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1. 发明申请

WO2009006567A3 PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为AKT蛋白激酶抑制剂的PYRIMIDYL CYCLOPENTANES
公开(公告)号：WO2009006567A3
公开(公告)日：2009-03-19
申请号：PCT/US2008069144
申请日：2008-07-03
申请人： ARRAY BIOPHARMA INC , GENENTECH INC , BENCSIK JOSEF , BLAKE JAMES F , GRAHAM JAMES M , HENTEMANN MARTIN F , KALLAN NICHOLAS C , MITCHELL IAN S , SCHLACTER STEPHEN T , SPENCER KEITH L , XIAO DENGMING , XU RUI , WELCH MIKE , LIANG JUN , SAFINA BRIAN S
发明人： BENCSIK JOSEF , BLAKE JAMES F , GRAHAM JAMES M , HENTEMANN MARTIN F , KALLAN NICHOLAS C , MITCHELL IAN S , SCHLACTER STEPHEN T , SPENCER KEITH L , XIAO DENGMING , XU RUI , WELCH MIKE , LIANG JUN , SAFINA BRIAN S
IPC分类号： C07D401/12 , A61K31/517 , A61P9/00 , A61P25/28 , A61P35/00 , C07D403/12
CPC分类号： C07D403/12 , C07D401/12
摘要： The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明提供式（I）化合物，其包括互变异构体，拆分的对映异构体，非对映异构体，溶剂合物，代谢物，盐和药学上可接受的前药。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

2. 发明申请

WO2009089453A9 HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR 审中-公开
公开(公告)号：WO2009089453A9
公开(公告)日：2009-07-16
申请号：PCT/US2009/030602
申请日：2009-01-09
申请人： ARRAY BIOPHARMA INC. , GENENTECH, INC. , BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
发明人： BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
摘要： The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.

3. 发明申请

WO2009089453A1 HYDROXYLATED PYRIMIDYL CYCLOPENTANE AS AKT PROTEIN KINASE INHIBITOR 审中-公开
标题翻译：羟丙基吡咯烷酮作为AKT蛋白激酶抑制剂
公开(公告)号：WO2009089453A1
公开(公告)日：2009-07-16
申请号：PCT/US2009/030602
申请日：2009-01-09
申请人： ARRAY BIOPHARMA INC. , GENENTECH, INC. , BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
发明人： BENCSIK, Josef , BLAKE, James, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , CHABOT, Christine , DO, Steven , LIANG, Jun , SAFINA, Brian , ZHANG, Birong
IPC分类号： C07D239/70 , A61K31/517 , A61P35/00
CPC分类号： C07D239/70
摘要： The present invention provides a compound and pharmaceutically acceptable salts thereof, comprising the Formula I. Also provided are methods of using the compound of this invention as an AKT protein kinase inhibitor and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明提供了包含式I的化合物及其药学上可接受的盐。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

4. 发明申请

WO2009006567A2 PYRIMIDYL CYCLOPENTANES AS AKT PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为AKT蛋白激酶抑制剂的嘧啶基环戊烷
公开(公告)号：WO2009006567A2
公开(公告)日：2009-01-08
申请号：PCT/US2008/069144
申请日：2008-07-03
申请人： ARRAY BIOPHARMA INC. , GENENTECH, INC. , BENCSIK, Josef , BLAKE, James, F. , GRAHAM, James, M. , HENTEMANN, Martin, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SCHLACTER, Stephen, T. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , WELCH, Mike , LIANG, Jun , SAFINA, Brian, S.
发明人： BENCSIK, Josef , BLAKE, James, F. , GRAHAM, James, M. , HENTEMANN, Martin, F. , KALLAN, Nicholas, C. , MITCHELL, Ian, S. , SCHLACTER, Stephen, T. , SPENCER, Keith, L. , XIAO, Dengming , XU, Rui , WELCH, Mike , LIANG, Jun , SAFINA, Brian, S.
IPC分类号： C07D401/12 , C07D403/12
CPC分类号： C07D403/12 , C07D401/12
摘要： The present invention provides compounds of Formula (I), including tautomers, resolved enantiomers, diastereomers, solvates, metabolites, salts and pharmaceutically acceptable prodrugs thereof. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明提供式（I）的化合物，包括其互变异构体，拆分的对映异构体，非对映异构体，溶剂化物，代谢物，盐和药学上可接受的前药。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂并用于治疗过度增殖性疾病如癌症的方法。

5. 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.

6. 发明申请

WO2005051304A3 AKT PROTEIN KINASE INHIBITORS 审中-公开
公开(公告)号：WO2005051304A3
公开(公告)日：2005-06-09
申请号：PCT/US2004/039094
申请日：2004-11-19
申请人： ARRAY BIOPHARMA INC. , MITCHELL, Ian, S. , SPENCER, Keith, L. , STENGEL, Peter , HAN, Yongxin , KALLAN, Nicholas, C. , MUNSON, Mark , VIGERS, Guy, P., A. , BLAKE, James , PISCOPIO, Anthony , JOSEY, John , MILLER, Scott , XIAO, Dengming , XU, Riu , RAO, Chang , WANG, Bin , BERNACKI, April, L.
发明人： MITCHELL, Ian, S. , SPENCER, Keith, L. , STENGEL, Peter , HAN, Yongxin , KALLAN, Nicholas, C. , MUNSON, Mark , VIGERS, Guy, P., A. , BLAKE, James , PISCOPIO, Anthony , JOSEY, John , MILLER, Scott , XIAO, Dengming , XU, Riu , RAO, Chang , WANG, Bin , BERNACKI, April, L.
IPC分类号： A61K31/53 , A61K31/519 , A61K31/496 , C07D257/12 , C07D253/00 , C07D401/00
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

7. 发明申请

WO2005051304A2 AKT PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： AKT蛋白激酶抑制剂
公开(公告)号：WO2005051304A2
公开(公告)日：2005-06-09
申请号：PCT/US2004039094
申请日：2004-11-19
申请人： ARRAY BIOPHARMA INC , MITCHELL IAN S , SPENCER KEITH L , STENGEL PETER , HAN YONGXIN , KALLAN NICHOLAS C , MUNSON MARK , VIGERS GUY P A , BLAKE JAMES , PISCOPIO ANTHONY , JOSEY JOHN , MILLER SCOTT , XIAO DENGMING , XU RIU , RAO CHANG , WANG BIN , BERNACKI APRIL L
发明人： MITCHELL IAN S , SPENCER KEITH L , STENGEL PETER , HAN YONGXIN , KALLAN NICHOLAS C , MUNSON MARK , VIGERS GUY P A , BLAKE JAMES , PISCOPIO ANTHONY , JOSEY JOHN , MILLER SCOTT , XIAO DENGMING , XU RIU , RAO CHANG , WANG BIN , BERNACKI APRIL L
IPC分类号： A61K20060101 , A61K31/496 , A61K31/519 , A61K31/53 , A61K
CPC分类号： C07D239/94 , B41M3/008 , B44F1/10 , C07D231/56 , C07D237/28 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D409/04 , C07D409/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D495/04 , G09F13/16 , Y10T428/24802 , Y10T428/24851 , Y10T428/25 , Y10T428/31507 , Y10T428/31551 , Y10T428/31786 , Y10T428/31855
摘要： The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.
摘要翻译：本发明提供包括分解对映异构体，非对映异构体，溶剂化物和药学上可接受的盐的化合物，其包含式为：A-L-CR，其中CR为环状核心基团，L为连接基团，A如本文所定义。还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

8. 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。

9. 发明申请

WO2007035309A1 TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：酪氨酸激酶抑制剂
公开(公告)号：WO2007035309A1
公开(公告)日：2007-03-29
申请号：PCT/US2006/035314
申请日：2006-09-11
申请人： MERCK & CO., INC. , DINSMORE, Christopher, J. , GUERIN, David, J. , HANNEY, Barbara , KIM, Yuntae , SPENCER, Keith, L. , TORRENT, Maricel
发明人： DINSMORE, Christopher, J. , GUERIN, David, J. , HANNEY, Barbara , KIM, Yuntae , SPENCER, Keith, L. , TORRENT, Maricel
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/404 , A61K31/416 , A61K31/4192 , A61P19/02 , A61P35/00
CPC分类号： C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D487/04
摘要： The present invention relates to pyridinyloxy- and pyrimidinyloxyindole derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译：本发明涉及可用于治疗细胞增殖性疾病的吡啶氧基 - 和嘧啶氧基吲哚衍生物，用于治疗与MET活性相关的疾病，以及用于抑制受体酪氨酸激酶MET。本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。

10. 发明申请

WO2003024969A1 TYROSINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2003024969A1
公开(公告)日：2003-03-27
申请号：PCT/US2002/028779
申请日：2002-09-10
申请人： MERCK & CO., INC. , ARRINGTON, Kenneth, L. , FRALEY, Mark, E. , HANNEY, Barbara , KIM, Yuntae , SPENCER, Keith, L.
发明人： ARRINGTON, Kenneth, L. , FRALEY, Mark, E. , HANNEY, Barbara , KIM, Yuntae , SPENCER, Keith, L.
IPC分类号： C07D487/04
CPC分类号： C07D401/14 , C07D401/04 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04
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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