3-amino-1-benzazepin-2-one-1-alkanoic acids

C - Chemistry – Metallurgy – 07 – D

Patent

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260/241.15, 260/

C07D 223/16 (2006.01) C07D 491/056 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1218993

- 1 - 4-14336/CGC 949/4/+ 3-Amino-1-benzazepin-2-one-1-alkanoic acids Abstract of the disclosure The invention concerns angiotensin-converting enzyme inhibitor compounds of the formula Image (I) wherein RA and RB are radicals of the formula Image and Image , respectively, in which R0 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 - 2 - alkylenedioxy; R5 is hydrogen or lower alkyl; 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 or 6,7,8,9-tetrahydro; with the proviso, that, if R1 represents hydrogen, lower alkyl, amino lower alkyl, aryl, aryl lower alkyl, cycloalkyl, or cycloalkyl lower alkyl, X is acylated hydroxy together with one hydrogen; and salts thereof. They are prepared, for example, by reducing a starting material corresponding to formula I, which contains a double bond located at the carbon atom in 3-position.

446970

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