848485-50-7Relevant academic research and scientific papers
Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series
McGowan, David,Vendeville, Sandrine,Lin, Tse-I,Tahri, Abdellah,Hu, Lili,Cummings, Maxwell D.,Amssoms, Katie,Berke, Jan Martin,Canard, Maxime,Cleiren, Erna,Dehertogh, Pascale,Last, Stefaan,Fransen, Els,Van Der Helm, Elisabeth,Van Den Steen, Iris,Vijgen, Leen,Rouan, Marie-Claude,Fanning, Gregory,Nyanguile, Origène,Van Emelen, Kristof,Simmen, Kenneth,Raboisson, Pierre
scheme or table, p. 4431 - 4436 (2012/09/07)
Novel conformationaly constrained 1,6- and 2,6-macrocyclic HCV NS5b polymerase inhibitors, in which either the nitrogen or the phenyl ring in the C2 position of the central indole core is tethered to an acylsulfamide acid bioisostere, have been designed and tested for their anti-HCV potency. This transformational route toward non-zwitterionic finger loop-directed inhibitors led to the discovery of derivatives with improved cell potency and pharmacokinetic profile.
MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS
-
Page/Page column 100-101, (2009/07/25)
The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, formula (I), wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
Development of carboxylic acid replacements in indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase
Stansfield, Ian,Pompei, Marco,Conte, Immacolata,Ercolani, Caterina,Migliaccio, Giovanni,Jairaj, Mark,Giuliano, Claudio,Rowley, Michael,Narjes, Frank
, p. 5143 - 5149 (2008/02/12)
Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here 2 series of indole-N-acetamides, bearing
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase
Harper, Steven,Pacini, Barbara,Avolio, Salvatore,Di Filippo, Marcello,Migliaccio, Giovanni,Laufer, Ralph,De Francesco, Raffaele,Rowley, Michael,Narjes, Frank
, p. 1314 - 1317 (2007/10/03)
Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here a novel class of allosteric inhibitor of NS5B that shows potent affinity for the NS5B enzyme and effective inhibition of subgenomic HCV RNA replication in HUH-7 cells. Inhibitors from this class have promising characteristics for further development as anti-HCV agents.
INDOLES AND AZAINDOLES AS ANTIVIRAL AGENTS
-
Page/Page column 22, (2010/02/11)
The present invention relates to indoles and azaindoles of formula (I): wherein X1, X2, X3, X4, A1, Ar1, Ar, n, p and q are as defined herein and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.
