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公开(公告)号：US08008348B2
公开(公告)日：2011-08-30
申请号：US10861923
申请日：2004-06-07
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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12.发明授权公开(公告)号：US07855229B2
公开(公告)日：2010-12-21
申请号：US11220414
申请日：2005-09-07
IPC分类号： A61K31/275 , A61K31/32 , A61K31/16 , A61K31/165
CPC分类号： A61K31/277
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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公开(公告)号：US07547728B2
公开(公告)日：2009-06-16
申请号：US10310150
申请日：2002-12-05
IPC分类号： A61K31/275 , A61K31/32 , A61K31/16 , A61K31/165
CPC分类号： A61K31/00 , A61K31/167 , Y02A50/465
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 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：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/或其类似物衍生物，治疗，预防，抑制，减少或抑制患有肌肉消瘦疾病的受试者中的肌肉蛋白分解代谢的方法 ，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。
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公开(公告)号：US20080249183A1
公开(公告)日：2008-10-09
申请号：US12071591
申请日：2008-02-22
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 。
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15.发明授权公开(公告)号：US07524866B2
公开(公告)日：2009-04-28
申请号：US10778334
申请日：2004-02-17
IPC分类号： A61K31/445 , A61K31/38 , A61K31/135
CPC分类号： A61K31/138
摘要： This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof.
摘要翻译： 本发明提供：1）在患有前列腺癌的男性受试者中治疗雄激素剥夺诱导的骨质疏松症和/或骨折和/或骨矿物质密度（BMD）丧失的方法; 2）在患有前列腺癌的男性受试者中预防雄激素剥夺诱导的骨质疏松症和/或骨折和/或骨矿物质密度（BMD）丧失的方法; 3）在患有前列腺癌的男性受试者中抑制或抑制雄激素剥夺诱导的骨质疏松症和/或骨折和/或BMD损失的方法; 和4）通过向受试者施用包含抗雌激素剂的药物组合物，降低在患有前列腺癌的男性受试者中发展雄激素剥夺诱导的骨质疏松症和/或骨折和/或BMD损失的风险的方法 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，水合物，N-氧化物或其任何组合。
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16.发明授权公开(公告)号：US06899888B2
公开(公告)日：2005-05-31
申请号：US10305363
申请日：2002-11-27
IPC分类号： A61K31/015 , A61K31/138 , A61K45/00 , A61P5/26 , A61P15/10 , A61P19/08 , A61P19/10 , A61P43/00 , A61F2/02 , A61F6/06 , A61F9/02 , A61F13/02 , A61K9/48
CPC分类号： A61K31/015 , A61K31/138
摘要： This invention provides: 1) a method of treating androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 2) a method of preventing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of Bone Mineral Density (BMD) in a male subject suffering from prostate cancer; 3) a method of suppressing or inhibiting androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer; and 4) a method of reducing the risk of developing androgen-deprivation induced osteoporosis and/or bone fractures and/or loss of BMD in a male subject suffering from prostate cancer, by administering to the subject a pharmaceutical composition comprising an anti-estrogen agent 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：1）在患有前列腺癌的男性受试者中治疗雄激素剥夺诱导的骨质疏松症和/或骨折和/或骨矿质密度（BMD）丧失的方法; 2）在患有前列腺癌的男性受试者中预防雄激素剥夺诱导的骨质疏松症和/或骨折和/或骨矿物质密度（BMD）丧失的方法; 3）在患有前列腺癌的男性受试者中抑制或抑制雄激素剥夺诱导的骨质疏松症和/或骨折和/或BMD损失的方法; 和4）通过向受试者施用包含抗雌激素剂的药物组合物，降低在患有前列腺癌的男性受试者中发展雄激素剥夺诱导的骨质疏松症和/或骨折和/或BMD损失的风险的方法 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，水合物，N-氧化物或其任何组合。
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公开(公告)号：US09427418B2
公开(公告)日：2016-08-30
申请号：US13215679
申请日：2011-08-23
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
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公开(公告)号：US08546451B2
公开(公告)日：2013-10-01
申请号：US12710693
申请日：2010-02-23
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.
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公开(公告)号：US20100267773A1
公开(公告)日：2010-10-21
申请号：US12710693
申请日：2010-02-23
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。
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公开(公告)号：US20150087712A1
公开(公告)日：2015-03-26
申请号：US14523333
申请日：2014-10-24
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。
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