Cycloalkyl-substituted glutaramide antihypertensive agents

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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514403, 514404, 514419, 514423, 514428, 514467, 514471, 514481, 514484, 514488, 514510, 514530, 514562, 514563, 546323, 548342, 548372, 548495, 548539, 548567, 549229, 549487, 560 10, 560 12, 560 13, 560 27, 560 28, 560 38, 560 39, 560 41, 560115, 560118, 562427, 562430, 562443, 562444, 562450, 562500, A61K 31195, A61K 3124, C07C22910

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049754440

ABSTRACT:
Compounds of the formula ##STR1## wherein A is a carbocyclic, saturated or unsaturated ring; R.sup.1 is hydrogen or alkyl; R and R.sup.4 are each alkyl, cycloalkyl, benzyl or a readily hydrolyzable ester group; Y is a bond or a straight or branch alkylene; R.sup.2 is hydrogen, aryl, heterocyclic, R.sup.6 CONR.sup.5, R.sup.7 NR.sup.5 CO, R.sup.7 NR.sup.5 SO.sub.2 --or R.sup.8 SO.sub.2 NR.sup.5 --where R.sup.5 is hydrogen, alkyl or aralkyl; R.sup.6 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group of the formula ##STR2## where R.sup.9 is hydrogen, hydroxy, alkoxy, alkyl, hydroxyalkyl, aralkyl, alkylene, heterocyclic, heterocyclylalkyl, R.sup.12 CONH--, R.sup.12 SO.sub.2 NH-- or (R.sup.13).sub.2 N--; R.sup.10 and R.sup.11 are each hydrogen or alkyl; or R.sup.10 is hydrogen and R.sup.11 is aminoalkyl, imidazolylmethyl, aryl, aralkyl, aralkoxyalkoxy, hydroxyalkyl or methylthioalkyl; or R.sup.10 and R.sup.11 together with the carbon to which they are attached form a carbocyclic or heterocyclic ring optionally substituted by amino, alkanoyl or aroyl; R.sup.12 is alkyl, cycloalkyl, aryl, aralkyl, heterocyclic or heterocyclylalkyl; each R.sup.13 is hydrogen, alkyl, aralkyl or both R.sup.13 together with the nitrogen to which they are attached form a heterocyclic ring; R.sup.7 is alkyl, aryl, aralkyl, heterocyclic, heterocyclyalkyl or a group ##STR3## where R.sup.10 and R.sup.11 are as defined and R.sup.14 is (R.sup.13).sub.2 NCO, R.sup.12 OCH.sub.2 -- or R.sup.15 OCO, where R.sup.12 and R.sup.13 are as defined and R.sup.15 is alkyl, cycloalkyl or aralkyl; and R.sup.8 is alkyl, aryl, aralkyl, heterocyclic or heterocyclylalkyl; R.sup.3 is a group ##STR4## where R.sup.16 is hydrogen, halo, hydroxy, alkoxy, cycloalkoxy, alkenyloxy, alkoxycarbonyloxy, cycloalkoxycarbonylalkoxy or alkyl SO.sub.2 NH--; and R.sup.20 is hydrogen, alkyl, alkoxy, alkanoyl or halo; or R.sup.3 is 3-indolylmethyl or 3-indazolylmethyl, each optionally substituted in the benzenoid ring by alkyl, alkoxy, hydroxy or trifluoromethyl as antihypertensive agents.

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