公开(公告)号：EP1242426B1

公开(公告)日：2007-10-31

申请号：EP00980679.5

申请日：2000-11-21

申请人： Merck & Co., Inc.

发明人： TATA, James, R. ,  CHAPMAN, Kevin, T. ,  DUFFY, Joseph, Leslie ,  KEVIN, Nancy, J. ,  CHENG, Yuan ,  RANO, Thomas, A. ,  ZHANG, Fengqi ,  HUENING, Tracy ,  KIRK, Brian, Anthony ,  LU, Zhijian ,  RAGHAVAN, Subharekha ,  FLEITZ, Fred, J. ,  PETRILLO, Daniel, E. ,  ARMSTRONG, Joseph, D., III ,  VARSOLONA, Richard, J. ,  ASKIN, David ,  HOERRNER, R., Scott ,  PURICK, Robert

IPC分类号： C07D491/048 ,  C07D405/14 ,  C07D405/06 ,  C07D401/06 ,  C07D495/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/495 ,  A61P31/18

CPC分类号： C07D401/06 ,  A61K31/00 ,  A61K45/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

摘要： η-(Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease 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. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

公开(公告)号：EP1242426A1

公开(公告)日：2002-09-25

申请号：EP00980679.5

申请日：2000-11-21

申请人： Merck & Co., Inc.

发明人： TATA, James, R. ,  CHAPMAN, Kevin, T. ,  DUFFY, Joseph, Leslie ,  KEVIN, Nancy, J. ,  CHENG, Yuan ,  RANO, Thomas, A. ,  ZHANG, Fengqi ,  HUENING, Tracy ,  KIRK, Brian, Anthony ,  LU, Zhijian ,  RAGHAVAN, Subharekha ,  FLEITZ, Fred, J. ,  PETRILLO, Daniel, E. ,  ARMSTRONG, Joseph, D., III ,  VARSOLONA, Richard, J. ,  ASKIN, David ,  HOERRNER, R., Scott ,  PURICK, Robert

IPC分类号： C07D491/048 ,  C07D405/14 ,  C07D405/06 ,  C07D401/06 ,  C07D495/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  A61K31/495 ,  A61P31/18

CPC分类号： C07D401/06 ,  A61K31/00 ,  A61K45/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

摘要： η-(Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease 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. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

摘要翻译： η-（羟基-2-（氟烷基氨基羰基）-1-哌嗪戊酰胺化合物是HIV蛋白酶抑制剂和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，或者作为化合物，药物 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，抗生素或疫苗组合，还描述了治疗AIDS的方法以及预防或治疗HIV感染的方法，这些化合物对抗HIV病毒突变体 目前用于治疗艾滋病和HIV感染的HIV蛋白酶抑制剂。