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67 条记录 (耗时 0.228 秒)

    Carbonylamino-benzimidazole derivatives as androgen receptor modulators
    51.
    发明授权
    Carbonylamino-benzimidazole derivatives as androgen receptor modulators 失效
    羰基氨基 - 苯并咪唑衍生物作为雄激素受体调节剂

    公开(公告)号：US07622592B2

    公开(公告)日：2009-11-24

    申请号：US10533259

    申请日：2003-10-28

    申请人： Yuntae Kim ,  Barbara Hanney ,  Mark E. Duggan ,  Keith L. Spencer

    发明人： Yuntae Kim ,  Barbara Hanney ,  Mark E. Duggan ,  Keith L. Spencer

    IPC分类号： A61K31/427 ,  C07D417/04

    CPC分类号： C07D417/04 ,  C07D401/04 ,  C07D403/04 ,  C07D417/14

    摘要： 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.

    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。 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。

    Androstane 17-beta-carboxamides as androgen receptor modulators
    52.
    发明授权
    Androstane 17-beta-carboxamides as androgen receptor modulators 失效
    雄甾烷17-β-甲酰胺作为雄激素受体调节剂

    公开(公告)号：US07402577B2

    公开(公告)日：2008-07-22

    申请号：US10491403

    申请日：2002-09-27

    申请人： Jiabing Wang ,  Mark E. Duggan ,  David B. Whitman

    发明人： Jiabing Wang ,  Mark E. Duggan ,  David B. Whitman

    IPC分类号： A61K31/56 ,  C07J3/00

    CPC分类号： A61K31/568 ,  A61K31/56 ,  A61K31/663 ,  C07J3/00 ,  A61K2300/00

    摘要： Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, female sexual dysfunction, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, prostate cancer, arthritis and joint repair, alone or in combination with other active agents.

    摘要翻译： 公开了本文定义的结构式的化合物可用于在需要这种调节的患者中以组织选择性方式调节雄激素受体的方法，以及在患者中激活雄激素受体功能的方法 特别是其中雄性患者的前列腺或女性患者的子宫中的雄激素受体的功能被阻断并在骨和/或肌肉组织中活化的方法。 这些化合物可用于治疗雄激素缺乏症或由雄激素给药引起的疾病，包括骨质疏松症，牙周病，骨折，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老皮肤，男性性腺机能减退，女性性 功能障碍，妇女绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，再生障碍性贫血和其他造血障碍，胰腺癌，肾癌，前列腺癌，关节炎和关节修复，单独或与其他活性剂组合。

    Integrin antagonists
    59.
    发明授权
    Integrin antagonists 失效
    整合素拮抗剂

    公开(公告)号：US6017925A

    公开(公告)日：2000-01-25

    申请号：US6626

    申请日：1998-01-13

    申请人： Mark E. Duggan

    发明人： Mark E. Duggan

    IPC分类号： C07D471/04 ,  A61K31/435

    CPC分类号： C07D471/04

    摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, viral disease, and tumor growth.

    摘要翻译： 本发明涉及某些新化合物及其衍生物，其合成及其作为玻连蛋白受体拮抗剂的用途。 本发明的玻连蛋白受体拮抗剂化合物是可用于抑制骨吸收，治疗和预防骨质疏松症以及抑制再狭窄的糖尿病性视网膜病变的αvβ3拮抗剂，αvβ5拮抗剂或双重αvβ3 /αvβ5拮抗剂 ，黄斑变性，血管生成，动脉粥样硬化，炎症，病毒性疾病和肿瘤生长。