Fused pyrimidines, their production and use

Details Fused pyrimidines, their production and use Fused pyrimidines, their production and use

1989-03-27

1990-08-07

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

544279, 544280, A61K 31505, C07D47104

Patent

active

049468464

ABSTRACT:
New fused pyrimidines of the general formula (I): ##STR1## wherein the ring .circle. A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, fluorine or a lower alkyl group, and --COOR.sup.5 and --COOR.sup.6 are independently a carboxyl group which may be esterified, and salts thereof have excellent anti-tumor effects, and they can be produced by the following reaction scheme: ##STR2## in which .circle. A is, X, R.sup.1 to R.sup.4, --COOR.sup.5 have the above meanings.

REFERENCES:
patent: 4460591 (1984-07-01), DeGraw et al.
patent: 4684653 (1987-08-01), Taylor et al.
patent: 4725687 (1988-02-01), Piper et al.
Edward C. Taylor et al., "Synthesis of the Antileukemic Agents 5,10-Dideazaaminopterin and 5,10-Dideaza-5,6,7,8-tetrahydro-aminopterin", Journal of Medicinal Chemistry, vol. 28, pp. 914-921 (1985).
Bianchi, C. Paul, "1-Pharmacology", Chemical Abstracts, vol. 103, pp. 607, 6688 (1985).
Haynes, J. B., et al., "Synthesis of Quinazoline Analogs of Isofolic Acid", Journal of Medicinal Chemistry, vol. 18, No. 6, pp. 632-634, (1975).

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