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    • 6. 发明授权
    • CNS active substituted azetidinone compounds
    • CNS活性取代的氮杂环丁酮化合物
    • US4719207A
    • 1988-01-12
    • US747018
    • 1985-06-20
    • Toshinari TamuraMakoto YoshidaShin-ichi TsukamotoHidenori IwamotoMinoru YamamotoSoichi Kagami
    • Toshinari TamuraMakoto YoshidaShin-ichi TsukamotoHidenori IwamotoMinoru YamamotoSoichi Kagami
    • C07D205/08C07D205/085C07F7/10C07K5/097A61K31/415C07D403/12C07D403/14
    • C07K5/0821C07D205/08C07D205/085C07F7/10
    • Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.
    • 提供具有下式的取代的氮杂环丁酮化合物:其中R 1和R 2之一表示取代的低级烷基,叠氮基,氨基,低级酰氨基,巯基或低级烷硫基 另一个表示氢基团,或者都表示氢原子或低级烷基; R3表示氢原子或由下式表示的基团:其中X表示(其中R5表示氢原子或低级烷基),Y表示羟基,低级烷氧基,氨基 ,一或二低级烷基氨基); R 4表示氢原子,取代或未取代的低级烷基或由式-CH 2 CO-A(其中A表示氨基或由下式表示的基团:其中X和Y如上所定义) ),条件是当R 1和R 2均为氢原子时,至少R 4表示氢原子以外的基团,只要R 3或R 4表示除氢原子以外的基团,则该化合物具有强CNS作用。