Di- or tetra hydro-azepino (4,5-b) or (4,3-b)-quinolines - anorexigenics which have only weak cardiovascular and motility effects

摘要

Cpds. of formula (I) their 6-N-oxides and acid addn. salts (where A is -CH2-N R1 R1 is H, opt. branched 1-6C alkyl (opt. substd. by hydroxy methoxy, carboxy, cyano, dimethylaminocarbonyl, morpholino-carbonyl or 2-6C carbalkoxy), opt. branched 1-12C aliphatic acyl (opt. methoxy substd.) opt. halo substd. benzoyl, 2-7C carbalkoxy, 4-7C carbocycloalkoxy, opt. methyl-substd. benzyl, opt. methyl or halo substd. phenyl-sulphonyl, 2-6C alkenyl, phenyl, trifluoroacetyl, amidino, amido, thioamido, phenoxycarbonyl, benzyloxycarbonyl or methylsulphonyl, R2 is H, hydroxy, 1-3C alkyl, 1-3C alkoxy 1-3C acyloxy, 2-4C alkyloxy-carbonyloxy, amino, dimethylamino, morpholino or halo, R3 is H, halo, hydroxy, carboxy, opt. branched 1-6C alkyl, 3-6C cycloalkyl, 1-3C alkoxy (opt. substd. by phenyl or 2-4C carbalkoxy), 2-4C carbalkoxy, hydroxymethyl, phenyl, phenoxy, amino, pyrrolidino or morpholino, R4,R5,R6 are each H, halo, methyl, hydroxy, methoxy, cyano, amino, nitro, trifluoromethyl, carboxy, acetyl 2-4C carbalkoxy or two of the gps. together form a methlenedioxy, X1,X2 are H or together form a bond. Specif. claimed are (I) where A forms the (4 5-b) cpd. R3 is methyl and (a) R1 is carbethoxy, propyl, tert-butyl-OOC-2-hydroxypropyl, alkyl and carbmethoxy and R2,R4,R5,R6, X1 and X2 are H (b) where R1 is carbethoxy R2 is hydroxy and R4,R5,R6,X1 and X2 are H. (I) are anorexigenics which have only a weak effect on motility and several of which have weak or no cardiovascular effects. They also have hypolipaemiant, hypoglycemiant, anti-depressive, anti-allergic, anti-asthmatic and/or selective inhibitory lipid resorption activities.