发明名称 PHOSPHONOXY QUINAZOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
摘要 Quinazoline derivatives of formula (I):;;wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
申请公布号 US2014162984(A1) 申请公布日期 2014.06.12
申请号 US201213590662 申请日期 2012.08.21
申请人 HERON Nicola Murdoch;MORTLOCK Andrew Austen;JUNG Frederic Henri;PASQUET Georges Rene 发明人 HERON Nicola Murdoch;MORTLOCK Andrew Austen;JUNG Frederic Henri;PASQUET Georges Rene
分类号 C07F9/6558 主分类号 C07F9/6558
代理机构 代理人
主权项 1. A compound of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and optionally containing one or two further nitrogen atoms; X is O, S, S(O), S(O)2 or NR14; m is 0, 1, 2 or 3; Z is a group selected from —NR1R2, phosphonooxy, C3-6cycloalkyl (substituted by phosphonooxy or C1-4alkyl (substituted by phosphonooxy)) and a 4- to 7-membered ring linked via a carbon atom containing a nitrogen atom and optionally containing a further nitrogen atom, which ring may be saturated, partially saturated or unsaturated wherein the ring is substituted on carbon or nitrogen by phosphonooxy or C1-4alkyl (substituted by phosphonooxy) and wherein the ring is optionally further substituted on carbon or nitrogen by 1, 2 or 3 halo or C1-4alkyl groups; R1 is —COR8, —CONR8R9 or C1-6alkyl (substituted by phosphonooxy and optionally further substituted by 1 or 2 halo or methoxy groups); R2 is hydrogen, —COR10, —CONR10R11, C1-6alkyl (optionally substituted by 1, 2 or 3 halo or C1-4alkoxy groups or —S(O)pR11 (where p is 0, 1 or 2) or phosphonooxy), C2-6alkenyl, C2-6alkynyl, C3-6cycloalkyl and C3-6cycloalkylC1-4alkyl; or R1 and R2 together with the nitrogen to which they are attached form a 4- to 7-membered ring optionally containing a further nitrogen atom which may be saturated, partially saturated or unsaturated wherein the ring is substituted on carbon or nitrogen by a group selected from phosphonooxy and C1-4alkyl (substituted by phosphonooxy or —NR8R9) and where the ring is optionally further substituted on carbon or nitrogen by 1, 2 or 3 halo or C1-4alkyl groups; R3 is hydrogen, halo, cyano, nitro, C1-6alkoxy, C1-6alkyl, —OR12, —CHR12R13, —OC(O)R12, —C(O)R12, —NR12C(O)R13, —C(O)NR12R13, —NR12SO2R13 or —NR12R13; R4 is hydrogen or a group selected from C1-4alkyl, heteroaryl, heteroarylC1-4alkyl, aryl and arylC1-4alkyl which group is optionally substituted by 1, 2 or 3 substitutents selected from halo, methyl, ethyl, cyclopropyl and ethynyl; R5 is selected from hydrogen, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C3-6cycloalkyl and C3-6 cyclo alkylC1-4alkyl; R6 and R7 are independently hydrogen, halo, C1-4alkyl, C3-6cycloalkyl, hydroxy and C1-4 alkoxy; R8 is C1-4alkyl substituted by phosphonooxy and optionally further substituted by 1 or 2 halo or methoxy groups; R9 is hydrogen or C1-4alkyl; R10 is hydrogen or C1-4alkyl (optionally substituted by halo, C1-4alkoxy, —S(O)q (where q is 0, 1 or 2) or phosphonoxy); R11, R12, R13 and R14 are independently hydrogen, C1-4alkyl or heterocyclyl; or a pharmaceutically acceptable salt thereof.
地址 Macclesfield GB