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applied in the field of 2'-fluoro CARBA-nucleoside analogs for antiviral therapy, can solve problems such as unpublished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
View PDF28 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these compounds have not been dis

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0482] Example

[0483] In describing the details of the experiment, certain abbreviations and acronyms were used. Although most of them can be understood by those skilled in the art, Table 1 contains a list 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, 1.61mL, 2.41mmol) 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) in anhydrous THF (5 mL) suspension. After 5 minutes, the suspension became a reddish brown solution, and 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, add saturated NH 4 Cl to quench the reaction. The mixture was diluted with ethyl...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap