Finger-loop inhibitors of the HCV NS5b polymerase. Part 1: Discovery and optimization of novel 1,6- and 2,6-macrocyclic indole series
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.
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)
MACROCYCLIC INDOLES AS HEPATITIS C VIRUS INHIBITORS
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.
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Page/Page column 109
(2009/07/25)
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