| abstract |
ABSTRACT OF THE DISCLOSURE The disclosure describes derivatives of 3,4,5-tri-methoxybenzene, their preparation as well as their therapeutical use, in particular as tranquillisers, myorelaxants and anti-convulsants. They are compounds of the formula I (I) wherein each of m and n, which may be the same or different, represents 0, 1 or 2, X represents an oxygen atom or an imine group of formula NR3 (wherein R3 represent; a hydrogen atom or a benzyl or morpholinoethyl group), Y represents cne of the divalent groups CO, CONH, COO or SO2, and NR1R2 represents a dimethylamino, diethylamino, dipropyl-amino, dibutylamino, allylamino, isobutenylamino, cyclopentylamino, cyclohexylamino, cycloheptylamino, cyclooctylamino, N-methyl N-cyclopentylamino, N-methyl N-cyclohexylamino, N-allyl N-cyclohexylamino, adamantyl-amino, diethoxyethylamino, dimethylaminoethylamino, dimethylaminopropylamino, N-methyl N-dimethylamino-propyl-amino, benzylamino, 3,4,5-trimethoxybenzylamino, phenethylamino, p-chlorophenethylamino, tetrahydrofur-furylamino, tetrahydropyranyl-methylamino, pyrrolidino, isoxazolidinyl, piperidino, 4-hydroxypiperidino, 4-p-chlorophenyl-4-hydroxypiperidino, homopiperidino, 1,2,3,6-tetrahydropyridyl, morpholino, 2-methyl-morpholino, 2,6-dimethylmorpholino, 2-morpholino-ethylamino, thiamorpholino, piperazino, 4-methylpipera-zino, 4-(?-m-chlorophenyl-benzyl)-piperazino, 4-(3,4,5-trimethoxyphenylaminocarbonyl)-piperazino, 4-(3,4,5-trimethoxyphenylaminocarbonylmethyl)-piperazino, 4-phenylpiperazino, 4-m-trifluoromethylphenyl-piperazino, 4-piperidino carbonylmethyl-piperazino, 1,2,3,4-tetrahydroquinolyl, 1,2,3,4-tetrahydroisoquinolyl, (7-chloro-4-quinolyl)-amino, 1,2,3,4-tetrahydro-benzoxazinyl or 1,2,3,4-tetrahydro-6-chloro-benzoxazinyl group, as well as their pharmaceutically acceptable acid addition salts. The compounds of the formula I may be obtained from known compounds according to the following general scheme: In these formulae A represents a -N=C=O, NH2, OH or -NH-(CH2)m-CO-hal group, B represents H, NH2, OH, hal-CO- or hal-SO2-, hal being a halogen, preferably chlorine atom, and NR1R2, m and n have the same meanings aq in formula I. |