发明名称 PYRIMIDINE DERIVATIVES AND GUANINE DERIVATIVES, AND THEIR USE IN TREATING TUMOUR CELLS
摘要 The invention provides compounds exhibiting the ability to deplete <u>O</u><6>-alkylguanine-DNA alkyltransferase (ATase) activity in tumour cells. The compounds include certain pyrimidine derivatives of formula (II), wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof, R<2> is selected from H, C<1>-C<5> alkyl, halogen or NH<2>, R<4> and R<5> which are the same or different are selected from H, NH-Y' or NOn wherein Y' is H, ribosyl, deoxyribosyl, arabinosyl, (a) wherein X is O or S, R" is alkyl and R''' is H or alkyl, or substituted derivatives thereof, n = 1 or 2 or R<4> and R<5> together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more hetero atoms, and pharmaceutically acceptable salts thereof. They include certain guanine derivatives of formula (XIII), wherein R<6> is as defined at (i) for R above and Y' is as defined above.
申请公布号 WO9720843(A1) 申请公布日期 1997.06.12
申请号 WO1996IE00084 申请日期 1996.12.09
申请人 CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED;MCMURRY, THOMAS, BRIAN, HAMILTON;MCELHINNEY, ROBERT, STANLEY;MCCORMICK, JOAN, ELIZABETH;DONNELLY, DOROTHY, JOSEPHINE;MURRAY, PAUL;CAROLA, CHRISTOPHE;ELDER, RHODERICK, HUGH;KELLY, JANE;MARGISON, GEOFFREY, PAUL;WATSON, AMANDA, JEAN;RAFFERTY, JOSEPH, ANTHONY;WILLINGTON, MARK, ANDREW;MIDDLETON, MARK, ROSS 发明人 MCMURRY, THOMAS, BRIAN, HAMILTON;MCELHINNEY, ROBERT, STANLEY;MCCORMICK, JOAN, ELIZABETH;DONNELLY, DOROTHY, JOSEPHINE;MURRAY, PAUL;CAROLA, CHRISTOPHE;ELDER, RHODERICK, HUGH;KELLY, JANE;MARGISON, GEOFFREY, PAUL;WATSON, AMANDA, JEAN;RAFFERTY, JOSEPH, ANTHONY;WILLINGTON, MARK, ANDREW;MIDDLETON, MARK, ROSS
分类号 C07D239/47;A61K31/00;A61K31/17;A61K31/505;A61K31/519;A61K31/52;A61K31/522;A61K31/529;A61K31/70;A61K31/7042;A61K31/7052;A61K31/706;A61K31/7064;A61K31/7076;A61K31/708;A61P35/00;A61P43/00;C07D239/46;C07D239/48;C07D401/12;C07D405/12;C07D409/12;C07D471/04;C07D473/00;C07D473/18;C07D473/22;C07D473/30;C07D473/40;C07D475/02;C07D475/04;C07D487/04;C07D498/04;C07D513/04;C07H19/04;C07H19/06;C07H19/16;C07H19/167;C07H19/173;C07H19/19;C07H19/23 主分类号 C07D239/47
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