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    Condensed pyrimidine derivatives, their production and use as antitumor agents
    2.
    发明公开
    Condensed pyrimidine derivatives, their production and use as antitumor agents 失效
    Kondensierte Pyrimidinderivate，ihre Herstellung und ihre Verwendung als Antitumormittel。

    公开(公告)号：EP0530537A1

    公开(公告)日：1993-03-10

    申请号：EP92113523.2

    申请日：1992-08-07

    申请人： TAKEDA CHEMICAL INDUSTRIES, LTD.

    发明人： Akimoto, Hiroshi ,  Ootsu, Koichiro ,  Itoh, Fumio

    IPC分类号： C07D487/04 ,  C07D495/04 ,  C07D491/048 ,  A61K31/505

    CPC分类号： C07D487/04 ,  C07D491/04 ,  C07D495/04

    摘要： A condensed pyrimidine derivative of the formula (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:

    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.

    摘要翻译： 式（I）的稠合嘧啶衍生物：其中环A代表任选取代的5元环; B代表任选取代的二价5-或6-元同 - 或杂 - 环基团; X代表氨基; Y代表氢原子，卤原子或氨基; Z代表具有五个或更少个原子的二价脂族基，其形成直链，任选具有氮，其链部分可以任选具有杂原子; W代表-NH-CO-或-CO-NH-; R 1代表任选取代的环状或链状基团; COOR <2>代表任意酯化的羧基; 并且p表示1至4的整数，条件是当-WR 1表示由下式表示的部分时：其中COOR 1> 6和COOR 1 <7>分别独立地为 任意酯化的羧基，n表示1〜5的整数，p表示1,3或4或其盐，对各种肿瘤细胞具有高度特异性的毒性，对甲氨蝶呤耐药肿瘤细胞也具有优异的治疗效果。