N,N-二(低级烷基) - 氨基甲酰基; 氢原子,吗啉代,吡咯烷基,哌啶基,六亚甲基亚氨基,低级烷基,环(低级烷基),环(低级烷基) - (低级烷基),羟基 - (低级烷基),(低级烷氧基) - (低级烷基) 取代苯基; k为0或1,m为0,1或2); 和n为3或4,及其药学上可接受的盐,其具有优异的镇静,抗心律失常,抗感觉,抗惊厥,抗精神病,镇静,止痛或抗高血压活性。