Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1987-10-16
1989-11-14
Ford, John M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514 16, 514 17, 514 18, 514 19, 530331, 530330, 530329, 544321, 2609982, A61K 31505, C07D23949, C07D23936
Patent
active
048808121
ABSTRACT:
The present invention provides a compound of formula (I): ##STR1## wherein R.sup.1 is hydrogen , C.sub.1-4 alkyl, acetyl or formyl; R.sup.2 and R.sup.3 are the same or different and are hydrogen or C.sub.1-4 alkyl; R.sup.4 is NR.sup.11 R.sup.12 ; R.sup.11, R.sup.12, R.sup.5 and R.sup.6 are the same or different and are hydrogen, C.sub.1-4 alkyl or C.sub.1-12 acyl; R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are the same or different and are hydrogen, halo, C.sub.1-4 haloalkyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and n is 2, 3, 4 or 5; m is 0 or an integer from 1 to 6; or a salt thereof, methods for the preparation of the compounds of the formula (I), intermediates in their preparations, pharmaceutical formulations containing them, and their use in the treatment of tumors.
REFERENCES:
Chemische Berichte, vol. 110, No. 4, 1977, pp. 1462-1469, F. Seela, et al: Mannich-Reaktion AM 2-Amino-3,7-Dihydropyrrolo (2,3-d)-Pyrimidin-4-ON, dem Chromophor des Ribonucleosids `Q`.
Khim Farm. ZH., vol. 1, No. 6, 1967, pp. 5-9, V. M. Berezovskij, et al, Synthesis pyrimidine Analogs of Folic Acid.
J. of Pharm. Sci., vol. 52, No. 9, Sep. 1963, pp. 840-843, B. R. Baker, et al, Analogs of Tetrahydrofolic Acid VII, Synthesis of N-(1-(2-amino-4-hydroxy-6-methyl-5-pyrimidil)-3propyl)-p-aminobenzoyl-L-gl utamic acid, an inhibitor of folic reductase.
J. of Medicinal Chem., vol. 6, Nov. 1963, pp. 664-669, B. R. Baker, et al, Analogs of Tetrahydrofolic Acid. IX, Synthesis of N-(1-(2-amino-4-hydroxy-6-phenyl-5-pyrimidyl)-3-propyl)-p-aminobenzoyl-L-g lutamic acid, a nonclassical' inhibitor of some folic cofactor area enzymes.
Chemical Abstracts, vol. 68, no. 11, (1968), p. 4797, col. 1, abstract no. 49546a, Columbus, Ohio, U.S..
Brown Donald
Burroughs Wellcome Co.
Ford John M.
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