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    • 37. 发明授权
    • Certain 1-methyl-piperidine-4-spiro-4'-(1'-3'-oxazolines) and
corresponding -(1',3' thiazolines)
    • 某些1-甲基 - 哌啶-4-螺-4' - (1'-3'-恶唑啉)和相应的 - (1',3'噻唑啉)
    • US5407938A
    • 1995-04-18
    • US137690
    • 1993-10-14
    • Abraham FisherYoffi SegallEzra ShirinYishai KartonHaim Meshulam
    • Abraham FisherYoffi SegallEzra ShirinYishai KartonHaim Meshulam
    • C07D471/10C07D471/20C07D491/10C07D497/10C07D498/10C07D498/20C07D513/10A61K31/44C07D491/20C07D495/20C07D497/20
    • C07D471/10C07D491/10C07D497/10C07D513/10
    • The invention relates to compounds (I) for treating diseases of the central and peripheral nervous system, including enantiomers, racemates and acid addition and quaternary salts, ##STR1## wherein Q is selected from two H atoms, (CH.sub.2).sub.m and C(CH.sub.3).sub.2 where m is 1, 2 or 3 and n and p are; each independently 0, 1, 2 or 3, provided that n+p=1-3, and R.sup.0 is H, methyl or OH; the moiety ##STR2## R is selected from H, NH.sub.2, NH-C.sub.1-6 -alkyl, N(C.sub.1-6 -alkyl).sub.2, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, C.sub.3-7 - cycloalkyl, C.sub.1-6 -alkyl substituted by 1-6 halogen atoms, hydroxy- C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, C.sub.1-6 -alkoxy-C.sub.1-6 -alkyl, carboxy-C.sub.1-6 -alkyl, (C.sub.1-6 -alkoxy)carbonyl-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, mono-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, di-(C.sub.1-6 -alkyl)amino-C.sub.1-6 -alkyl, 2-oxo-pyrrolidin-1-yl-methyl, aryl, diarylmethylol, and C.sub.1-6 -alkyl substituted by one or two aryl groups; R' is independently selected from the group from which R is selected and C.sub.1-6 -alkanoyl and arylcarbonyl; and aryl denotes unsubstituted phenyl or phenyl substituted by 1-3 substituents selected from halogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy and CF.sub.3, subject to certain provisos.
    • 本发明涉及用于治疗中枢和周围神经系统疾病的化合物(I),包括对映体,外消旋体和酸加成和季盐。其中Q选自两个H原子,(CH 2)m和 C(CH 3)2,其中m为1,2或3,n和p为 每个独立地为0,1,2或3,条件是n + p = 1-3,R 0为H,甲基或OH; R 1选自H,NH 2,NH-C 1-6 - 烷基,N(C 1-6 - 烷基)2,C 1-6 - 烷基,C 2-6 - 烯基,C 2-6 - 炔基,C 3 -7-环烷基,被1-6个卤素原子取代的C 1-6 - 烷基,羟基-C 1-6 - 烷基,C 1-6 - 烷氧基,C 1-6 - 烷硫基,C 1-6 - 烷氧基-C 1-6 - 烷基, 羧基-C 1-6 - 烷基,(C 1-6 - 烷氧基)羰基-C 1-6 - 烷基,氨基-C 1-6 - 烷基,单 - (C 1-6 - 烷基)氨基-C 1-6 - 烷基, (C 1-6 - 烷基)氨基-C 1-6 - 烷基,2-氧代 - 吡咯烷-1-基 - 甲基,芳基,二芳基羟甲基和被一个或两个芳基取代的C 1-6 - 烷基; R'独立地选自选自R的基团和C 1-6 - 烷酰基和芳基羰基; 并且芳基表示未取代的苯基或被1-3个选自卤素,C 1-6 - 烷基,C 1-6 - 烷氧基和CF 3的取代基取代的苯基,具有一定条件。