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,—( )n-
哌啶基,—( )n-
哌嗪基,—( )n-
哌嗪-N(C1-C3烷基),—( )n-
吡咯烷基或—( )n-
咪唑基;n为1至4;R4为—( )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。