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    • 6. 发明授权
    • Novel cyclopropylmethylamine derivatives
    • 新型环丙基甲胺衍生物
    • US4103030A
    • 1978-07-25
    • US635331
    • 1975-11-26
    • Atsuyuki KojimaYoshito KamenoJunki KatsubeShigeho InabaHisao Yamamoto
    • Atsuyuki KojimaYoshito KamenoJunki KatsubeShigeho InabaHisao Yamamoto
    • A61K31/13A61K31/135A01N9/20A01N9/24C07C91/16C07C91/28
    • Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.2 are each as defined above and X is a conventional leaving (removable) group with amines of the formula: ##STR4## wherein R and R' are each as defined above.
    • 新的下式的环丙基甲胺化合物:其中Ar 1表示具有一个或多个选自卤素,C 1 -C 4烷基,C 1 -C 4烷氧基和三氟甲基的取代基的苯基,其中至少一个存在于 或位置,Ar 2表示未取代的苯基或被一个或多个选自卤素和C 1 -C 4烷基的取代基取代的苯基,R表示氢,C 1 -C 4烷基或C 2 -C 4羟烷基, R'表示C1-C4烷基或C2-C4羟基烷基及其无毒盐,它们具有各种有用的药理活性,可以通过还原相应的下式化合物来制备:其中Ar1,Ar2,R和 R'各自如上所定义,或通过下式的相应化合物的缩合:其中Ar 1和Ar 2各自如上所定义,X是具有下式的胺的常规离去(可除去)基团:其中 R和R'各自如上所定义。
    • 8. 发明授权
    • Novel morpholine derivatives and treating depression therewith
    • 新型吗啉衍生物和治疗抑郁症
    • US4169146A
    • 1979-09-25
    • US811944
    • 1977-06-30
    • Junki KatsubeAtsuyuki KojimaMakoto SunagawaYoshinori TakashimaYoshito KamenoHisao Yamamoto
    • Junki KatsubeAtsuyuki KojimaMakoto SunagawaYoshinori TakashimaYoshito KamenoHisao Yamamoto
    • C07D265/30C07D267/10A61K27/00
    • C07D265/30C07D267/10
    • Novel morpholine compounds of the formula: ##STR1## wherein R.sub.1 represents hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.2 represents hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.5 alkenyl, C.sub.3 -C.sub.5 alkynyl, aryl-(C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.6)cycloalkyl(C.sub.1 -C.sub.4)alkyl, polyhalo(C.sub.2 -C.sub.4) alkyl or hydroxy(C.sub.2 -C.sub.4)alkyl, A represents straight or branched C.sub.2 -C.sub.4 alkylene, B represents a divalent radical selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 --O--, --CH.sub.2 --S--, --S-- and --O--, >D--E-- represents a trivalent radical selected from the group consisting of >CH--CH.sub.2 -- and >C.dbd.CH-- and C.sub.1 and C.sub.2 each represent 1,2-phenylene optionally substituted with one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy, and their non-toxic salts, which are useful as antidepressants and can be produced by various methods.
    • 式中:R1代表氢或C1-C4烷基,R2代表氢,C1-C4烷基,C3-C5烯基,C3-C5炔基,芳基 - (C1-C4)烷基,(C3 -C 6)环烷基(C 1 -C 4)烷基,多卤代(C 2 -C 4)烷基或羟基(C 2 -C 4)烷基,A表示直链或支链C 2 -C 4亚烷基,B表示选自-CH 2 -CH 2 - , - CH = CH-, -CH 2 -O-,-CH 2 -S-,-S-和-O-,> DE-表示选自下组的三价基团:CH-CH 2 - 和> C = CH-和C1和C2各自表示任选被一个或多个选自卤素,C 1 -C 4烷基和C 1 -C 4烷氧基的取代基取代的1,2-亚苯基及其无毒盐, 其可用作抗抑郁药并且可以通过各种方法制备。