N-substituted 3,4-dihydropyrimidine compounds as agents for trea

Details N-substituted 3,4-dihydropyrimidine compounds as agents for trea N-substituted 3,4-dihydropyrimidine compounds as agents for trea

1988-02-19

1990-04-24

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544335, 544229, A61K 31505, C07D23902

Patent

active

049201247

ABSTRACT:
N-substituted 3,4-dihydropyrimidine compounds of the formula: ##STR1## wherein R is straight, branched, cyclic or cyclo-straight alkyl having from one to four carbon atoms; and X.sup.1, X.sup.2 and X.sup.3 are the same or different and are hydrogen, halogen, lower alkyl having from one to four carbon atoms, lower alkoxy having from one to four carbon atoms, nitro, trifluoromethyl, hydroxy, or t-butyldimethylsilyloxy with the proviso that the case wherein X.sup.1, X.sup.2 and X.sup.3 are all hydrogen is not applicable have substantially strong and lasting vasodilative effects. Therefore, the compounds are useful as agents for treating disorders of the cardiovascular system, for example, antihypertensive agents, circulation improver and antianginal agents.

REFERENCES:
patent: 4640922 (1987-02-01), Cho et al.
patent: 4683234 (1987-07-01), Cho et al.
Iwanami et al., Chem. Pharm. Bull., vol. 27, No. 6, pp. 1426-1440, (1979).
C. Kashima et al., "Independent Synthesis of Three Types of N-Substituted Dihydrophyrimidines and Their Reactions with Malachite Green", Tetrahedron Letters, vol. 24, No. 2, 1983, pp. 209-212.
D. Nasipuri et al., "Phase-Transfer Catalysis; I.S.-Methylation of 1-Aryl-4,4,6-Trimethyl-2-Thioxo-1,2,3,4-Tetrahydropyrimidines", Communications, Dec. 1982, pp. 1073-1075.
E. F. Silversmith, J. Org. Chem. 27:4090-4091 (1962).

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