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    • 5. 发明授权
    • Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
    • 6,7-二烷氧基-4-苯基氨基 - 喹唑啉的合成和抗肿瘤活性
    • US06258820B1
    • 2001-07-10
    • US09357404
    • 1999-07-20
    • Faith M. UckunXing-Ping LiuRama Krishna Narla
    • Faith M. UckunXing-Ping LiuRama Krishna Narla
    • A61K35517
    • C07D239/94
    • 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.
    • 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。