申请人:Fakhoury Stephen Alan
公开号:US20100190977A1
公开(公告)日:2010-07-29
This invention provides quinazoline compounds of the formula:
wherein: R
1
is halo; R
2
is H or halo; R
3
is a) C
1
-C
3
alkyl, optionally substituted by halo; or b) —(CH
2
)
n
-morpholino, —(CH
2
)
n
-piperidine, —(CH
2
)
n
-piperazine, —(CH
2
)
n
-piperazine-N(C
1
-C
3
alkyl), —(CH
2
)
n
-pyrrolidine, or —(CH
2
)
n
-imidazole; n is 1 to 4; R
4
is —(CH
2
)
m
-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C
1
-C
3
alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH
2
, NH(C
1
-C
3
alkyl) or N(C
1
-C
3
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.
本发明提供了公式如下的
喹唑啉化合物:其中:R1为卤素;R2为
氢或卤素;R3为a)C1-C3烷基,可选地被卤素取代;或b)—(
CH2)n-
吗啡啉,—( )n-
哌啶,—( )n-
哌嗪,—( )n-
哌嗪-N(C1-C3烷基),—( )n-
吡咯烷或—( )n-
咪唑;n为1至4;R4为—( )m-Het;Het为
吗啡啉,
哌啶,
哌嗪,
哌嗪-N(C1-C3烷基),
咪唑,
吡咯烷,
氮杂七环,3,4-二
氢-2H-
吡啶或3,6-二
氢-2H-
吡啶,每个基团可选地被烷基,卤素,羟基,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。