NOVEL DERIVATIVES OF PYRIMIDINE (VARIANTS) Russian patent published in 2003 - IPC

FIELD: organic chemistry, heterocyclic compounds, pharmacy. SUBSTANCE: invention relates to novel derivatives of pyrimidine of the general formula (I) or their pharmaceutically acceptable salts exhibiting high antisecretory activity with properties of reversible inhibitor of proton pump and can be used in preparing valuable medicinal agents. In compounds of the general formula (I) B represents C_3-7-cycloalkyl, C_1-3- alkoxyethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl; R₁ represents hydrogen atom or methyl; R₂,R₃,R₄,R₅ are hydrogen atom; or B represents group of formula (II) where R₇ means hydrogen or halogen atom; R₁ represents hydroxymethyl or C_1-3-alkoxymethyl; R₂,R₃,R₄,R₅,R₆ are hydrogen atom; or B represents group of the formula (II) indicated above; R₁ represents hydrogen atom or methyl and one or two among R₂,R₃,R₄,R₅,R₆ are hydroxy-group, methoxy-radical or group of the formula (III): -O-C(O)-Z where Z represents C_1-4-alkyl, C_2-4-alkenyl, C_3-6-cycloalkyl, morpholinomethyl, piperidinomethyl, phenyl, naphthyl, thiophene-2-ylmethyl or CHR₈NHR₉ where R₈ represents hydrogen atom, methyl, isopropyl, benzyl, benzyloxymethyl, methylthioethyl, benzyloxycarbonylmethyl, carbamoylmethyl, carbamoylethyl or 1-benzimidazol-4-ylmethyl; and R₉ represents hydrogen atom or tert.-butoxycarbonyl and another R₂,R₃,R₄,R₅,R₆ are hydrogen atom or methyl. EFFECT: valuable medicinal properties of compounds. 13 cl, 2 tbl