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    Haloacetamide and azide substituted compounds and methods of use thereof
    2.
    发明申请
    Haloacetamide and azide substituted compounds and methods of use thereof 审中-公开
    卤代乙酰胺和叠氮化物取代的化合物及其使用方法

    公开(公告)号：US20050137172A1

    公开(公告)日：2005-06-23

    申请号：US10963761

    申请日：2004-10-14

    申请人： James Dalton ,  Duane Miller ,  Vipin Nair ,  Huiping Xu

    发明人： James Dalton ,  Duane Miller ,  Vipin Nair ,  Huiping Xu

    IPC分类号： A61K31/165 ,  A61K31/21 ,  A61K31/277 ,  A61K31/655 ,  A61K31/66 ,  C07C235/24 ,  C07C255/60 ,  C07D207/44 ,  C07D207/452 ,  A61K31/195 ,  A61K31/32 ,  A61K31/4015

    CPC分类号： C07D207/452 ,  C07C235/24 ,  C07C255/60

    摘要： The present invention relates to a novel class of anti-cancer compounds, which contain a haloacetamide or azide moiety and are, in one embodiment, alkylating agents. These agents, either alone or in a composition, are useful for treating cancer, preventing cancer, delaying the progression of cancer, treating and/or preventing the recurrence of cancer, suppressing, inhibiting or reducing the incidence of cancer, or inducing apoptosis in a cancer cell. Accordingly, the present invention provides a) methods of treating cancer in a subject; b) methods of preventing cancer in a subject; c) methods of delaying the progression of cancer in a subject; d) methods of treating the recurrence of cancer in a subject; e) methods of preventing the recurrence of cancer in a subject; f) methods of suppressing, inhibiting or reducing the incidence of cancer in a subject; and g) methods of inducing apoptosis in a cancer cell; by administering to the subject an anti-cancer compound of the present invention or an analog or metabolite thereof, its N-oxide, ester, pharmaceutically acceptable salt, hydrate, or any combination thereof as described herein.

    摘要翻译： 本发明涉及一类新的抗癌化合物，其含有卤代乙酰胺或叠氮化物部分，在一个实施方案中是烷化剂。 这些药物单独或组合物可用于治疗癌症，预防癌症，延缓癌症进展，治疗和/或预防癌症复发，抑制，抑制或降低癌症发生率或诱导癌细胞凋亡 癌细胞。 因此，本发明提供了a）在受试者中治疗癌症的方法; b）预防受试者癌症的方法; c）延缓受试者癌症进展的方法; d）治疗患者癌症复发的方法; e）预防受试者癌症复发的方法; f）抑制或抑制受试者癌症发病率的方法; 和g）诱导癌细胞凋亡的方法; 通过向受试者施用本文所述的抗癌化合物或其类似物或代谢物，其N-氧化物，酯，药学上可接受的盐，水合物或其任何组合。

    Selective androgen receptor modulators
    5.
    发明申请
    Selective androgen receptor modulators 失效
    选择性雄激素受体调节剂

    公开(公告)号：US20060276540A1

    公开(公告)日：2006-12-07

    申请号：US11353225

    申请日：2006-02-14

    申请人： James Dalton ,  Duane Miller ,  Yali He ,  Donghua Yin

    发明人： James Dalton ,  Duane Miller ,  Yali He ,  Donghua Yin

    IPC分类号： A61K31/277 ,  C07C255/20

    CPC分类号： C07C255/60

    摘要： The present invention relates to androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity, which are nonsteroidal ligands for the androgen receptor. The selective androgen receptor modulators (SARM) 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.

    摘要翻译： 本发明涉及雄激素和合成代谢活性的雄激素受体靶向剂（ARTA），其是雄激素受体的非甾体配体。 选择性雄激素受体调节剂（SARM）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。

    Multi-substituted selective androgen receptor modulators and methods of use thereof
    6.
    发明申请
    Multi-substituted selective androgen receptor modulators and methods of use thereof 有权
    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：US20060183931A1

    公开(公告)日：2006-08-17

    申请号：US10371155

    申请日：2003-02-24

    申请人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Dong Hwang ,  Jiyun Chen

    发明人： James Dalton ,  Duane Miller ,  Mitchell Steiner ,  Karen Veverka ,  Dong Hwang ,  Jiyun Chen

    IPC分类号： C07F9/02 ,  C07F7/22 ,  C07C395/00 ,  C07C255/60 ,  C07C237/10

    CPC分类号： C07C235/24

    摘要： This invention provides 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

    Synthesis of selective androgen receptor modulators
    7.
    发明申请
    Synthesis of selective androgen receptor modulators 失效
    选择性雄激素受体调节剂的合成

    公开(公告)号：US20060009529A1

    公开(公告)日：2006-01-12

    申请号：US11062752

    申请日：2005-02-23

    申请人： James Dalton ,  Duane Miller ,  Donghua Yin ,  Yali He

    发明人： James Dalton ,  Duane Miller ,  Donghua Yin ,  Yali He

    IPC分类号： A61K31/165 ,  C07C235/84

    CPC分类号： C07C231/12 ,  C07C235/24

    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。

    Substituted acylanilides and methods of use thereof
    9.
    发明申请
    Substituted acylanilides and methods of use thereof 审中-公开
    取代的酰基酰苯胺及其使用方法

    公开(公告)号：US20080076828A1

    公开(公告)日：2008-03-27

    申请号：US11826195

    申请日：2007-07-12

    申请人： James Dalton ,  Duane Miller

    发明人： James Dalton ,  Duane Miller

    IPC分类号： A61K31/165 ,  C07C233/00

    CPC分类号： C07C255/60

    摘要： This invention provides substituted acylanilide 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.

    摘要翻译： 本发明提供取代的酰基酰苯胺化合物及其在治疗受试者中的多种疾病或病症的用途，特别包括肌肉消瘦疾病和/或病症或与骨相关的疾病和/或病症。

    Selective androgen receptor modulators and method of use thereof
    10.
    发明申请
    Selective androgen receptor modulators and method of use thereof 审中-公开
    选择性雄激素受体调节剂及其使用方法

    公开(公告)号：US20070173546A1

    公开(公告)日：2007-07-26

    申请号：US11505363

    申请日：2006-08-17

    申请人： James Dalton ,  Duane Miller

    发明人： James Dalton ,  Duane Miller

    IPC分类号： A61K31/277

    CPC分类号： C07C255/60

    摘要： 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.

    摘要翻译： 本发明提供了SARM化合物及其用于治疗受试者中各种疾病或病症的用途，包括特别是肌肉消耗疾病和/或病症或骨相关疾病和/或病症。