公开(公告)号：EP1326610B1

公开(公告)日：2006-11-15

申请号：EP01994068.3

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.

IPC分类号： A61K31/44 ,  A61K31/495 ,  A61K31/50 ,  A61K31/52 ,  A61K31/53 ,  A61K31/519 ,  A61K31/517 ,  A61K31/47 ,  A61P31/18 ,  C07D215/12 ,  C07D215/16

CPC分类号： C07D471/04

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.

公开(公告)号：EP1326611B1

公开(公告)日：2007-06-13

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： A61K31/4709 ,  A61K31/4375 ,  C07D471/04 ,  C07D403/12 ,  A61P31/18

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.

公开(公告)号：EP1326610A2

公开(公告)日：2003-07-16

申请号：EP01994068.3

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.

IPC分类号： A61K31/44 ,  A61K31/495 ,  A61K31/50 ,  A61K31/52 ,  A61K31/53 ,  A61K31/519 ,  A61K31/517 ,  A61K31/47 ,  A61P31/18 ,  C07D215/12 ,  C07D215/16

CPC分类号： C07D471/04

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.

摘要翻译： 包括某些喹啉甲酰胺和萘啶甲酰胺衍生物的氮杂 - 和多氮 - 萘基甲酰胺衍生物被描述为HIV整合酶抑制剂和HIV复制抑制剂。 这些化合物可用于预防或治疗HIV感染和治疗AIDS，作为化合物或药学上可接受的盐，或作为药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合。 还描述了预防，治疗或延迟AIDS发作的方法以及预防或治疗HIV感染的方法。

公开(公告)号：EP1326865B1

公开(公告)日：2009-05-06

申请号：EP01979582.2

申请日：2001-10-09

申请人： Merck & Co., Inc.

发明人： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  YOUNG, Steven, D. ,  EGBERTSON, Melissa ,  WAI, John, S. ,  ZHUANG, Linghang ,  EMBREY, Mark ,  TRAN, Lekhanh ,  MELAMED, Jeffrey, Y. ,  LANGFORD, H., Marie ,  GUARE, James, P. ,  FISHER, Thorsten, E. ,  JOLLY, Samson, M. ,  KUO, Michelle, S. ,  PERLOW, Debra, S. ,  BENNETT, Jennifer, J. ,  FUNK, Timothy, W.

IPC分类号： C07D471/04 ,  A61K31/47 ,  A61K31/4375 ,  A61P31/18 ,  C07D519/00 ,  C07D215/48 ,  C07D471/16

CPC分类号： C07D471/04

摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and 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.

公开(公告)号：EP1003374A1

公开(公告)日：2000-05-31

申请号：EP97954798.1

申请日：1997-12-22

申请人： MERCK & CO., INC.

发明人： YOUNG, Steven, D. ,  ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  TRAN, Lekhanh, O.

IPC分类号： A01N43/40 ,  A01N43/54 ,  A01N43/58 ,  C07D401/00 ,  C07D401/06 ,  C07D401/14 ,  A61K31/44

CPC分类号： C07D401/06 ,  C07D401/14

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.

公开(公告)号：EP0891343A1

公开(公告)日：1999-01-20

申请号：EP97920032.0

申请日：1997-04-01

申请人： MERCK & CO., INC.

发明人： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  SOLINSKY, Kelly, M.

IPC分类号： A61K31 ,  A61P9 ,  A61P13 ,  A61P27 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D233 ,  C07D401 ,  C07D403 ,  C07D409 ,  C07D413 ,  C07D417

CPC分类号： C07D233/56 ,  C07D233/64 ,  C07D233/70 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D409/10 ,  C07D409/14 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  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.

公开(公告)号：EP0891339A1

公开(公告)日：1999-01-20

申请号：EP97917830.0

申请日：1997-04-01

申请人： MERCK & CO., INC.

发明人： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  YOUNG, Steven, D.

IPC分类号： C07D261 ,  A61K31 ,  A61P31 ,  A61P35 ,  C07D233 ,  C07D403 ,  C07D413 ,  C07D417

CPC分类号： C07D233/56 ,  C07D233/64 ,  C07D233/70 ,  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.

公开(公告)号：EP0783517A2

公开(公告)日：1997-07-16

申请号：EP95935104.0

申请日：1995-09-26

申请人： Merck & Co., Inc.

发明人： ANTHONY, Neville, J. ,  DESOLMS, S., Jane ,  GOMEZ, Robert, P. ,  GRAHAM, Samuel, L. ,  HUTCHINSON, John, H. ,  STOKKER, Gerald, E.

IPC分类号： C07D233 ,  A61K31 ,  A61K38 ,  A61P35 ,  A61P43 ,  C07K5

CPC分类号： C07D233/64 ,  A61K38/00 ,  C07K5/0205 ,  C07K5/06026

摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogs differ from those previously described as inhibitors of Ras farnesyl 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.

公开(公告)号：EP1326865A2

公开(公告)日：2003-07-16

申请号：EP01979582.2

申请日：2001-10-09

申请人： Merck & Co., Inc.

发明人： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  YOUNG, Steven, D. ,  EGBERTSON, Melissa ,  WAI, John, S. ,  ZHUANG, Linghang ,  EMBREY, Mark ,  TRAN, Lekhanh ,  MELAMED, Jeffrey, Y. ,  LANGFORD, H., Marie ,  GUARE, James, P. ,  FISHER, Thorsten, E. ,  JOLLY, Samson, M. ,  KUO, Michelle, S. ,  PERLOW, Debra, S. ,  BENNETT, Jennifer, J. ,  FUNK, Timothy, W.

IPC分类号： C07D471/04 ,  A61K31/47 ,  A61K31/4375 ,  A61P31/18 ,  C07D519/00 ,  C07D215/48 ,  C07D471/16

CPC分类号： C07D471/04

摘要： Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and 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.

公开(公告)号：EP0891361A1

公开(公告)日：1999-01-20

申请号：EP97920000.0

申请日：1997-04-01

申请人： MERCK & CO., INC.

发明人： ANTHONY, Neville, J. ,  GOMEZ, Robert, P. ,  GRAHAM, Samuel, L.

IPC分类号： A61K31 ,  A61P9 ,  A61P13 ,  A61P27 ,  A61P31 ,  A61P35 ,  A61P43 ,  C07D233 ,  C07D401 ,  C07D403 ,  C07D413 ,  C07D417

CPC分类号： C07D233/56 ,  C07D233/64 ,  C07D233/70 ,  C07D401/06 ,  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.