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公开(公告)号：EP0373891B1
公开(公告)日：1994-11-02
申请号：EP89312986.6
申请日：1989-12-12
发明人： Hughes, Leslie Richard , Oldfield, John , Pegg, Stephen John , Barker, Andrew John , Marsham, Peter Robert
IPC分类号： C07D239/90 , C07D239/95 , C07D239/96 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D413/12 , A61K31/505
CPC分类号： C07D401/12 , C07D239/90 , C07D239/95 , C07D239/96 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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公开(公告)号：EP0373891A2
公开(公告)日：1990-06-20
申请号：EP89312986.6
申请日：1989-12-12
发明人： Hughes, Leslie Richard , Oldfield, John , Pegg, Stephen John , Barker, Andrew John , Marsham, Peter Robert
IPC分类号： C07D239/90 , C07D239/95 , C07D239/96 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D413/12 , A61K31/505
CPC分类号： C07D401/12 , C07D239/90 , C07D239/95 , C07D239/96 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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.摘要翻译： 本发明涉及具有抗肿瘤活性的喹唑啉衍生物或其药学上可接受的盐; 制造过程; 以及含有它们的药物组合物。 本发明提供下式的喹唑啉：其中R 1为氢或氨基，或至多6个碳原子的烷基或烷氧基; 或R 1是至多3个碳原子的取代的烷基或烷氧基; R 2是至多6个碳原子的氢，烷基，烯基，炔基，羟基烷基，卤代烷基或氰基烷基; Ar是亚苯基或杂环烯; L是式-CO.NH-，-NH.CO-，-CO.NR 3 - ，-NR 3 CO - ， - CH = CH - ， - CH 2 O-，-OCH 2 - ，-CH 2 S - ， - CH 2 - ， - CO.CH 2 - ， - CH 2 CO-或-CO.O-，其中R 3是至多6个碳原子的烷基; Y为芳基或杂芳基或其氢化衍生物; 或Y是式-A-Y 1的基团，其中A是至多6个碳原子的亚烷基，亚环烷基，亚烯基或亚炔基，Y 1是芳基或杂芳基或其氢化衍生物; 或其药学上可接受的盐。
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公开(公告)号：EP0373891A3
公开(公告)日：1990-12-05
申请号：EP89312986.6
申请日：1989-12-12
发明人： Hughes, Leslie Richard , Oldfield, John , Pegg, Stephen John , Barker, Andrew John , Marsham, Peter Robert
IPC分类号： C07D239/90 , C07D239/95 , C07D239/96 , C07D401/12 , C07D403/12 , C07D407/12 , C07D409/12 , C07D417/12 , C07D413/12 , A61K31/505
CPC分类号： C07D401/12 , C07D239/90 , C07D239/95 , C07D239/96 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
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.
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