Anti-tumor agents
    4.
    发明授权
    Anti-tumor agents 失效
    抗肿瘤药

    公开(公告)号:US4985441A

    公开(公告)日:1991-01-15

    申请号:US504740

    申请日:1990-04-03

    摘要: The invention relates to quinazoline derivatives which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl or halogenoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH-- or --CO.NR.sup.3 --, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is hydrogen or alkyl, cycloalkyl, alkenyl or alkynyl each of up to 6 carbon atoms; orY is a group of the formula --A--Y.sup.1 in which A is alkylene of up to 6 carbon atoms and Y.sup.1 includes hydroxy, amino and cyano, and alkoxy, alkylamino and alkylthio each of up to 6 carbon atoms.

    6-substituted quinazolines processing anti-tumor activity
    5.
    发明授权
    6-substituted quinazolines processing anti-tumor activity 失效
    6-取代喹唑啉加工抗肿瘤活性

    公开(公告)号:US5395838A

    公开(公告)日:1995-03-07

    申请号:US91828

    申请日:1993-07-13

    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: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 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.NR.sup.3 --, --NR.sup.3.CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2.CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof; orY is a group of the formula --A--Y.sup.1 in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y.sup.1 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是氢或氨基,或至多6个碳原子的烷基或烷氧基; 或R 1为至多3个碳原子的取代烷基或烷氧基; R2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 - , - SCH2-,-CO.CH 2 - , - CH 2 CO-或-COO - ,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-Y1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。

    Anti-tumor agents
    6.
    发明授权
    Anti-tumor agents 失效
    抗肿瘤药

    公开(公告)号:US5252573A

    公开(公告)日:1993-10-12

    申请号:US793183

    申请日:1991-11-18

    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: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 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.NR.sup.3 --, --NR.sup.3.CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2 CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof; orY is a group of the formula --A--Y.sup.1 in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y.sup.1 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是氢或氨基,或至多6个碳原子的烷基或烷氧基; 或R 1为至多3个碳原子的取代烷基或烷氧基; R2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 - , - SCH 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-Y1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; 或其药学可接受的盐。