3-CYCLOBUTENE-1,2-DIONE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF

摘要

PURPOSE: Provided are a 3-cyclobutene-1,2-dione derivative which has excellent inhibition effect on cathepsins and its non-toxic salts. Also, provided are its preparation process and a composition containing it as an active ingredient. CONSTITUTION: The 3-cyclobutene-1,2-dione derivative is represented by the formula(1), R1 is phenoxypropionylamino, 2(S)-(1-oxo-1,3-dihydro-isoindole-2-yl)-4-methylpentanoylamino or leucyl of which N-terminus amino group is substituted with benzyloxycarbonyl, phthaloyl, methyl, benzoyl, cyclohexanecarbonyl, phenylpropanoyl, trifluoromethoxybenzoyl, toluoyl, thiophenecarbonyl, benzenesulfonyl, butanesulfonyl, naphthalenesulfonyl or chlorophenylthiocarbamoyl; and R2 is linear or branched C1-C4 alkyl, phenyl, diethylamino, trimethylsilanyl, sulfanyl substituted with phenyl, pyridyl, C1-C3 alkoxybenzyl, pentafluorophenyl or aminophenyl, benzenesulfinyl, phthalimido, or benzyloxy.