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公开(公告)号：EP0891355A1
公开(公告)日：1999-01-20
申请号：EP97917780.0
申请日：1997-04-01
申请人： MERCK & CO., INC.
IPC分类号： A61K31 , A61P1 , A61P9 , A61P13 , A61P27 , A61P31 , A61P35 , A61P43 , C07D233 , C07D401 , C07D403 , C07D413 , C07D417
CPC分类号： C07D233/56 , C07D233/64 , C07D233/70 , C07D401/10 , C07D403/10 , C07D403/14 , C07D413/06 , C07D417/06 , C07D417/14
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：EP0833633A1
公开(公告)日：1998-04-08
申请号：EP96919068.0
申请日：1996-06-03
申请人： MERCK & CO., INC.
发明人： ANTHONY, Neville, J. , SOLINSKY, Kelly, M. , GOMEZ, Robert, P. , WILLIAMS, Theresa, M. , BERGMAN, Jeffrey, M. , DeSOLMS, S., Jane , DINSMORE, Christopher, J. , MacTOUGH, Suzanne, C.
CPC分类号： C07D233/64 , C07D401/14
摘要： The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
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13.发明公开AZA- AND POLYAZA-NAPHTHALENYL-CARBOXAMIDES USEFUL AS HIV INTEGRASE INHIBITORS 有权氮杂和多氮NAPHTHALENYLCARBONSÄUREAMIDEAS HIV整合酶抑制剂
公开(公告)号：EP1326611A1
公开(公告)日：2003-07-16
申请号：EP01983939.8
申请日：2001-10-09
申请人： Merck & Co., Inc.
发明人： ANTHONY, Neville, J. , GOMEZ, Robert, P. , BENNETT, Jennifer, J. , YOUNG, Steven, D. , EGBERTSON, Melissa , WAI, John, S.
IPC分类号： A61K31/47 , A61K31/44 , A61K31/495 , A61K31/50 , A61K31/54 , A61P31/18 , C07D417/00 , C07D237/30 , C07D471/02 , C07D215/38
CPC分类号： C07D471/04 , A61K31/44 , A61K31/47 , A61K31/495 , A61K31/50 , A61K31/54 , A61K45/06 , C07D401/12
摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.
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公开(公告)号：EP0951285A1
公开(公告)日：1999-10-27
申请号：EP97953451.0
申请日：1997-12-22
申请人： MERCK & CO., INC.
发明人： YOUNG, Steven, D. , ANTHONY, Neville, J. , GRAHAM, Samuel, L. , TRAN, Lekhanh, O. , BELL, Ian, M. , deSOLMS, S., Jane , GOMEZ, Robert, P. , KUO, Michelle, Sparks , LUMMA, William, C., Jr. , PERLOW, Debra, S. , SHAW, Anthony, W. , WAI, John, S.
IPC分类号： A61K31 , A61P9 , A61P13 , A61P27 , A61P31 , A61P35 , A61P43 , C07D401 , C07D403 , C07D405 , C07D417 , C07D471
CPC分类号： C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D405/14 , C07D417/14 , C07D471/04
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：EP0944388A2
公开(公告)日：1999-09-29
申请号：EP97921256.0
申请日：1997-03-27
申请人： MERCK & CO., INC.
发明人： ANTHONY, Neville, J. , DINSMORE, Christopher , GOMEZ, Robert, P. , HUTCHINSON, John, H. , WAI, John, S. , WILLIAMS, Theresa, M. , BELL, Ian, M. , EMBREY, Mark, W. , FISHER, Thorsten, E.
CPC分类号： C07D401/06 , C07D211/62 , C07D401/12 , C07D401/14 , C07D413/14
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：EP0891333A1
公开(公告)日：1999-01-20
申请号：EP97920031.0
申请日：1997-04-01
申请人： MERCK & CO., INC.
发明人： ANTHONY, Neville, J. , STOKKER, Gerald, E. , GOMEZ, Robert, P. , SOLINSKY, Kelly, M. , WAI, John, S. , WILLIAMS, Theresa, M. , YOUNG, Steven, D. , HUTCHINSON, John, H. , HALCZENKO, Wasyl
CPC分类号： C07D233/56 , C07D213/57 , C07D233/64 , C07D233/70 , C07D401/14 , C07D403/10 , C07D403/14 , C07D409/10 , C07D409/14 , C07D413/06 , C07D417/06 , C07D417/14
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：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.
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