Idenix Pharmaceuticals, Inc.

Centre National De La Recherche Scientifique

Merck Sharp + Dohme Corp.

Universitè De Montpellier

Université Montpellier 2 Sciences Et Techniques

Benjamin Alexander Mayes

Adel M Moussa

Alistair James Stewart

Cyril B Dousson

David Dukhan

Gilles J Gosselin

Francois-Rene Alexandre

Christophe Parsy

Claire Pierra

Dominique Surleraux

Richard Storer

Jing Yang Wang

Peter Emmanuel Maligres

Yong-Li Zhong

Kevin Campos

Artis Klapars

Houcine Rahali

Gilles Gosselin

Edward Bridges

Bryon Ladd Simmons

Guillaume Brandt

Alan Michael Hyde

Steven Mark Silverman

Jean-Francois Griffon

Kenneth Baker

Kara Van Valkenburg

Jean-François Griffon

Alistar James Stewart

Elodie Rosinovsky

Jeevanandam Arumugasamy

Francois-René Alexandre

Christophe Claude Parsy

Jingyang Wang

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2',4&#x2032;-bridged nucleosides which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the 2&#x2032;,4&#x2032;-bridged nucleosides are of Formula 3001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, where PD, B, W, X, R, R, Rand Rare as described herein.

2',4&#x2032;-bridged nucleosides for HCV infection

Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

D-amino acid compounds for liver disease

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 4'-OR nucleosides of Formula I: or a pharmaceutically acceptable salt thereof, wherein Base, PD, R, Z, Z, Z, and Zare as defined herein.

4'-or nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2'-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.

2'-chloro nucleoside analogs for HCV infection

The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I). 

Process for making nucleoside phosphoramidate compounds

Provided herein are compounds, compositions, and methods for the treatment of viral infections, for example, Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are D-amino acid phosphoramidate halogeno pyrimidine nucleoside analog compounds which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human. In certain embodiments, the compounds are of Formula I: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein: PD, X, R, R, R, and Rare as described herein.

D-amino acid phosphoramidate pronucleotides of halogeno pyrimidine compounds for liver disease

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2'-cyano, azido or amino nucleosides according to Formula 1001 or 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, W, Rand Rare as described herein.

Amino acid phosphoramidate pronucleotides of 2'-cyano, azido and amino nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001: where PD, Base, Rand Rare as provided herein. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

Thiophosphate nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3'-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Baseand Baseare as provided herein.

3'-deoxy nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are according to Formula 1501: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, PD, R, R, R, L, M and Z are as described herein.

4'-fluoro nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, provided herein are compounds according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein Base, Y, Z, A, Rand Rare as described herein.

Esters and malonates of SATE prodrugs

Provided herein are compounds, methods and pharmaceutical compositions for use in treatment of viral infections, including hepatitis C virus (HCV) infections, in hosts in need thereof. In certain embodiments, the compounds are 2',4&#x2032;-fluoro nucleosides according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, R, and PD are as described herein. In certain embodiments, 2&#x2032;,4&#x2032;-fluoro nucleosides are provided which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human.

2',4&#x2032;-fluoro nucleosides for the treatment of HCV

Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.

3',5&#x2032;-cyclic phosphoramidate prodrugs for HCV infection

3-phosphoindole compounds substantially in the form of a single enantiomer useful for the treatment of Flaviviridae virus infections, and particularly for HIV infections are provided. Also provided are pharmaceutical compositions comprising the 3-phosphoindole compounds alone or in combination with one or more other anti-viral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.

Enantiomerically pure phosphoindoles as HIV inhibitors

Provided herein are macrocyclic serine protease inhibitor compounds, for example, of Formula I, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof. 

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Boston, MA, United States of America

Benjamin Alexander Mayes