CATECHOL OXAZOLIDINONE DERIVATIVES AND PHARMACEUTICAL COMPOSITION THEREOF

摘要

PURPOSE: Catechol oxazolidinone is provided which inhibits phosphodiesterase IV and tumor necrosis factor, and also provided is pharmaceutical compositions thereof which is effective for treatment of the diseases such as asthma, arthritis, osteoarthritis, bronchitis, chronic airway obstruction, psoriasis, allergic rhinitis, dermatitis, depression, AIDS, HIV, Crohn's disease, sepsis and septic shock. CONSTITUTION: Catechol oxazolidinone derivative is described in formula (1), wherein R1 represents methyl, ethyl, difluoromethyl or trifluoromethyl; R2 represents C1-C6 alkyl or C3-C7 cycloalkan; R3 represents CO2R4, CH2OR4, C(=O)NHOH, CH2NR5 or CH(=NR6); R4 and R5 are hydrogen, C1-C6 alkyl, -(CH2)nCONH2 or -(CH2)n phenyl each; R6 is hydrogen, -OR7, trifluoromethyl, C1-C6 alkyl, -(CH2)nCONR7, (CH2)nCOR7, (CH2)nOR7, -NHC(=NH)NR7, -NHC(=O)NR7, -NHC(=S)NR7 or -(CH2)nNR7; R7 represents hydrogen or C1-C6 alkyl; n is integer from 0 to 5; Y is O or S.