Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias
    9.
    发明授权
    Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias 失效
    凋亡诱导金刚烷基衍生物及其作为抗癌剂的用途,特别是对于宫颈癌和发育不良

    公开(公告)号:US06825226B2

    公开(公告)日:2004-11-30

    申请号:US10176778

    申请日:2002-06-24

    IPC分类号: A61K31415

    摘要: The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoicacid, 2-[3-(1-adamantyl)-4-methoxyphenyl]-5-benzimidazole carboxylic acid, and 6-[3-(1-adamantyl)-4,5-methylenedioxyphenyl]-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

    摘要翻译: 本发明涉及含有类视黄醇相关化合物的具体金刚烷基或金刚烷基衍生物诱导癌细胞凋亡的发现,因此可用于治疗癌症,包括晚期癌症。 此外,本发明涉及含有维甲酸类化合物的新型金刚烷基或金刚烷基衍生物及其用于治疗和/或预防癌症,角化失调,皮肤病学条件和其它疗法的用途。更具体地,已经显示,这种金刚烷基化合物,例如 ,6- [3-(1-金刚烷基)-4-甲氧基苯基] -2-萘甲酸,2- [3-(1-金刚烷基)-4-甲氧基苯基] -5-苯并咪唑羧酸和6- [3- 1-金刚烷基)-4,5-亚甲二氧基苯基] -2-萘甲酸可用于治疗或预防子宫颈癌和前列腺增生症,如宫颈发育异常,包括高等级和低度发育不良。

    Method of inhibiting transcription utilizing nuclear receptors
    10.
    发明授权
    Method of inhibiting transcription utilizing nuclear receptors 失效
    使用核受体抑制转录的方法

    公开(公告)号:US06683047B1

    公开(公告)日:2004-01-27

    申请号:US09139525

    申请日:1998-08-25

    IPC分类号: A61K3800

    摘要: This invention provides a method of inhibiting the transcription of a gene, which is activated by AP-1 or an AP-1 component, comprising binding AP-1 or the component with a nuclear receptor so as to prevent the binding of AP-1 to the gene. The nuclear receptor can be the retinoic acid receptor, glucocorticoid receptor, vitamin D3 receptor, thyroid receptor, or estrogen receptor. Also provided is a composition of matter comprising AP-1 or an AP-1 component bound to a nuclear receptor. These methods and compositions can be used to treat arthritis and cancer.

    摘要翻译: 本发明提供一种抑制由AP-1或AP-1成分激活的基因转录的方法,其包括将AP-1或组分与核受体结合,以防止AP-1与 基因。 核受体可以是视黄酸受体,糖皮质激素受体,维生素D3受体,甲状腺受体或雌激素受体。 还提供了包含AP-1或与核受体结合的AP-1成分的物质组合物。 这些方法和组合物可用于治疗关节炎和癌症。