4,1-Benzoxazepines of the following formula are central nervous system drugs: <IMAGE> wherein R is hydrogen or C1 to C5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and <IMAGE> is a group of the formula: <IMAGE> +TR <IMAGE> (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur; R1 is hydrogen, halogen, C1 to C5 alkyl, C1 to C5 alkylthio, 5- or 6-membered heterocycle or C1 to C5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C1 to C5 alkoxy, C1 to C5 alkanoyloxy, C1 to C5 alkylthio, C7 to C9 aralkyldithio, C2 to C10 dialkylamino, C3 to C15 dialkylaminoalkoxy, C3 to C15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle; R2 is C1 to C5 alkyl; and R3 is C1 to C5 alkyl or C3 to C10 dialkylaminoalkyl; with a proviso that when R1 is C1 to C5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl).
4,1-Benzoxazepines and compositions