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：EP0986554A1

公开(公告)日：2000-03-22

申请号：EP98923741.7

申请日：1998-05-26

申请人： Merck & Co., Inc. (a New Jersey corp.)

发明人： ASKIN, David ,  HOERRNER, R., Scott ,  PURICK, Robert, M. ,  REIDER, Paul ,  VARSOLONA, Richard, J. ,  VOLANTE, Ralph, P.

IPC分类号： C07D405/06 ,  A61K31/495 ,  A61K31/34

CPC分类号： C07D405/06

摘要： This invention relates to a sulfate salt of an HIV protease inhibitor, Compound (A), which is useful in the treatment of AIDS, ARC or HIV infection in adults and children. More specifically, the invention provides a sulfate salt of the HIV protease inhibitor, Compound (A) having substantially improved solibility in dilute HC1 (gastric acid) solution which results in much greater oral absorption and bioavailability in animal models. Processes for making the sulfate salt of the particular HIV protease inhibitor compounds are also disclosed.

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。

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。