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1. 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。

2. 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。

3. 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。

4. 发明授权

US09078888B2 Nuclear receptor binding agents 有权
公开(公告)号：US09078888B2
公开(公告)日：2015-07-14
申请号：US12010225
申请日：2008-01-22
申请人： James T. Dalton , Duane D. Miller , Michael L. Mohler , Seoung-Soo Hong , Zhongzhi Wu , Devesh Srivastava
发明人： James T. Dalton , Duane D. Miller , Michael L. Mohler , Seoung-Soo Hong , Zhongzhi Wu , Devesh Srivastava
IPC分类号： A61K31/47 , A61K31/472 , C07D217/22 , C07D217/24
CPC分类号： A61K31/472 , C07D217/22 , C07D217/24 , Y02A50/463
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs 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, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.

5. 发明申请

US20090030036A1 Nuclear receptor binding agents 有权
标题翻译：核受体结合剂
公开(公告)号：US20090030036A1
公开(公告)日：2009-01-29
申请号：US12010225
申请日：2008-01-22
申请人： James T. Dalton , Duane D. Miller , Michael L. Mohler , Seoung-Soo Hong , Zhongzhi Wu , Devesh Srivastava
发明人： James T. Dalton , Duane D. Miller , Michael L. Mohler , Seoung-Soo Hong , Zhongzhi Wu , Devesh Srivastava
IPC分类号： A61K31/47 , C07D217/00 , A61P25/00 , A61P9/00
CPC分类号： A61K31/472 , C07D217/22 , C07D217/24 , Y02A50/463
摘要： The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBAs 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, inflammatory diseases, oxidative stress related disorders such as Parkinson's and stroke, neurological disorders, ophthalamic disorders, cardiovascular disease, and obesity.
摘要翻译：本发明涉及一类新的核受体结合剂（NRBAs）。 NRBAs适用于预防和/或治疗各种疾病和病症，包括预防和治疗前列腺癌和乳腺癌等癌症，骨质疏松症，激素相关疾病，炎性疾病，氧化应激相关疾病如帕金森病和中风，神经障碍，眼科疾病，心血管疾病和肥胖。

6. 发明授权

US06838484B2 Formulations comprising selective androgen receptor modulators 有权
标题翻译：包含选择性雄激素受体调节剂的制剂
公开(公告)号：US06838484B2
公开(公告)日：2005-01-04
申请号：US10270232
申请日：2002-10-15
申请人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
发明人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller , Yali He , Donghua Yin
IPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/22 , C07D215/227 , C07D271/12 , G01N30/72 , G01N30/88 , G01N33/543 , G01N33/74 , A61K31/16
CPC分类号： A61K31/167 , A61K31/404 , A61K31/4706 , A61K31/661 , C07C235/24 , C07D209/08 , C07D215/227 , C07D271/12 , G01N30/7233 , G01N33/5438 , G01N33/74 , G01N2030/8813
摘要： The present invention relates to pharmaceutical compositions and formulations comprising 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; and/or e) decreasing the incidence of, halting or causing a regression of prostate cancer. The present invention provides pharmaceutical compositions comprising the selective androgen receptor modulator compounds, together with pharmaceutically acceptable excipients.
摘要翻译：本发明涉及包含新型雄激素受体靶向剂（ARTA）的药物组合物和制剂，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; 和/或e）降低前列腺癌的发生率，停止或导致消退。本发明提供了包含选择性雄激素受体调节剂化合物以及药学上可接受的赋形剂的药物组合物。

7. 发明授权

US06569896B2 Selective androgen receptor modulators and methods of use thereof 失效
公开(公告)号：US06569896B2
公开(公告)日：2003-05-27
申请号：US09935045
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： A01N3222
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.

8. 发明授权

US06998500B2 Selective androgen receptor modulators and methods of use thereof 失效
公开(公告)号：US06998500B2
公开(公告)日：2006-02-14
申请号：US10270732
申请日：2002-10-16
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： C07C255/50 , A61K31/275
CPC分类号： C07C235/24 , C07B2200/07 , C07C255/60
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; and/or g) decreasing the incidence of, halting or causing a regression of prostate cancer.

9. 发明申请

US20090156614A1 Selective androgen receptor modulators, analogs and derivatives thereof and uses thereof 审中-公开
标题翻译：选择性雄激素受体调节剂，其类似物和衍生物及其用途
公开(公告)号：US20090156614A1
公开(公告)日：2009-06-18
申请号：US11826985
申请日：2007-07-19
申请人： James T. Dalton , Duane D. Miller , Igor Rakov , Casey Bohl , Michael L. Mohler
发明人： James T. Dalton , Duane D. Miller , Igor Rakov , Casey Bohl , Michael L. Mohler
IPC分类号： A61K31/495 , C07C311/10 , A61K31/18 , C07C215/68 , A61K31/135 , C07D307/02 , A61K31/34 , C07D207/12 , A61K31/4015 , C07D305/12 , C07C255/49 , A61K31/275 , C07D213/57 , A61K31/435 , C07D241/04 , A61P15/16 , A61P35/00 , A61P5/00 , A61P19/08 , A61P21/00 , A61P3/10
CPC分类号： C07D241/04 , C07C255/54 , C07C255/58 , C07C255/60 , C07C317/46 , C07C323/60 , C07C335/18 , C07D233/86
摘要： This invention provides new compounds and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, prostate cancer, muscle wasting diseases and/or disorders or a bone-related diseases and/or disorders.
摘要翻译：本发明提供了新的化合物及其用于治疗受试者中各种疾病或病症的新用途，包括前列腺癌，肌肉消瘦疾病和/或病症或与骨相关的疾病和/或病症。

10. 发明授权

US07919647B2 Selective androgen receptor modulators and methods of use thereof 有权
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：US07919647B2
公开(公告)日：2011-04-05
申请号：US11355187
申请日：2006-02-16
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： C07C255/49 , A61K31/275 , A61K31/13 , A01N37/34 , A01N33/02
CPC分类号： A61K31/277
摘要： This invention provides a class of androgen receptor targeting agents. The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM).
摘要翻译：本发明提供一类雄激素受体靶向剂。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）。

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