Idenix Pharmaceuticals, Inc.

Novartis Ag

Jing Yang Wang

Adel M Moussa

Richard Storer

Cyril B Dousson

Francois-Rene Alexandre

Benjamin Alexander Mayes

Alistair James Stewart

Edward Bridges

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

An industrially scalable two-step process for preparing a &#x3b2;-L-2'-deoxy-nucleoside that results in a predominance of the &#x3b2;- over the &#x3b1;-anomeric form of the compound is described. An optional third step may be used to prepare 3&#x2032;-prodrugs of desirable &#x3b2;-L-2&#x2032;-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of &#x3b2;-L-2&#x2032;-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

Industrially scalable nucleoside synthesis

Growing community of inventors

Acton, MA, United States of America

Jing Yang Wang