GB866761A - 4-metathiazanone-1-oxides - Google Patents

Abstract

The invention comprises 2-(lower aromatic-, 3-(lower hydrocarbyl)-4-metathiazanone-1-oxides and -(lower aromatic)-4-metathiazanone-1-oxides having optionally up to three lower alkyl radicals substituted in the 5- and 6-metathiazanine ring positions, wherein "lower aromatic" means aromatic radicals having one or two aromatic rings each having five or six atoms which are carbocyclic or heterocyclic including unsubstituted phenyl, and phenly substituted by halogen atoms, C1-6 alkyl or C1-6 alkoxy groups; "lower hydrocarbyl" means C1-8 hydrocarbyl radicals and having an aliphatic carbon atom linked to the ring nitrogen atom and "lower alkyl" means C1-3 alkyl radicals, and the preparation thereof by oxidising the corresponding 2-(lower aromatic)-4-metathiazanone with an oxidising agent effective to oxidise sulphides to sulpoxides. 2-(3,4-Dichloro-), (2-4-dichloro-), (2-chloro-) and (4-isopropylphenyl)-3-ethyl-4-metathiazanone and 2-(3,4-dimethoxyphenyl)-3-methyl-4-methiazanone are prepared from b -mercapto propionic acid and the appropriately substituted benzal-N-ethyl- or -methylimine. Reference has been directed by the Comptroller to Specification 815,203.ALSO:Pharmaceutical compositions comprise an inert diluent or carrier together with a 2-(lower aromatic) - 3 - (lower hydrocarbyl) - 4 - metathiazanone - 1 - oxides or 2 - (lower - aromatic)-4-metalthiazanone-1-oxides having optionally up to three lower alkyl radicals substituted in the 5- and 6-positions of the metathiazanine ring, wherein "lower aromatic" means aromatic radicals having one or two aromatic rings each having five or six ring atoms which are carbocyclic or heterocyclic, including phenyl halogen-, C1-6-alkyl-, and C1-6-alkoxy-substituted phenyl, "lower hydrocarbyl" means C1-8-hydrocarbyl radicals and having an aliphatic carbon atom linked to the ring nitrogen atom and "lower alkyl" means C1-3 alkyl radical. The compositions may be prepared for oral administration in tablet or capsule form or as an aqueous suspension, aqueous-alcoholic solutions, oil solutions or oil-water emulsions. Reference has been directed by the Comptroller to Specification 815,203.