Pharmaceutically useful dihydropyridinyldicarboxylate amides and

Details Pharmaceutically useful dihydropyridinyldicarboxylate amides and Pharmaceutically useful dihydropyridinyldicarboxylate amides and

1985-01-22

1988-07-05

Hollrah, Glennon H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514253, 544295, 544296, 544357, 544364, 544365, 546321, A61K 3144, A61K 31495, C07D40112, C07D40114

Patent

active

047555122

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 electronwithdrawing 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 0 or NH; Y is lower alkylene, alkoxyalkylene, alkylaminoalkylene; and Z is phenyl, substituted phenyl, pyridinyl, substituted pyridinyl, or pyrimidinyl. Compounds of this series demonstrate activity as calcium and alphaadrenergic blockers in in vitro testing and antihypertensive, antiischemic, and platelet function inhibiting actions in in vivo screens.

REFERENCES:
patent: 3485847 (1969-12-01), Bossert et al.
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.
Bossert, et al., "4-Aryldihydropyridines, a New Class of Highly Active Calcium Antagonists", Angew. Chem., Int. Ed. Engl. 20, (1981) pp. 762-769.
Schramm, et al., "Novel Dihydropyridines with Positive Inotropic Action Through Activation of CA.sup.2+ Channels", Nature, 30 (Jun. 9, 1983), pp. 535-537.
Aritomi, et al., Chem. Pharm. Bull., 29 (11) 3163-6171 (1980).

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