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    Treating muscle wasting with selective androgen receptor modulators
    22.
    发明申请
    Treating muscle wasting with selective androgen receptor modulators 失效
    用选择性雄激素受体调节剂治疗肌肉消瘦

    公开(公告)号：US20100144871A1

    公开(公告)日：2010-06-10

    申请号：US10861923

    申请日：2004-06-07

    Applicant: Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

    Inventor： Mitchell S. Steiner ,  Karen A. Veverka ,  James T. Dalton ,  Duane D. Miller

    IPC: A61K31/277 ,  A61P21/00 ,  A61K31/165

    CPC classification number: A61K31/00 ,  A61K31/167

    Abstract: 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.

    Abstract translation: 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。

    Methylene-bridged selective androgen receptor modulators and methods of use thereof
    24.
    发明申请
    Methylene-bridged selective androgen receptor modulators and methods of use thereof 审中-公开
    亚甲基桥接选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US20080319009A1

    公开(公告)日：2008-12-25

    申请号：US11882073

    申请日：2007-07-30

    Applicant: James T. Dalton ,  Duane D. Miller ,  Igor Rakov

    Inventor： James T. Dalton ,  Duane D. Miller ,  Igor Rakov

    IPC: A61K31/4704 ,  A61K31/167 ,  A61K31/404

    CPC classification number: C07C237/22 ,  A61K31/167 ,  C07C235/38 ,  C07C255/60

    Abstract: 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; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

    Abstract translation: 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; 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。

    Selective androgen receptor modulators and methods of use thereof
    26.
    发明授权
    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

    Applicant: James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    Inventor： James T. Dalton ,  Duane D. Miller ,  Yali He ,  Donghua Yin

    IPC: C07C255/50 ,  A61K31/275

    CPC classification number: C07C235/24 ,  C07B2200/07 ,  C07C255/60

    Abstract: 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.

    Estrogen receptor ligands and methods of use thereof
    30.
    发明授权
    Estrogen receptor ligands and methods of use thereof 有权
    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

    Applicant: James T. Dalton ,  Mitchell S. Steiner ,  Ronald A. Morton

    Inventor： James T. Dalton ,  Mitchell S. Steiner ,  Ronald A. Morton

    IPC: A61K31/165 ,  A61K31/167 ,  A61K31/137 ,  A61K31/4453 ,  A61K45/06

    CPC classification number: A61K31/167 ,  A61K31/137 ,  A61K31/4453 ,  A61K45/06 ,  A61K2300/00

    Abstract: 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.

    Abstract translation: 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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