Smithkline Beecham Corporation

Emory University

Other

Triangle Pharmaceuticals, Inc.

Gilead Sciences, Inc.

Aerie Pharmaceuticals, Inc.

Bukwang Pharmaceuticals Ind Co., Ltd.

Marcos Sznaidman

George R Painter

Merrick R Almond

Darryl G Cleary

Dennis C Liotta

Millard Hurst Lambert, Iii

Daniel David Sternbach

Jos&egrave; D Soria

Timothy Mark Willson

Michael Lawrence Sierra

Curt Dale Haffner

Huaqiang Eric Xu

Patrick Reed Maloney

Amir Pesyan

Esther Yu-Hsuan Chao

Mitchell Anthony deLong

Allen E Eckhardt

Thomas E Richardson

Rodolfo Cadilla

Stephen William Rafferty

Brian H Heasley

Robert H Oakley

Michael Robert Peel

Christine Hudson

Jeffrey David Yingling

Paresma R Patel

Pierette Banker

Darryl G Gleary

José D Soria

Claire Louise Murray

Byappanahally N Narasinga Rao

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

Isoquinoline compounds with G are provided that influence, inhibit or reduce the action of a G-protein receptor kinase. Pharmaceutical compositions including therapeutically effective amounts of the isoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, osteoporosis and glaucoma are also provided.

Isoquinoline compounds

The present invention provides a compound of formula (I): 

Thiazole and oxazole derivatives as activators of human peroxisome proliferator activated receptors

The present invention is directed to the process for the preparation of 2'-deoxy-2&#x2032;-halo-&#x3b2;-L-arabinofuranosyl nucleosides, and in particular, 2&#x2032;-deoxy-2&#x2032;-fluoro-&#x3b2;-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and less expensive than L-ribose or L-xylose, in ten steps. All of the reagents and starting materials are inexpensive and no special equipment is required to carry out the reactions.

Process for the preparation of 2'-halo-&#x3b2;-L-arabinofuranosyl 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

Activator of PPAR delta

Compounds of Formula (1) are disclosed. These compounds include selective activators of human PPAR delta.

Activators of PPAR delta

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

Growing community of inventors

Durham, NC, United States of America

Marcos Sznaidman