Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-01-05
1993-04-13
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544316, 544317, 544318, 514255, A61K 31495, C07D23922
Patent
active
052023303
ABSTRACT:
Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.
REFERENCES:
patent: 4048171 (1977-09-01), Bossert et al.
patent: 4572908 (1966-02-01), Campbell et al.
patent: 4609494 (1986-09-01), Baldwin et al.
patent: 4640922 (1987-02-01), Cho et al.
patent: 4675321 (1987-06-01), Baldwin et al.
patent: 4683234 (1987-07-01), Cho et al.
patent: 4684655 (1987-08-01), Atwal
patent: 4684656 (1987-08-01), Atwal
patent: 4689414 (1987-08-01), Atwal
J. Org. Chem., vol. 50, pp. 4227-4230, Cho et al.--"Synthesis of Novel Dihydropyrimidines and Tetra-hydropyrimidines", (1978).
Khanina et al., Khim. Farm. Zh., vol. 12, pp. 1321-1322 (1978) "Synthesis and Pharmacological Investigation . . . ".
George et al., Synthesis (1975) pp. 405-407, "Condensed Heterocycles from 5-Ethoxycarbonyl-6-methyltetra hydropyrimidine-2-ones".
Sweet et al., J. Amer. Chem. Soc., vol. 95, pp. 8741-8749 (1973), "On the Synthesis of 3,4-Dihydro-2(1H)-pyrimidones . . . ".
Konyukhov et al., Zh. Organ. Khim., vol. 1, No. 8, pp. 1487-1489 (1965), "Synthesis and Investigation . . . ".
Folkers et al., J. Am. Chem. Soc., vol. 56, pp. 1374-1377, (1934) "Researches on Pyrimidines . . . ".
Goerlitzer et al., Arch. Pharm. vol. 314, pp. 938-949 (1981).
Burger, Medicinal Chemistry, 2nd Ed., 1960, pp. 551-564, 572-578, 582-591, 606-620.
Derwent, 87-15 2482/22, Apr. 22, 1987.
Elkasaby, Pakistan J.Sci.Ind.Res., vol. 21, No. 2, pp. 58-61 (1978), "Condensation of Ethyl .alpha.-Acetylcinnametes With Thioureas".
George et al., Synthesis (1975) pp. 405-407, Condensed Heterocycles from 5-Ethoxycarbonyl-6-methyltetrahydropyrimidin-2-ones.
Zidermane et al., "Antitumor Action of Dihydropyridine and Dihydropyrimidine Derivatives", Chem. Abst., 75, 47266e (1971).
Iwanami et al., "N-Substituted-1,4-Dihydropyridine Derivatives", Chem. Abst., 86, 43570d (1977).
Goerlitzer et al., Chem. Abst., 96, 85501u (1982).
Stolefuss, "Dihydropyrimidines Useful In Treating Circulatory Ailments" Chem. Abst. 101, 55110v (1984).
Merck Index, 10th Ed., "Nifedipine" 6374, (1983).
Bianchi et al., "Long Lasting Anti-hypertensive Effects . . . " IRCS Med. Sci., vol. 14, pp. 817-818 (1986).
Tamazawa et al., "Stereoselectivity of a Potent Calcium Antagonist . . . ", J. Med. Chem., vol. 29, pp. 2504-2511 (1986).
Goodman et al. The Pharmacological Basis of Therapeutics, 6 ed., p. 28.
Atwal Karnail
Kimball Spencer D.
Rovnyak George C.
Davis Stephen B.
E. R. Squibb & Sons Inc.
Richter Johann
LandOfFree
2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxyl does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxyl, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxyl will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-1155569