Inventors:
Raymond F. Schinazi - Atlanta GA, US
John W. Mellors - Pittsburgh PA, US
Nicolas Paul Sluis-Cremer - Pittsburgh PA, US
Frank Amblard - Atlanta GA, US
Steven J. Coats - McDonough GA, US
Junxing Shi - Duluth GA, US
Richard Anthony Whitaker - Loganville GA, US
Assignee:
RFS PHARMA, LLC - Tucker GA
EMORY UNIVERSITY - Atlanta GA
UNIVERSITY OF PITTSBURGH - Pittsburgh PA
International Classification:
A61K 31/70, C07H 19/16, C07D 473/00, A61K 31/522, A61P 31/18
US Classification:
514 45, 536 2722, 544276, 51426337
Abstract:
The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, HBV, and HCV, in human patients or other animal hosts. The compounds are 3′-azido-2′,3′-dideoxy purine nucleosides or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 resistance mutants including HIV-1, HTV-1, HIV-1, HIV-1, HIV-1and inhibitory activity against HIV-1 RT harboring TAMS or insertion mutations including HIV-1, HIV-1, HIV-1, HIV-1, or HIV-1. In one embodiment, the compounds are 3′-azido-ddA, 3′-azido-ddG, or combinations thereof, administered with one or more additional antiviral agents that select for TAM mutations and/or the M 184V mutation, along with a pharmaceutically acceptable carrier.