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公开(公告)号：EP1861366A2
公开(公告)日：2007-12-05
申请号：EP06737641.8
申请日：2006-03-10
申请人： Merck & Co., Inc.
IPC分类号： C07D209/04 , A61K31/404
CPC分类号： C07D231/06
摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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公开(公告)号：EP1697381A1
公开(公告)日：2006-09-06
申请号：EP04814749.0
申请日：2004-12-15
申请人： Merck & Co., Inc.
IPC分类号： C07D495/04 , A61K31/519
CPC分类号： C07D498/02 , A61K41/00 , C07D495/04
摘要： The present invention relates to 2-phenylthienylpyrimidinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
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公开(公告)号：EP1664026A1
公开(公告)日：2006-06-07
申请号：EP04780791.2
申请日：2004-08-11
申请人： Merck & Co., Inc.
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/454 , A61K31/506 , A61K31/497 , A61P35/00
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to dihydropyrrole compounds of Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及式（I）的二氢吡咯化合物，其用于治疗细胞增殖性疾病，用于治疗与KSP驱动蛋白活性相关的病症，和用于抑制KSP驱动蛋白。 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。
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公开(公告)号：EP1558609A2
公开(公告)日：2005-08-03
申请号：EP03779322.1
申请日：2003-10-24
申请人： Merck & Co., Inc.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427
CPC分类号： C07D417/12 , C07D417/14
摘要： The present invention relates to compounds which inhibit, regulate and/or modulate kinase signal transduction, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, retinal ischemia, macular edema, diabetic retinopathy, inflammatory diseases, and the like in mammals.
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公开(公告)号：EP1496981A2
公开(公告)日：2005-01-19
申请号：EP03746147.2
申请日：2003-04-04
申请人： Merck & Co., Inc.
发明人： BARNETT, Stanley, F. , DEFEO-JONES, Deborah , HASKELL, Kathleen, M. , HUBER, Hans, E. , NAHAS, Deborah, D. , LINDSLEY, Craig, W. , ZHAO, Zhijian , HARTMAN, George, D.
IPC分类号： A61N1/00
CPC分类号： A61K45/06 , A61K31/415 , A61K31/495 , A61K31/50 , A61K31/53 , A61K38/45 , A61K2300/00
摘要： The present invention is directed to a method of treating cancer which comprises administration of a compound which selectively inhibits the activity of one or two of the isoforms of Akt, a serine/threonine protein kinase. The invention is particularly directed to the method wherein the compound is dependent on the presence of the pleckstrin homology domain of Akt for its inhibitory activity.
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公开(公告)号：EP1341540A2
公开(公告)日：2003-09-10
申请号：EP01991965.3
申请日：2001-11-30
申请人： Merck & Co., Inc.
发明人： BILODEAU, Mark, T. , HARTMAN, George, D. , HOFFMAN, Jacob, M., Jr. , LUMMA, William, C., Jr. , MANLEY, Peter, J. , RODMAN, Leonard , SISKO, John, T. , SMITH, Anthony, M. , TUCKER, Thomas, J.
IPC分类号： A61K31/5355 , A61K31/495 , A61K31/505 , A61K31/506 , A61P7/00
CPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D487/04 , C07D487/08 , C07D491/08
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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公开(公告)号：EP0901373B1
公开(公告)日：2002-11-06
申请号：EP97920270.2
申请日：1997-04-08
申请人： MERCK & CO., INC.
IPC分类号： C07D209/46 , A61K31/40 , C07D403/12 , A61K31/495 , C07D401/12 , A61K31/44
CPC分类号： C07D401/12 , C07D209/46 , C07D403/12
摘要： This invention relates to certain novel isoindolone compounds and derivatives thereof, their synthesis, and their use as αvβ3 receptor antagonists. The αvβ3 receptor antagonist compounds of this invention are useful for inhibiting bone resorption, treating and preventing osteoporosis and cancer, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
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公开(公告)号：EP1226136A2
公开(公告)日：2002-07-31
申请号：EP00978230.1
申请日：2000-10-16
申请人： Merck & Co., Inc.
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： C07D401/00
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.
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公开(公告)号：EP1011669A1
公开(公告)日：2000-06-28
申请号：EP97905699.1
申请日：1997-01-27
申请人： MERCK & CO., INC.
IPC分类号： A61K31/415 , C07D233/54 , C07D233/60 , C07D233/61 , C07D233/66 , C07D233/90
CPC分类号： C07D233/64 , C07D231/12
摘要： The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
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公开(公告)号：EP0973396A1
公开(公告)日：2000-01-26
申请号：EP98915318.4
申请日：1998-04-06
申请人： MERCK & CO., INC.
IPC分类号： A01N43/42 , A01N43/60 , A61K31/445 , A61K31/495
CPC分类号： A61K31/472 , A61K31/195 , A61K31/223 , A61K31/365 , A61K31/4164 , A61K31/4184 , A61K31/425 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/505
摘要： The present invention relates to methods of treating cancer using a combination of a compound which is an integrin antagonist and a compound which is an inhibitor of farnesyl-protein transferase, which methods comprise administering to said mammal, either sequentially in any order or simultaneously, amounts of at least two therapeutic agents selected from a group consisting of a compound which is an integrin antagonist and a compound which is an inhibitor of farnesyl-protein transferase. The invention also relates to methods of preparing such compositions.
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