N4-hydroxycytidine and derivatives and anti-viral uses related thereto
AssigneeEmory University
InventorsGeorge R. PAINTER, Gregory R. Bluemling, Michael G. Natchus, David Guthrie
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Abstract
This disclosure relates to certain N4-hydroxycytidine derivatives, pharmaceutical compositions, and methods related thereto. In certain embodiments, the disclosure relates to the treatment or prophylaxis of viral infections, such as Eastern, Western, and Venezuelan Equine Encephalitis (EEE, WEE and VEE, respectively), Chikungunya fever (CHIK), Ebola, Influenza, RSV, and Zika virus infection with the disclosed compounds.
Claims8
1-60. (canceled)
A process for producing a compound, comprising
- a) reacting uridine having hydroxyl groups at positions 2′, 3′, and 5′ with a compound to protect or esterify the hydroxyl groups at positions 2′ and 3′ of uridine thereby forming a first intermediate;
- b) simultaneously or subsequent to step a), esterifying the hydroxyl group at position 5′ of the first intermediate to form a carboxylic acid ester as a second intermediate;
- c) reacting the second intermediate with a 1,2,4-triazole compound followed by reaction with a hydroxylamine moiety at position 4, thereby forming a third intermediate;
- and
- d) optionally deprotecting the third intermediate.
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound as claimed in claim 66.
Dependencies are inferred from the claim text.