Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids
AssigneeWarner-Lambert Company
InventorsMilton L. Hoefle, Sylvester Klutchko
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Abstract
Substituted acyl derivatives of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids and the pharmaceutically acceptable salts thereof are produced by coupling a suitably substituted 1,2,3,4-tetrahydroisoquinoline with a suitably substituted amino acid and when desired hydrolyzing or removing protecting groups of the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.
Claims15
A substituted acyl compound of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid having the formula ##STR5## where R is hydrogen, lower alkyl or phenylalkyl;
- R.sub.1 is hydrogen, lower alkyl, or benzyl;
- R.sub.2 is hydrogen, or lower alkyl and Ar is phenyl, or substituted phenyl having 1 or 2 substituents selected from the group consisting of fluorine, chlorine, bromine, lower alkyl, lower alkoxy, hydroxy or amino;
- X and Y are independently hydrogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, hydroxy, or X and Y together are methylenedioxy;
- and m is 0 to 3;
- wherein lower alkyl, alkyl in the group phenylalkyl;
- and lower alkoxy has 1 to 4 straight or branched carbon atoms and the pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.