Calcium antagonist N-hetero ester 1,4-dihydropyridines

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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514228, 514234, 514236, 514252, 514253, 514316, 514318, 514338, 514343, 514788, 514947, 546187, 546194, 546270, 546272, 546281, 544121, 544130, 544131, 544357, 544364, C07D40112, C07D41314, C07D40114, A61K 31455

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active

046525734

ABSTRACT:
Compounds having calcium channel antagonist activity of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each independently amino, trifluoromethyl, pentafluoroethyl, alkoxy, lower alkenyl, or lower alkynyl or branched or unbranched lower alkyl, which is unsubstituted or is substituted with cyano, hydroxy, acyloxy, hydrazino, lower alkyl amino, or di(lower alkyl)-amino or 5 or 6 membered saturated nitrogen-containing heterocyclic-1-yl, which is unsubstituted or is substituted with oxo, hydroxy, alkyl, and hydroxy (lower alkyl) R.sub.3 is straight- or branched-chain C.sub.1 to C.sub.12 alkyl, alkenyl, alkynyl, or cycloalkyl, and is either unsubstituted or substituted with hydroxy, acyloxy, cyano, di(lower alkyl) amino 5- or 6-membered saturated nitrogen-containing heterocyclic-1-yl or R.sub.3 is --A-R.sub.4, A is a straight- or branched-chain hydrocarbon moiety containing from 2 to 12 carbon atoms and from 0 to 2 double bonds, R.sub.4 is selected from the group consisting of: ##STR2## R.sub.5 is hydrogen, nitro, cyano, azido, amino, trifluoromethyl, alkylamino, dialkylamino, halo, carboxyl, carbalkoxy, alkyl, alkenyl, alkynyl, cycloalkyl, acylamino, carboxamido, sulfonamide, and SO.sub.m -(lower)alkyl where m is 0, 1, or 2 and R.sub.6 is aryl or heteroaryl or a pharmaceutically-acceptable salt thereof are disclosed. Also disclosed is a method of treating hypertension and other disorders by administering an effective amount of a compound of the present invention.

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