Substituted azetidinone compounds, their preparation, and medicaments containing them
    1.
    发明公开
    Substituted azetidinone compounds, their preparation, and medicaments containing them 失效
    Substituierte Azetidinonverbindungen,deren Herstellung und ihre enthaltenden Arzneimittel。

    公开(公告)号:EP0171159A1

    公开(公告)日:1986-02-12

    申请号:EP85304532.6

    申请日:1985-06-25

    IPC分类号: C07K5/08 C07D205/08 A61K37/02

    摘要: Compounds of the following general formula (1) and salts thereof are useful pharmaceuticals having central nervous system activitv:
    wherein one of R 1 and R 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 a hydrogen atom or a lower alkyl group; R 3 represents a hydrogen atom or a group shown by formula:
    [wherein X represents

    (wherein R 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]; and R 4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula -CH 2 CO-A [wherein A represents an amino group or a group shown by formula
    (wherein X and Y are as defined above)]; provided that (a) at least one of R 3 and R 4 is other than a hydrogen atom and (b) when R 1 and R 2 are both hydrogen atoms at least R 4 is other than a hydrogen atom.

    摘要翻译: 下列通式(I)的化合物及其盐是具有中枢神经系统活性的有用药物: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,另一方代表氢基,或二者均表示氢原子或低级烷基; R 3表示氢原子或由式表示的基团:... ... [其中X表示... ...或... ...(其中R 5表示氢原子或低级烷基 ),Y表示羟基,低级烷氧基,氨基,单 - 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式-CH 2 CO-A [其中A表示氨基或上述定义的基团]所示的基团]; 条件是(a)R 3和R 4中的至少一个不是氢原子,和(b)当R 1和R 2都是氢原子时,至少R 4是其它的 比氢原子。