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    • 6. 发明申请
    • 2,4-Diamino pyrimidine compounds having anti-cell proliferative activity
    • 具有抗细胞增殖活性的2,4-二氨基嘧啶化合物
    • US20050090493A1
    • 2005-04-28
    • US10771118
    • 2004-02-04
    • Gloria BreaultJanet Pease
    • Gloria BreaultJanet Pease
    • C07D239/49A61K31/505A61K31/506A61K31/5355A61P9/00A61P9/10A61P13/12A61P17/06A61P19/00A61P27/02A61P29/00A61P35/00A61P37/00A61P43/00C07D239/48C07D403/12C07D413/02A61K31/5377C07D43/02
    • C07D239/48
    • A pyrimidine derivative of formula (I) wherein, for example, R1 is hydrogen, (1-6C)alkyl, (3-5C)alkenyl or (3-5C)alkynyl; Q1 and Q2 are independently selected from phenyl, naphthyl, indanyl and 1,2,3,4-tetrahydronaphthyl; and one or both of Q1 and Q2 bears on any available carbon atom one substituent of formula (Ia) [provided that when present in Q1 the substituent of formula (Ia) is not adjacent to the —NH— link]; wherein, for example, X is CH2, O, S or NH; Y is H or as defined for Z; Z is OH, SH, NH2, (1-4C)alkoxy, (1-4C)alkylthio, —NH(1-4C)alkyl, —N[(1-4C)alkyl]2 or —NH—(3-8C)cycloalkyl; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may optionally bear other substituents selected, for example, from halogeno, (1-6C)alkyl, cyano and (2-4C)alkenyl; or a pharmaceutically-acceptable salt or in-vivo-hydrolysable ester thereof; are useful as anti-cancer agents; and processes for heir manufacture and pharmaceutical compositions containing them are described.
    • 式(I)的嘧啶衍生物,其中例如R 1是氢,(1-6C)烷基,(3-5C)烯基或(3-5C)炔基; Q 1和Q 2个独立地选自苯基,萘基,茚满基和1,2,3,4-四氢萘基; 并且Q 1和Q 2中的一个或两个在任何可用的碳原子上具有式(Ia)的一个取代基[条件是当存在于Q 1中时, 式(Ia)的取代基不与-NH-连接相邻]; 其中,例如,X是CH 2,O,S或NH; Y为H或Z定义; Z是OH,SH,NH 2,(1-4C)烷氧基,(1-4C)烷硫基,-NH(1-4C)烷基,-N [(1-4C)烷基] 或-NH-(3-8C)环烷基; n为1,2或3; m为1,2或3; 且Q 1和Q 2可任选地具有其它取代基,例如选自卤代,(1-6C)烷基,氰基和(2-4C)烯基; 或其药学上可接受的盐或体内可水解的酯; 可用作抗癌剂; 并描述了继承人制造的方法和含有它们的药物组合物。