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1. 发明申请

WO0216310A9 SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性雄激素受体调节剂及其使用方法
公开(公告)号：WO0216310A9
公开(公告)日：2002-07-18
申请号：PCT/US0126328
申请日：2001-08-23
申请人： GTX INC , DALTON JAMES , MILLER DUANE D , YIN DONGHUA , HE YALI
发明人： DALTON JAMES , MILLER DUANE D , YIN DONGHUA , HE YALI
IPC分类号： A61P5/28 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , A61P7/06 , A61P13/08 , A61P15/00 , A61P15/08 , A61P15/16 , A61P19/10 , A61P35/00 , C07C235/24 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , G01N33/543 , G01N33/74 , C07C233/15 , A01N31/16 , A01N37/18 , C07C233/33 , C07C233/48 , C07C235/26 , C07C237/14 , A01N31/165
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N33/5438 , G01N33/74
摘要： This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.
摘要翻译：本发明提供了一类新的雄激素受体靶向剂（ARTA）。这些代理定义了一种化合物的新亚类，它们是组织选择性雄激素受体调节剂（SARM），其可用于口服睾酮替代疗法，男性避孕，维持女性性欲，治疗前列腺癌和成像前列腺癌。这些药剂对于雄激素受体的非甾体配体的雄激素和合成代谢活性具有意想不到的体内活性。这些药物可以单独活性或与孕激素或雌激素联合使用。本发明进一步提供了一类新型的非甾体激动剂化合物。本发明进一步提供了含有选择性雄激素调节剂化合物或非甾体激动剂化合物的组合物以及结合雄激素受体，调节精子发生，治疗和成像前列腺癌以及提供雄激素依赖性病症的激素疗法的方法。

2. 发明申请

WO2004035736A3 HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体选择性受体调节剂及其使用方法
公开(公告)号：WO2004035736A3
公开(公告)日：2004-07-15
申请号：PCT/US0332507
申请日：2003-10-14
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
发明人： DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI , STEINER MITCHELL S , VEVERKA KAREN A
IPC分类号： A61K31/165 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/60 , C07C335/18 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , C07C233/05 , A61K31/275 , C07C255/50
CPC分类号： C07D215/227 , A61K31/165 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/16 , C07C235/24 , C07C255/60 , C07C335/18 , C07D209/08 , C07D271/12
摘要： 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.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。已经发现几种SARM化合物对于雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。已经发现其他SARM化合物对于雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 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，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，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，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低有关的疾病（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞凋亡。

3. 发明申请

WO2005113565A3 METABOLITES OF SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：选择性受体调节剂的代谢物及其使用方法
公开(公告)号：WO2005113565A3
公开(公告)日：2006-07-27
申请号：PCT/US2005017588
申请日：2005-03-19
申请人： UNIV TENNESSEE RES FOUNDATION , DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI
发明人： DALTON JAMES T , MILLER DUANE D , YIN DONGHUA , HE YALI
IPC分类号： A61K31/275 , A61K31/70 , C07C233/05 , C07C233/87 , C07C235/24 , C07C255/49 , C07F7/22 , C07G3/00
CPC分类号： A61K31/166 , A61K31/7036 , C07C235/24 , C07H15/18 , C07H15/203
摘要： This invention provides metabolites of a class of androgen receptor targeting agents (ARTA). The SARM compounds and their metabolites, 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.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）的代谢物。 SARM化合物及其代谢物，单独或作为组合物，可用于a）男性避孕; b）治疗各种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，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，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; （ADIF），性功能障碍，性欲降低，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变，情绪，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞中的细胞凋亡。

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