公开(公告)号：EP1755572B1

公开(公告)日：2012-02-15

申请号：EP05756622.6

申请日：2005-06-03

申请人： Merck Sharp & Dohme Corp.

发明人： HANNEY, Barbara ,  KIM, Yuntae ,  KROUT, Michael, R. ,  MEISSNER, Robert, S. ,  MITCHELL, Helen, J. ,  MUSSELMAN, Jeffrey ,  PERKINS, James, J. ,  WANG, Jiabing

IPC分类号： C07D213/61 ,  C07C235/06 ,  C07C233/13 ,  A61K31/165 ,  A61P5/26

CPC分类号： C07D295/205 ,  C07C233/13 ,  C07C235/34 ,  C07C255/60 ,  C07C271/12 ,  C07C271/22 ,  C07C2601/02 ,  C07D213/61 ,  C07D213/73

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, Alzhheiner’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减弱的肌肉紧张度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 手术，肌营养不良，虚弱，衰老皮肤，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，炎症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，自身免疫性疾病，单独或与其他活性剂组合。