- 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)
-
- Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
-
The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
- -
-
Page/Page column 54
(2010/09/05)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 6; 29-30
(2009/05/28)
-
- CYCLOPROPYL FUSED INDOLOBENZAZEPINE HCV NS5B INHIBITORS
-
The invention encompasses compounds of formula (I) as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV
- -
-
Page/Page column 58
(2009/06/27)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 5; 32
(2009/05/28)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 30
(2008/12/07)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 21
(2008/12/06)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 20-21
(2008/12/07)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 39
(2008/12/07)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 36
(2008/12/07)
-
- Compounds for the Treatment of Hepatitis C
-
The invention encompasses compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 71
(2008/12/07)
-
- Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 22-23
(2008/06/13)
-
- Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 46
(2008/06/13)
-
- Cyclopropyl Fused Indolobenzazepine HCV NS5B Inhibitors
-
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
- -
-
Page/Page column 28
(2008/06/13)
-
- INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
-
The present invention relates to indole compounds of the formula (I): wherein R1, R2, R3, R4, A, E and X are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
- -
-
Page/Page column 37-38
(2010/10/20)
-
- TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
-
The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, A, Ar, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.
- -
-
Page/Page column 29
(2010/11/08)
-