Certain benzazocinone and benzazoninone derivatives

C - Chemistry – Metallurgy – 07 – D

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260/237.3, 260/2

C07D 225/06 (2006.01) C07D 491/056 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1218989

4-14320/CGC 1035/+ Certain benzazocinone and benzazoninone derivatives. Abstract of the disclosure The invention concerns angiotensin-converting enzyme inhibitors of the formla I Image (I) wherein RA and RB are radicals of the formula Image and Image respectively, in which R° is carboxy or a functionally modified carboxy; R1 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, carboxy lower alkyl, esterified carboxy lower alkyl, carbamoyl lower alkyl, N-substituted carbamoyl lower alkyl, hydroxy lower alkyl, etherified or acylated hydroxy lower alkyl, aryloxy lower alkyl, aryl-(thio-, sulfinyl-, or sulfonyl-) lower alkyl, aryl-N-lower alkylamino lower alkyl, or arylamino lower alkyl; R2 is hydrogen or lower alkyl; R3 and R4, each independently, represent hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, hydroxy, halogen, trifluoromethyl, or R3 and R4 taken together represent lower alkylenedioxy; R5 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 the carbocyclic ring may also be hexahydro; salts and stereoisomers of all these compounds.

446969

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