知搜-全球专利检索

  1. 登录
  2. 注册

搜索结果

44 条记录 (耗时 0.026 秒)

    Lactams Compositions and pharmaceutical methods of use
    7.
    发明授权
    Lactams Compositions and pharmaceutical methods of use 失效
    Lactams组合物和药物使用方法

    公开(公告)号：US4399145A

    公开(公告)日：1983-08-16

    申请号：US318389

    申请日：1981-11-05

    申请人： Ivars Graudums ,  Elmar Friderichs

    发明人： Ivars Graudums ,  Elmar Friderichs

    IPC分类号： A61K31/445 ,  A61P25/08 ,  A61P25/20 ,  C07D211/76 ,  C07D417/04

    CPC分类号： C07D211/76

    摘要： The invention relates to new lactam compounds, pharmaceutical compositions containing them (especially those for oral or rectal application) and to processes for the preparation of these compounds and compositions. The new compounds have the general formula ##STR1## wherein X represents a straight or branched alkyl radical with 1 to 4 carbon atoms, preferably a methyl group. The new compounds of formula (I) have sedating-tranquilizing properties. In higher dosages some of them also act as hypno-anesthetics. Moreover the derivative in which X represents the methyl group has anticonvulsant activities. The valuable compounds of formula (I) are prepared in a manner known per se e.g. by reacting an 3-alkyl-3-halogen-2-oxopiperidine (the alkyl having 1-4 carbon atoms) with a metal derivative of 2,3-dihydro-3-oxo-1,2-benzisothiazoldioxid-(1,1) or by reacting an 3-alkyl-3-amino-2-oxopiperidine with o-sulfobenzoic acid dichloride or dibromide or with an o-halomercaptobenzoylhalide, followed by oxydation. Other processes known per se, such as cyclizations to form lactam rings, are also suitable for the preparation of the compounds of formula (I).

    摘要翻译： 本发明涉及新的内酰胺化合物，含有它们的药物组合物（特别是用于口服或直肠施用的药物组合物）和制备这些化合物和组合物的方法。 新化合物具有通式（I）其中X表示具有1至4个碳原子的直链或支链烷基，优选甲基。 新的式（I）化合物具有镇静镇静特性。 在较高剂量下，其中一些也作为hypno-anesthetics。 此外，X代表甲基的衍生物具有抗惊厥活性。 式（I）的有价值的化合物以本身已知的方式制备，例如， 通过使3-烷基-3-卤代-2-氧代哌啶（具有1-4个碳原子的烷基）与2,3-二氢-3-氧代-1,2-苯并异噻唑啉氧化物（1,1）的金属衍生物反应， 或通过使3-烷基-3-氨基-2-氧代哌啶与邻磺基苯甲酰氯或二溴化物或邻 - 卤代巯基苯甲酰卤反应，然后进行氧化反应。 本身已知的其它方法，例如环化形成内酰胺环，也适用于制备式（I）化合物。