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：EP0696277A1

公开(公告)日：1996-02-14

申请号：EP94915427.0

申请日：1994-04-26

申请人： MERCK & CO. INC.

发明人： VACCA, Joseph, P. ,  DORSEY, Bruce, D. ,  GUARE, James, P. ,  HOLLOWAY, M., Katharine ,  HUNGATE, Randall, W. ,  LEVIN, Rhonda, B.

IPC分类号： A61K31 ,  A61K45 ,  A61P31 ,  A61P37 ,  C07C237 ,  C07D207 ,  C07D211 ,  C07D217 ,  C07D241 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D417

CPC分类号： C07D401/06 ,  A61K31/70 ,  A61K45/06 ,  C07C237/20 ,  C07C2602/08 ,  C07D207/16 ,  C07D211/60 ,  C07D217/26 ,  C07D241/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K2300/00

摘要： Compounds of formula (I), where R?1 and R2¿ are independently hydrogen or optionally-substituted C¿1-4?alkyl or aryl, and R?1¿ also forms a heterocycle or heterocycle-C¿1-4?alkyl, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in 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.

摘要翻译： 其中R 1和R 2独立地为氢或任选取代的C 1-4烷基或芳基，或R 1和R 2连接在一起形成单环或双环环系的式“IMAGE”的化合物是HIV蛋白酶抑制剂。 这些化合物可用于治疗艾滋病毒和艾滋病感染，作为化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和治疗HIV感染的方法。

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：EP1333831A2

公开(公告)日：2003-08-13

申请号：EP01990637.9

申请日：2001-10-09

申请人： Merck & Co., Inc.

发明人： ZHUANG, Linghang ,  WAI, John, S. ,  PAYNE, Linda, S. ,  YOUNG, Steven, D. ,  FISHER, Thorsten, E. ,  EMBREY, Mark ,  GUARE, James, P.

IPC分类号： A61K31/47 ,  A61K31/495 ,  C07D215/26 ,  C07D471/04

CPC分类号： C07D215/04 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D471/04

摘要： Certain aza- and polyaza-naphthalenyl ketones including certain quinolinyl and naphthyridinyl ketones 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 or the delay in the onset 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 treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described.

摘要翻译： 包括某些喹啉基和萘啶酮酮的某些氮杂 - 和多氮 - 萘基酮被描述为HIV整合酶抑制剂和HIV复制抑制剂。 这些化合物可用作预防或治疗HIV感染和治疗或延迟AIDS的发作，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，任选地与其它抗病毒剂，免疫调节剂，抗生素或 疫苗。 还描述了治疗或延缓AIDS发作的方法以及预防或治疗HIV感染的方法。