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    Inhibitors of Akt activity
    2.
    发明授权
    Inhibitors of Akt activity 失效
    Akt活性抑制剂

    公开(公告)号：US07399764B2

    公开(公告)日：2008-07-15

    申请号：US10530252

    申请日：2003-10-24

    申请人： Mark E. Duggan ,  Craig W. Lindsley ,  Zhijian Zhao

    发明人： Mark E. Duggan ,  Craig W. Lindsley ,  Zhijian Zhao

    IPC分类号： A61K31/50 ,  A61K31/497 ,  C07D241/00 ,  C07D487/00

    CPC分类号： A61K31/495 ,  A61K45/06 ,  C07D487/04 ,  C07D495/04

    摘要： The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

    摘要翻译： 本发明涉及含有与被抑制Akt（丝氨酸/苏氨酸蛋白激酶）活性的取代吡嗪部分稠合的五元杂环的化合物。 本发明还涉及含有本发明化合物的治疗组合物和治疗癌症的方法，包括施用本发明化合物。

    N-(Pyridin-3-Yl)-2-Phenylbutanamides As Androgen Receptor Modulators
    9.
    发明申请
    N-(Pyridin-3-Yl)-2-Phenylbutanamides As Androgen Receptor Modulators 审中-公开
    N-（吡啶-3-基）-2-苯基丁酰胺作为雄激素受体调节剂

    公开(公告)号：US20080124402A1

    公开(公告)日：2008-05-29

    申请号：US11666525

    申请日：2005-10-25

    申请人： Yuntae Kim ,  Joshua Close ,  Mark E. Duggan ,  Barbara Hanney ,  Robert S. Meissner ,  Jeffrey Musselman ,  James J. Perkins ,  Jiabing Wang

    发明人： Yuntae Kim ,  Joshua Close ,  Mark E. Duggan ,  Barbara Hanney ,  Robert S. Meissner ,  Jeffrey Musselman ,  James J. Perkins ,  Jiabing Wang

    IPC分类号： A61K33/16 ,  C07D213/02 ,  A61K31/44 ,  A61K31/56 ,  A61K38/16 ,  A61K31/59 ,  A61P19/10 ,  A61P19/08 ,  A61K31/66 ,  A61K31/4535 ,  A61K33/10 ,  A61K33/06

    CPC分类号： C07D213/64 ,  A61K31/44 ,  C07D213/74

    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。