Gilead Pharmasset LLC

Gilead Sciences, Inc.

F. Hoffmann-la Roche Ag

Cardlogix

Bruce Ross

Michael Joseph Sofia

Ganapati Reddy Pamulapati

Suguna Rachakonda

Hai-Ren Zhang

Byoung-Kwon Chun

Peiyuan Wang

Dhanapalan Nagarathnam

Jinfa Du

Dustin S Siegel

Wonsuk Chang

Andrew W Waltman

James G Taylor

Darryl Kato

Adam James Schrier

Michael Sangi

Ruben Martinez

Nathan D Shapiro

Kapil Kumar Karki

Jonathan Clive Tripp

Katie Ann Keaton

Denise A Colby

Troy Evan Reynolds

Johann Chan

Dominika Pcion

Lina Chan

Donald Tang

Jiang Zhu

Xianghong Wang

Edward Doerffler

Robert William Scott

Keshab Sarma

Willard Lew

Lars V Heumann

Katrien Brak

Justin Philip Vitale

Silvio A Campagna

Amy Cagulada

Lawrence Yu

Chris Levins

Adam Littke

Pamela Seng

Tiago Vieira

Andrew C Stevens

Robert Ronald Milburn

Pavel Robertovich Badalov

Sean Timothy Neville

Qingwu Jin

Andrei Chtchemelinine

Morin Mae Frick

Detian Gao

Mark Charles Whitcomb

Clarissa Tadeus

Sudha Kondappally

Brittanie Hoang

Lydia Wolfe

Chia-Yun Yu

Sudha Kondapally

Silvio Campagna

Dhanpalan Nagarathnam

Steven Donald Axt

Steven D Axt

Quingwu Jin

Devan Naduthambi

Erik Rueden

Troy Reynolds

Jonathan Tripp

Dustin Siegel

Erick Rueden

Tiago Viera

Provided are methods of preparing compounds and pharmaceutical compositions comprising a compound Formula VIII for treating Filoviridae virus infections. In one aspect, the compound of Formula VIII is formed from a reaction mixture comprising the compound of Formula IX, the compound of Formula X, a coupling agent such as magnesium chloride and a non-nucleophilic base such as diisopropylethylamine. The compound of Formula IX can be formed from a compound of Formula V and a cyanating agent. The compound of Formula V can be synthesized from a reaction mixture comprising a deprotonating agent such as phenylmagnesium chloride; a silylating agent such as chlorotrimethylsilane; a coupling agent such as isopropylmagnesium chloride, an additive such as LaCl-2LiCl, LaCl, CeCl, NdCl, or YCl; a compound of Formula VI; and 7-iodopyrrolo[2,1-f][1,2,4]triazin-4-amine. The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.

Methods for the preparation of ribosides

The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

Synthesis of an antiviral compound

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

Nucleoside phosphoramidates

Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.

A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.

Synthesis of purine nucleosides

The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydrofuran-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase. 

Preparation of nucleosides ribofuranosyl pyrimidines

Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same.

Stereoselective synthesis of phosphorus containing actives

Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure: 

Nucleoside cyclicphosphates

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El Granada, CA, United States of America

Bruce Ross