Condensed pyrimidine derivatives, their production and use

C - Chemistry – Metallurgy – 07 – D

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C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 38/04 (2006.01) C07D 239/70 (2006.01) C07D 403/12 (2006.01) C07D 491/04 (2006.01) C07D 491/048 (2006.01) C07D 495/04 (2006.01) C07K 5/04 (2006.01)

Patent

CA 2075787

Condensed Pyrimidine Derivatives, Their Production and Use Abstract of the Disclosure A condensed pyrimidine derivative of the formula (I): Image (I) 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-; R1 stands for an optionally substituted cyclic or chain-like group ; COOR2 stands for an optionally esterified carboxyl group; and p denotes an integer of 1 to 4, provided that when -W-R1 denotes a moiety represented by the formula: Image wherein COOR16 and COOR17 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.

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