公开(公告)号：EP1725556A1

公开(公告)日：2006-11-29

申请号：EP05725120.9

申请日：2005-03-09

申请人： Merck & Co., Inc.

发明人： HAN, Wei ,  EGBERTSON, Melissa ,  WAI, John, S. ,  ZHUANG, Linghang ,  RUZEK, Rowena, D. ,  PERLOW, Debra, S. ,  ISAACS, Richard, C., A. ,  CAMERON, Mark ,  FOSTER, Bruce, S. ,  DOLLING, Ulf, H. ,  HOERRNER, R., Scott ,  OBLIGADO, Vanessa, E. ,  NEILSON, Lou, Anne ,  KIM, Boyoung ,  PAYNE, Linda, S. ,  MORRISSETTE, Matthew, M. ,  WILLIAMS, Peter, D. ,  PYE, Philip, J. ,  ANGELAUD, Remy ,  ASKIN, David

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P31/12 ,  A61P37/02

CPC分类号： C07D471/04

摘要： Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1, R2, R3, R4 and R5 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.

摘要翻译： 式I的羟基（四或六）氢化萘啶二酮化合物是HIV整合酶抑制剂和HIV复制抑制剂：（I）其中a，R1，R2，R3，R4和R5如本文所定义。 这些化合物可用于预防和治疗HIV感染以及预防，延缓艾滋病的发作和治疗。 这些化合物本身作为化合物或以药学上可接受的盐的形式用于抗HIV感染和AIDS。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

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.

公开(公告)号：EP1677599A1

公开(公告)日：2006-07-12

申请号：EP04795564.6

申请日：2004-10-18

申请人： Merck & Co., Inc.

发明人： WAI, John, S. ,  FISHER, Thorsten, E. ,  ZHUANG, Linghang ,  STAAS, Donnette, D. ,  LYLE, Terry, A. ,  KIM, Boyoung ,  EMBREY, Mark, W. ,  WISCOUNT, Catherine, M. ,  TRAN, Lekhanh, O. ,  EGBERTSON, Melissa ,  SAVAGE, Kelly, L.

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50 ,  C07D239/00 ,  C07D471/00 ,  C07D487/00 ,  C07D491/00

CPC分类号： C07D471/14

摘要： Hydroxy-substituted pyridopyrrolopyrazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I): (I) wherein a, b, A, B, R1, R2, R3, R4, R5, R6, R7 and R8 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.

公开(公告)号：EP1082121A1

公开(公告)日：2001-03-14

申请号：EP99926094.6

申请日：1999-06-01

申请人： MERCK & CO., INC. ,  TULARIK, INC.

发明人： YOUNG, Steven, D. ,  EGBERTSON, Melissa ,  PAYNE, Linda, S. ,  WAI, John, S. ,  FISHER, Thorsten, E. ,  GUARE, James, P., Jr. ,  EMBREY, Mark, W. ,  TRAN, Lee ,  ZHUANG, Linghang ,  VACCA, Joseph, P. ,  LANGFORD, Marie ,  MELAMED, Jeffrey ,  CLARK, David, L. ,  MEDINA, Julio, C. ,  JAEN, Juan

IPC分类号： A61K31/535

CPC分类号： C07D213/64 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C69/738 ,  C07C217/60 ,  C07C229/34 ,  C07C229/42 ,  C07C233/63 ,  C07C235/60 ,  C07C255/41 ,  C07C271/16 ,  C07C271/28 ,  C07C323/62 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/12 ,  C07D241/12 ,  C07D253/08 ,  C07D263/58 ,  C07D295/088 ,  C07D295/155 ,  C07D295/192 ,  C07D333/22

摘要： Certain six-membered aromatic and heteroaromatic-dioxo-butyric acid 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, 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：EP1496836A2

公开(公告)日：2005-01-19

申请号：EP03716466.2

申请日：2003-03-12

申请人： Merck & Co., Inc.

发明人： EGBERTSON, Melissa ,  LANGFORD, H. Marie ,  MELAMED, Jeffrey, Y. ,  WAI, John, S. ,  HAN, Wei ,  PERLOW, Debbie, S. ,  ZHUANG, Linghang ,  EMBREY, Mark

IPC分类号： A61K6/00

CPC分类号： C07D471/04

摘要： N-(Substituted benzyl)-8-hydroxy- 1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1', R2' and R3' 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.

公开(公告)号：EP1549315A2

公开(公告)日：2005-07-06

申请号：EP03749574.4

申请日：2003-09-10

申请人： Merck & Co., Inc.

发明人： WAI, John, S. ,  KIM, Boyoung ,  FISHER, Thorsten, E. ,  ZHUANG, Linghang ,  WILLIAMS, Peter, D. ,  LYLE, Terry, A. ,  LANGFORD, H. Marie ,  ROBINSON, Kyle, A.

IPC分类号： A61K31/4985 ,  A61K31/5377 ,  A61K31/541 ,  C07D487/04 ,  C07D487/14

CPC分类号： C07D471/14 ,  C07D471/04

摘要： 8,9-Dihydroxydihydropyridopyrazine-1,6-diones and 8,9-dihydroxypyridopyrazine-1,6-diones are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the pyridopyrazinediones are of Formula (I): (I),wherein R1, R2, R3, R4 and R5 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are 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：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：EP1496836B1

公开(公告)日：2008-09-24

申请号：EP03716466.2

申请日：2003-03-12

申请人： Merck & Co., Inc.

发明人： EGBERTSON, Melissa ,  LANGFORD, H. Marie ,  MELAMED, Jeffrey, Y. ,  WAI, John, S. ,  HAN, Wei ,  PERLOW, Debbie, S. ,  ZHUANG, Linghang ,  EMBREY, Mark

IPC分类号： C07D471/04 ,  A61K31/4375 ,  A61P31/18

CPC分类号： C07D471/04

摘要： N-(Substituted benzyl)-8-hydroxy- 1,6-naphthyridine-7-carboxamides are inhibitors of HIV integrase and inhibitors of HIV replication. The naphthyridine carboxamides are of Formula (I): wherein R1', R2' and R3' 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. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are 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。