ESTRATRIENE DERIVATIVES COMPRISING HETEROCYCLIC BIOISOSTERES FOR THE PHENOLIC A-RING
    26.
    发明申请
    ESTRATRIENE DERIVATIVES COMPRISING HETEROCYCLIC BIOISOSTERES FOR THE PHENOLIC A-RING 审中-公开
    包含苯酚环的杂环生物活性成分的雌激素衍生物

    公开(公告)号:US20110190246A1

    公开(公告)日:2011-08-04

    申请号:US13055388

    申请日:2009-07-14

    CPC分类号: C07J71/0047

    摘要: The present invention is directed to novel pyrazolo-estrien and triazolo-estrien-derivatives, pharmaceutical compositions containing them and their use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compounds of the invention are selective estrogen receptor modulators.

    摘要翻译: 本发明涉及新颖的吡唑并雌三烯衍生物,含有它们的药物组合物及其用于治疗或预防由雌激素受体介导的疾病和疾病,例如潮热,阴道干燥,骨质减少,骨质疏松症, 高脂血症,认知功能丧失,退行性脑疾病,心血管疾病,脑血管疾病,激素敏感性癌症和增生(包括男性和女性前列腺中的乳腺,子宫内膜和子宫颈组织),子宫内膜异位症,子宫肌瘤,骨关节炎; 并且作为避孕药单独使用或与孕激素或孕激素拮抗剂组合。 本发明的化合物是选择性雌激素受体调节剂。