发明公开
- 专利标题： Anti-tumour agents
- 专利标题（中）： Antitumormittel。
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申请号： EP89312986.6申请日： 1989-12-12
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公开(公告)号： EP0373891A2公开(公告)日： 1990-06-20
- 发明人: Hughes, Leslie Richard , Oldfield, John , Pegg, Stephen John , Barker, Andrew John , Marsham, Peter Robert
- 申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , NATIONAL RESEARCH DEVELOPMENT CORPORATION
- 申请人地址： Imperial Chemical House, Millbank London SW1P 3JF GB
- 专利权人： IMPERIAL CHEMICAL INDUSTRIES PLC,NATIONAL RESEARCH DEVELOPMENT CORPORATION
- 当前专利权人： IMPERIAL CHEMICAL INDUSTRIES PLC,NATIONAL RESEARCH DEVELOPMENT CORPORATION
- 当前专利权人地址： Imperial Chemical House, Millbank London SW1P 3JF GB
- 代理机构： Tait, Brian Steele
- 优先权： GB8829296 19881215
- 主分类号： C07D239/90
- IPC分类号： C07D239/90 ; C07D239/95 ; C07D239/96 ; C07D401/12 ; C07D403/12 ; C07D407/12 ; C07D409/12 ; C07D417/12 ; C07D413/12 ; A61K31/505
摘要：
The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.
The invention provides a quinazoline of the formula:-
wherein R¹ is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R¹ is substituted alkyl or alkoxy each of up to 3 carbon atoms;
R² is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;
Ar is phenylene or heterocyclene;
L is a group of the formula -CO.NH-, -NH.CO-, -CO.NR³-, -NR³.CO-, -CH=CH-, -CH₂O-, -OCH₂-, -CH₂S-, -SCH₂-, -CO.CH₂-, -CH₂.CO- or -CO.O-, wherein R³ is alkyl of up to 6 carbon atoms; and
Y is aryl or heteroaryl or a hydrogenated derivative thereof; or Y is a group of the formula -A-Y¹ in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y¹ is aryl or heteroaryl or a hydrogenated derivative thereof; or a pharmaceutically-acceptable salt thereof.
The invention provides a quinazoline of the formula:-
wherein R¹ is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R¹ is substituted alkyl or alkoxy each of up to 3 carbon atoms;
R² is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;
Ar is phenylene or heterocyclene;
L is a group of the formula -CO.NH-, -NH.CO-, -CO.NR³-, -NR³.CO-, -CH=CH-, -CH₂O-, -OCH₂-, -CH₂S-, -SCH₂-, -CO.CH₂-, -CH₂.CO- or -CO.O-, wherein R³ is alkyl of up to 6 carbon atoms; and
Y is aryl or heteroaryl or a hydrogenated derivative thereof; or Y is a group of the formula -A-Y¹ in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y¹ is aryl or heteroaryl or a hydrogenated derivative thereof; or a pharmaceutically-acceptable salt thereof.
公开/授权文献
- EP0373891B1 Anti-tumour agents 公开/授权日：1994-11-02
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