| 摘要 |
The present invention is directed to 2-aminobenzoyl-alkylamines, -alkylamides and -alkylthioamides having NMDA receptor antagonistic activity and having the formula (I): (see formula I) and stereoisomers and pharmaceutically acceptable salts thereof, wherein: A is C1-6 alkylene; R, R1 and R2 are independently hydrogen, halo, haloalkyl, aryl, a heterocyclic group, a heteroaryl group, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, hydroxyalkyl, nitro, amino, cyano, cyanamido, guanidine, amidino, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, carboxy, carbonylamido, S-alkyl or alkylyhiol; X is > C1-6 alkylene, >C=O or >C=S or a single bond; and Y is hydrogen, halo, haloalkyl, aryl, a heterocyclic group, a heteroaryl group, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, hydroxyalkyl, nitro, amino, cyano, cyanamido, guanidine, amidino, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, carboxy, carbonylamido, styryl which may be ring-substituted by up to four substituents independently selected from among hydrogen, halo, haloalkyl, aryl, a heterocyclic group, a heteroaryl group, alkyl, alkenyl, alkynyl, arylalkyl, arylalkenyl, arylalkynyl, hydroxyalkyl, nitro, amino, cyano, cyanamido, guanidine, amidino, acylamido, hydroxy, thiol, acyloxy, azido, alkoxy, S-alkyl, alkylyhiol or -COQ, where Q is hydroxy, C1-6 alkoxy, amino, mono- C1-6 alkylamino, di- C1-6 alkylamino, hydroxylamino, C1-4 alkoxyamino or aryl- C1-4 alkoxyamino.
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