公开(公告)号：EP1481077A2

公开(公告)日：2004-12-01

申请号：EP02786830.6

申请日：2002-12-02

申请人： Merck & Co., Inc.

发明人： FRALEY, Mark, E. ,  HARTMAN, George, D. ,  HOFFMAN, William, F.

IPC分类号： C12Q1/00 ,  C12Q1/48 ,  C12Q1/37 ,  C12Q1/02

CPC分类号： C07D513/04

摘要： The present invention relates to azolopyrimidinone 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.

公开(公告)号：EP1463733A2

公开(公告)日：2004-10-06

申请号：EP02804714.0

申请日：2002-12-02

申请人： Merck & Co., Inc.

发明人： FRALEY, Mark, E. ,  HARTMAN, George, D. ,  HOFFMAN, William, F.

IPC分类号： C07D495/04 ,  A61K31/519

CPC分类号： C07D495/04 ,  C07D519/00

摘要： The present invention relates to thienopyrimidinone 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.

公开(公告)号：EP1404672A1

公开(公告)日：2004-04-07

申请号：EP02744810.9

申请日：2002-06-18

申请人： Merck & Co., Inc.

发明人： BILODEAU, Mark, T. ,  HARTMAN, George, D.

IPC分类号： C07D417/12 ,  C07D417/14 ,  A61K31/44 ,  A61P35/00 ,  A61P43/00 ,  A61P27/02 ,  A61P29/00 ,  A61P19/02 ,  A61P17/06 ,  A61P17/00

CPC分类号： C07D417/12 ,  C07D417/14

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. A compound of Formula (I) wherein n is 0 or 1; X is C-H or N, provided X is C-H if n=1 and R1 is SO¿2?-(C1-C6 alkyl) and provided that X is C-H if R?1¿ is NH(C=O)NR3H; R1 is SO¿2?-(C1-C6 alkyl), (C=O)NR?3¿H, or NH(C=O)NR3H; R2 is OH OC¿1?-C6 alkyl, C1-C6 alkyl, or halo; and R?3 is C¿1-C6 alkyl.

公开(公告)号：EP1218376A1

公开(公告)日：2002-07-03

申请号：EP00961583.2

申请日：2000-09-06

申请人： Merck & Co., Inc.

发明人： BILODEAU, Mark, T. ,  HUNGATE, Randall, W. ,  RODMAN, Leonard ,  HARTMAN, George, D. ,  MANLEY, Peter, J.

IPC分类号： C07D413/12 ,  C07D417/12 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/427 ,  A61K31/433

CPC分类号： C07D417/12 ,  C07D417/14

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.

公开(公告)号：EP0714295B1

公开(公告)日：2000-12-20

申请号：EP94925195.3

申请日：1994-08-04

申请人： Merck & Co., Inc.

发明人： HARTMAN, George, D. ,  PRUGH, John, D. ,  HALCZENKO, Wasyl ,  EGBERTSON, Melissa ,  IHLE, Nathan

IPC分类号： C07D495/04 ,  A61K31/38

CPC分类号： C07D487/04 ,  A61K45/06 ,  C07D491/04 ,  C07D493/04 ,  C07D495/04 ,  C07D497/04 ,  C07D513/04

公开(公告)号：EP0664792B1

公开(公告)日：2000-01-05

申请号：EP93923845.7

申请日：1993-10-12

申请人： Merck & Co., Inc.

发明人： HARTMAN, George, D. ,  EGBERTSON, Melissa, S. ,  HALCZENKO, Wasyl ,  ASKEW, Ben

IPC分类号： A61K31/445 ,  A61K31/34 ,  A61K31/38 ,  C07D409/06 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  A61K31/395 ,  A61K31/415 ,  A61K31/42 ,  A61K31/405 ,  A61K31/335

CPC分类号： C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D409/06

摘要： Fibrinogen receptor antagonists of formulae (I) and (II) are disclosed for use in inhibiting the binding of fibrinogen to blood platelets and for inhibiting the aggregation of blood platelets.

公开(公告)号：EP0946165A1

公开(公告)日：1999-10-06

申请号：EP97947280.0

申请日：1997-10-27

申请人： MERCK & CO., INC.

发明人： DUGGAN, Mark, E. ,  HARTMAN, George, D.

IPC分类号： C07D235 ,  A61K31 ,  A61K45 ,  A61P9 ,  A61P19 ,  A61P35 ,  A61P43 ,  C07D213 ,  C07D401 ,  C07D471

CPC分类号： C07D213/73 ,  A61K45/06 ,  C07D401/12 ,  C07D471/04

摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are αvβ3 antagonists, αvβ5 antagonists or dual αvβ3/αvβ5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.

公开(公告)号：EP0820445A1

公开(公告)日：1998-01-28

申请号：EP96909851.0

申请日：1996-03-25

申请人： MERCK & CO., INC.

发明人： ANTHONY, Neville, J. ,  CICCARONE, Terrence, M. ,  GOMEZ, Robert, P. ,  HUTCHINSON, John, H. ,  WILLIAMS, Theresa, M. ,  DINSMORE, Christopher, J. ,  STOKKER, Gerald, E. ,  HARTMAN, George, D.

IPC分类号： C07D233 ,  A61K31 ,  A61P1 ,  A61P3 ,  A61P13 ,  A61P15 ,  A61P27 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D241 ,  C07D295 ,  C07D401 ,  C07D403

CPC分类号： C07D233/64 ,  C07D241/08 ,  C07D295/192 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12

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.

公开(公告)号：EP0673247A1

公开(公告)日：1995-09-27

申请号：EP94904069.0

申请日：1993-11-29

申请人： MERCK & CO. INC.

发明人： EGBERTSON, Melissa, S. ,  TURCHI, Laura, M. ,  HARTMAN, George, D. ,  HALCZENKO, Wasyl ,  WHITMAN, David, B. ,  PERKINS, James, J. ,  KRAUSE, Amy, E. 570 W. Dekalb Pike ,  IHLE, Nathan ,  CLAREMON, David, Alan ,  HOFFMAN, William ,  DUGGAN, Mark, E.

IPC分类号： C07D295 ,  A61K31 ,  A61P7 ,  A61P43 ,  C07C255 ,  C07C271 ,  C07C309 ,  C07C311 ,  C07D205 ,  C07D207 ,  C07D211 ,  C07D213 ,  C07D233 ,  C07D401 ,  C07D409 ,  C07D521

CPC分类号： C07D213/30 ,  C07C311/19 ,  C07D205/04 ,  C07D211/22 ,  C07D211/26 ,  C07D211/34 ,  C07D211/46 ,  C07D211/70 ,  C07D213/71 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D249/08 ,  C07D295/084 ,  C07D295/088 ,  C07D295/096 ,  C07D295/155 ,  C07D401/12 ,  C07D409/12

摘要： Novel fibrinogen receptor antagonists of the formula: X-Y-Z-Aryl-A-B are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.

公开(公告)号：EP1492487B1

公开(公告)日：2009-11-11

申请号：EP03745083.0

申请日：2003-03-04

申请人： Merck & Co., Inc.

发明人： BRESLIN, Michael, J. ,  COLEMAN, Paul, J. ,  COX, Christopher, D. ,  CULBERSON, J., Christopher ,  HARTMAN, George, D. ,  MARIANO, Brenda, J. ,  TORRENT, Maricel

IPC分类号： C07D231/06 ,  A61K31/415 ,  A61P35/00 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D417/04

CPC分类号： C07D401/04 ,  C04B35/632 ,  C07D231/06 ,  C07D401/06 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D417/04

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.