Antihypertensive 7-trifluoromethyl-4-aminoquinolones

Details Antihypertensive 7-trifluoromethyl-4-aminoquinolones Antihypertensive 7-trifluoromethyl-4-aminoquinolones

1978-05-05

1979-09-04

Wheeler, David

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546161, A61K 3147, C07D21544

Patent

active

041668537

ABSTRACT:
Antihypertensive compounds of the formula II ##STR1## wherein D is a piperidino or 1,2,5,6-tetrahydropyridino ring; wherein X is chloro or trifluoromethyl; wherein R.sub.1 is hydrogen or hydroxy when the D ring is piperidino, or nothing when the D ring is 1,2,5,6-tetrahydropyridino; and, wherein the moiety Ar is 2-oxo-1-benzimidazolinyl, phenyl, or phenyl substituted by one or two halo, trifluoromethyl, or alkyl, alkoxy, in which the carbon moieties are of 1 to 3 carbon atoms, inclusive, and halo is chloro, bromo, or fluoro, are produced by reacting 4-[[7-(chloro) or (trifluoromethyl)-4-quinolinyl]-amino]benzoic acid with thionyl chloride or a carbonyl diimidazole and subsequent reaction with the selected substituted piperidine or 1,2,5,6-tetrahydropyridine.
The pharmacologically acceptable acid addition salts of II can also be used as antihypertensives.

REFERENCES:
patent: 3632761 (1972-01-01), Graham et al.
patent: 3875165 (1975-04-01), Archibald et al.
patent: 3971787 (1976-07-01), Archibald et al.
patent: 4025629 (1977-05-01), Coverdale
March, Advanced Org. Chem., pp. 335-339, (1968).
Morrison et al., Org. Chem., (1966), pp. 590-591.

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