Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
    1.
    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。

    Organic arsenic compounds
    7.
    发明授权
    Organic arsenic compounds 失效
    有机砷化合物

    公开(公告)号:US06482816B1

    公开(公告)日:2002-11-19

    申请号:US09723220

    申请日:2000-11-27

    IPC分类号: C07C24510

    CPC分类号: C07F9/80

    摘要: Novel organic arsenic compounds are described as cytotoxic agents with potent anti-tumor activity against cancer cells and particularly, with regard to human leukemic cells and breast cancer cells.

    摘要翻译: 新型有机砷化合物被描述为对癌细胞具有强抗肿瘤活性的细胞毒性剂,特别是关于人类白血病细胞和乳腺癌细胞。

    Melamine derivatives as potent anti-cancer agents
    8.
    发明授权
    Melamine derivatives as potent anti-cancer agents 失效
    三聚氰胺衍生物作为有效的抗癌剂

    公开(公告)号:US06262053B1

    公开(公告)日:2001-07-17

    申请号:US09338679

    申请日:1999-06-23

    IPC分类号: A61K3153

    CPC分类号: C07D251/70

    摘要: Novel pharmaceutical compositions including melamine derivatives and methods for the treatment of cancer including prostate, brain, breast, and leukemia are described. The methods are directed to administering a therapeutically effective amount of a pharmaceutical composition including melamine derivatives having potent cytotoxic activity.

    摘要翻译: 描述了包括三聚氰胺衍生物和用于治疗癌症的方法的新型药物组合物,包括前列腺,脑,乳腺和白血病。 该方法涉及给予治疗有效量的药物组合物,包括具有强力细胞毒活性的三聚氰胺衍生物。

    Lipid-lowering quinazoline derivative
    10.
    发明授权
    Lipid-lowering quinazoline derivative 失效
    降脂喹唑啉衍生物

    公开(公告)号:US06172071B2

    公开(公告)日:2001-01-09

    申请号:US09126940

    申请日:1998-07-30

    IPC分类号: A61K31517

    CPC分类号: C07D239/74

    摘要: A novel carbonyl-substituted quinazoline, preferably 4-(3′-bromobenzoyl)-6,7-dimethoxyquinazoline (WHI-P164), and methods for lowering blood cholesterol, including reducing total cholesterol and LDL-cholesterol levels by administration of the carbonyl quinazolines and compositions thereof.

    摘要翻译: 一种新的羰基取代喹唑啉,优选4-(3'-溴苯甲酰基)-6,7-二甲氧基喹唑啉(WHI-P164)和降低血液胆固醇的方法,包括通过施用羰基喹唑啉降低总胆​​固醇和低密度脂蛋白胆固醇水平 及其组合物。