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    • 6. 发明申请
    • HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    • 卤化选择性雄激素受体调节剂及其使用方法
    • WO2004035736A2
    • 2004-04-29
    • PCT/US2003/032507
    • 2003-10-14
    • UNIVERSITY OF TENNESSEE RESEARCH FOUNDATIONDALTON, James, T.MILLER, Duane, D.YIN, DonghuaHE, YaliSTEINER, Mitchell, S.VEVERKA, Karen, A.
    • DALTON, James, T.MILLER, Duane, D.YIN, DonghuaHE, YaliSTEINER, Mitchell, S.VEVERKA, Karen, A.
    • C12N
    • C07D215/227A61K31/165A61K31/404A61K31/4706A61K31/661C07C235/16C07C235/24C07C255/60C07C335/18C07D209/08C07D271/12
    • This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.
    • 本发明提供了一类雄激素受体靶向剂(ARTA)。 代理商定义了一类新的化合物,它们是选择性雄激素受体调节剂(SARM)。 已经发现几种SARM化合物具有雄激素受体的非甾体配体的意想不到的雄激素和合成代谢活性。 已经发现其他SARM化合物对雄激素受体的非甾体配体具有出乎意料的抗雄激素活性。 SARM化合物单独或作为组合物可用于a)男性避孕; b)治疗多种激素相关病症,例如与衰老男性(ADAM)中的雄激素降低相关的病症,例如疲劳,抑郁症,性欲减退,性功能障碍,勃起功能障碍,性腺机能减退,骨质疏松症,脱发,贫血, 肥胖症,肌肉减少症,骨质减少症,骨质疏松症,良性前列腺增生症,情绪和认知改变以及前列腺癌; c)治疗与女性雄激素降低(ADIF)有关的病症,例如性功能障碍,性欲减退,性腺功能减退症,肌肉减少症,骨质减少症,骨质疏松症,认知和情绪改变,抑郁症,贫血,脱发,肥胖症,子宫内膜异位症,乳房 癌症,子宫癌和卵巢癌; d)治疗和/或预防急性和/或慢性肌肉萎缩症状; e)预防和/或治疗干眼症; f)口服雄激素替代疗法; g)降低前列腺癌的发病率,停止或导致其消退; 和/或h)诱导癌细胞凋亡。