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DMPK and Metabolism Studies of Nucleoside Phosphoramidates Including INX-08189, A Novel Double Pro-drug and Clinical Candidate for Hepatitis C Virus Therapy

โœ Scribed by Jeff T. Hutchins; Christopher McGuigan; Stanley D. Chamberlain; Karolina W. Madela; Mohamed Aljarah; John Vernachio; Joseph M. Patti; Geoffrey Henson


Book ID
113458506
Publisher
Elsevier Science
Year
2011
Tongue
English
Weight
85 KB
Volume
90
Category
Article
ISSN
0166-3542

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Design, synthesis and evaluation of a no
โœ Christopher McGuigan; Karolina Madela; Mohamed Aljarah; Arnaud Gilles; Andrea Br ๐Ÿ“‚ Article ๐Ÿ“… 2010 ๐Ÿ› Elsevier Science ๐ŸŒ English โš– 728 KB

We herein report a novel double pro-drug approach applied to the anti-HCV agent 2'-beta-C-methyl guanosine. A phosphoramidate ProTide motif and a 6-O-methoxy base pro-drug moiety are combined to generate lipophilic prodrugs of the monophosphate of the guanine nucleoside. Modification of the ester an