公开(公告)号：EP0949926A1

公开(公告)日：1999-10-20

申请号：EP97911906.0

申请日：1997-10-27

申请人： MERCK & CO., INC.

发明人： BELL, Ian, M. ,  GUARE, James, P., Jr. ,  HAZUDA, Daria, Jean ,  MUNSON, Peter, M. ,  THOMPSON, Wayne, J. ,  VACCA, Joseph, P.

IPC分类号： A61K31 ,  C07D243 ,  C07D403

CPC分类号： C07D403/12 ,  A61K31/5513 ,  C07D243/20

摘要： Compounds having a benzodiazepine hydrazide core are described. These compounds are useful in the inhibition of HIV integrase, 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.

摘要翻译： 描述了具有苯并二氮杂肼核心的化合物。 这些化合物可用作抑制HIV整合酶，预防或治疗HIV感染和治疗AIDS，作为化合物，药学上可接受的盐，药物组合物成分，不论是否与其他抗病毒剂，免疫调节剂，抗生素或 疫苗。 还描述了治疗AIDS的方法和预防或治疗HIV感染的方法。

公开(公告)号：EP1083897A1

公开(公告)日：2001-03-21

申请号：EP99926096.1

申请日：1999-06-01

申请人： MERCK & CO., INC. ,  Tularik Inc.

发明人： SELNICK, Harold, G. ,  HAZUDA, Daria, Jean ,  EGBERTSON, Melissa ,  GUARE, James, P., Jr. ,  WAI, John, S. ,  YOUNG, Steven, D. ,  CLARK, David, L. ,  MEDINA, Julio, C.

IPC分类号： A61K31/40 ,  A61K31/415 ,  A61K31/445 ,  C07D207/30 ,  C07D207/333 ,  C07D209/04 ,  C07D209/12 ,  C07D211/18 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/40 ,  C07D231/10 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D401/04

CPC分类号： C07D207/333 ,  A61K31/40 ,  A61K45/06 ,  C07D207/34 ,  C07D209/12 ,  C07D231/12 ,  C07D401/04 ,  A61K2300/00

摘要： Nitrogen-containing heteroaryl 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：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.