Ardea Biosciences, Inc

Valeant Pharmaceuticals North America

Stephanie Shaw

Zhi Hong

Jean-Luc Girardet

Martha Alicia De La Rosa

Esmir Gunic

Yung-Hyo Koh

Haoyun An

Hong Woo Kim

Kanda Ramasamy

Yili Ding

Shahul Nilar

Nanhua Yao

Zhijun Zhang

Hongwoo Kim

Robert Hamatake

Jean Luc Girardet

An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.

Synthesis and use of 2'-substituted-N6-modified nucleosides

This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

Pyrrolo [2,3-D] pyrimidines as non-nucleoside reverse transcriptase inhibitors for treatment of HIV

This application concerns certain 4-cyanophenylamino-substituted bicyclic heterocycles of formula I where the dashed line represents a double bond that may be located either between A and C(V) or between C(V) and D, where A is S or C(Z); D is S or C(W); provided that one and only one of A and D is S; where T is NH, O, or S; and where other substituents are defined herein. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.

Substituted thieno [2,3-d] pyrimidines as HIV inhibitors

Diaryl-purines, azapurines and -deazapurines as non-nucleoside reverse transcriptase inhibitor for treatment of HIV

Substituted thieno[3,2-d]pyrimidines as HIV inhibitors

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Substituted thieno[3,2-D]pyrimidines as HIV inhibitors

Various 2'-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.

2-beta -modified-6-substituted adenosine analogs and their use as antiviral agents

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Rowland Heights, CA, United States of America

Stephanie Shaw