发明名称 ARYLQUINAZOLINES
摘要 The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.
申请公布号 US2016083401(A1) 申请公布日期 2016.03.24
申请号 US201414890214 申请日期 2014.05.08
申请人 MERCK PATENT GMBH 发明人 FUCHSS Thomas;EMDE Ulrich;BUCHSTALLER Hans-Peter;MEDERSKI Werner
分类号 C07D513/04;C07D401/10;A61K31/5377;C07D403/10;C07D403/14;C07D487/04;C07D495/04;C07D405/14;C07D471/04;C07D498/08;A61K31/5386;C07D239/74;C07D417/14;C07D417/10;C07D491/048;C07D473/00;A61K45/06 主分类号 C07D513/04
代理机构 代理人
主权项 1. Compounds of the formula (I) in which X is CH, CF, S or N, Y is CH, S or N, Z is C or N, - - - - forms, if Z═C, a double bond together with the single bond, is absent if Z═N, n is 1 or 2, where if n=1, X═S,and if n=2, both X═CH, or the X linked to the pyrimidine ring is CF and the X not linked to the pyrimidine ring is CH, or one X is CH and the other X is N; m is 1 or 2, where if m=1, Y═S,and if m=2, both Y═CH, or one Y is CH and the other Y is N; R1, R2, R3, R4, independently of one another, are H, Hal, CN, OH, CONH2, CONH(LA) or LA; R5 is H, Hal, CN or C≡CH; Cyc is phenyl, which may be unsubstituted or mono- or disubstituted, independently of one another, by R6, or is Het1; Het1 is a mono- or bicyclic, 5-10-membered heterocycle, having 1-3 N, O and/or S atoms, or 1-4 N atoms, which may be unsubstituted or mono-, di- or trisubstituted, independently of one another, by R6, or may be monosubstituted by Het2; R6 is Hal, LA, oxo, CN, or NH2; LA is unbranched or branched alkyl having 1-5 C atoms, which may be saturated or partially unsaturated, in which 1-3 H atoms may be replaced by Hal, and/or one H atom may be replaced by CN or Het2, and/or one or two CH2 groups may be replaced by O, NH, NH2, N(CH3) or CO; Het2 is a 3-5-membered aliphatic homo- or heterocycle having 0, 1, 2 or 3 N, O and/or S atoms, which is unsubstituted; Hal is F, Cl, Br or I; and/or physiologically acceptable salts, tautomers and/or stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE