2-indolinone derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors
    3.
    发明授权
    2-indolinone derivatives as multi-target protein kinase inhibitors and histone deacetylase inhibitors 有权
    2-二氢吲哚酮衍生物作为多靶蛋白激酶抑制剂和组蛋白脱乙酰酶抑制剂

    公开(公告)号:US08158656B2

    公开(公告)日:2012-04-17

    申请号:US12463107

    申请日:2009-05-08

    IPC分类号: A61K31/4439 C07D401/14

    CPC分类号: C07D401/14

    摘要: The present invention relates to 2-indolinone derivatives which are capable of inhibiting protein kinases and histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal protein kinase activities or abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.

    摘要翻译: 本发明涉及能够抑制蛋白激酶和组蛋白脱乙酰酶的2-二氢吲哚酮衍生物。 因此,本发明的化合物可用于治疗与异常蛋白激酶活性或异常组蛋白脱乙酰酶活性相关的疾病。 还公开了包含这些化合物的药物组合物,利用包含这些化合物的药物组合物治疗疾病的方法,以及制备这些化合物的方法。

    Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias
    5.
    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。

    Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias
    6.
    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

    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-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
    10.
    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

    IPC分类号: A61K31/517 A61K31/47

    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。