Other

Emory University

Gilead Pharmasset LLC

Gilead Sciences, Inc.

Triangle Pharmaceuticals, Inc.

Dennis C. Liotta

George R. Painter

Jose Soria

Merrick Almond

Marcos Sznaidman

Darryl Cleary

Darryl G Cleary

George R Painter

Merrick R Almond

Dennis C Liotta

Jos&egrave; D Soria

Adrian S Ray

Dimitrios Stefanidis

Reza Oliyai

Vahid Zia

Rowchanak Pakdaman

Hongmei Mo

Melissa Jean Casteel

Charles J Reynolds

Miriam Michelle Berrey

Robert G Hindes

William T Symonds

Christy M Hebner

Amir Pesyan

José D Soria

Marcos L Sznaidman

Disclosed herein are a composition and unit dosage form for the treatment of hepatitis C virus (HCV) infection comprising GS-7977 and at least one pharmaceutically acceptable excipient, as well as methods for making said composition and unit dosage form. Also disclosed herein is a method of treating a subject, preferably a human, infected with hepatitis C virus, said method comprising administering to the subject for a time period an effective amount of GS-7977 and an effective amount of ribavirin. In one aspect, the method comprises administering to the subject an interferon-free treatment regimen comprising an effective amount of GS-7977 and an effective amount of ribavirin. In a particular aspect, the method is sufficient to produce an undetectable amount of HCV RNA in the subject for at least 12 weeks after the end of the time period.

Compositions and methods for treating hepatitis C virus

This application provides a process for preparing enantiomerically pure &#x3b2;-D-dioxolane nucleosides. In particular, a new synthesis of (&#x2212;)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure &#x3b2;-D- or &#x3b2;-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected &#x3b2;-D- or &#x3b2;-L-1,3-dioxolane nucleoside.

Methods to manufacture 1,3-dioxolane nucleosides

Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include reacting a 5-O-protected-oxymethyl-1,3-oxathiolane with a silylated nucleoside in the presence of (Cl)Ti(isopropoxide). Using the processes described herein, the compounds can be provided as isolated enantiomers.

Process of manufacture of 1,3-oxathiolane nucleosides using titanium trichloride mono-isopropoxide

Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

Method of manufacture of 1,3-oxathiolane nucleosides

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Chapel Hill, NC, United States of America

Darryl G Cleary