公开(公告)号：EP1756114B1

公开(公告)日：2014-11-19

申请号：EP05743968.9

申请日：2005-05-03

申请人： Merck Sharp & Dohme Corp.

发明人： WAI, John, S. ,  VACCA, Joseph, P. ,  ZHUANG, Linghang ,  KIM, Boyoung ,  LYLE, Terry, A. ,  WISCOUNT, Catherine, M. ,  EGBERTSON, Melissa, S. ,  NEILSON, Lou Anne ,  EMBREY, Mark ,  FISHER, Thorsten, E. ,  STAAS, Donnette, D.

IPC分类号： C07D487/14 ,  A61K31/5025 ,  A61K31/4985

CPC分类号： A61K31/5025 ,  C07D487/14 ,  Y02A50/414

摘要： Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 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：EP1804794B1

公开(公告)日：2013-07-31

申请号：EP05812233.4

申请日：2005-10-12

申请人： Merck Sharp & Dohme Corp. ,  Sunesis Pharmaceuticals, Inc.

发明人： BARROW, James, C. ,  COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  MCGAUGHEY, Georgia, B. ,  MCWHERTER, Melody, A. ,  NEILSON, Lou, Anne ,  SELNICK, Harold, G. ,  STAUFFER, Shaun, R. ,  YANG, Zhi-Qiang ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce ,  RITTLE, Kenneth, E.

IPC分类号： A61K31/438 ,  C07D401/04

CPC分类号： C07D471/10

公开(公告)号：EP1910364B1

公开(公告)日：2012-03-21

申请号：EP06787495.8

申请日：2006-07-14

申请人： Merck Sharp & Dohme Corp. ,  Sunesis Pharmaceuticals, Inc.

发明人： COBURN, Craig, A. ,  EGBERTSON, Melissa, S. ,  GRAHAM, Samuel, L. ,  MCGAUGHEY, Georgia, B. ,  STAUFFER, Shaun, R. ,  RAJAPAKSE, Hemaka, A. ,  NANTERMET, Philippe, G. ,  STACHEL, Shawn, R. ,  YANG, Wenjin ,  LU, Wanli ,  FAHR, Bruce

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P25/28

CPC分类号： C07D471/10

摘要： The present invention is directed to spiropiperidine compounds of formula (I) and tautomers thereof, which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.