Pyrrolopyrimidinyalglutaminate derivatives and their use

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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514183, 514212, 514252, 514255, 540452, 540465, 540481, 540485, 540486, 540600, 544116, 544117, 544238, 544253, 544280, A61K 31505, C07D48704

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active

054038430

ABSTRACT:
A condensed pyrimidine derivative of the formula (I): ##STR1## wherein the ring A stands for an optionally substituted 5-membered ring; B stands for an optionally substituted divalent 5- or 6-membered homo- or hetero-cyclic group; X stands for, among others, amino group; Y stands for, among others, hydrogen atom, halogen atom or amino group; Z stands for a divalent aliphatic group having five or less atoms forming straight chain, optionally having nitrogen, whose chain portion may optionally have a hetero-atom; W stands for, among others, --NH--CO-- or --CO--NH--; R.sup.1 stands for an optionally substituted cyclic or chain-like group; COOR.sup.2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when --W--R.sup.1 denotes a moiety represented by the formula: ##STR2## wherein COOR.sup.16 and COOR.sup.17 are, independently, an optionally esterified carboxyl group and n denotes an integer of 1 to 5, p denotes 1, 3 or 4, or a salt thereof, exhibiting highly specific toxicities to various tumor cells and excellent therapeutic effects on methotrexate-resistant tumor cells as well.

REFERENCES:
patent: 4767761 (1988-08-01), Rosowsky
patent: 4895946 (1990-01-01), Taylor et al.
patent: 4946846 (1990-08-01), Nomura et al.
patent: 4996206 (1991-02-01), Taylor et al.
patent: 4997838 (1991-03-01), Akimoto et al.

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