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    HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    3.
    发明申请
    HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
    选择性受体选择性受体调节剂及其使用方法

    公开(公告)号：WO2004035736A3

    公开(公告)日：2004-07-15

    申请号：PCT/US0332507

    申请日：2003-10-14

    申请人： UNIV TENNESSEE RES FOUNDATION ,  DALTON JAMES T ,  MILLER DUANE D ,  YIN DONGHUA ,  HE YALI ,  STEINER MITCHELL S ,  VEVERKA KAREN A

    发明人： DALTON JAMES T ,  MILLER DUANE D ,  YIN DONGHUA ,  HE YALI ,  STEINER MITCHELL S ,  VEVERKA KAREN A

    IPC分类号： A61K31/165 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/16 ,  C07C235/24 ,  C07C255/60 ,  C07C335/18 ,  C07D209/08 ,  C07D215/22 ,  C07D215/227 ,  C07D271/12 ,  C07C233/05 ,  A61K31/275 ,  C07C255/50

    CPC分类号： C07D215/227 ,  A61K31/165 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/16 ,  C07C235/24 ,  C07C255/60 ,  C07C335/18 ,  C07D209/08 ,  C07D271/12

    摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

    摘要翻译： 本发明提供一类雄激素受体靶向剂（ARTA）。 这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。 已经发现几种SARM化合物对于雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。 已经发现其他SARM化合物对于雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗多种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血， 肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低有关的疾病（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌 癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞凋亡。

    SIMPLIFIED RESINIFERATOXIN ANALOGUES AS VANILLOID RECEPTOR AGONIST SHOWING EXCELLENT ANALGESIC ACTIVITY AND THE PHARMACEUTICAL CO MPOSITIONS CONTAINING THE SAME
    6.
    发明申请
    SIMPLIFIED RESINIFERATOXIN ANALOGUES AS VANILLOID RECEPTOR AGONIST SHOWING EXCELLENT ANALGESIC ACTIVITY AND THE PHARMACEUTICAL CO MPOSITIONS CONTAINING THE SAME 审中-公开
    简化的树脂类似物作为VANILLOID受体激动剂显示出优异的活性和含有其的药物组合物

    公开(公告)号：WO2003027064A1

    公开(公告)日：2003-04-03

    申请号：PCT/KR2002/001746

    申请日：2002-09-18

    申请人： DIGITAL BIOTECH CO. LTD,. ,  LEE, Jee-Woo

    发明人： LEE, Jee-Woo

    IPC分类号： C07C335/18

    CPC分类号： C07C275/24 ,  C07C235/34 ,  C07C333/04 ,  C07C335/18

    摘要： The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonistsand potent analgesics.The present invention provides a pharmaceutical composition for preventing, alleviating or treating pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neutopathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease or urgent urinary incontinence.

    摘要翻译： 本发明涉及含有树脂毒素药效学的新型香草酸类似物，包含这种类似物的药物组合物及其作为香草素受体激动剂和强效止痛剂的用途。本发明提供了一种用于预防，缓解或治疗疼痛，急性疼痛，慢性疼痛， 神经性疼痛，手术后疼痛，偏头痛，关节痛，神经病变，神经损伤，糖尿病性神经病变，神经变性，神经性皮肤病，中风，膀胱过敏反应，肠易激综合征，呼吸系统疾病如哮喘或慢性阻塞性肺疾病，刺激性 皮肤，眼睛或粘膜，发炎，胃十二指肠溃疡，炎性肠病，炎症性疾病或急性尿失禁。