3-Amino-[1]-benzazepin-2-one-1-alkanoic acids
AssigneeCiba-Geigy Corporation
InventorJeffrey W. H. Watthey
Life of this patent
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Abstract
Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-2,3,4,5-tetrahydro-1H-[1]benzazepin -2-ones and functional derivatives are angiotension converting enzyme inhibitors and are useful as antihypertensive agents. Synthesis of, compositions and methods of treatment utilizing such compounds are included.
Claims29
A compound of the formula ##STR25## wherein R.sub.A and R.sub.B are radicals of the formula ##STR26## respectively, in which R.sub.o is carboxy or functionally modified carboxy represented by COR.sub.6 in radical R.sub.A and represented by COR.sub.7 in radical R.sub.B wherein one or both of R.sub.6 and R.sub.7 represent hydroxy;
- lower alkoxy;
- (amino- 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]heptyl-oxycarbonyl-substituted lower alkoxy;
- 3-phthalidoxy;
- (lower alkyl, lower alkoxy, halo)-substituted 3-phthalidoxy;
- amino;
- lower alkylamino;
- di-lower alkylamino;
- di-lower alkylamino in which both alkyl groups are linked by a carbon to carbon bond and together with the amino nitrogen form pyrrolidino, piperidino or perhydroazepino;
- (amino)-substituted lower alkylamino;
- .alpha.-(carboxy or lower alkoxycarbonyl)-substituted lower alkylamino;
- aryl-substituted lower alkylamino which can be substituted on the .alpha.-carbon by carboxy or lower alkoxycarbonyl;
- R.sub.1 is hydrogen, lower alkyl, amino (lower) alkyl, aryl, aryl (lower) alkyl, cycloalkyl or cycloalkyl (lower) alkyl;
- R.sub.2 is hydrogen or lower alkyl;
- R.sub.3 and R.sub.4, each independently represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, hydroxy, halogen, trifluoromethyl, or
- R.sub.3 and R.sub.4 taken together represent lower alkylenedioxy;
- R.sub.5 is hydrogen or lower alkyl, and
- X represents oxo, two hydrogens, or one hydroxy together with one hydrogen;
- and wherein the carbocyclic ring may also be hexahydro or 6,7,8,9-tetrahydro;
- and wherein within the above definitons 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.
Dependencies are inferred from the claim text.