ISOXAZOLE AND ISOTHIAZOLE DERIVATIVE

摘要

PURPOSE:To obtain a new 3-phenylisothiazole derivative, having inhibitory action on xanthine oxidase and useful for treating gout or hyperuricemia. CONSTITUTION:The compound of the formula [A is O or S; R<1> is NO2, halogen, 1C haloalkyl or CN; R<2> is unsubstituted or substituted 1-6C alkoxy, 1-4C alkylamino or dialkylamino or NRR' (R and R' are saturated carbon atomic group that, together with N to which both are bound, forms a 5- to 7-membered heterocyclic ring that may contain O); R<3> is H, amino, 1-2C alkylamino or dialkylamino, 1-2C alkyl or halogen; R<4> is OH, 1-6C alkoxy, NH2 or 1-2C alkylamino] or its pharmaceutically permissible salt, e.g. 4-amino-3-(4- isobutoxy-3-nitrophenyl)-5-isothiazolecarboxylic acid. The daily dose of the compound is within the range of usually 1-500mg, preferably 10-300mg for an adult.