公开(公告)号：EP1196384A1

公开(公告)日：2002-04-17

申请号：EP00944756.6

申请日：2000-06-21

申请人： Merck & Co., Inc. ,  TULARIK, INC.

发明人： PAYNE, Linda, S. ,  TRAN, Lekhanh, O. ,  ZHUANG, Linghang, H. ,  YOUNG, Steven, D. ,  EGBERTSON, Melissa, S. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  FISHER, Thorsten, E. ,  GUARE, James, P. ,  LANGFORD, H., Marie ,  MELAMED, Jeffrey, Y. ,  CLARK, David, L.

IPC分类号： C07D213/30 ,  C07D233/64 ,  C07D241/14 ,  C07D249/12 ,  C07D257/04 ,  C07D277/24 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/4402 ,  A61K31/4427 ,  A61K31/4436 ,  A61K31/4965 ,  A61K31/497

CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/61 ,  C07D213/643 ,  C07D213/65 ,  C07D213/68 ,  C07D213/74 ,  C07D231/12 ,  C07D233/56 ,  C07D233/64 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D277/24 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D409/06 ,  C07D409/10 ,  C07D417/06 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D473/00 ,  C07D473/04 ,  C07D473/08

摘要： Certain 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones 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, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

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：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：EP1725102A1

公开(公告)日：2006-11-29

申请号：EP05724457.6

申请日：2005-03-04

申请人： Merck & Co., Inc.

发明人： WILLIAMS, Peter, D. ,  WAI, John, S. ,  EMBREY, Mark, W. ,  STAAS, Donnette, D. ,  ZHUANG, Linghang ,  LANGFORD, H., Marie

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/54 ,  A61K31/50 ,  A61K31/535 ,  C07D279/00 ,  C07D285/00 ,  C07D295/00 ,  C07D417/00 ,  C07D413/00

CPC分类号： C07D487/04 ,  A61K31/495 ,  A61K31/50 ,  A61K31/535 ,  A61K31/54 ,  A61K45/06 ,  A61K2300/00

摘要： Bicyclic uracils and related compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the compounds are of Formula (I) wherein a, b, Y, R1, R2, R3 and R4 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.