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    • 5. 发明申请
    • 2-HYDROXY-2-PHENYL/THIOPHENYL PROPIONAMIDES AS ANDROGEN RECEPTOR MODULATORS
    • 作为雄激素受体调节剂的2-羟基-2-苯基/噻吩基丙酰胺
    • WO2008048540A3
    • 2008-08-14
    • PCT/US2007021984
    • 2007-10-15
    • MERCK & CO INCKIM YUNTAEMEISSNER ROBERT SMITCHELL HELEN JPERKINS JAMES JROSSI MICHAEL AWANG JIABING
    • KIM YUNTAEMEISSNER ROBERT SMITCHELL HELEN JPERKINS JAMES JROSSI MICHAEL AWANG JIABING
    • A01N43/54A61K31/497A61K31/517
    • C07D213/40C07D409/12
    • 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, HFV-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.
    • 结构式(I)的化合物以组织选择性方式是雄激素受体(AR)的调节剂。 这些化合物可用于增强肌肉张力减弱和由雄激素缺乏引起的病症的治疗,或可通过施用雄激素改善,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,骨重建后的骨损伤 女性绝经后症状,动脉粥样硬化,高胆固醇血症,高脂血症,肥胖症,再生障碍性贫血和其他造血障碍,炎性关节炎和关节修复,HFV消瘦,前列腺癌,良性前列腺增生症(BPH) ),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,认知衰退,性功能障碍,睡眠呼吸暂停,抑郁症,卵巢早衰和自身免疫疾病,单独或与其他活性剂组合。