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    Azetidine derivatives production
    3.
    发明公开
    Azetidine derivatives production 失效
    Herstellung von Azetidin-Derivaten。

    公开(公告)号：EP0204440A1

    公开(公告)日：1986-12-10

    申请号：EP86303546.5

    申请日：1986-05-09

    申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

    发明人： Tamura, Toshinari ,  Yoshida, Makoto ,  Tamazawa, Kazuharu ,  Iwamoto, Hidenori

    IPC分类号： C07F7/10

    CPC分类号： C07D205/08 ,  C07F7/10

    摘要： The present invention relates to 1-substituted silyl-4-oxo-2-azetidine-carboxylic acid lower alkyl esters shown by general formula (I)
    wherein R represents a lower alkyl group and ⓟ represents a substituted silyl group. These compounds are useful as intermediates for various drug syntheses.

    摘要翻译： 本发明涉及通式（I）所示的1-取代甲硅烷基-α-氧代-2-氮杂环丁烷 - 羧酸低级烷基酯其中R表示低级烷基，P表示取代甲硅烷基。 这些化合物可用作各种药物合成的中间体。

    Substituted azetidinone compounds, their preparation, and medicaments containing them
    5.
    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

    申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.

    发明人： Tamura, Toshinari ,  Yoshida, Makoto ,  Tsukamoto, Shin-ichi ,  Iwamoto, Hidenori ,  Yamamoto, Minoru ,  Kagami, Soichi

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

    CPC分类号： C07K5/0821 ,  C07D205/08 ,  C07D205/085 ,  C07F7/10

    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。