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    Substituted acylanilides and methods of use thereof
    33.
    发明授权
    Substituted acylanilides and methods of use thereof 有权
    取代的酰基酰苯胺及其使用方法

    公开(公告)号：US08426465B2

    公开(公告)日：2013-04-23

    申请号：US13302988

    申请日：2011-11-22

    Applicant: James T. Dalton ,  Duane D. Miller

    Inventor： James T. Dalton ,  Duane D. Miller

    IPC: A61K31/275

    CPC classification number: C07C255/60 ,  C07B2200/07

    Abstract: 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.

    Abstract translation: 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。

    Treating benign prostate hyperplasia with SARMS
    35.
    发明授权
    Treating benign prostate hyperplasia with SARMS 失效
    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

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

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

    IPC: A61K31/16

    CPC classification number: A61K31/277 ,  A61K31/00 ,  A61K31/167 ,  A61K31/56

    Abstract: 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.

    Abstract translation: 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。

    Multi-substitued selective androgen receptor modulators and methods of use thereof
    38.
    发明授权
    Multi-substitued selective androgen receptor modulators and methods of use thereof 失效
    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

    Applicant: James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Dong Jin Hwang ,  Jiyun Chen

    Inventor： James T. Dalton ,  Duane D. Miller ,  Mitchell S. Steiner ,  Karen A. Veverka ,  Dong Jin Hwang ,  Jiyun Chen

    IPC: C07C233/05 ,  A61K31/65

    CPC classification number: C07C235/24

    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.

    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; 和/或g）降低前列腺癌的发生率，停止或导致消退。

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