Benzazocinone and benzazoninone derivatives, and their pharmaceutical use

Claim 1

A compound of the formula ##STR24## wherein the carbocyclic ring may also be hexahydro; R A and R B are radicals of the formula ##STR25## wherein R o represents COR 6 in radical R A and COR 7 in radical R B ; and R 6 and R 7 represent independently hydroxy; lower alkoxy; (amino, mono- or di-lower alkylamino)-substituted lower alkoxy; carboxy-substituted lower alkoxy; lower alkoxycarbonyl-substituted lower alkoxy; aryl-substituted lower alkoxy; (hydroxy, lower alkanoyloxy or lower alkoxy)-substituted lower alkoxy; (hydroxy, lower alkanoyloxy or lower alkoxy)-substituted lower alkoxymethoxy; bicyclo[2,2,1]-heptyloxycarbonyl-substituted lower alkoxy; 3-phthalidoxy; (lower alkyl, lower alkoxy, halo)-substituted 3-phthalidoxy; amino; lower alkylamino; di-lower alkylamino; pyrrolidino, piperidino or perhydroazepino; (amino or acylamino)-substituted lower alkylamino; α-(carboxy or lower alkoxycarbonyl)-substituted lower alkylamino; aryl-substituted lower alkylamino which can be substituted on the α-carbon by carboxy or lower alkoxycarbonyl; R 1 is hydrogen, lower alkyl, amino(lower)alkyl, aryl, aryl (lower)alkyl, cycloalkyl, cycloalkyl(lower)alkyl, acylamino (lower)alkyl, mono- or di(lower)alkylamino(lower)alkyl, lower alkylthio(lower)alkyl, hydroxy(lower)alkyl, lower alkoxy(lower) alkyl, acylated hydroxy(lower)alkyl, aryloxy(lower)alkyl, aryl-(thio-,sulfinyl-, or sulfonyl-)lower alkyl, aryl-N-(lower) alkylamino(lower)alkyl, or arylamino(lower)alkyl; or R 1 is carboxy(lower)alkyl, esterified carboxy-(lower) alkyl, carbamoyl(lower)alkyl or N-substituted carbamoyl(lower) alkyl, and esterified carboxy, N-substituted carbamoyl have meaning as represented by COR 6 and COR 7 ; R 2 is hydrogen or lower alkyl; R 3 and R 4 , each independently, represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, hydroxy, halogen, trifluoromethyl; or R 3 and R 4 taken together represent lower alkylenedioxy; R 5 is hydrogen or lower alkyl; m is 2 or 3; and X represents oxo, two hydrogens, or one hydroxy or acylated hydroxy together with one hydrogen; and wherein within the above definitions acylamino represents lower alkanoylamino; lower alkoxycarbonylamino; aryl(lower) alkanoylamino; aryl(lower) alkoxycarbonylamino; or aroylamino in which aroyl represents benzoyl or benzoyl substituted by lower alkyl, lower alkoxy or halogen, or nicotinoyl; and wherein within the above definitions acylated hydroxy represents lower alkanoyloxy, nicotinoloxy, benzoyloxy or benzoyloxy substituted on the phenyl ring by lower alkyl, halogen or lower alkoxy; and wherein within the above definitions aryl represents phenyl unsubstituted or mono- or di-substituted by lower alkyl, lower alkoxy, lower alkylenedioxy, lower alkanoyloxy, hydroxy, halogen or trifluoromethyl; and cycloalkyl contains 3 to 8 carbons; or a pharmaceutically acceptable salt thereof.