Lactams Compositions and pharmaceutical methods of use

US4399145A · kind A · utility

Assignee

• GRUNENTHAL GMBH · DE

Inventors

• Ivars Graudums · Stolberg, DE
• Elmar Friderichs · Stolberg, DE

Key dates

• Filing date: Nov 5, 1981
• Grant date: Aug 16, 1983
• Expiry date: Nov 5, 2001

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P25/20
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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).