Sulfur-containing fused pyrimidine derivatives, their production

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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5142242, 514258, 540552, 544 48, 544278, C07D51500, C07D51300, A61K 3155, A61K 31505

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active

050828380

ABSTRACT:
Disclosed is a compound represented by the formula (I) or a salt thereof: ##STR1## wherein R.sup.1 represents an aliphatic hydrocarbon, aralkyl or aryl group which may be substituted; R.sup.2 represents hydrogen, an aliphatic hydrocarbon group having one or more substituents, an aryl group which may be substituted, an amino group which may be substituted, a formyl group, a nitro group or a halogeno group; A represents a divalent hydrocarbon chain of 2 to 4 carbon atoms which may be substituted; and m represents an integer of 0 to 2, which is useful for treatment and prevention of diseases induced by abnormalities in regulation of reactions in vivo mediated through endothelin or interleukin 1, and of immune diseases and inflammatory diseases.

REFERENCES:
patent: 4394505 (1983-07-01), Kamata et al.
Tetrahedron, vol. 28, pp. 4737-4746 (1972), Tsuge et al., "Studies of Acyl and Thioacyl Isocyanates X.sup.1 The Reactions of Benzoyl and Thiobenzoyl Isocyanates with 2-Thiazolines and 2-Oxazolines".
J. C. S. Perkin I, (1972), pp. 2385-2391, Brown et al., "The Synthesis of Some 1-Substituted Cytosine and Uracil Derivatives".
Jnl. of Pharm. Sciences, vol. 71, No. 8, Aug. 1982, pp. 897-900, Kaul et al., "2-.sup.14 C-1-Allyl-3,5-Diethyl-6-Chlorouracil II: Isolation and Structures . . . ".
Arzneim-Forsch/Drug Res. 32(I), No. 6 (1982) Kaul et al., "Identifizierung eines Dritten S-Haltigen Metaboliten von 1-Allyl-3,5-Diethyl-6-Chloruracil und Bildungsmechanismus der SCH.sub.3 -Metaboliten".
Xenobiotica, vol. 12, No. 8, 1982, pp. 495-498, Kaul et al., "Structure of a Novel Sulphur-Containing Metabolite of Acluracil (1-Allyl-3,5-Diethyl-6-Chlorouracil)".

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