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    Treating muscle wasting with selective androgen receptor modulators
    41.
    发明授权
    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：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。

    Treating wasting disorders with selective androgen receptor modulators
    42.
    发明授权
    Treating wasting disorders with selective androgen receptor modulators 有权
    用选择性雄激素受体调节剂治疗浪费障碍

    公开(公告)号：US07855229B2

    公开(公告)日：2010-12-21

    申请号：US11220414

    申请日：2005-09-07

    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： 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。

    TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS
    44.
    发明申请
    TREATING ANDROGEN DECLINE IN AGING MALE (ADAM)-ASSOCIATED CONDITIONS WITH SARMS 有权
    治疗老年男性（ADAM）的SARS治疗条件恶化

    公开(公告)号：US20100137430A1

    公开(公告)日：2010-06-03

    申请号：US12632619

    申请日：2009-12-07

    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： A61K31/277 ,  A61K31/167 ,  A61P5/26

    CPC分类号： C07C235/24 ,  A61K31/16 ,  A61K31/167 ,  A61K31/277 ,  C07C255/60

    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。

    Treating muscle wasting with selective androgen receptor modulators
    46.
    发明授权
    Treating muscle wasting with selective androgen receptor modulators 有权
    用选择性雄激素受体调节剂治疗肌肉消瘦

    公开(公告)号：US07547728B2

    公开(公告)日：2009-06-16

    申请号：US10310150

    申请日：2002-12-05

    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 ,  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。

    Synthesis of selective androgen receptor modulators
    49.
    发明授权
    Synthesis of selective androgen receptor modulators 有权
    选择性雄激素受体调节剂的合成

    公开(公告)号：US06995284B2

    公开(公告)日：2006-02-07

    申请号：US10277108

    申请日：2002-10-22

    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： C07C233/05 ,  C07C231/12

    CPC分类号： C07D215/227 ,  A61K31/167 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/24 ,  C07D209/08 ,  C07D271/12 ,  G01N30/7233 ,  G01N33/5438 ,  G01N33/74 ,  G01N2030/8813

    摘要： The present invention relates to a synthetic process for the preparation of 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; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.

    摘要翻译： 本发明涉及一种用于制备新型雄激素受体靶向剂（ARTA）的合成方法，其表现出雄激素受体的非甾族化合物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; e）降低前列腺癌的发生率，停止或导致消退; f）口服雄激素替代和/或其他临床治疗和/或诊断领域。 本发明的方法适用于大规模制备，因为所有步骤都产生高纯度的化合物，因此避免了复杂的纯化方法，从而降低产率。 因此，本发明提供了可用于工业大规模合成的非甾体激动剂化合物的合成方法，并以高产率提供高纯度产品。

    Selective androgen receptor modulators and methods of use thereof
    50.
    发明授权
    Selective androgen receptor modulators and methods of use thereof 失效
    选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US06492554B2

    公开(公告)日：2002-12-10

    申请号：US09935044

    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： C07C23305

    CPC分类号： A61K31/167 ,  C07C235/24 ,  G01N33/5438 ,  G01N33/74

    摘要： The present invention relates to 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 male hormone therapy such as oral testosterone replacement therapy, treating prostate cancer, imaging prostate cancer.

    摘要翻译： 本发明涉及一种新型雄激素受体靶向剂（ARTA），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。 这些试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，可用于男性激素治疗，如口服睾酮替代疗法，治疗前列腺癌，成像前列腺癌。