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    17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
    2.
    发明授权
    17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators 失效
    17-羟基-4-氮杂 - 雄甾烷-3-酮作为雄激素受体调节剂

    公开(公告)号：US07605152B2

    公开(公告)日：2009-10-20

    申请号：US10501640

    申请日：2003-01-10

    申请人： William P. Dankulich ,  Robert S. Meissner ,  Helen J. Mitchell ,  James J. Perkins

    发明人： William P. Dankulich ,  Robert S. Meissner ,  Helen J. Mitchell ,  James J. Perkins

    IPC分类号： A61K31/56 ,  A61K31/58

    CPC分类号： C07J73/005 ,  A61K31/473 ,  A61K31/58 ,  A61K45/06 ,  A61K2300/00

    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 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 osteoporesis, 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, obesity, 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I化合物，其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，以及在一种激活雄激素受体的功能的方法中 特别是其中雄性患者的前列腺中或在女性患者的子宫中阻断雄激素受体的功能并在骨和/或肌肉组织中活化的方法。 这些化合物可用于治疗由雄激素缺乏引起的或可由雄激素给药改善的病症，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，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，肥胖，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。

    Polymorphs of an androgen receptor modulator
    3.
    发明授权
    Polymorphs of an androgen receptor modulator 失效
    雄激素受体调节剂的多态性

    公开(公告)号：US07365202B2

    公开(公告)日：2008-04-29

    申请号：US11633152

    申请日：2006-12-04

    申请人： Lushi Tan ,  Robert S. Meissner ,  Wenjie Li ,  James J. Perkins ,  Aaron S. Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    发明人： Lushi Tan ,  Robert S. Meissner ,  Wenjie Li ,  James J. Perkins ,  Aaron S. Cote ,  Joyce Stellabott ,  Yuan-Hon Kiang

    IPC分类号： C07D221/18

    CPC分类号： C07J73/005 ,  C07D471/04

    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, Alzheimer'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弱化肌张力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，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，老化的皮肤，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，阿尔茨海默氏病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其它活性剂组合。

    &agr;v integrin receptor antagonists
    4.
    发明授权
    &agr;v integrin receptor antagonists 失效
    alphav整合素受体拮抗剂

    公开(公告)号：US06410526B1

    公开(公告)日：2002-06-25

    申请号：US09583522

    申请日：2000-05-31

    申请人： Mark E. Duggan ,  George D. Hartman ,  Robert S. Meissner ,  James J. Perkins

    发明人： Mark E. Duggan ,  George D. Hartman ,  Robert S. Meissner ,  James J. Perkins

    IPC分类号： A61K3155

    CPC分类号： C07D239/48 ,  C07D401/06 ,  C07D471/04

    摘要： The present invention relates to novel nonanoic acid derivatives, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

    摘要翻译： 本发明涉及新的壬酸衍生物，它们的合成及其作为alphav整联蛋白受体拮抗剂的用途。 更具体地说，本发明的化合物是整联蛋白受体alphavbeta3和alphavbeta5的拮抗剂，可用于抑制骨吸收，治疗和预防骨质疏松，抑制血管再狭窄，糖尿病性视网膜病变，黄斑变性，血管生成，动脉粥样硬化，炎症，炎症性关节炎 ，病毒性疾病，癌症和转移性肿瘤生长。

    N-(Pyridin-4-Yl)-2-Phenylbutanamides as Androgen Receptor Modulators
    5.
    发明申请
    N-(Pyridin-4-Yl)-2-Phenylbutanamides as Androgen Receptor Modulators 审中-公开
    N-（吡啶-4-基）-2-苯基丁酰胺作为雄激素受体调节剂

    公开(公告)号：US20090088458A1

    公开(公告)日：2009-04-02

    申请号：US11989412

    申请日：2006-07-28

    申请人： Robert S. Meissner ,  James J. Perkins ,  Yuntae Kim ,  Barbara Hanney ,  Carol A. McVean

    发明人： Robert S. Meissner ,  James J. Perkins ,  Yuntae Kim ,  Barbara Hanney ,  Carol A. McVean

    IPC分类号： A61K31/4418 ,  C07D213/36 ,  A61P19/02 ,  A61K38/27 ,  C07D213/63

    CPC分类号： C07D213/61 ,  A61K31/44 ,  C07D213/64 ,  C07D213/65 ,  Y02A50/401

    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, Alzheimer'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弱化肌张力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，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，老化的皮肤，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，阿尔茨海默氏病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其它活性剂组合。

    N-(Pyridin-3-Yl)-2-Phenylbutanamides As Androgen Receptor Modulators
    6.
    发明申请
    N-(Pyridin-3-Yl)-2-Phenylbutanamides As Androgen Receptor Modulators 审中-公开
    N-（吡啶-3-基）-2-苯基丁酰胺作为雄激素受体调节剂

    公开(公告)号：US20080124402A1

    公开(公告)日：2008-05-29

    申请号：US11666525

    申请日：2005-10-25

    申请人： Yuntae Kim ,  Joshua Close ,  Mark E. Duggan ,  Barbara Hanney ,  Robert S. Meissner ,  Jeffrey Musselman ,  James J. Perkins ,  Jiabing Wang

    发明人： Yuntae Kim ,  Joshua Close ,  Mark E. Duggan ,  Barbara Hanney ,  Robert S. Meissner ,  Jeffrey Musselman ,  James J. Perkins ,  Jiabing Wang

    IPC分类号： A61K33/16 ,  C07D213/02 ,  A61K31/44 ,  A61K31/56 ,  A61K38/16 ,  A61K31/59 ,  A61P19/10 ,  A61P19/08 ,  A61K31/66 ,  A61K31/4535 ,  A61K33/10 ,  A61K33/06

    CPC分类号： C07D213/64 ,  A61K31/44 ,  C07D213/74

    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, Alzheimer'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弱化肌张力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，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，老化的皮肤，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，阿尔茨海默氏病，肌营养不良症，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰以及自身免疫性疾病，单独或与其它活性剂组合。

    Fluorinated 4-azasteroid derivatives as androgen receptor modulators
    7.
    发明授权
    Fluorinated 4-azasteroid derivatives as androgen receptor modulators 失效
    氟化4-氮杂甾体衍生物作为雄激素受体调节剂

    公开(公告)号：US07186838B2

    公开(公告)日：2007-03-06

    申请号：US10507239

    申请日：2003-03-07

    申请人： Robert S. Meissner ,  James J. Perkins

    发明人： Robert S. Meissner ,  James J. Perkins

    IPC分类号： C07D221/18 ,  C07D401/12

    CPC分类号： A61K31/473 ,  C07J73/005

    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 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, cancer cachexia, 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，这些化合物可用于治疗由雄激素缺乏引起的或可通过雄激素给药改善的病症，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，骨重建手术后的骨损伤，肌营养不良，虚弱， 老化皮肤，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，癌症恶病质，肌营养不良，卵巢早衰，及 自身免疫疾病，单独或与其他活性剂组合。

    Fluorinated 4-azasteroids as androgen receptor modulators
    10.
    发明授权
    Fluorinated 4-azasteroids as androgen receptor modulators 失效
    氟化4-氮杂甾酮作为雄激素受体调节剂

    公开(公告)号：US07410977B2

    公开(公告)日：2008-08-12

    申请号：US11578755

    申请日：2005-04-22

    申请人： Robert S. Meissner ,  James J. Perkins

    发明人： Robert S. Meissner ,  James J. Perkins

    IPC分类号： A61K31/473 ,  C07D221/18

    CPC分类号： C07J73/005

    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), cancer cachexia, Alzheimer'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弱化肌张力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，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，老化的皮肤，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 ），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，以及自身免疫疾病，单独或与其它活性剂组合。