6,7-ASYMMETRICALLY DISUBSTITUTED QUINOXALINECARBOXYLIC ACID DERI VATIVES, ADDITION SALTS THEREOF, AND PROCESSES FOR THE PREPARATION OF BOTH

摘要

Excitatory amino acid receptors comprising as the active ingredient 6,7-asymmetrically disubstituted quinoxalinecarboxylic acid derivatives or addition salts thereof, particularly compounds exhibiting antagonism against AMPA receptors; and processes for the preparation of both. The disubstituted quinoxalinecarboxylic acid derivatives are represented by formula (1), wherein Q is halogeno, optionally halogenated lower alkyl, Ar-P- (wherein Ar is phenyl optionally substituted with one or more substituting groups, or naphthyl; and P is lower alkylene, lower alkenylene, lower alkynylene, oxygen or sulfur) or L-A-; R is nitro, trifluoromethyl, optionally substituted amino or a group of general formula (7), R<1> is aralkyl, phenyl, naphthyl, a 5- or 6-membered heterocycle or a fused ring thereof (which may have one or more substituting groups on the aromatic ring or the heterocycle), hydrogen, optionally halogenated lower alkyl or cycloalkyl; and R<2> is hydroxyl, lower alkoxy or a group of general formula (6).