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11. 发明申请

US20060035966A1 Irreversible selective androgen receptor modulators and methods of use thereof 审中-公开
标题翻译：不可逆选择性雄激素受体调节剂及其使用方法
公开(公告)号：US20060035966A1
公开(公告)日：2006-02-16
申请号：US10995567
申请日：2004-11-24
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Leonid Kirkovsky , Dong Hwang , Arnab Mukherjee
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka , Leonid Kirkovsky , Dong Hwang , Arnab Mukherjee
IPC分类号： C07C331/28
CPC分类号： C07C323/60 , A61K31/16 , A61K31/26 , A61K31/275 , C07C261/02 , C07C265/12 , C07C331/10 , C07C331/28
摘要： In one embodiment, 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). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor In another embodiment, the SARM compounds are androgen receptor antagonists, which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. 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：在一个实施方案中，本发明提供了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）。 SARM化合物对雄激素受体的非甾体配体具有意想不到的抗雄激素活性。在一个实施方案中，SARM化合物不可逆地与雄激素受体结合。在另一个实施方案中，SARM化合物是雄激素受体拮抗剂，其不可逆地结合雄激素受体。在另一个实施方案中，SARM化合物是烷化剂。 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; 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。

12. 发明申请

US20060004042A1 Formulations comprising selective androgen receptor modulators 审中-公开
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：US20060004042A1
公开(公告)日：2006-01-05
申请号：US11029022
申请日：2005-01-05
申请人： James Dalton , Duane Miller , Karen Veverka
发明人： James Dalton , Duane Miller , Karen Veverka
IPC分类号： A61K31/4706 , A61K31/405 , A61K31/165
CPC分类号： A61K31/165 , A61K31/4706
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。

13. 发明申请

US20050080055A1 Method of treating breast cancer with androgen receptor antagonists 审中-公开
标题翻译：用雄激素受体拮抗剂治疗乳腺癌的方法
公开(公告)号：US20050080055A1
公开(公告)日：2005-04-14
申请号：US10760152
申请日：2004-01-20
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K20060101 , A61K31/165 , A61K31/21 , A61K31/26 , A61K31/277 , A61K31/32 , A61K31/66 , A61P35/00
CPC分类号： A61K31/66 , A61K31/21 , A61K31/26
摘要： This invention relates to the prevention and treatment of breast cancer in a subject, for example a female subject. Accordingly, this invention provides methods of a) treating a subject suffering from breast cancer; b) preventing, suppressing, inhibiting or reducing the incidence of breast cancer in a subject; c) delaying the progression of breast cancer in a subject suffering from breast cancer; d) preventing the recurrence of breast cancer in a subject; e) treating the recurrence of breast cancer in a subject suffering from breast cancer; and/or f) treating, preventing, suppressing or inhibiting metastasis in a subject suffering from breast cancer, by administering to the subject a therapeutically effective amount of an Androgen Receptor Antagonist and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, crystal, polymorph, prodrug or any combination thereof, as described herein.
摘要翻译：本发明涉及预防和治疗受试者，例如女性受试者的乳腺癌。因此，本发明提供了a）治疗患有乳腺癌的受试者的方法; b）预防，抑制，抑制或降低患者乳腺癌的发生率; c）延缓乳腺癌患者乳腺癌的进展; d）预防受试者乳腺癌的复发; e）治疗乳腺癌患者乳腺癌的复发; 和/或f）通过向受试者施用治疗有效量的雄激素受体拮抗剂和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，治疗，预防，抑制或抑制患有乳腺癌的受试者的转移，药物产品，水合物，N-氧化物，晶体，多晶型物，前药或其任何组合。

14. 发明申请

US20050038110A1 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：US20050038110A1
公开(公告)日：2005-02-17
申请号：US10863524
申请日：2004-06-09
申请人： Mitchell Steiner , James Dalton , Duane Miller , Karen Veverka
发明人： Mitchell Steiner , James Dalton , Duane Miller , Karen Veverka
IPC分类号： A61K31/277 , A61K31/32 , C07F7/24
CPC分类号： C07C255/60 , C07C235/24 , C07C255/54
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）。

15. 发明申请

US20080076829A1 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：US20080076829A1
公开(公告)日：2008-03-27
申请号：US11892595
申请日：2007-08-24
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： C07C255/51 , A61K31/167 , A61P15/16
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。

16. 发明申请

US20080057068A1 SARMS and method of use thereof 有权
标题翻译： SARMS及其使用方法
公开(公告)号：US20080057068A1
公开(公告)日：2008-03-06
申请号：US11785250
申请日：2007-04-16
申请人： James Dalton , Duane Miller
发明人： James Dalton , Duane Miller
IPC分类号： A61K31/167 , A61K31/17 , A61K31/4985 , A61K31/56 , A61K38/16 , A61K38/28 , A61K38/47 , A61K39/395 , A61P15/16 , A61P35/00 , C07C233/04
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。

17. 发明申请

US20060276539A1 Treating Androgen Decline in Aging Male (ADAM)- associated conditions with SARMS 审中-公开
标题翻译：老年男性（ADAM）治疗雄激素下降 - 与SARMS相关的病症
公开(公告)号：US20060276539A1
公开(公告)日：2006-12-07
申请号：US11324753
申请日：2006-01-04
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： A61K31/277
CPC分类号： A61K31/277 , C07K14/721
摘要： This invention provides methods for treatment and inhibition of a male subject having an Androgen Decline in Aging Male (ADAM)-associated condition, for example sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, an alteration in cognition and mood, depression, anemia, hair loss, obesity, muscle loss, dry eye, memory loss, benign prostate hyperplasia and/or prostate cancer, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, pro-drug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了用于治疗和抑制雄性雄性雄激素降低（ADAM）相关病症的男性受试者的方法，例如性功能障碍，性欲性降低，勃起功能障碍，性腺机能减退，肌肉减少症，骨质减少症，骨质疏松症，认知改变通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

18. 发明申请

US20060241180A1 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：US20060241180A1
公开(公告)日：2006-10-26
申请号：US11394181
申请日：2006-03-31
申请人： James Dalton , Duane Miller , Craig Marhefka , Wenqing Gao
发明人： James Dalton , Duane Miller , Craig Marhefka , Wenqing Gao
IPC分类号： A61K31/66 , A61K31/277 , A61K31/165 , A61K31/32 , C07F9/28 , C07C255/20 , C07C235/24
CPC分类号： A61K31/275 , A61K31/277 , A61K31/415 , A61K31/421 , A61K31/426 , A61K31/433 , A61K31/44 , A61K31/505 , A61K31/557 , A61K31/65 , A61K31/66 , C07C255/60 , C07D211/72 , C07D233/44 , C07D239/02
摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The compounds are selective androgen receptor modulators (SARM) useful for, inter-alia, suppressing spermatogenesis, treating a subject having a hormone related condition, treating a subject suffering from prostate cancer, delaying the progression of prostate cancer, preventing the recurrence of prostate cancer, and treating the recurrence of prostate cancer.
摘要翻译：本发明提供一类雄激素受体靶向剂（ARTA）。这些化合物是选择性雄激素受体调节剂（SARM），其用于除其他外抑制精子发生，治疗具有激素相关病症的受试者，治疗患有前列腺癌的受试者，延缓前列腺癌的进展，预防前列腺癌的复发，并治疗前列腺癌的复发。

19. 发明申请

US20060035965A1 Selective androgen receptor modulators and methods of use thereof 有权
公开(公告)号：US20060035965A1
公开(公告)日：2006-02-16
申请号：US11146427
申请日：2005-06-07
申请人： James Dalton , Duane Miller , Karen Veverka
发明人： James Dalton , Duane Miller , Karen Veverka
IPC分类号： A01N37/34 , A61K31/277
CPC分类号： A61K31/277
摘要： This invention provides SARM compounds and their use 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.

20. 发明申请

US20050080054A1 Treating androgen decline in aging male (ADAM)-associated conditions with SARMS 审中-公开
标题翻译：老年男性（ADAM）治疗雄激素相关性SARS的病情下降
公开(公告)号：US20050080054A1
公开(公告)日：2005-04-14
申请号：US10683161
申请日：2003-10-14
申请人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
发明人： James Dalton , Duane Miller , Mitchell Steiner , Karen Veverka
IPC分类号： C07K14/72 , A61K31/66 , A61K31/165 , A61K31/195 , A61K31/21 , A61K31/277 , A61K31/32
CPC分类号： C07K14/721
摘要： The present invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of an Androgen Decline in Aging Male (ADAM)-associated condition in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof. The present invention further provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of sexual dysfunction, decreased sexual libido, erectile dysfunction, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, benign prostate hyperplasia or prostate cancer due to ADAM in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) compound and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, crystal, or any combination thereof.
摘要翻译：本发明提供了通过向受试者施用选择性雄激素受体调节剂（SARM）化合物，治疗，预防，抑制，抑制或降低男性受试者的老年男性（ADAM）相关状态的雄激素下降的发生率的方法和/或其类似物，衍生物，异构体，代谢物，药学上可接受的盐，药物产品，水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。本发明还提供了治疗，预防，抑制或降低性功能障碍，性欲降低，勃起功能障碍，性腺机能减退，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，脱发通过向受试者施用选择性雄激素受体调节剂（SARM）化合物和/或其类似物，衍生物，异构体，代谢产物，药学上可接受的盐，药物产品，由此引起的ADAM在男性受试者中的肥胖，良性前列腺增生或前列腺癌。水合物，N-氧化物，前药，多晶型物，晶体或其任何组合。

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