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    Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
    3.
    发明授权
    Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines 失效
    6,7-二烷氧基-4-苯基氨基 - 喹唑啉的合成和抗肿瘤活性

    公开(公告)号：US06258820B1

    公开(公告)日：2001-07-10

    申请号：US09357404

    申请日：1999-07-20

    申请人： Faith M. Uckun ,  Xing-Ping Liu ,  Rama Krishna Narla

    发明人： Faith M. Uckun ,  Xing-Ping Liu ,  Rama Krishna Narla

    IPC分类号： A61K35517

    CPC分类号： C07D239/94

    摘要： Compounds of the formula: wherein: Ra is iodo, (C1-C4)hydroxyalkyl, benzyloxy, OCF3, SCF3, SO3H, SO2F, SO2NR2R3 where R2 is hydrogen or (C1-C4)alkyl and R3 is hydrogen, (C1-C4)alkyl, or phenyl, NR2R4 where R2 is hydrogen or (C1-C4)alkyl and R4 is phenyl; or a group of the formula wherein R5 and R6 are each independently, hydrogen, (C1-C4)alkyl, or (C1-C4) perfluoroalkyl, and R7 is hydrogen, halo, hydroxy, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)hydroxyalkyl, or N(R2)2, where R2 is hydrogen or (C1-C4)alkyl; n is an integer of 1-4; Rb is each, independently, hydrogen, halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, nitro, cyano, methylenedioxy, ethylenedioxy, COCH3, CF3, OCF3, SCF3, COOH, SO3H, SO2F, phenyl, or phenyl substituted by a group selected from halo, hydroxy, mercapto, (C1-C4)alkyl, (C1-C4) alkoxy, (C1-C4)thioalkyl, (C1-C4)hydroxyalkyl, amino, nitro, cyano, CF3, COOH, SO3H, SO2NR2R3, SO2F where R2 is H or (C1-C4)alkyl and R3 is H, (C1-C4)alkyl, phenyl, or phenyl substituted by a group as defined above; benzyloxy or benzyloxy substituted on the phenyl portion by a group defined above; NR2R3 where R2 is H or (C1-C4)alkyl and R3 is H, (C1-C4)alkyl, phenyl, or phenyl substituted by a group as defined above; and R1 is (C1-C4)alkyl or a pharmaceutically acceptable salt thereof; and methods for the treatment of cancer and for the treatment of allergic reactions.

    摘要翻译： 下式的化合物：其中：R a为碘，（C 1 -C 4）羟基烷基，苄氧基，OCF 3，SCF 3，SO 3 H，SO 2 F，SO 2 NR 2 R 3，其中R 2为氢或（C 1 -C 4）烷基且R 3为氢，（C 1 -C 4） 烷基或苯基，NR2R4，其中R2是氢或（C1-C4）烷基，R4是苯基; 或者一组式R 5和R 6各自独立地为氢，（C 1 -C 4）烷基或（C 1 -C 4）全氟烷基，R 7为氢，卤素，羟基，（C 1 -C 4）烷基， ）烷氧基，（C1-C4）羟基烷基或N（R2）2，其中R2是氢或（C1-C4）烷基; n是1-4的整数; Rb各自独立地是氢，卤素，羟基， 巯基，（C 1 -C 4）烷基，（C 1 -C 4）烷氧基，（C 1 -C 4）硫代烷基，（C 1 -C 4）羟烷基，硝基，氰基，亚甲二氧基，亚乙二氧基，COCH 3，CF 3，OCF 3，SCF 3，COOH，SO 3 H， SO2F，苯基或被选自卤素，羟基，巯基，（C1-C4）烷基，（C1-C4）烷氧基，（C1-C4）硫代烷基，（C1-C4）羟基烷基，氨基，硝基， 氰基，CF 3，COOH，SO 3 H，SO 2 NR 2 R 3，SO 2 F，其中R 2是H或（C 1 -C 4）烷基，R 3是H，（C 1 -C 4）烷基，苯基或被如上定义的基团取代的苯基; 在苯基部分被苄基氧基或苄氧基取代上述定义; NR2R3，其中R2是H或（C1-C4）烷基，R3是H，（C1-C4）烷基，苯基或被如上定义的基取代的苯基; 并且R 1是（C 1 -C 4）烷基或其药学上可接受的盐; 以及用于治疗癌症和治疗过敏反应的方法。