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11. 发明授权

US06995284B2 Synthesis of selective androgen receptor modulators 有权
标题翻译：选择性雄激素受体调节剂的合成
公开(公告)号：US06995284B2
公开(公告)日：2006-02-07
申请号：US10277108
申请日：2002-10-22
申请人： James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
发明人： James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
IPC分类号： C07C233/05 , C07C231/12
CPC分类号： C07D215/227 , A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which 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 chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
摘要翻译：本发明涉及一种用于制备新型雄激素受体靶向剂（ARTA）的合成方法，其表现出雄激素受体的非甾族化合物的雄激素和合成代谢活性。这些药剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，它们可用于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; c）治疗与男性雄激素降低相关的病症（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/或预防慢性肌肉消瘦; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。本发明的方法适用于大规模制备，因为所有步骤都产生高纯度的化合物，因此避免了复杂的纯化方法，从而降低产率。因此，本发明提供了可用于工业大规模合成的非甾体激动剂化合物的合成方法，并以高产率提供高纯度产品。

12. 发明授权

US06492554B2 Selective androgen receptor modulators and methods of use thereof 失效
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：US06492554B2
公开(公告)日：2002-12-10
申请号：US09935044
申请日：2001-08-23
申请人： James T. Dalton , Duane D. Miller , Donghua Yin , Yali He
发明人： James T. Dalton , Duane D. Miller , Donghua Yin , Yali He
IPC分类号： C07C23305
CPC分类号： A61K31/167 , C07C235/24 , G01N33/5438 , G01N33/74
摘要： The present invention relates to a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for male hormone therapy such as oral testosterone replacement therapy, treating prostate cancer, imaging prostate cancer.
摘要翻译：本发明涉及一种新型雄激素受体靶向剂（ARTA），其表现出雄激素受体的非甾体配体的雄激素和合成代谢活性。这些试剂定义了一种新的选择性雄激素受体调节剂（SARM）的化合物亚类，可用于男性激素治疗，如口服睾酮替代疗法，治疗前列腺癌，成像前列腺癌。

13. 发明授权

US08158828B2 Nuclear receptor binding agents 有权
标题翻译：核受体结合剂
公开(公告)号：US08158828B2
公开(公告)日：2012-04-17
申请号：US11785251
申请日：2007-04-16
申请人： James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人： James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号： C07C233/65 , A61K31/165
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译：本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖。

14. 发明授权

US08637706B2 Nuclear receptor binding agents 失效
标题翻译：核受体结合剂
公开(公告)号：US08637706B2
公开(公告)日：2014-01-28
申请号：US13362242
申请日：2012-01-31
申请人： James T. Dalton , Christina Barrett , Duane D. Miller , Seoung-Soo Hong , Yali He , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人： James T. Dalton , Christina Barrett , Duane D. Miller , Seoung-Soo Hong , Yali He , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号： C07C233/65 , A61K31/165
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07C233/60 , C07C233/65 , C07C233/75 , C07C233/84 , C07C235/38 , C07C235/56 , C07C235/66 , C07C251/48 , C07C255/57 , C07C311/29 , C07C2601/14 , C07D221/12 , C07D265/34 , Y02A50/402 , Y02A50/411 , Y02A50/414 , Y02A50/423
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译：本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖。

15. 发明申请

US20090062341A1 Nuclear receptor binding agents 审中-公开
标题翻译：核受体结合剂
公开(公告)号：US20090062341A1
公开(公告)日：2009-03-05
申请号：US11604884
申请日：2006-11-28
申请人： James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
发明人： James T. Dalton , Christina Barrett , Yali He , Seoung-Soo Hong , Duane D. Miller , Michael L. Mohler , Ramesh Narayanan , Zhongzhi Wu
IPC分类号： A61K31/4545 , C07C233/64 , A61K31/166 , A61K31/445 , C07D401/02 , C07K14/72 , C07D211/60 , C07D213/81 , A61K31/44
CPC分类号： A61K31/138 , A61K31/40 , A61K31/445 , A61K31/55 , C07D221/12
摘要： The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.
摘要翻译：本发明涉及新型选择性雌激素受体调节剂（SERM）。 SERM化合物可用于预防和/或治疗各种疾病和病症，包括预防和治疗诸如前列腺和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管舒缩症状，神经系统疾病，心血管疾病和肥胖。

16. 发明授权

US08853266B2 Selective androgen receptor modulators for treating diabetes 有权
标题翻译：用于治疗糖尿病的选择性雄激素受体调节剂
公开(公告)号：US08853266B2
公开(公告)日：2014-10-07
申请号：US11785064
申请日：2007-04-13
申请人： James T. Dalton , Duane D. Miller
发明人： James T. Dalton , Duane D. Miller
IPC分类号： A01N37/34 , A61K31/275 , A01N37/12 , A01N37/44 , A01N37/18 , A61K31/165 , C07C255/00
CPC分类号： A61K31/167 , A61K31/277 , A61K31/32 , A61K31/404 , A61K31/47 , A61K31/555 , A61K31/66 , A61K31/675
摘要： This invention provides use of a SARM compound or a composition comprising the same in treating a variety of diseases or conditions in a subject, including, inter-alia, a diabetes disease, and/or disorder such as cardiovascular disease, atherosclerosis, cerebrovascular conditions, diabetic nephropathy, diabetic neuropathy and diabetic retinopathy.
摘要翻译：本发明提供了SARM化合物或其组合物在治疗受试者中的多种疾病或病症中的用途，包括尤其是糖尿病疾病和/或病症如心血管疾病，动脉粥样硬化，脑血管病症，糖尿病性肾病，糖尿病性神经病变和糖尿病性视网膜病变。

17. 发明授权

US08846756B2 Substituted acylanilides and methods of use thereof 有权
标题翻译：取代的酰基酰苯胺及其使用方法
公开(公告)号：US08846756B2
公开(公告)日：2014-09-30
申请号：US13868768
申请日：2013-04-23
申请人： James T. Dalton , Duane D. Miller
发明人： James T. Dalton , Duane D. Miller
IPC分类号： A61K31/275 , C07C255/60
CPC分类号： C07C255/60 , C07B2200/07
摘要： This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
摘要翻译：本发明提供了SARM化合物及其用于治疗受试者中的多种疾病或病症的用途，所述疾病或病症尤其包括肌肉消瘦疾病和/或病症或骨相关疾病和/或病症。

18. 发明授权

US08080682B2 Substituted acylanilides and methods of use thereof 有权
标题翻译：取代的酰基酰苯胺及其使用方法
公开(公告)号：US08080682B2
公开(公告)日：2011-12-20
申请号：US11892595
申请日：2007-08-24
申请人： James T. Dalton , Duane D. Miller
发明人： James T. Dalton , Duane D. Miller
IPC分类号： C07C255/50 , A61K31/275
CPC分类号： C07C255/60 , C07B2200/07
摘要： This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, a muscle wasting disease and/or disorder or a bone-related disease and/or disorder.
摘要翻译：本发明提供了SARM化合物及其用于治疗受试者中的多种疾病或病症的用途，所述疾病或病症尤其包括肌肉消瘦疾病和/或病症或骨相关疾病和/或病症。

19. 发明授权

US07772433B2 SARMS and method of use thereof 有权
标题翻译： SARMS及其使用方法
公开(公告)号：US07772433B2
公开(公告)日：2010-08-10
申请号：US11785250
申请日：2007-04-16
申请人： James T. Dalton , Duane D. Miller
发明人： James T. Dalton , Duane D. Miller
IPC分类号： C07C233/05 , A61K31/165
CPC分类号： C07C255/60 , A61K38/09 , A61K38/24 , A61K38/35 , A61K2300/00
摘要： This invention provides SARM compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter-alia, muscle wasting diseases and/or disorders, bone-related diseases and/or disorders, diabetes, cardiovascular disease, renal disease and others.
摘要翻译：本发明提供了SARM化合物及其用于治疗受试者中各种疾病或病症的用途，包括肌肉消耗疾病和/或病症，骨相关疾病和/或病症，糖尿病，心血管疾病，肾脏疾病和别的。

20. 发明授权

US07705182B2 Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
标题翻译：多取代的选择性雄激素受体调节剂及其使用方法
公开(公告)号：US07705182B2
公开(公告)日：2010-04-27
申请号：US10371155
申请日：2003-02-24
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Dong Jin Hwang , Jiyun Chen
IPC分类号： C07C233/05 , A61K31/16
CPC分类号： C07C235/24
摘要： This invention provides 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; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.
摘要翻译：本发明提供雄激素受体靶向剂（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; c）治疗与男性雄激素降低相关的病症（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; 和/或g）降低前列腺癌的发生率，停止或导致消退。

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