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    2,4-diamino pyrimidine compounds having anti-cell proliferative activity
    4.
    发明授权
    2,4-diamino pyrimidine compounds having anti-cell proliferative activity 失效
    具有抗细胞增殖活性的2,4-二氨基嘧啶化合物

    公开(公告)号：US07176212B2

    公开(公告)日：2007-02-13

    申请号：US10771118

    申请日：2004-02-04

    申请人： Gloria Anne Breault ,  Janet Elizabeth Pease

    发明人： Gloria Anne Breault ,  Janet Elizabeth Pease

    IPC分类号： C07D239/48 ,  A61K31/505 ,  C07D239/42

    CPC分类号： C07D239/48

    摘要： 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–C)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-hydrolyzable ester thereof; are useful as anti-cancer agents; and processes for heir manufacture and pharmaceutical compositions containing them are described

    摘要翻译： 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-C）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

    Pyrimidine compounds
    6.
    发明授权
    Pyrimidine compounds 失效
    嘧啶化合物

    公开(公告)号：US06632820B1

    公开(公告)日：2003-10-14

    申请号：US09763681

    申请日：2001-02-26

    申请人： Gloria Anne Breault ,  Philip John Jewsbury ,  Janet Elizabeth Pease

    发明人： Gloria Anne Breault ,  Philip John Jewsbury ,  Janet Elizabeth Pease

    IPC分类号： C07D23948

    CPC分类号： C07D239/48

    摘要： A pyrimidine derivative of formula (I) wherein, for example, R1 is-(1-6C)alkyl or (3-5C)alkenyl [optionally substituted by a phenyl substituent]; 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 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 each optionally bear other substituents selected 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 their manufacture and pharmaceutical compositions containing them are described.

    摘要翻译： 式（I）的嘧啶衍生物，其中例如R 1为 - （1-6C）烷基或（3-5C）烯基[任选被 苯基取代基]; Q 1 和Q 2 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 中的一个或两个具有式（Ia）的一个取代基[条件是当存在于 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，（1-4C）烷氧基，（1-4C）烷硫基，-NH（1-4C）烷基，-N [（1 -4C）烷基]环烷基或-NH-（3-8C）环烷基; n为1,2或3; m为1,2或3; 并且Q 1 和Q 2 可以各自任选地具有选自卤代，（1-6C）烷基，氰基 和（2-4C）烯基，或其药学上可接受的盐或其体内可水解的酯; 可用作抗癌剂; 并描述了其制造方法和含有它们的药物组合物。