NOVEL CATECHOL N-METHYL HYDRAZIDE DERIVATIVE AND PREPARATION METHOD THEREOF

摘要

PURPOSE: A novel catechol N-methyl hydrazide derivative, its preparation method and a pharmaceutical acceptable composition containing the derivative are provided, wherein the derivative has a phosphodiesterase IV or tumor necrosis factor (TNF) inhibiting activity. CONSTITUTION: The catechol N-methyl hydrazide derivative is represented by the formula 1, wherein R1 is a cycloalkyl group of C3-C7, indanyl group or benzyl group; R2 is nitro group or -NH-Y-R3 (Y represents a direct bond or is -CO- or -SO2-); and R3 is H, an alkyl group of C1-C7 unsubstituted or mono- or disubstituted with OH or halogen atom, an alkyl group of C1-C2 unsubstituted or substituted with the substituent selected from the group consisting of phenyl group, phenoxy group and an alkylcarbonyloxy group of C1-C3, a five- or six-membered heteroaryl group containing one or two hetero atoms selected from the group consisting of N, O and S, or a phenyl group unsubstituted or substituted with the one or two substituent selected from the group consisting of nitro group, cyano group, halogen atom, an alkyl group of C1-C3 and an alkoxy group of C1-C3.