申请人:Grunenthal GmbH
公开号:US04399145A1
公开(公告)日:1983-08-16
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).
本发明涉及新的内酰胺化合物,包含它们的制药组合物(特别是口服或直肠应用的组合物)以及制备这些化合物和组合物的过程。新化合物的一般式为##STR1##其中X表示1至4个碳原子的直链或支链烷基,优选为甲基基团。式(I)的新化合物具有镇静催眠特性。在更高的剂量下,其中一些化合物也具有催眠麻醉作用。此外,其中X代表甲基基团的衍生物具有抗惊厥活性。式(I)的有价值的化合物可按已知的方式制备,例如通过将3-烷基-3-卤代-2-氧代哌啶(烷基具有1-4个碳原子)与2,3-二氢-3-氧代-1,2-苯并异噻唑二氧化物-(1,1)的金属衍生物反应或通过将3-烷基-3-氨基-2-氧代哌啶与o-磺酸苯甲酰二氯化物或二溴化物或o-卤代巯基苯甲酰卤反应,然后进行氧化。其他已知的过程,例如环化形成内酰胺环,也适用于制备式(I)的化合物。