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1. 发明申请

WO0232861A2 ORALLY ACTIVE SALTS WITH TYROSINE KINASE ACTIVITY 审中-公开
标题翻译： ORR活性盐与TYROSINE激酶活性
公开(公告)号：WO0232861A2
公开(公告)日：2002-04-25
申请号：PCT/US0132508
申请日：2001-10-17
申请人： MERCK & CO INC , FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
发明人： FRALEY MARK E , KARKI SHYAM B , KIM YUNTAE
IPC分类号： A61K31/4709 , A61K31/496 , A61K31/551 , A61P3/10 , A61P9/00 , A61P17/00 , A61P17/06 , A61P19/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/04 , C07D401/14 , C07D
CPC分类号： C07D401/04 , C07D401/14
摘要： The present invention relates to orally active salts of 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.
摘要翻译：本发明涉及化合物，其抑制，调节和/或调控酪氨酸激酶信号转导，含有这些化合物的组合物的口服活性的盐，以及使用它们来治疗酪氨酸激酶 - 依赖性疾病和病症，如血管生成，癌症的方法，肿瘤生长，动脉粥样硬化，年龄相关性黄斑变性，糖尿病性视网膜病，炎性疾病等。

2. 发明申请

WO0129025A3 TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO0129025A3
公开(公告)日：2001-11-01
申请号：PCT/US0028625
申请日：2000-10-16
申请人： MERCK & CO INC , ARRINGTON KENNETH L , BILODEAU MARK T , FRALEY MARK E , HARTMAN GEORGE D , HOFFMAN WILLIAM F , HUNGATE RANDALL W , KIM YUNTAE
发明人： ARRINGTON KENNETH L , BILODEAU MARK T , FRALEY MARK E , HARTMAN GEORGE D , HOFFMAN WILLIAM F , HUNGATE RANDALL W , KIM YUNTAE
IPC分类号： C07D401/04 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/00 , A61K45/06 , A61N5/10 , A61P9/10 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P27/02 , A61P29/00 , A61P35/00 , A61P43/00 , C07D401/00 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： C07D413/14 , A61K31/495 , A61K45/06 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14 , A61K2300/00
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.

3. 发明申请

WO03020699A3 TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO03020699A3
公开(公告)日：2003-05-22
申请号：PCT/US0227114
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： A61P35/00 , C07D401/04 , C07D401/14 , C07D417/14 , A61K31/395 , A61K31/47 , A61K31/495 , A61K31/55 , C07D215/00 , C07D243/00 , C07D285/36 , C07D401/00 , C07D487/02
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.
摘要翻译：本发明涉及抑制，调控和/或调节酪氨酸激酶信号转导的化合物，含有这些化合物的组合物及其用于治疗酪氨酸激酶依赖性疾病和病症如血管生成，癌症，肿瘤生长，动脉粥样硬化的方法，年龄相关性黄斑变性，糖尿病性视网膜病变，炎症性疾病等。

4. 发明申请

WO2007038444A3 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：WO2007038444A3
公开(公告)日：2007-08-09
申请号：PCT/US2006037273
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 , C07D239/90
CPC分类号： C07D403/06 , C07D239/90 , C07D409/12
摘要： The invention relates to substituted N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamid derivatives which modulate androgen receptors to treat conditions such as: osteoporosis, peridontal disease, bone fracture, frailty, and sarcopenia.
摘要翻译：本发明涉及调节雄激素受体以治疗诸如骨质疏松症，肠周周疾病，骨折，虚弱和肌肉减少症之类的病症的取代的N-（4-氧代-3,4-二氢喹唑啉-2-基）丁酰胺衍生物。

5. 发明申请

WO2008048540A3 2-HYDROXY-2-PHENYL/THIOPHENYL PROPIONAMIDES AS ANDROGEN RECEPTOR MODULATORS 审中-公开
标题翻译：作为雄激素受体调节剂的2-羟基-2-苯基/噻吩基丙酰胺
公开(公告)号：WO2008048540A3
公开(公告)日：2008-08-14
申请号：PCT/US2007021984
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： A01N43/54 , A61K31/497 , A61K31/517
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）的化合物以组织选择性方式是雄激素受体（AR）的调节剂。这些化合物可用于增强肌肉张力减弱和由雄激素缺乏引起的病症的治疗，或可通过施用雄激素改善，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，骨重建后的骨损伤女性绝经后症状，动脉粥样硬化，高胆固醇血症，高脂血症，肥胖症，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消瘦，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，阿尔茨海默氏病，肌营养不良，认知衰退，性功能障碍，睡眠呼吸暂停，抑郁症，卵巢早衰和自身免疫疾病，单独或与其他活性剂组合。

6. 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。

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