Gilead Pharmasset LLC

The Cleveland Clinic Foundation

Gilead Sciences, Inc.

F. Hoffmann-La Roche Ag

Suguna Rachakonda

Byoung-Kwon Chun

Bruce Ross

Michael Joseph Sofia

Ganapati Reddy Pamulapati

Hai-Ren Zhang

Peiyuan Wang

Jinfa Du

Bruce S Ross

Wonsuk Chang

Koichi Fukuda

Jun Qin

Julia Vaynberg

Jiang Zhu

Dhanapalan Nagarathnam

Keshab Sarma

Justin Philip Vitale

Qingwu Jin

Dhanpalan Nagarathnam

Steven D Axt

Quingwu Jin

The present invention relates to compounds that are modulators of Integrin Linked Kinase (ILK), and methods of treating diseases with such compounds. In certain embodiments, the compounds are within Formulas I-VII (e.g., Csbl-1). In some embodiments, the compounds are used to treat an ILK-mediated disease, such as cancer (e.g., triple negative breast cancer) or an inflammatory disease.

Compounds for treating ILK-mediated diseases

The present invention provides (i) processes for preparing a 2'-deoxy-2&#x2032;-fluoro-2&#x2032;-methyl-D-ribonolactone derivatives, (ii) conversion of intermediate lactones to nucleosides with potent anti-HCV activity, and their analogues, and (iii) methods to prepare the anti-HCV nucleosides containing the 2&#x2032;-deoxy-2&#x2032;-fluoro-2&#x2032;-C-methyl-&#xdf;-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside.

Preparation of 2'-fluoro-2&#x2032;-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives

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

Growing community of inventors

Twinsburg, OH, United States of America

Suguna Rachakonda