| abstract |
Heterocyclocyclylcarbonyl derivatives of urea for use in dissolving gallstones, having the formula RCONHCONR <1>R<2>, wherein R is pyridyl, monochloro-pyridyl, quinolyl, furyl, thiazolyl, 4-methyl-5-thiazolyl, 4-methyl-5-oxazolyl, isothiazolyl, 3-methyl-5-isothiazolyl, 3-(1,2-benzoisothiazolyl), 5-methyl-3-isoxazolyl, 3-methyl-5-isoxazolyl, 5-methyl-3-phenyl-4-isoxazolyl, 3-(1,2,5-thiadiazolyl) or 4-(1,2,3-thiadiazolyl); R<1> is hydrogen, alkyl having from one to ten carbon atoms naphthyl or phenyl; R<2> is hydrogen, alkyl having from one to ten carbon atoms, phenyl or phenylalkyl wherein the alkyl has from one to four carbon atoms; or R<1> and R<2> taken together with the nitrogen to which they are attached form a morpholino, thiomorpholino, 1-(1,2,3,6-tetrahydropyridyl), 1-azacycloheptyl, 1-azacyclooctyl or 3-(2,3,4,5-tetrahydro-3, 1-benzazepinyl) group, or a piperidino group optionally substituted with alkyl having from one to four carbon atoms, alkoxy having from one to four carbon atoms, chloro, or phenylalkyl having from one to four carbon atoms in the alkyl group; with the proviso that, where R is a 5-methyl-3-isoxazolyl group, then R<1> and R<2> are taken together with the nitrogen to which they are attached and form a group other than morpholino. These compounds are novel, except for those in which R is pyridyl, R<1> is hydrogen and R<2> is hydrogen, methyl or ethyl. |