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1. 发明申请

WO2005120477A2 N- (2-BENZYL) -2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（2-苄基）-2-苯基黄烷作为雄激素受体调节剂
公开(公告)号：WO2005120477A2
公开(公告)日：2005-12-22
申请号：PCT/US2005/019554
申请日：2005-06-03
申请人： MERCK & CO., INC. , HANNEY, Barbara , KIM, Yuntae , KROUT, Michael, R. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
发明人： HANNEY, Barbara , KIM, Yuntae , KROUT, Michael, R. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
IPC分类号： A61K31/00
CPC分类号： C07D295/205 , C07C233/13 , C07C235/34 , C07C255/60 , C07C271/12 , C07C271/22 , C07C2601/02 , C07D213/61 , C07D213/73
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, Alzhheiner’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施用引起的疾病的治疗，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，骨重建手术后的骨损伤，肌肉减少症，虚弱，衰老的皮肤，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，炎症性关节炎和关节修复，艾滋病毒消耗，前列腺癌，良性前列腺增生症（BPH），腹部肥胖，代谢综合征，II型糖尿病，癌症恶病质，Alzhheiner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，单独或与其他活性剂组合。

2. 发明申请

WO2006060108A1 N-(PYRIDIN-3-YL)-2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（PYRIDIN-3-YL）-2-苯基琥珀酸作为雄激素受体调节剂
公开(公告)号：WO2006060108A1
公开(公告)日：2006-06-08
申请号：PCT/US2005/039931
申请日：2005-10-25
申请人： MERCK & CO., INC. , KIM, Yuntae , CLOSE, Joshua , DUGGAN, Mark, E. , HANNEY, Barbara , MEISSNER, Robert, S. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
发明人： KIM, Yuntae , CLOSE, Joshua , DUGGAN, Mark, E. , HANNEY, Barbara , MEISSNER, Robert, S. , MUSSELMAN, Jeffrey , PERKINS, James, J. , WANG, Jiabing
IPC分类号： A61K31/44 , C07D213/02
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，炎症性关节炎和关节修复，HIV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，早期卵巢衰竭和自身免疫性疾病，单独或与其它活性剂组合。

3. 发明申请

WO2007038444A2 N-(4-OXO-3,4-DIHYDROQUINAZOLIN-2-YL)BUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酸钠作为雄激素受体调节剂
公开(公告)号：WO2007038444A2
公开(公告)日：2007-04-05
申请号：PCT/US2006/037273
申请日：2006-09-22
申请人： MERCK & CO., INC. , HANNEY, Barbara , KIM, Yuntae , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey, D. , PERKINS, James, J.
发明人： HANNEY, Barbara , KIM, Yuntae , MITCHELL, Helen, J. , MUSSELMAN, Jeffrey, D. , PERKINS, James, J.
IPC分类号： A61K31/517
CPC分类号： C07D403/06 , C07D239/90 , C07D409/12
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，炎症性关节炎和关节修复，HIV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，早期卵巢衰竭和自身免疫性疾病，单独或与其它活性剂组合。

4. 发明申请

WO2008048540A2 2-HYDROXY-2-PHENYL/THIOPHENYL PROPIONAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： 2-羟基-2-苯基/噻吩并噻唑类作为雄激素受体调节剂
公开(公告)号：WO2008048540A2
公开(公告)日：2008-04-24
申请号：PCT/US2007/021984
申请日：2007-10-15
申请人： MERCK & CO., INC. , KIM, Yuntae , MEISSNER, Robert, S. , MITCHELL, Helen, J. , PERKINS, James, J. , ROSSI, Michael, A. , WANG, Jiabing
发明人： KIM, Yuntae , MEISSNER, Robert, S. , MITCHELL, Helen, J. , PERKINS, James, J. , ROSSI, Michael, A. , WANG, Jiabing
IPC分类号： A61K31/4436
CPC分类号： C07D213/40 , C07D409/12
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, HFV-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减弱的肌肉紧张度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情况，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，肌肉减少症，虚弱，衰老皮肤，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，HFV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，早期卵巢衰竭和自身免疫性疾病，单独或与其它活性剂组合。

5. 发明申请

WO2007016358A1 N-(PYRIDIN-4-YL)-2-PHENYLBUTANAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译： N-（PYRIDIN-4-YL）-2-苯基琥珀酸作为雄激素受体调节剂
公开(公告)号：WO2007016358A1
公开(公告)日：2007-02-08
申请号：PCT/US2006/029457
申请日：2006-07-28
申请人： MERCK & CO., INC. , MEISSNER, Robert, S. , PERKINS, James, J. , KIM, Yuntae , HANNEY, Barbara , MCVEAN, Carol, A.
发明人： MEISSNER, Robert, S. , PERKINS, James, J. , KIM, Yuntae , HANNEY, Barbara , MCVEAN, Carol, A.
IPC分类号： C07D211/72 , C07D211/78 , A61K31/44
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，炎症性关节炎和关节修复，HIV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，早期卵巢衰竭和自身免疫性疾病，单独或与其它活性剂组合。

6. 发明申请

WO2003059293A2 17-HYDROXY-4-AZA-ANDROSTAN-3-ONES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的17-羟基-4-安非他酮-3-
公开(公告)号：WO2003059293A2
公开(公告)日：2003-07-24
申请号：PCT/US2003/000874
申请日：2003-01-10
申请人： MERCK & CO., INC. , DANKULICH, William, P. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , PERKINS, James, J.
发明人： DANKULICH, William, P. , MEISSNER, Robert, S. , MITCHELL, Helen, J. , PERKINS, James, J.
IPC分类号： A61K
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 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, 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疾病或可通过雄激素给药改善的疾病，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，肥胖症，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。

7. 发明申请

WO2005105091A1 FLUORINATED 4-AZASTEROIDS AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：氟化4-亚硫酸酯作为雄激素受体调节剂
公开(公告)号：WO2005105091A1
公开(公告)日：2005-11-10
申请号：PCT/US2005/013775
申请日：2005-04-22
申请人： MERCK & CO., INC. , MEISSNER, Robert, S. , PERKINS, James, J.
发明人： MEISSNER, Robert, S. , PERKINS, James, J.
IPC分类号： A61K31/473
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，炎症性关节炎和关节修复，HIV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。

8. 发明申请

WO2003077919A1 FLUORINATED 4-AZASTEROID DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的氟化四氮芥衍生物
公开(公告)号：WO2003077919A1
公开(公告)日：2003-09-25
申请号：PCT/US2003/008277
申请日：2003-03-07
申请人： MERCK & CO., INC. , MEISSNER, Robert, S. , PERKINS, James, J.
发明人： MEISSNER, Robert, S. , PERKINS, James, J.
IPC分类号： A61K31/473
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，HIV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。

9. 发明申请

WO2004100874A2 ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：雄激素受体调节剂及其使用方法
公开(公告)号：WO2004100874A2
公开(公告)日：2004-11-25
申请号：PCT/US2004/013787
申请日：2004-05-03
申请人： MERCK & CO., INC. , MEISSNER, Robert, S. , PERKINS, James, J.
发明人： MEISSNER, Robert, S. , PERKINS, James, J.
IPC分类号： A61K
CPC分类号： A61K31/58 , C07J73/005
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, female sexual dysfunction, 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，女性性功能障碍，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。

10. 发明申请

WO2007067490A1 POLYMORPHS OF ANDROGEN RECEPTOR MODULATOR - (N-3H-IMIDAZO [4 , 5-B] PYRIDIN-2-YL-METHYL) -2-FLUORO-4-METHYL-3-OXO-4-AZA-ANDROST- l-EN-17 . BETA . -CARBOXAMIDE 审中-公开
标题翻译：雄激素受体调节剂的多聚体 - （N-3H-咪唑并[4,5-B]吡啶-2-基]甲基）-2-氟-4-甲基-3-氧代-4-氮杂 - 安息列酸-EN- 17。 BETA。 - 甲酰胺
公开(公告)号：WO2007067490A1
公开(公告)日：2007-06-14
申请号：PCT/US2006/046263
申请日：2006-12-04
申请人： MERCK & CO., INC. , TAN, Lushi , MEISSNER, Robert, S. , LI, Wenjie , PERKINS, James, J. , COTE, Aaron, S. , STELLABOTT, Joyce , KIANG, Yuan-Hon
发明人： TAN, Lushi , MEISSNER, Robert, S. , LI, Wenjie , PERKINS, James, J. , COTE, Aaron, S. , STELLABOTT, Joyce , KIANG, Yuan-Hon
IPC分类号： C07J73/00 , A61K31/58 , A61P5/26
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。

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