NOVEL CATECHOL PYRIMIDINE DERIVATIVES, PREPARATION METHODS THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING CATECHOL PYRIMIDINE DERIVATIVES

摘要

PURPOSE: Provided are novel catechol pyrimidine derivatives, preparation methods thereof and pharmaceutical compositions containing catechol pyrimidine derivatives. The catechol pyrimidine derivatives have inhibition effects on phosphodiesterase IV or tumor necrosis factor(TNF), and are thus useful for the treatment of inflammatory diseases and TNF production related diseases. CONSTITUTION: The catechol pyrimidine derivatives are represented by the formula(1). In the formula R1 is C1-C7 alkyl group including methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl and their enantiomers, or C3-C7 cycloalkyl group including cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and cycloheptyl; R2 is hydrogen, C1-C5 alkyl group including methyl, ethyl, propyl, butyl, pentyl and their enantiomers, or aryl group; R3 is C1-C4 alkyl group including methyl, ethyl, propyl, butyl and their enantiomers, or polyfluoro substituted C1-C4 alkyl group; R4 is hydrogen or C1-C3 alkyl group including methyl, ethyl, propyl and their enantiomers; R5 is hydrogen or acetyl group; and X is oxygen or sulfur, wherein the alkyl group is linear or branched type.