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    Compounds and methods for modulation of estrogen receptors
    8.
    发明授权
    Compounds and methods for modulation of estrogen receptors 失效
    用于调节雌激素受体的化合物和方法

    公开(公告)号：US06436923B1

    公开(公告)日：2002-08-20

    申请号：US09527750

    申请日：2000-03-17

    申请人： Shripad S. Bhagwat ,  Leah M. Gayo-Fung ,  Bernd M. Stein ,  Qi Chao ,  Anthony R. Gangloff ,  Jeffrey A. McKie ,  Kenneth D. Rice

    发明人： Shripad S. Bhagwat ,  Leah M. Gayo-Fung ,  Bernd M. Stein ,  Qi Chao ,  Anthony R. Gangloff ,  Jeffrey A. McKie ,  Kenneth D. Rice

    IPC分类号： C07D21718

    CPC分类号： C07D223/16 ,  C07D209/44 ,  C07D217/04 ,  C07D217/16 ,  C07D217/18 ,  C07D217/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04

    摘要： Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

    摘要翻译： 公开了调节雌激素受体（ER）的化合物以及含有它们的药物组合物。 在一个具体的实施方案中，化合物是针对ER-α的ER-β的选择性调节剂。 公开了用于在表达其的细胞和/或组织中调节ER-β的方法，包括优先表达ER-β的细胞和/或组织。 更一般地，还公开了治疗雌激素相关病症的方法，包括诸如乳腺癌，睾丸癌，骨质疏松症，子宫内膜异位症，心血管疾病，高胆固醇血症，前列腺肥大，前列腺癌，肥胖症，潮热，皮肤效应，情绪波动 ，记忆丧失，尿失禁，脱发，白内障，天然荷尔蒙失衡，以及与暴露于环境化学品相关的不良生殖影响。