公开(公告)号：EP1896619A2

公开(公告)日：2008-03-12

申请号：EP06785052.9

申请日：2006-06-16

申请人： Merck & Co., Inc. ,  ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGELETTI S.P.A. ,  Rosetta Inpharmatics LLC.

发明人： ESPESETH, Amy, S. ,  HAZUDA, Daria ,  GATES, Adam, T. ,  MIGLIACCIO, Giovanni ,  DE FRANCESCO, Raffaele ,  LINSLEY, Peter

IPC分类号： C12Q1/70

CPC分类号： C12N15/111 ,  C12N2310/14 ,  C12N2320/12 ,  C12N2330/31 ,  C12Q1/70 ,  C12Q1/707

摘要： Liver expressed proteins involved in HCV replication were identified using a procedure measuring the effect of inhibiting expression of host cell proteins on HCV replicon activity. The identified proteins and encoding nucleic acid provide targets for inhibiting HCV replication and for evaluating the ability of compounds to inhibit HCV replication. Compounds inhibiting HCV replication include compounds targeting identified proteins and compounds targeting nucleic acid encoding the identified protein. Several of the host genes identified as targets for inhibiting HCV replication were also found to be a target for inhibiting HIV replication. The ability to serve as a target for inhibiting both HIV and HCV replication indicates that such an identified gene and encoded protein may be a useful target for inhibiting replication of different types of viruses and not limited to inhibiting replication of a particular virus.

公开(公告)号：EP1732906A1

公开(公告)日：2006-12-20

申请号：EP05733551.5

申请日：2005-03-25

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  ESPESETH, Amy, S. ,  STACHEL, Shawn, J. ,  OLSEN, David, B. ,  HAZUDA, Daria, J. ,  HOLLOWAY, M. Katharine

IPC分类号： C07D277/60

CPC分类号： C07D417/14 ,  C07D277/40 ,  C07D277/60 ,  C07D277/82 ,  C07D277/84 ,  C07D417/04 ,  C07D417/06 ,  C07D417/08

摘要： The present invention is directed to 2-aminothiazole compounds which are aspartyl protease inhibitors, and are inhibitors of both the beta-secretase enzyme and HIV protease, and that are useful in the treatment of diseases in which the beta-secretase enzyme and HIV are involved, such as Alzheimer's disease, HIV Infection and AIDS. 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 and HIV protease are involved.

公开(公告)号：EP1578356A2

公开(公告)日：2005-09-28

申请号：EP03743199.6

申请日：2003-02-23

申请人： Merck & Co., Inc.

发明人： ESPESETH, Amy, S. ,  FERRER, Marc ,  FLORES, Osvaldo, A. ,  HAZUDA, Daria, J. ,  INGLESE, James ,  MILLER, Michael, D. ,  REGISTER, Bruce ,  SHI, Xiao-Ping ,  SIMON, Adam, J. ,  ZUCK, Paul, D.

IPC分类号： A61K6/00

CPC分类号： C07K14/47 ,  C07K14/4702 ,  C07K14/4711 ,  C07K2319/00 ,  C07K2319/50 ,  G01N2500/10

摘要： The present invention provides DNA constructs, genetically engineered host cells, and methods for identifying inhibitors of amyloid precursor protein (APP) processing. The methods provide for the convenient identification, in a single assay, of inhibitors of β-secretase and Ϝ-secretase as well as other forms of APP processing. The methods rely on fusion proteins of APP and transcription factors in which APP processing releases the transcription factors, allowing the transcription factors to activate transcription of a reporter gene. Inhibitors are identified as substances that block or diminish transcription factor release from the fusion protein, thereby causing a diminution of reporter gene readout.

公开(公告)号：EP1743170A2

公开(公告)日：2007-01-17

申请号：EP05732580.5

申请日：2005-03-29

申请人： Merck & Co., Inc.

发明人： COBURN, Craig, A. ,  ESPESETH, Amy, S. ,  HAZUDA, Daria, J.

IPC分类号： G01N33/50

CPC分类号： G01N33/6896 ,  C07D307/79 ,  C07D405/12 ,  G01N2333/4709 ,  G01N2500/00

摘要： Disclosed are methods for identifying and evaluating the binding properties of substances to the amyoid precursor protein (APP) or to β-amyloid (Aβ) fragments of APP. Also disclosed is a class of benzofuran derivatives of formula (I), which interact specifically with APP or Aβ, and block interaction of APP or Aβ with secreatase or APP or Aβ binding antibodies.