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    Process for making fluorinated 4-azasteroid derivatives
    1.
    发明申请
    Process for making fluorinated 4-azasteroid derivatives 失效
    氟化4-氮灰石衍生物的制备方法

    公开(公告)号：US20060252937A1

    公开(公告)日：2006-11-09

    申请号：US11410179

    申请日：2006-04-24

    申请人： Lushi Tan ,  Benjamin Dorner ,  Wenjie Li ,  Nobuyoshi Yasuda ,  Frederick Hartner

    发明人： Lushi Tan ,  Benjamin Dorner ,  Wenjie Li ,  Nobuyoshi Yasuda ,  Frederick Hartner

    IPC分类号： C07D471/02 ,  C07D221/18

    CPC分类号： C07D471/04 ,  C07D221/18 ,  C07J73/005

    摘要： The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.

    摘要翻译： 本发明涉及可用于制备调节雄激素受体并且用于治疗由雄激素缺乏或雄激素受体多动症引起的疾病的合成方法，例如骨质疏松症，牙周病，骨折，虚弱， 勃起功能障碍，性欲丧失，雄激素依赖性癌症和肌肉减少症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。

    Process for Synthesizing 2-Phenyl-1H-Phenanthro[9,10-d]Imidazole Derivative
    3.
    发明申请
    Process for Synthesizing 2-Phenyl-1H-Phenanthro[9,10-d]Imidazole Derivative 审中-公开
    合成2-苯基-1H-菲并[9,10-d]咪唑衍生物的方法

    公开(公告)号：US20090203922A1

    公开(公告)日：2009-08-13

    申请号：US12085258

    申请日：2006-11-17

    申请人： Kevin Michael Belyk ,  Benjamin Dorner ,  Frederick Hartner ,  Naoki Yoshikawa ,  John Limanto ,  Lushi Tan ,  Enrique Vazquez ,  Joseph Payack

    发明人： Kevin Michael Belyk ,  Benjamin Dorner ,  Frederick Hartner ,  Naoki Yoshikawa ,  John Limanto ,  Lushi Tan ,  Enrique Vazquez ,  Joseph Payack

    IPC分类号： C07D235/02

    CPC分类号： C07D235/02

    摘要： The present invention describes an efficient and economical process for the preparation of a 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative that is useful for the large scale production of material for preclinical and clinical use. The process of the present invention represents a convergent approach to generate the 2,3-disubstituted 2-phenyl-1h-phenantrho[9,10-d]imidazole derivative in high overall yield. The compound made by the process of the invention is an inhibitor of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and is therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain.

    摘要翻译： 本发明描述了一种用于制备2,3-二取代的2-苯基-1h-异丁基[9,10-d]咪唑衍生物的有效和经济的方法，其用于大规模生产用于临床前和临床应用的材料 。 本发明的方法代表以高的总产率生成2,3-二取代的2-苯基-1h-异丁基[9,10-d]咪唑衍生物的收敛方法。 通过本发明方法制备的化合物是微粒体前列腺素E合酶-1（mPGES-1）酶的抑制剂，因此可用于治疗各种疾病或病症的疼痛和/或炎症，例如骨关节炎，类风湿病 关节炎和急性或慢性疼痛。

    Process for making fluorinated 4-azasteroid derivatives
    4.
    发明授权
    Process for making fluorinated 4-azasteroid derivatives 失效
    氟化4-氮灰石衍生物的制备方法

    公开(公告)号：US07301026B2

    公开(公告)日：2007-11-27

    申请号：US11410179

    申请日：2006-04-24

    申请人： Lushi Tan ,  Benjamin T. Dorner ,  Wenjie Li ,  Nobuyoshi Yasuda ,  Frederick W. Hartner

    发明人： Lushi Tan ,  Benjamin T. Dorner ,  Wenjie Li ,  Nobuyoshi Yasuda ,  Frederick W. Hartner

    IPC分类号： C07D221/18

    CPC分类号： C07D471/04 ,  C07D221/18 ,  C07J73/005

    摘要： The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.

    摘要翻译： 本发明涉及可用于制备调节雄激素受体并且用于治疗由雄激素缺乏或雄激素受体多动症引起的疾病的合成方法，例如骨质疏松症，牙周病，骨折，虚弱， 勃起功能障碍，性欲丧失，雄激素依赖性癌症和肌肉减少症。 本发明还包括在所公开的合成方法及其制备方法中有用的中间体。

    Polymorphs of an androgen receptor modulator
    8.
    发明授权
    Polymorphs of an androgen receptor modulator 失效
    雄激素受体调节剂的多态性

    公开(公告)号：US07365202B2

    公开(公告)日：2008-04-29

    申请号：US11633152

    申请日：2006-12-04

    申请人： Lushi Tan ,  Robert S. Meissner ,  Wenjie Li ,  James J. Perkins ,  Aaron S. Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    发明人： Lushi Tan ,  Robert S. Meissner ,  Wenjie Li ,  James J. Perkins ,  Aaron S. Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    IPC分类号： C07D221/18

    CPC分类号： C07J73/005 ,  C07D471/04

    摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

    摘要翻译： 结构式I的化合物是以组织选择性方式的雄激素受体（AR）的调节剂。 这些化合物可用于增强弱化肌张力和治疗由雄激素缺乏引起的疾病或可由雄激素给药改善的疾病，包括骨质疏松症，骨质减少，糖皮质激素诱导的骨质疏松症，牙周病，骨折，骨重建后的骨损伤 手术，肌营养不良，虚弱，老化的皮肤，男性性腺机能减退，女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖，再生障碍性贫血和其他造血障碍，炎性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生 ），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，阿尔茨海默氏病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其它活性剂组合。

    Polymorphs of an androgen receptor modulator
    9.
    发明申请
    Polymorphs of an androgen receptor modulator 失效
    雄激素受体调节剂的多态性

    公开(公告)号：US20070129548A1

    公开(公告)日：2007-06-07

    申请号：US11633152

    申请日：2006-12-04

    申请人： Lushi Tan ,  Robert Meissner ,  Wenjie Li ,  James Perkins ,  Aaron Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    发明人： Lushi Tan ,  Robert Meissner ,  Wenjie Li ,  James Perkins ,  Aaron Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    IPC分类号： A61K31/4745 ,  C07D471/02

    CPC分类号： C07J73/005 ,  C07D471/04

    摘要： Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

    摘要翻译： 结构式I的化合物是以组织选择性方式的雄激素受体（AR）的调节剂。 这些化合物可用于增强弱化肌张力和治疗由雄激素缺乏引起的疾病或可由雄激素给药改善的疾病，包括骨质疏松症，骨质减少，糖皮质激素诱导的骨质疏松症，牙周病，骨折，骨重建后的骨损伤 手术，肌营养不良，虚弱，老化的皮肤，男性性腺机能减退，女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖，再生障碍性贫血和其他造血障碍，炎性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生 ），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，阿尔茨海默氏病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其它活性剂组合。