Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
    6.
    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

    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。

    Dimethoxy quinazolines for treating diabetes
    8.
    发明授权
    Dimethoxy quinazolines for treating diabetes 失效
    用于治疗糖尿病的二甲氧基喹唑啉

    公开(公告)号:US06495556B2

    公开(公告)日:2002-12-17

    申请号:US09812098

    申请日:2001-03-19

    IPC分类号: A61K3152

    摘要: The invention provides novel JAK-3 inhibitors that are useful for treating leukemia and lymphoma. The compounds are also useful to treat or prevent skin cancer, as well as sunburn and UVB-induced skin inflammation. In addition, the compounds of the present invention prevent the immunosuppressive effects of UVB radiation, and are useful to treat or prevent autoimmune diseases, inflammation, and transplant rejection. The invention also provides pharmaceutical compositions comprising compounds of the invention, as well as therapeutic methods for their use.

    摘要翻译: 本发明提供了可用于治疗白血病和淋巴瘤的新型JAK-3抑制剂。 这些化合物也可用于治疗或预防皮肤癌,以及晒伤和UVB诱导的皮肤炎症。 此外,本发明的化合物可防止UVB辐射的免疫抑制作用,并且可用于治疗或预防自身免疫性疾病,炎症和移植排斥。 本发明还提供了包含本发明化合物的药物组合物,以及它们使用的治疗方法。