1208129-83-2Relevant 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 INDOLE DERIVATIVES USEFUL AS HEPATITIS C VIRUS INHIBITORS
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Page/Page column 45, (2010/04/03)
Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein Y, R1, R2, R4 and n 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.
