- 专利标题: Quinazoline derivatives and pharmaceutical compositions containing them
-
申请号: US11024840申请日: 2004-12-30
-
公开(公告)号: US20050239777A1公开(公告)日: 2005-10-27
- 发明人: Andrew Thomas , Craig Johnstone , Edward Clayton , Elaine Elizabeth Stokes , Jean-Jacques Lohmann , Laurent Andre Hennequin
- 申请人: Andrew Thomas , Craig Johnstone , Edward Clayton , Elaine Elizabeth Stokes , Jean-Jacques Lohmann , Laurent Andre Hennequin
- 优先权: EP96402033.3 19960925; EP97401042.3 19970509
- 主分类号: A61F13/00
- IPC分类号: A61F13/00 ; A61F13/02 ; A61F13/15 ; A61K20060101 ; A61K31/505 ; A61K31/517 ; A61K31/5377 ; A61K31/541 ; A61P3/10 ; A61P9/00 ; A61P9/10 ; A61P13/12 ; A61P17/06 ; A61P19/02 ; A61P27/02 ; A61P29/00 ; A61P35/00 ; A61P37/00 ; A61P37/02 ; A61P43/00 ; C07D20060101 ; C07D207/00 ; C07D211/00 ; C07D239/72 ; C07D239/93 ; C07D239/94 ; C07D309/02 ; C07D317/08 ; C07D401/12 ; C07D403/12 ; C07D405/12 ; C07D413/12 ; C07D417/02 ; C07D417/12 ; C07D43/02
摘要:
The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
信息查询