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1. 发明申请

WO0107436A3 Substituted oxoazaheterocyclyl compounds. 审中-公开
标题翻译：取代的含氮杂环基化合物。
公开(公告)号：WO0107436A3
公开(公告)日：2001-08-23
申请号：PCT/IB0001156
申请日：2000-07-26
申请人： AVENTIS PHARM PROD INC , EWING WILLIAM R , BECKER MICHAEL R , CHOI SLEDESKI YONG MI , PAULS HEINZ W , HE WEI , CONDON STEPHEN M , DAVIS RODERICK S , HANNEY BARBARA A , SPADA ALFRED P , BURNS CHRISTOPHER J , JIANG JOHN Z , LI AIWEN , MYERS MICHAEL R , LAU WAN F , POLI GREGORY B
发明人： EWING WILLIAM R , BECKER MICHAEL R , CHOI-SLEDESKI YONG MI , PAULS HEINZ W , HE WEI , CONDON STEPHEN M , DAVIS RODERICK S , HANNEY BARBARA A , SPADA ALFRED P , BURNS CHRISTOPHER J , JIANG JOHN Z , LI AIWEN , MYERS MICHAEL R , LAU WAN F , POLI GREGORY B
IPC分类号： C07D241/08 , A61K31/495 , A61K31/496 , A61K31/498 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P7/02 , A61P9/02 , A61P9/04 , A61P9/10 , A61P19/02 , A61P25/28 , A61P35/00 , A61P41/00 , A61P43/00 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D495/04 , C07D491/04
CPC分类号： C07D401/06 , C07D401/14 , C07D403/06 , C07D409/14 , C07D471/04 , Y02P20/582
摘要： This invention is directed to oxoazaheterocyclyl compounds which inhibit Factor Xa, to oxoazaheterocyclyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa.

2. 发明申请

WO2013009582A1 TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF 审中-公开
标题翻译： TrkA激酶抑制剂，其组合物及其方法
公开(公告)号：WO2013009582A1
公开(公告)日：2013-01-17
申请号：PCT/US2012/045638
申请日：2012-07-06
申请人： MERCK SHARP & DOHME CORP. , HANNEY, Barbara , MANLEY, Peter , RUDD, Michael, T. , SANDERS, John, M. , STACHEL, Shawn, J. , HENZE, Darrell
发明人： HANNEY, Barbara , MANLEY, Peter , RUDD, Michael, T. , SANDERS, John, M. , STACHEL, Shawn, J. , HENZE, Darrell
IPC分类号： A01N43/90 , A61K31/404 , C07D471/02
CPC分类号： C07D471/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D417/04 , C07D487/04
摘要： The present invention is directed to compounds of formula I and la: which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
摘要翻译：本发明涉及式I和Ia的化合物：它们是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成，与神经生长因子（NGF）受体TrkA的异常活动相关的疾病，失调，损伤或功能障碍，或与脱髓鞘或脱髓鞘相关的疾病或障碍。

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

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。

5. 发明申请

WO2004041277A1 CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的羧苄基苯并咪唑衍生物
公开(公告)号：WO2004041277A1
公开(公告)日：2004-05-21
申请号：PCT/US2003/034345
申请日：2003-10-28
申请人： MERCK & CO., INC. , KIM, Yuntae , SPENCER, Keith, L. , HANNEY, Barbara , DUGGAN, Mark, E.
发明人： KIM, Yuntae , SPENCER, Keith, L. , HANNEY, Barbara , DUGGAN, Mark, E.
IPC分类号： A61K31/427
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，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。

6. 发明申请

WO2013066736A1 QUINOLINE CARBOXAMIDE AND QUINOLINE CARBONITRILE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译：喹啉羧酰胺和喹啉衍生物作为mGluR2负离子调节剂，组合物及其用途
公开(公告)号：WO2013066736A1
公开(公告)日：2013-05-10
申请号：PCT/US2012/062027
申请日：2012-10-26
申请人： MERCK SHARP & DOHME CORP. , BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , SHU, Youheng
发明人： BUNGARD, Christopher James , CONVERSO, Antonella , DE LEON, Pablo , HANNEY, Barbara , HARTINGH, Timothy John , MANIKOWSKI, Jesse Josef , MANLEY, Peter, J. , MEISSNER, Robert , MENG, Zhaoyang , PERKINS, James, J. , RUDD, Michael, T. , SHU, Youheng
IPC分类号： A01N43/42
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, R Q , -L-, R 1 , n, R 2 , and R 3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
摘要翻译：本发明提供式（I）的喹啉羧酰胺和喹啉腈化合物，其中环A，RQ，-L-，R1，n，R2和R3如本文所定义。本发明的化合物可用作非竞争性mGluR2拮抗剂或mGluR2负变构调节剂（NAM），以及用于治疗患有（其中涉及mGluR2-NAM受体的疾病或病症）的患者（优选人）的方法，例如作为阿尔茨海默病，认知障碍，精神分裂症和其他情绪障碍，疼痛障碍和睡眠障碍，通过向患者施用治疗有效量的本发明化合物或其药学上可接受的盐。本发明还涉及包含本发明化合物或其药学上可接受的盐（任选与一种或多种另外的活性成分组合）和药学上可接受的载体的药物组合物，以及该化合物和药物组合物的用途的本发明治疗这些疾病。

7. 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。

8. 发明申请

WO2005120477A3 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：WO2005120477A3
公开(公告)日：2006-03-02
申请号：PCT/US2005019554
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 , A61K31/165 , A61K31/277 , A61K31/44 , C07C233/13 , C07C235/34 , C07C271/12 , C07D213/61 , C07D295/205 , A61P5/26 , C07C235/06
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，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，脆弱，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，艾滋病毒消耗，前列腺癌，良性前列腺增生（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。

9. 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。

10. 发明申请

WO2003020699A2 TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2003020699A2
公开(公告)日：2003-03-13
申请号：PCT/US2002/027114
申请日：2002-08-26
申请人： MERCK & CO., INC. , PECKHAM, Jennifer, P. , HOFFMAN, William, F. , ARRINGTON, Kenneth, L. , FRALEY, Mark, E. , HARTMAN, George, D. , KIM, Yuntae , HANNEY, Barbara , SPENCER, Keith, L.
发明人： PECKHAM, Jennifer, P. , HOFFMAN, William, F. , ARRINGTON, Kenneth, L. , FRALEY, Mark, E. , HARTMAN, George, D. , KIM, Yuntae , HANNEY, Barbara , SPENCER, Keith, L.
IPC分类号： C07D
CPC分类号： C07D417/14 , C07D401/04 , C07D401/14
摘要： The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.

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