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    Process for making fluorinated 4-azasteroid derivatives
    2.
    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。