公开(公告)号：EP1558586B1

公开(公告)日：2011-03-30

申请号：EP03779301.5

申请日：2003-10-24

申请人： Merck Sharp & Dohme Corp.

发明人： DUGGAN, Mark, E. ,  LINDSLEY, Craig, W. ,  ZHAO, Zhijian

IPC分类号： A61K31/4985 ,  A61K31/52 ,  A61K31/519 ,  A61P35/00 ,  A61K45/06 ,  C07D495/04 ,  C07D241/36 ,  A61K31/495

CPC分类号： A61K31/495 ,  A61K45/06 ,  C07D487/04 ,  C07D495/04

摘要： The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.

公开(公告)号：EP1252162B1

公开(公告)日：2012-07-25

申请号：EP01942625.3

申请日：2001-01-16

申请人： Merck Sharp & Dohme Corp.

发明人： DUGGAN, Mark, E. ,  HALCZENKO, Wasyl ,  HUTCHINSON, John, H. ,  LI, Aiwen ,  MEISSNER, Robert, S. ,  PERKINS, James, J. ,  STEELE, Thomas, G. ,  WANG, Jiabing ,  PATANE, Michael, A.

IPC分类号： A61K31/444 ,  A61K31/4166 ,  A61P19/10 ,  A61K31/4178 ,  C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D471/10

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D471/04 ,  C07D471/10

摘要： The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as αν integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors αvβ3 and/or αvβ5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

公开(公告)号：EP1729772B8

公开(公告)日：2017-04-19

申请号：EP05726105.9

申请日：2005-03-23

申请人： Merck Sharp & Dohme Corp. ,  MERCK SHARP & DOHME LTD.

发明人： BLACKABY, Wesley ,  DUGGAN, Mark, E. ,  HALLETT, David ,  HARTMAN, George, D. ,  JENNINGS, Andrew, S. ,  LEISTER, William, H. ,  LEWIS, Richard, T. ,  LINDSLEY, Craig, W. ,  NAYLOR, Elizabeth ,  STREET, Leslie, J. ,  WANG, Yi ,  WISNOSKI, David, D. ,  WOLKENBERG, Scott, E. ,  ZHAO, Zhijian

IPC分类号： C07D409/14 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04

CPC分类号： C07D409/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

公开(公告)号：EP1729772B1

公开(公告)日：2016-12-07

申请号：EP05726105.9

申请日：2005-03-23

申请人： Merck Sharp & Dohme Corp. ,  MERCK SHARP & DOHME LTD.

发明人： BLACKABY, Wesley ,  DUGGAN, Mark, E. ,  HALLETT, David ,  HARTMAN, George, D. ,  JENNINGS, Andrew, S. ,  LEISTER, William, H. ,  LEWIS, Richard, T. ,  LINDSLEY, Craig, W. ,  NAYLOR, Elizabeth ,  STREET, Leslie, J. ,  WANG, Yi ,  WISNOSKI, David, D. ,  WOLKENBERG, Scott, E. ,  ZHAO, Zhijian

IPC分类号： C07D409/14 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04

CPC分类号： C07D409/14 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

公开(公告)号：EP1622616B1

公开(公告)日：2011-06-15

申请号：EP04760294.1

申请日：2004-04-20

申请人： Merck Sharp & Dohme Corp.

发明人： BILODEAU, Mark, T. ,  DUGGAN, Mark, E. ,  HARTNETT, John, C. ,  LINDSLEY, Craig, W. ,  WU, Zhicai ,  ZHAO, Zhijian

IPC分类号： C07D401/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  A61P35/00 ,  C07D401/14

CPC分类号： C07F9/65583 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

摘要： The present invention is directed to compounds which contain a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.