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67 条记录 (耗时 0.059 秒)

    Androgen receptor modulators and methods for use thereof
    55.
    发明授权
    Androgen receptor modulators and methods for use thereof 失效
    雄激素受体调节剂及其使用方法

    公开(公告)号：US06645974B2

    公开(公告)日：2003-11-11

    申请号：US10205634

    申请日：2002-07-25

    申请人： John H. Hutchinson ,  Michael J. Breslin ,  Gideon A. Rodan ,  Soumya P. Sahoo ,  Mark E. Duggan ,  Shun-Ichi Harada ,  Azriel Schmidt ,  Wasyl Halczenko ,  Dwight A. Towler

    发明人： John H. Hutchinson ,  Michael J. Breslin ,  Gideon A. Rodan ,  Soumya P. Sahoo ,  Mark E. Duggan ,  Shun-Ichi Harada ,  Azriel Schmidt ,  Wasyl Halczenko ,  Dwight A. Towler

    IPC分类号： A61K3158

    CPC分类号： C07J73/005 ,  A61K31/435 ,  A61K31/473 ,  A61K31/58 ,  C07D221/18 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

    摘要： Compounds of structural formula (I) 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 agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized 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, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

    摘要翻译： 公开了本文定义的结构式（I）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，以及在患者中激动雄激素受体的方法 ，特别是其中雄性受体在男性患者的前列腺或女性患者的子宫中被拮抗并在骨和/或肌肉组织中激动的方法。 这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素施用而改善的病症，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 妇女的绝经症状，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，关节炎和关节修复，单独或与其他活性剂组合。 此外，这些化合物可单独用作药物组合物成分并与其它活性剂组合使用。

    Integrin antagonists
    58.
    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。