Pharmaceutically useful dihydropyridinyldicarboxylate amides and

Details Pharmaceutically useful dihydropyridinyldicarboxylate amides and Pharmaceutically useful dihydropyridinyldicarboxylate amides and

1987-12-18

1990-01-23

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514254, 544295, 544296, 544357, 544360, 544364, 544365, A61K 31495, C02D40112

Patent

active

048958468

ABSTRACT:
A series of 1,4-dihydropyridin-3,5-yl dicarboxylic acid amides and esters incorporating an arylpiperazinylalkyl moiety have been prepared possessing the general formula ##STR1## wherein R.sup.4 is cycloalkyl, aryl or hetaryl, generally with electron-withdrawing substituents; R.sup.2 and R.sup.6 are lower alkyl, alkanol, alkoxyalkyl, or alkylaminoalkyl; R.sup.5 is R.sup.2 or arylpiperazinylalkyl; X is O or NH; Y is lower alkylene, alkoxyalkylene, alkylaminoalkylene; and Z is phenyl, substituted pheny, pyridinyl, substituted pyridinyl, or pyrimidinyl. Compounds of this series demonstrate activity as calcium and alpha-adrenergic blockers in in vitro testing and antihypertensive, anti-ischemic, and platelet function inhibiting actions in in vivo screens.

REFERENCES:
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patent: 3821225 (1974-06-01), Regnier et al.
patent: 3905970 (1975-09-01), Bossert et al.
patent: 3974275 (1976-08-01), Bossert et al.
patent: 3996234 (1976-12-01), Bossert et al.
patent: 4393070 (1983-07-01), Sato et al.
Aritomi, et al., Chem. Pharm. Bull., 29(11) 3163-3171 (1980).
Bossert, et al., Angew. Chem., Ing. Ed. Engl. 20 (1981) pp. 762-769.
Schramm, et al., Nature, 30 (Jun. 9, 1983) pp. 535-537.

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