首页> 外国专利> A compound or a pharmaceutically acceptable salt or an enantiomer thereof, methods for modulating an androgen receptor-mediated function in a mammal in need of such modulation, for activating androgen receptor function in a mammal in need of such activation, to treat a condition in a mammal, and to treat osteoporosis in a mammal in need thereof, pharmaceutical composition, methods for increasing bone mineral density in a mammal in need of it, to reduce the risk of vertebral or nonvertebral fractures in a mammal in need of it, and to produce a bone modification marker in a mammal in need thereof, process for producing a pharmaceutical composition, and method for treating or preventing an arthritic condition in a mammal in need thereof

A compound or a pharmaceutically acceptable salt or an enantiomer thereof, methods for modulating an androgen receptor-mediated function in a mammal in need of such modulation, for activating androgen receptor function in a mammal in need of such activation, to treat a condition in a mammal, and to treat osteoporosis in a mammal in need thereof, pharmaceutical composition, methods for increasing bone mineral density in a mammal in need of it, to reduce the risk of vertebral or nonvertebral fractures in a mammal in need of it, and to produce a bone modification marker in a mammal in need thereof, process for producing a pharmaceutical composition, and method for treating or preventing an arthritic condition in a mammal in need thereof

机译:化合物或其药学上可接受的盐或对映体,用于在需要这种调节的哺乳动物中调节雄激素受体介导的功能,在需要这种活化的哺乳动物中活化雄激素受体的功能,以治疗疾病的方法。哺乳动物,以及在有需要的哺乳动物中治疗骨质疏松症的药物组合物,增加有需要的哺乳动物中骨矿物质密度,降低有需要的哺乳动物中椎骨或非椎骨骨折的风险的方法以及生产方法有需要的哺乳动物中的骨修饰标记,制备药物组合物的方法以及在有需要的哺乳动物中治疗或预防关节炎的方法

摘要

"COMPOUND OR A PHARMACEUTICALLY ACCEPTABLE SALT OR ITS ENERGY, METHODS FOR MODULATING A FUNCTION MEDIATED BY ANDROGEN RECEIVER IN A MAMMER IN NEED OF SUCH MODULATION, AND ACTIVATING THE NECESSARY RECEIVER TREATMENT A CONDITION IN A MAMMER, AND TO TREAT OSTEOPOROSIS IN A MAMMER AT ITS NEED, PHARMACEUTICAL COMPOSITION, METHODS TO INCREASE BONE MINERAL DENSITY INTO THIS MISFER IN NEBRA NISIS IN THE NEED , AND TO PRODUCE A BONE MODIFICATION MARKER IN A MAMMALIAN NEEDED, PROCESS TO PRODUCE A PHARMACEUTICAL COMPOSITION, AND METHOD TO TREAT OR PREVENT AN ARTHRITIC CONDITION IN A MAMMALIAN NEEDED ". The compounds of structural formula I are androgen receptor (AR) modulators in a selective tissue manner. They are useful as androgen receptor agonists in bone and / or muscle tissue while antagonizing RA in a male patient's prostate or in a female patient's uterus. These compounds are therefore useful in treating conditions caused by androgen deficiency or that may be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone loss. following bone reconstructive surgery, sarcopenia, weakness, skin aging, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other haematopoietic disorders, inflammatory arthritis and joint repair, HIV emaciation, prostate cancer, cancerous cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.
机译:“化合物或药学上可接受的盐或其能量,用于通过调制来调制由男性中的雄激素受体介导的功能的方法,并在母亲中激活必要的接收条件,以治疗染色体畸变必要的药物成分,增加Nebra Nisis骨密度的方法,以及在哺乳动物中产生骨修饰标记,产生药物成分的过程以及治疗或预防关节疾病的方法需要哺乳动物”。结构式I的化合物以选择性组织方式是雄激素受体(AR)调节剂。它们可用作骨和/或肌肉组织中的雄激素受体激动剂,同时拮抗男性患者前列腺或女性患者子宫中的RA。因此,这些化合物可用于治疗由雄激素缺乏引起的病症或可通过雄激素施用而改善的病症,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,骨丢失。进行骨重建手术,肌肉减少症,肌无力,皮肤衰老,男性性腺功能减退,妇女绝经后症状,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疾病,炎症性关节炎和关节修复,HIV消瘦,前列腺癌,恶性肿瘤恶病质,肌肉营养不良症,卵巢早衰和自身免疫性疾病,单独或与其他活性剂联合使用。

著录项

  • 公开/公告号BR0308355A

    专利类型

  • 公开/公告日2005-01-25

    原文格式PDF

  • 申请/专利权人 MERCK & CO. INC.;

    申请/专利号BR20030308355

  • 发明设计人 ROBERT S. MEISSNER;JAMES J. PERKINS;

    申请日2003-03-07

  • 分类号A61K31/473;C07D221/18;

  • 国家 BR

  • 入库时间 2022-08-21 22:18:38

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