Spasmolytic, vaso-dilating and anti-hypertensive compositions an

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Parasitic organism or component thereof or substance...

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424251, 424263, A61K 31455

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active

039669483

ABSTRACT:
1,4-Dihydropyridines of the formula: ##SPC1##
Wherein
R is hydrogen, straight, branched or cyclic lower alkyl, lower alkenyl, or lower alkinyl, unsubstituted or substituted by hydroxyl or alkoxy of 1 to 3 carbon atoms; or benzyl, or phenethyl, unsubstituted or substituted in the aryl portion by 1 to 7 members selected from the group consisting of 1 to 3 alkoxy moieties of 1 to 3 carbon atoms, 1 or 2 alkyl moieties of 1 to 3 carbon atoms, and 1 or 2 halogen atoms;
R.sub.1 is straight or branched chain alkyl of 1 to 4 carbon atoms;
R.sub.2 is straight or branched chain alkyl of 1 to 6 carbon atoms, straight or branched chain dialkyl of 1 to 6 carbon atoms, straight or branched chain alkenyl of 2 to 6 carbon atoms, straight or branched chain alkinyl of 2 to 6 carbon atoms, cyclic alkyl of 3 to 6 carbon atoms, cyclic alkenyl of 3 to 6 carbon atoms, straight or branched chain alkyl or alkenyl of 2 to 6 carbon atoms interrupted by 1 or 2 oxygen atoms, straight or branched chain alkyl of 1 to 6 carbon atoms substituted by hydroxyl, or straight or branched chain alkenyl of 2 to 6 carbon atoms substituted by hydroxyl;
R.sub.3 is aryl, unsubstituted or substituted by 1 to 3 members selected from the group consisting of 1 to 3 nitro moieties, 1 or 2 cyano moieties, 1 to 3 halogen atoms, 1 or 2 hydroxyl moieties, 1 or 2 acyloxy moieties of 1 or 2 carbon atoms in the acyl portion, 1 to 3 alkoxy moieties of 1 to 4 carbon atoms, a dioxymethylene moiety of the formula: ##SPC2##
An alkylmercapto moiety of 1 to 4 carbon atoms in the alkyl portion, trifluoromethyl, carboxyl, carbalkoxy of 1 to 4 carbon atoms in the alkoxy portion and an alkyl-sulphonyl moiety of 1 to 4 carbon atoms in the alkyl portion; benzyl; styryl; pyridyl; pyrimidyl; furyl; thienyl; pyrrolyl; pyridyl, pyrrolyl, thienyl or furyl substituted by alkyl of 1 to 2 carbon atoms; or pyrimidyl substituted by at least one member selected from the group consisting of alkyl of 1 or 2 carbon atoms, 1 or 2 methoxy moieties and 1 or 2 ethoxy moieties; and
R.sub.4 is straight or branched chain alkyl of 1 to 4 carbon atoms, are useful for their coronary dilating effect, their nitrite-like effect on the heart, their anti-fibrillation effect, their vascular-spasmolytic effect and muscular-spasmolytic effect, and as anti-hypertensives.

REFERENCES:
patent: 3647807 (1972-03-01), Bossert et al.
Merck Index, 7th Ed. p. 1434, (1960).

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