Mitotic kinesin inhibitors
    5.
    发明授权
    Mitotic kinesin inhibitors 失效
    有丝分裂驱动蛋白抑制剂

    公开(公告)号:US07427637B2

    公开(公告)日:2008-09-23

    申请号:US10559855

    申请日:2004-06-08

    IPC分类号: A01N42/52 A61K31/42

    CPC分类号: C07D487/04 C07D491/048

    摘要: The present invention relates to bicyclic dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

    摘要翻译: 本发明涉及可用于治疗细胞增殖性疾病,用于治疗与KSP驱动蛋白活性相关的病症和用于抑制KSP驱动蛋白的双环二氢吡咯化合物。 本发明还涉及包含这些化合物的组合物,以及使用它们治疗哺乳动物癌症的方法。

    Androgen receptor modulators and methods of use thereof
    6.
    发明授权
    Androgen receptor modulators and methods of use thereof 失效
    雄激素受体调节剂及其使用方法

    公开(公告)号:US07196076B2

    公开(公告)日:2007-03-27

    申请号:US10493013

    申请日:2002-10-15

    摘要: Compounds of structural formula (I) are disclosed as useful for modulating the androgen receptor (AR) in a tissue selective manner in a patient in need of such modulation, and in particular for antagonizing AR in the prostate of a male patient or in the uterus of a female patient and agonizing AR in bone and/or muscle tissue. These compounds are useful in the treating conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

    摘要翻译: 公开了结构式(I)的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体(AR),特别是用于拮抗男性患者或子宫中前列腺中的AR 的女性患者和在骨和/或肌肉组织中激动的AR。 这些化合物可用于由雄激素缺乏引起的治疗条件或可通过雄激素给药改善,包括:骨质疏松症,牙周病,骨折,骨重建手术后的骨损伤,肌肉减少症,虚弱,衰老皮肤,男性性腺机能减退,女性性 功能障碍,妇女绝经后症状,动脉粥样硬化,高胆固醇血症,高脂血症,再生障碍性贫血和其他造血障碍,胰腺癌,肾癌,前列腺癌,关节炎和关节修复,单独或与其他活性剂组合。 此外,这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。