Roche Palo Alto LLC

Gilead Pharmasset LLC

Hoffmann-La Roche Inc.

Syntex (u.s.a.) Inc.

Agouron Pharmaceuticals, Inc.

Gilead Sciences, Inc.

F. Hoffmann-La Roche Ag

Keshab Sarma

Ganapati Reddy Pamulapati

Scott Alan Wolckenhauer

Lars V Heumann

Benjamin James Roberts

Martin Gerald Teresk

Shinji Fujimori

Kevin McCormack Allan

Xiang Wang

David Bernard Smith

Joseph Armstrong Martin

Jiang Zhu

Christopher M Levins

Andrew S Thompson

Mark Smith

Gregory Notte

Byoung-Kwon Chun

Terrence Joseph Connolly

Brandon Heath Brown

Katie Ann Keaton

Anna Chiu

Troy Evan Reynolds

Nolan Griggs

Stephen Paul Lathrop

Grace May

Katie Ann Brown

Grace May Huynh

Tao Wang

Brenda J Chan

David Allen Siler

Gary M Lee

Michael Martin

Zachary Kevin Sweeney

Yan Lou

Peiyuan Wang

Arlindo Lucas Castelhano

Matthew C Lucas

Jeffrey Allen Campbell

Timothy D Owens

Fariborz Firooznia

Steven Lee Bender

Lawrence Emerson Fisher

Chris Allen Broka

Bruce Ross

Stephen Matthew Lynch

Humberto Bartolome Arzeno

Suguna Rachakonda

Stefan Hildbrand

Peter John Harrington

Steven Joseph Berthel

Eric Roy Humphreys

Thimma R Rawalpally

Robert Than Hendricks

Jeremy Clark

Thomas Cleary

Justin Philip Vitale

Anthony Prince

Lianhe Shu

Joshua Paul Gergely Taygerly

Gary R Lee

Daniel Vincent Fishlock

Yaohui Ji

Qingwu Jin

Pankaj Rege

Robert Patrick Farrell

Kevin M Allan

Chen Gu

Daniel Fishlock

Brenda J Burke Chan

Andrew S Thomson

Steven D Axt

Quingwu Jin

Steven Berthel

Jun-Bae Hong

Han Ma

Chrisopher M Levins

Stephen M Lynch

Pankaj Devdatta Rege

Stephan P Lathrop

Eric R Humphreys

Thimothy D Owens

Robert P Farrell

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

Processes for preparing antiviral compounds

The invention relates to a process for the preparation of 4-{[(2R,3S,4R,5S)-3-(3-chloro-2-fluoro-phenyl)-4-(4-chloro-2-fluoro-phenyl)-4-cyano-5-(2,2-dimethyl-propyl)-pyrrolidine-2-carbonyl]-amino}-3-methoxy-benzoic acid of the formula (I) as well as intermediates thereof and pharmaceutical preparations thereof, comprising the step of reacting a compound of the formula (IV) with a compound of the formula (V), as defined in the specification, in the presence of a chiral silver- or copper catalyst.

Asymmetric synthesis of a substituted pyrrolidine-2-carboxamide

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

This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X', Y, Y, Y, Y, Y, Y, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.

Inhibitors of Bruton's tyrosine kinase

Compounds having the formula I wherein R, Rand Rare as defined herein are Hepatitis C virus NS5polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication. 

Antiviral nucleosides

Compounds having the formula I wherein Ris as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, and processes for making the compounds of formula I 

The present process provides a improved method for the preparation of alkylsulfanyl substituted triazoles 2 which are useful intermediates in a new process for the preparation of triazolones 20. 

Process for preparing triazolones

Compounds having the formula I wherein Ris as herein defined are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis replication, processes for making the compounds and synthetic intermediates used in the process 

The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.

Process for the preparation of 3-amino-pentan-1,5-diol

The invention relates to a novel process for the preparation of 4'-azido-cytidine (I) or a pharmaceutically accepted salt thereof. The compound of formula I is useful for treating virus mediated diseases, particularly for treating HCV mediated diseases.

Process for the preparation of 4'-azido cytidine derivatives

A method comprising: with vitride, to form an aminopropyl indole compound of formula i wherein m, Ar, Rand Rare as defined herein. The compounds prepared by the method of the invention are useful as monoamine reuptake inhibitors useful for treatment of CNS indications.

Methods for synthesis of 3-amino-1-arylpropyl indoles

The present invention relates to a one-step process for the selective O-acylation of the hydroxy groups of a nucleoside under basic conditions utilizing DMAP and a carboxylic acid anhydride in aqueous heterogenous solvent mixture.

Selective O-acylation of nucleosides

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Sunnyvale, CA, United States of America

Keshab Sarma