公开(公告)号：EP0783518A1

公开(公告)日：1997-07-16

申请号：EP95935199.0

申请日：1995-09-27

申请人： Merck & Co., Inc.

发明人： ANTHONY, Neville, J. ,  deSOLMS, S., Jane ,  GRAHAM, Samuel, L. ,  STOKKER, Gerald, E. ,  WISCOUNT, Catherine, M. ,  CICCARONE, Terence, M.

IPC分类号： A61K31 ,  A61K38 ,  A61P9 ,  A61P31 ,  A61P43 ,  C07D207 ,  C07D401 ,  C07D403 ,  C07K5

CPC分类号： C07D401/06 ,  A61K38/00 ,  C07D207/28 ,  C07D403/06 ,  C07K5/0207 ,  C07K5/06026

摘要： The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit farnesyl-protein transferase. Furthermore, these CAAX analogs differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.

公开(公告)号：EP2044068A1

公开(公告)日：2009-04-08

申请号：EP07796862.6

申请日：2007-07-13

申请人： Merck & Co., Inc.

发明人： WILLIAMS, Peter, D. ,  VENKATRAMAN, Shankar ,  LANGFORD, H. Marie ,  KIM, Boyoung ,  BOOTH, Theresa, M. ,  GROBLER, Jay, A. ,  STAAS, Donnette ,  RUZEK, Rowena, D. ,  EMBREY, Mark, W. ,  WISCOUNT, Catherine, M. ,  LYLE, Terry, A.

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, 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 anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and 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：EP0639184A1

公开(公告)日：1995-02-22

申请号：EP93910860.0

申请日：1993-04-28

申请人： MERCK & CO. INC.

发明人： LYLE, Terry, A. ,  TUCKER, Thomas, J. ,  WISCOUNT, Catherine, M.

IPC分类号： C07D471 ,  A61K31 ,  A61P31 ,  C07D239 ,  C07D401 ,  C07D403 ,  C07D405

CPC分类号： C07D401/06 ,  C07D239/80 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12

摘要： Compounds having a quinazolin-2-one nucleus with a substituted alkynyl or substituted alkenyl at the 4-position are described. These compounds are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), 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.