Methotrexate derivatives useful for treating cancer and arthritis
    1.
    发明申请
    Methotrexate derivatives useful for treating cancer and arthritis 审中-公开
    甲氨喋呤衍生物可用于治疗癌症和关节炎

    公开(公告)号:US20060035901A1

    公开(公告)日:2006-02-16

    申请号:US11186404

    申请日:2005-07-21

    IPC分类号: C07D475/02 A61K31/525

    摘要: The present invention provides novel derivatives of MTX. The novel derivatives have increased selectivity, inhibit the activity of Her2, EGFR, or B-Raf to a greater degree than MTX, and display greater antiproliferative activity than MTX. Also provided are pharmaceutical compositions containing the novel derivatives, to methods of preparation of such derivatives, to methods of inhibiting the biological activity of polypeptides, methods of inhibiting cell proliferation, and the use of the novel compounds in therapy, particularly for the treatment of neoplastic, hyperproliferative, and immune disorders, including cancer, arthritis, and psoriasis.

    摘要翻译: 本发明提供MTX的新型衍生物。 新型衍生物具有增加的选择性,抑制Her2,EGFR或B-Raf的活性比MTX更大程度,并且显示比MTX更大的抗增殖活性。 还提供了含有新衍生物的药物组合物,这些衍生物的制备方法,抑制多肽的生物学活性的方法,抑制细胞增殖的方法,以及新型化合物在治疗中的用途,特别是用于治疗肿瘤 ,过度增殖和免疫疾病,包括癌症,关节炎和牛皮癣。

    Cyclohexylamino Benzene, Pyridine, and Pyridazine Derivatives
    2.
    发明申请
    Cyclohexylamino Benzene, Pyridine, and Pyridazine Derivatives 审中-公开
    环己基氨基苯,吡啶和哒嗪衍生物

    公开(公告)号:US20070207984A1

    公开(公告)日:2007-09-06

    申请号:US11678975

    申请日:2007-02-26

    CPC分类号: C07D209/08 C07D231/56

    摘要: Disclosed are compounds and pharmaceutically acceptable salts of Formula (I), wherein Q1, Q2, RN, R1, R2, R5, R6, R7, R8, X1, X2, X4, and Y are as defined herein. Compounds of Formula (I) are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

    摘要翻译: 公开了式(I)的化合物和药学上可接受的盐,其中Q 1,Q 2,R N,R 1, R 2,R 5,R 6,R 7,R 8, X 1,X 2,X 4和Y如本文所定义。 式(I)的化合物可用于治疗与细胞增殖有关的疾病和/或病症,例如癌症,炎症,关节炎,血管生成等。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。

    Carbazole derivatives
    5.
    发明申请
    Carbazole derivatives 审中-公开
    咔唑衍生物

    公开(公告)号:US20070185184A1

    公开(公告)日:2007-08-09

    申请号:US11532340

    申请日:2006-09-15

    IPC分类号: A61K31/403 C07D209/82

    摘要: Disclosed are compounds and pharmaceutically acceptable salts of Formula I: wherein n, R1, R2, R3, X, R4, R5, R6, R8, R9, and Y are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation and/or abnormal cell mitosis, such as cancer, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.

    摘要翻译: 公开了式I的化合物和药学上可接受的盐:其中n,R 1,R 2,R 3,X,R 1, R 5,R 5,R 6,R 8,R 9和Y分别为 本文定义。 式I的化合物可用于治疗与细胞增殖和/或异常细胞有丝分裂相关的疾病和/或病症,例如癌症,炎症和炎症相关疾病以及与血管发生相关的病症。 还公开了包含本发明化合物的药物组合物和使用这些化合物治疗上述病症的方法。