NEW CATECHOL DERIVATIVES

摘要

Compounds of formula (I), wherein R1 is an electronegative substituent, preferably nitro, cyano, formyl or carboxy, R2 is -A-R4, wherein A is branched or straight chain C1-9 alkylene and R4 is carboxy or 5-tetrazolyl, R5 or CO-R5, wherein R5 is phenyl or C3-7 cycloalkyl which is substituted by at least one carboxy or 5-tetrazolyl; R3 is an electronegative substituent, preferably nitro, cyano, halogen, formyl, carboxy, C1-5 alkyl carbonyl, aryl carbonyl or SO2R6, wherein R6 is branched or straight chain C1-5 alkyl, aryl alkyl, aryl or NR7R8, wherein R7 and R8 are independently hydrogen, branched or straight chain C1-5 alkyl or together form a C3-6 ring or a pharmaceutically acceptable ester or salt thereof, their preparation, use and pharmaceutical compositions comprising them are described. The compounds are peripheral, long acting COMT (catechol-O-methyl transferase) inhibitors and are useful e.g. in the treatment of Parkinson's disease and hypertension.