申请人:Warner-Lambert Company LLC
公开号:US07772243B2
公开(公告)日:2010-08-10
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.
该发明提供了以下式子的喹唑啉化合物:其中:R1为卤素;R2为H或卤素;R3为a)C1-C3烷基,可选择由卤素取代;或者b)—(CH2)n-吗啉基,—(CH2)n-哌啶基,—(CH2)n-哌嗪基,—(CH2)n-哌嗪-N(C1-C3烷基),—(CH2)n-吡咯烷基或—(CH2)n-咪唑基;n为1至4;R4为—(CH2)m-Het;Het为吗啡基,哌啶基,哌嗪基,哌嗪-N(C1-C3烷基),咪唑基,吡咯烷基,氮杂七环,3,4-二氢-2H-吡啶基或3,6-二氢-2H-吡啶基,每个基团可选择由烷基,卤素,OH,NH2,NH(C1-C3烷基)或N(C1-C3烷基)2取代;m为1-3;X为O,S或NH;或其药学上可接受的盐,以及制备它们的过程和中间体化合物,有用的制药组合物和使用这些化合物治疗增殖性疾病的方法。