3-Hydroxy-ethyl 1,3,4,5-tetra:hydro 1,3-benzodiazepine-2-thione(s) - and related cpds. are antidepressants, intermediate 2-amino-phenyl-ethyl-amino-ethanol derivs. are also new

摘要

X1,X2 substd. 3-CHR1-CHR2-(CH2)n-O-A -S-R-1,3,4,5-tetrahydro-1, 3-benzo diazepine-2-thiones of formula (I) are new (where X1,X2 are H, halo or lower alkoxy; R is H, lower alkyl or phenyl; one of R1 and R2 is H, the other is H, lower alkyl or phenyl; A is H, lower alkyl or tetrahydropyranyl; and n is 0 or 1. "Lower" implies 1-6C, opt. branched). CNS active cpds. used to treat depressive states and psychic troubles. Reserpene antagonism and S-HTP potentiator tests are described. (I) may be used as antidepressants by oral administration in daily doses of 0.05-100 mg. Activity tests compare the cpds. with imipramine and amitriptyline and LD50 of tests cpds. is over 3200 mg/kg.