Pyrimidine derivatives and processes for the preparation thereof

Abstract

The present invention relates to novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof wherein: when A is piperidin- -yl or —NH—B, wherein B is C -C alkyl, C -C alkenyl, C -C cycloalkyl, C -C alkoxyethyl, phenylethl which may be substituted or unsubstituted, 3-trifluoromethylphenylmethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl, R is hydrogen or methyl; and R , R , R and R are hydrogen; or when A is a group of formula (II); when R is hydroxymethyl or C -C alkoxymethyl, R , R , R , R and R are hydrogen; and R is hydrogen or halogen; or when R is hydrogen or methyl, R is hydrogen or halogen; and one or two of R , R , R , R and R is hydroxy, methoxy, or a group of formula (III) wherein Z is C -C alkyl, substituted or unsubstituted C -C alkenyl, cyloalkyl, benzyloxyalkyl, alkoxycarbonylalkyl, morpholinomethyl, piperidinomethyl, 4-substituted-piperazinomethyl, substituted or unsubstituted phenyl, naphthyl, substituted or unsubstituted benzyl, thiophen-2-yl-methyl, 1-substituted-pyrrolidin-2-yl or —CHR NHR , wherein R is hydrogen, methyl, isopropyl, benzyl, benzyloxymethyl, methylthioethyl, benzyloxycarbonylmethyl, carbamolymethyl, carbamoylethyl, or 1-benzylimidazol-4-ylmethyl and R is hydrogen or t-butoxycarbonyl; and the others are hydrogen or methyl.