Yuhan Corporation

Song Jin Lee

Jong Wook Lee

Bong Yong Lee

Chang Seop Kim

Seung Kyu Lee

Keun Seog Song

Man Soon Hwang

Woo Jeon Shim

The present invention relates to novel pyrimidine derivatives and pharmaceutically acceptable non-toxic salts thereof which possess an excellent inhibitory activity against gastric acid secretion, a pharmaceutical composition containing the same as an active ingredient, and a process for the preparation thereof.

Pyrimidine derivatives and processes for the preparation thereof

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 &mdash;NH&mdash;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 &mdash;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.

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Kyonggi-do, South Korea

Song Jin Lee