University of Minnesota

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Emory University

University of Missouri

Zhengqiang Wang

Yves Pommier

Stefan G Sarafianos

Jing Tang

Jayakanth Kankanala

Andrew D Huber

Stefanos G Sarafianos

The invention provides a compound of formula I, formula II, or formula III: or a salt thereof, wherein R-Rhave any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as HIV-1 CA-targeting molecules and as antiviral agents.

Antiviral compounds

The present invention provides novel compounds and methods for treating, preventing or inhibiting hepatitis B virus (HBV).

Inhibitors of hepatitis B virus targeting capsid assembly

The invention provides a compound of formula (I), (II) or (III): wherein R, R, R, Rand Rhave any of the values described in the specification, as well as compositions comprising a compound of formula (I), (II) or (III). The compounds and compositions are useful as chemotherapeutic sensitizing agents.

Compounds for cancer chemotherapeutic sensitization

Various embodiments described herein are directed to compounds of formula (I), (II), (III) or (IV) for use as potent inhibitors of HIV integrase and for treatment of patients afflicted with AIDS. A major challenge of human immunodeficiency virus (HIV) chemotherapy continues to be the inevitable selection of resistance by the virus towards known drug regimens. Treating resistant HIV strains calls for novel antivirals with unique structural cores. Some embodiments are directed to compounds featuring a 3-hydroxypyrimidine-2,4-dione-5-carboxamide core that consistently confers low nanomolar potencies against HIV-1 in cell culture. Biochemical testing and molecular modeling results corroborate an antiviral mechanism of action of inhibiting integrase strand transfer (INST). Preliminary testing against raltegravir-resistant HIVs showed marginal cross resistance, suggesting that the chemotypes of the various embodiments described herein could fit an inhibitory profile of second generation INSTIs. 

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Eden Prairie, MO, United States of America

Zhengqiang Wang