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1. 发明授权

US09427418B2 Estrogen receptor ligands and methods of use thereof 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US09427418B2
公开(公告)日：2016-08-30
申请号：US13215679
申请日：2011-08-23
申请人： James T. Dalton , Mitchell S. Steiner , Ronald A. Morton
发明人： James T. Dalton , Mitchell S. Steiner , Ronald A. Morton
IPC分类号： A61K31/165 , A61K31/167 , A61K31/137 , A61K31/4453 , A61K45/06
CPC分类号： A61K31/167 , A61K31/137 , A61K31/4453 , A61K45/06 , A61K2300/00
摘要： The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
摘要翻译：本发明涉及通过减少黄体激素（LH）或独立于男性受试者的LH水平来降低睾酮水平的方法以及治疗，抑制，降低发病率，降低严重性或抑制前列腺癌，晚期前列腺癌的方法，抗阉割前列腺癌（CRPC）和姑息治疗前列腺癌，晚期前列腺癌和去势抗原前列腺癌（CRPC）。本发明的化合物抑制游离或总睾丸激素水平的阉割水平，其可用于治疗前列腺癌，晚期前列腺癌和CRPC，而不引起骨丢失，骨矿物质密度降低，骨折的增加风险，增加的身体脂肪，热闪烁和/或男子女子气概

2. 发明授权

US08546451B2 Estrogen receptor ligands and methods of use thereof 有权
公开(公告)号：US08546451B2
公开(公告)日：2013-10-01
申请号：US12710693
申请日：2010-02-23
申请人： James T. Dalton , Mitchell S. Steiner , Jeetendra Eswaraka
发明人： James T. Dalton , Mitchell S. Steiner , Jeetendra Eswaraka
IPC分类号： A61K31/165
CPC分类号： C07D211/06 , A61K31/137 , A61K31/167 , A61K31/445 , A61K31/4453 , C07C215/82 , C07C233/75 , C07C235/56 , C07D221/12 , C07D295/155
摘要： The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.

3. 发明授权

US08088828B2 Treating benign prostate hyperplasia with SARMS 失效
标题翻译：用SARMS治疗良性前列腺增生
公开(公告)号：US08088828B2
公开(公告)日：2012-01-03
申请号：US12826842
申请日：2010-06-30
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka , Wenqing Gao
IPC分类号： A61K31/16
CPC分类号： A61K31/277 , A61K31/00 , A61K31/167 , A61K31/56
摘要： This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-α reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of inhibiting a 5-α reductase type 1 and/or type 2 enzyme, comprising contacting the enzyme with an effective 5-α reductase inhibitory amount of a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, as described herein.
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）和/或其类似物，衍生物，异构体，代谢物来治疗，预防，抑制或降低男性患者良性前列腺增生的发生率的方法，药学上可接受的盐，药物产品，水合物，N-氧化物或其任何组合。本发明还提供了一种治疗脱发患者的方法，包括向受试者施用治疗有效量的1型和/或2型抑制剂的5-α还原酶的步骤，其中所述抑制剂是选择性雄激素受体调节剂（SARM）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-氧化物或其任何组合。本发明还提供抑制1型和/或2型5α还原酶的方法，包括使酶与有效的5-α还原酶抑制量的选择性雄激素受体调节剂（SARM）和/或其类似物接触，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-氧化物或其任何组合。

4. 发明申请

US20100267773A1 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US20100267773A1
公开(公告)日：2010-10-21
申请号：US12710693
申请日：2010-02-23
申请人： James T. DALTON , Mitchell S. Steiner , Jeetendra Eswaraka
发明人： James T. DALTON , Mitchell S. Steiner , Jeetendra Eswaraka
IPC分类号： A61K31/4453 , A61K31/167 , A61K31/136 , A61P43/00
CPC分类号： C07D211/06 , A61K31/137 , A61K31/167 , A61K31/445 , A61K31/4453 , C07C215/82 , C07C233/75 , C07C235/56 , C07D221/12 , C07D295/155
摘要： The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.
摘要翻译：本发明涉及治疗雄激素剥夺疗法（ADT）诱发受试者的热潮红和严重潮热的方法。

5. 发明授权

US07803970B2 Multi-substitued selective androgen receptor modulators and methods of use thereof 失效
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：US07803970B2
公开(公告)日：2010-09-28
申请号：US10861905
申请日：2004-06-07
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 , A61K31/65
CPC分类号： C07C235/24
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.
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。

6. 发明申请

US20080249183A1 Treatment of androgen-deprivation induced osteoporosis 审中-公开
标题翻译：雄激素剥夺诱导的骨质疏松症的治疗
公开(公告)号：US20080249183A1
公开(公告)日：2008-10-09
申请号：US12071591
申请日：2008-02-22
申请人： Mitchell S. Steiner , Karen A. Veverka
发明人： Mitchell S. Steiner , Karen A. Veverka
IPC分类号： A61K31/138 , A61P19/10 , A61P5/26
CPC分类号： A61K9/0019 , A61K31/138
摘要： This invention provides a method of treating androgen-deprivation induced osteoporosis, bone fractures or loss of bone mineral density (BMD) in a male human subject suffering from prostate cancer, wherein the subject has a precipitous decline in androgen levels, by administering a pharmaceutical composition comprising Toremifene or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof, to the subject, wherein the method increases bone density without increasing androgen and specifically testosterone levels in the subject.
摘要翻译：本发明提供了一种在患有前列腺癌的男性人类受试者中治疗雄激素剥夺诱导的骨质疏松症，骨折或骨矿物质密度（BMD）丧失的方法，其中所述受试者的雄激素水平急剧下降，通过施用药物组合物包括托拉米芬或其类似物，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-氧化物或其任何组合，其中所述方法增加骨密度，而不增加受试者的雄激素和特异性睾酮水平。

7. 发明授权

US07026500B2 Halogenated selective androgen receptor modulators and methods of use thereof 失效
标题翻译：卤代选择性雄激素受体调节剂及其使用方法
公开(公告)号：US07026500B2
公开(公告)日：2006-04-11
申请号：US10371213
申请日：2003-02-24
申请人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka
发明人： James T. Dalton , Duane D. Miller , Mitchell S. Steiner , Karen A. Veverka
IPC分类号： C07C255/50 , A61K31/275
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; and/or g) decreasing the incidence of, halting or causing a regression 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。

8. 发明申请

US20150087712A1 ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF 有权
标题翻译：雌激素受体配体及其使用方法
公开(公告)号：US20150087712A1
公开(公告)日：2015-03-26
申请号：US14523333
申请日：2014-10-24
申请人： James T. Dalton , Mitchell S. Steiner , Christopher C. Coss , Robert H. Getzenberg
发明人： James T. Dalton , Mitchell S. Steiner , Christopher C. Coss , Robert H. Getzenberg
IPC分类号： C07C235/64 , C07C215/50 , A61K31/137 , A61K45/06 , A61K31/167 , C07C233/75 , C07C215/82
CPC分类号： C07C235/64 , A61K31/136 , A61K31/137 , A61K31/167 , A61K45/06 , C07C215/50 , C07C215/82 , C07C233/75 , C07D295/088
摘要： The present invention relates to methods for reducing testosterone levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC), metastatic castration resistant prostate cancer (mCRPC), and methods of reducing high or increasing PSA levels and/or increasing SHBG levels in a subject suffering from prostate cancer, advanced prostate cancer, castration resistant prostate cancer (CRPC) and metastatic castration resistant prostate cancer (mCRPC). The compounds of this invention suppress free or total testosterone levels despite castrate levels secondary to ADT and reduce high or increasing PSA levels. This reduction in testosterone levels may be used to treat prostate cancer, advanced prostate cancer, CRPC and mCRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
摘要翻译：本发明涉及降低男性受试者睾丸激素水平的方法以及治疗，抑制，降低发病率，降低严重程度或抑制前列腺癌，晚期前列腺癌，抗阉割前列腺癌（CRPC），转移性阉割抗性前列腺的方法癌症（mCRPC），以及在患有前列腺癌，晚期前列腺癌，抗阉割前列腺癌（CRPC）和转移性阉割抗性前列腺癌（mCRPC）的受试者中降低高水平或增加PSA水平和/或增加SHBG水平的方法。本发明的化合物尽管阉割水平继发于ADT并降低高水平或增加PSA水平，但抑制游离或总睾丸激素水平。睾丸激素水平的降低可用于治疗前列腺癌，晚期前列腺癌，CRPC和mCRPC，而不会引起骨丢失，骨矿物质密度降低，骨折的风险增加，身体脂肪增加，潮热和/或男子乳房发育。

9. 发明申请

US20110237664A1 SELECTIVE ANDROGEN RECEPTOR MODULATORS FOR TREATING DIABETES 审中-公开
标题翻译：用于治疗糖尿病的选择性安定剂受体调节剂
公开(公告)号：US20110237664A1
公开(公告)日：2011-09-29
申请号：US13082830
申请日：2011-04-08
申请人： James T. Dalton , Shontelle Dodson , Mitchell S. Steiner
发明人： James T. Dalton , Shontelle Dodson , Mitchell S. Steiner
IPC分类号： A61K31/277 , A61P21/02
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 and preventing muscle wasting in patients with non-small cell lung cancer (NSCLC); treating pre-cachexia or early cachexia (preventing muscle wasting in a cancer patient); treating and preventing loss of physical function due to cancer or cancer therapy; increase of physical function; and increasing survival in a patient with NSCLC.
摘要翻译：本发明提供了一种SARM化合物或其组合物用于治疗和预防非小细胞肺癌（NSCLC）患者肌肉消瘦的用途; 治疗恶病质前期或早期恶病质（预防癌症患者的肌肉消瘦）; 治疗和预防由于癌症或癌症治疗而导致的身体功能丧失; 身体功能增加; 并增加NSCLC患者的生存率。

10. 发明授权

US08008348B2 Treating muscle wasting with selective androgen receptor modulators 失效
标题翻译：用选择性雄激素受体调节剂治疗肌肉消瘦
公开(公告)号：US08008348B2
公开(公告)日：2011-08-30
申请号：US10861923
申请日：2004-06-07
申请人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller
发明人： Mitchell S. Steiner , Karen A. Veverka , James T. Dalton , Duane D. Miller
IPC分类号： A61K31/275 , A61K31/32 , A61K31/16 , A61K31/165
CPC分类号： A61K31/00 , A61K31/167
摘要： This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.
摘要翻译：本发明提供：1）治疗患有肌肉消瘦障碍的受试者的方法; 2）预防受试者的肌肉消瘦障碍的方法; 3）治疗，预防，抑制，抑制或减轻患有肌肉消瘦障碍的受试者的肌肉损失的方法; 4）一种治疗，预防，抑制，减少或抑制患有肌肉消瘦障碍的受试者的肌肉消瘦的方法; 和/或5）通过向受试者施用选择性雄激素受体调节剂（SARM）和/或类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者的肌肉蛋白分解代谢的方法，所述SARM化合物的异构体，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，杂质或晶体，或其任何组合。

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