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2' -fluoro substituted CARBA-nucleoside analogs for antiviral treatment

A C2-C8, C4-C8 technology, applied in the field of 2'-fluoro CARBA-nucleoside analogs for antiviral therapy, can solve problems such as unpublished

Inactive Publication Date: 2012-07-18
GILEAD SCI INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these compounds have not been disclosed to be useful in the treatment of HCV

Method used

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  • 2' -fluoro substituted CARBA-nucleoside analogs for antiviral treatment
  • 2' -fluoro substituted CARBA-nucleoside analogs for antiviral treatment
  • 2' -fluoro substituted CARBA-nucleoside analogs for antiviral treatment

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Experimental program
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Effect test

Embodiment

[0483] In describing experimental details, certain abbreviations and acronyms are used. Although most of them will be understood by those skilled in the art, Table 1 contains a listing of many such abbreviations and acronyms.

[0484] Table 1. List of abbreviations and acronyms

[0485]

[0486]

[0487]

[0488]

[0489] Compound preparation

[0490] Compound 1

[0491]

[0492] BuLi (1.6M in hexane, 1.61 mL, 2.41 mmol) was added dropwise to 7-bromo-2,4-bis-methylsulfanyl-imidazo[2,1-f] at -78°C [1,2,4] Triazine (prepared according to WO2008116064, 500 mg, 1.72 mmol) suspension in anhydrous THF (5 mL). After 5 minutes the suspension turned into a red-brown solution, then a mixture of 1a (prepared according to WO200631725, 675 mg, 1.81 mmol) and boron trifluoride etherate (2.40 mL, 1.89 mmol) in THF (5 mL) was added dropwise to the mixture. After stirring at -78°C for 2 hours, saturated NH 4 Cl to quench the reaction. The mixture was diluted with ethyl ac...

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Abstract

Provided are pyrrolo[1,2-f][1,2,4]triazinyl, imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][ 1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2' position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.

Description

field of invention [0001] The present invention relates generally to compounds having antiviral activity, more particularly to nucleosides having activity against infection of the Flaviviridae family, and most particularly to inhibitors of hepatitis C virus RNA-dependent RNA polymerase. Background of the invention [0002] Viruses comprising the Flaviviridae family comprise at least 3 distinguishable genera, including Pestivirus, Flavivirus and Hepacivirus (Calisher, et al., J. Gen. Virol., 1993, 70, 37-43 ). Although Pestiviruses are responsible for many economically important animal diseases, such as bovine viral diarrhea virus (BVDV), classical swine fever virus (CSFV, hog cholera) and sheep border disease (BDV), their role in human diseases is The importance has not been clearly characterized (Moennig, V., et al., Adv. Vir. Res. 1992, 48, 53-98). Flaviviruses cause important human diseases such as dengue and yellow fever, while HCVs cause hepatitis C virus infection in...

Claims

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Application Information

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IPC IPC(8): C07D487/04
CPCA61K31/706C07D487/04A61P31/12A61P31/14A61P43/00C07F9/6561C07F9/572C07F9/5728C07F9/2458C07F9/65744A61K31/53C07D405/04G03C7/3835
Inventor A·丘金正恩S·E·梅托博A·S·雷许洁
Owner GILEAD SCI INC
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