Antihypertensive diphenylpropyl aminopropyl ester of 1,4-dihydro

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546321, A61K 31455, C07D21190

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active

047726210

ABSTRACT:
Novel antihypertensive and coronary dilating asymmetric diesters of 1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylic acid (or the stereoisomers or pharmaceutically acceptable acid addition salts thereof) have the general formula (I): ##STR1## wherein Ph is phenyl, Ar is 2-nitrophenyl, 3-nitrophenyl, 2,3-dichlorophenyl or benzofurazan-4-yl, A is a straight or branched chain alkylene radical having from 2 to 6 carbon atoms, R is a straight or branched chain alkyl radical having from 1 to 6 carbon atoms, optionally mono-substituted by an alkoxy substituent having from 1 to 6 carbon atoms, R.sub.1 is hydrogen, hydroxy or an alkyl radical having from 1 to 4 carbon atoms, and R.sub.2 is hydrogen or methyl. The subject diesters are facilely prepared from the aldehydes ArCHO and esters of acetoacetic and 3-aminocrotonic acids.

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Burger, A., "Selected Pharmaceutical Testing Methods", vol. 8, Marcel Dekker, Inc., New York (1968) pp. 29-42.
Bossert, et al., "4-Aryldihydropyridines", Angew. Chem. Int. Ed. Engl. 20 (1981) pp. 762-769.
Schramm, et al., "Novel Dihydropyridines with Positive Inotropic Action", Nature, vol. 303 (Jun. 9, 1983) pp. 535-537.

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