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    • 4. 发明授权
    • Carbonylamino-benzimidazole derivatives as androgen receptor modulators
    • 羰基氨基 - 苯并咪唑衍生物作为雄激素受体调节剂
    • US07622592B2
    • 2009-11-24
    • US10533259
    • 2003-10-28
    • Yuntae KimBarbara HanneyMark E. DugganKeith L. Spencer
    • Yuntae KimBarbara HanneyMark E. DugganKeith L. Spencer
    • A61K31/427C07D417/04
    • C07D417/04C07D401/04C07D403/04C07D417/14
    • Compounds of structural formula (I) are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore 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, arthritic condition and joint repair, HIV-wasting, prostate cancer, cancer cachexia, Alzheimer s disease, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
    • 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。 它们可用作骨和/或肌肉组织中雄激素受体的激动剂,同时拮抗男性患者的前列腺中或在女性患者的子宫中的AR。 因此,这些化合物可用于增强减弱的肌肉紧张度和治疗由雄激素缺乏引起的或由雄激素给药引起的疾病的治疗,包括骨质疏松症,骨质减少症,糖皮质激素诱导的骨质疏松症,牙周病,骨折,骨骼骨损伤 重建手术,肌肉减少症,脆弱性,皮肤老化,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,关节炎病症和关节修复,艾滋病毒消耗,前列腺癌,癌症恶病质,阿尔茨海默病 疾病,肌营养不良,卵巢早衰,自身免疫疾病,单独或与其他活性剂组合。