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    • 3. 发明授权
    • 4-phenylamino-quinazolin-6-yl-amides
    • 4-苯基氨基 - 喹唑啉-6-基 - 酰胺
    • US08623883B2
    • 2014-01-07
    • US13914410
    • 2013-06-10
    • Warner-Lambert Company LLC
    • Stephen Alan FakhouryHelen Tsenwhei LeeJessica Elizabeth ReedKevin Matthew SchlosserKaren Elaine SextonHaile TecleRoy Thomas Winters
    • A01N43/54A61K31/519C07D239/72C07D401/00
    • C07D239/94C07D401/12C07D403/12
    • This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
    • 本发明提供下式的喹唑啉化合物:其中:R1是卤素; R2是H或卤素; R3是a)任选被卤素取代的C 1 -C 3烷基; 或(b) - (CH 2)n - 吗啉代, - (CH 2)n - 哌啶, - (CH 2)n - 哌嗪, - (CH 2)n - 哌嗪-N(C 1 -C 3烷基), - (CH 2) ,或 - (CH 2)n - 咪唑; n为1〜4; R4是 - (CH2)m-Het; Het是吗啉,哌啶,哌嗪,哌嗪-N(C 1 -C 3烷基),咪唑,吡咯烷,氮杂环庚烷,3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶,各自任选被烷基 ,卤素,OH,NH 2,NH(C 1 -C 3烷基)或N(C 1 -C 3烷基)2; m为1-3; X为O,S或NH; 或其药学上可接受的盐,以及制备它们的方法和中间体化合物,有用的药物组合物和使用该化合物治疗增殖性疾病的方法。