4H-3,1-BENZOXAZIN-4-ONES UND VERWANDTE VERBINDUNGEN, SIE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND VERFAHREN IHRER HERSTELLUNG.

摘要

Novel 2-amino-4H-3,1-benzoxazin-4-ones represented by the formula and the pharmaceutically acceptable esters and salts thereof wherein R<1> is hydrogen or lower alkyl; R<2> and R<3> are each independently hydrogen, halo, lower alkyl, hydroxy, lower alkoxy, lower thioalkyl, -NO2, -N(R min )2, -NR min COR min , -NHCON(R min )2 or -NHCOOR min , with the proviso that at least one of R<1>, R<2> and R<3> is not hydrogen when X is NHR or NR min COR sec ; and X is a radical chosen from in which: R is lower alkyl, lower alkenyl, lower alkynyl, optionally substituted lower cycloalkyl or optionally substituted phenyl lower alkyl; each R min is independently hydrogen or lower alkyl, or lower alkenyl or lower alkynyl where the unsaturated bond is at least one carbon removed from the O or N atom; each R sec is independently R, lower alkoxy, NHR min or AOR min ; and A is an amino acid residue, or a peptide of 2 to 3 amino acid residues, are useful as enzyme inhibitors in animals.