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    Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias
    1.
    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

    申请人： Magnus Pfahl ,  Xian-Ping Lu ,  Darryl Rideout ,  Hongyue Zhang

    发明人： Magnus Pfahl ,  Xian-Ping Lu ,  Darryl Rideout ,  Hongyue Zhang

    IPC分类号： A61K31415

    CPC分类号： A61K31/192 ,  A61K31/235 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/385 ,  A61K31/4166 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/7048

    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。

    Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias
    2.
    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：US06462064B1

    公开(公告)日：2002-10-08

    申请号：US09498347

    申请日：2000-02-04

    申请人： Magnus Pfahl ,  Xian-Ping Lu ,  Darryl Rideout ,  Hongyue Zhang

    发明人： Magnus Pfahl ,  Xian-Ping Lu ,  Darryl Rideout ,  Hongyue Zhang

    IPC分类号： A61K31415

    CPC分类号： A61K31/192 ,  A61K31/235 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/36 ,  A61K31/38 ,  A61K31/385 ,  A61K31/4166 ,  A61K31/495 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/7048

    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-naphthoic acid, 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宫颈癌，宫颈发育不良，包括高等级和低度发育不良。

    Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
    7.
    发明授权
    Naphthamide derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors 有权
    作为多靶蛋白激酶抑制剂和组蛋白脱乙酰酶抑制剂的萘普生衍生物

    公开(公告)号：US08211901B2

    公开(公告)日：2012-07-03

    申请号：US12785111

    申请日：2010-05-21

    申请人： Xian-Ping Lu ,  Zhibin Li ,  Song Shan ,  Jindi Yu ,  Zhiqiang Ning

    发明人： Xian-Ping Lu ,  Zhibin Li ,  Song Shan ,  Jindi Yu ,  Zhiqiang Ning

    IPC分类号： A61K31/517 ,  A61K31/47

    CPC分类号： A61K31/517 ,  C07D215/20 ,  C07D215/233 ,  C07D215/26 ,  C07D215/28 ,  C07D239/88 ,  C07D239/90 ,  C07D401/12

    摘要： Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.

    摘要翻译： 描述了分离的式I化合物及其立体异构体，对映异构体，非对映异构体及其药学上可接受的盐，以及这些化合物及其组合物用于治疗与异常蛋白激酶活性相关疾病的生产方法和使用方法，以及 /或异常的组蛋白脱乙酰酶活性，包括例如炎性疾病，自身免疫疾病，癌症，神经和神经变性疾病，心血管疾病，代谢疾病，过敏和哮喘和/或激素相关疾病。