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1. 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.

2. 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。

3. 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。

4. 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。

5. 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。

6. 发明申请

WO2017083216A1 CYANOPYRIDINE DERIVATIVES AS LIVER X RECEPTOR BETA AGONISTS, COMPOSITIONS, AND THEIR USE 审中-公开
标题翻译： CYANOPYRIDINE衍生物作为肝X受体β激动剂，组合物及其应用
公开(公告)号：WO2017083216A1
公开(公告)日：2017-05-18
申请号：PCT/US2016/060765
申请日：2016-11-07
申请人： MERCK SHARP & DOHME CORP. , RUDD, Michael, T. , BRNARDIC, Edward, J. , KIM, Yuntae , MEISSNER, Robert, S. , RADA, Vanessa , STACHEL, Shawn, J. , ZERBINATTI, Celina, V.
发明人： RUDD, Michael, T. , BRNARDIC, Edward, J. , KIM, Yuntae , MEISSNER, Robert, S. , RADA, Vanessa , STACHEL, Shawn, J. , ZERBINATTI, Celina, V.
IPC分类号： A61K31/496 , C07D401/04 , C07D241/04
CPC分类号： A61K31/496 , C07D213/74 , C07D213/85 , C07D295/192 , C07D295/205 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/08 , C07D487/08 , C07D487/18 , C07D515/04
摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供了取代的含氰基吡啶的式（I）化合物及其可接受的盐，其中R 1，R 2， R 3，R 4，R 5，X，Y，Q和部分如本文所定义。本发明的新化合物和包含其化合物的药学上可接受的组合物可用作肝X-β受体（LXRβ）激动剂，并且可用于治疗或预防与其有关的病状。这样的病理学包括但不限于炎症性疾病和以胆固醇和脂质代谢缺陷为特征的疾病，例如阿尔茨海默氏病。

7. 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。

8. 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。

9. 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。

10. 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。

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