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Publication Number
US-10874687-B1
Publication Date
2020-12-29
Expiration Date
Abstract
The present invention is the use of a small group of purine nucleotide phosphoramidate disclosed herein or a pharmaceutically acceptable salt thereof in an effective amount for the treatment or prevention of the novel 2019 coronavirus disease (COVID-19) in a host, for example a human, in need thereof.
Core Innovation
The disclosure provides methods for treating or preventing 2019 coronavirus disease (COVID-19) caused by SARS-CoV-2 in a human in need thereof. The method comprises administering an effective amount of Compound 1, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier. In addition, the disclosure identifies purine nucleotide phosphoramidate prodrugs, including Formula II compounds, stabilized phosphate prodrug forms, and isotopically substituted nucleoside compounds.
The disclosure demonstrates antiviral activity for Compound 1A and its hemisulfate salt against SARS-CoV-2 and other coronaviruses. Compound 1A forms a persistent active triphosphate metabolite in human airway epithelial cells, while animal data show preferential lung accumulation supporting respiratory targeting. Formulated solid oral compositions exhibit chemical stability, enabling administration outside medical facilities. Because the background section is omitted, the technical problem being solved is not explicitly described in patent.
Claims Coverage
The claims identify one independent claim directed to the treatment of COVID-19, reciting one inventive feature.
Treatment of COVID-19 with Compound 1
A method for the treatment of 2019 coronavirus disease (COVID-19) caused by the SARS-CoV-2 virus in a human in need thereof, comprising administering an effective amount of Compound 1 or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
The independent claim covers administering an effective amount of Compound 1, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to treat COVID-19 caused by SARS-CoV-2 in a human.
Stated Advantages
The disclosure describes convenient solid oral dosing outside medical facilities.
Compound 1A forms a persistent active triphosphate in nasal and bronchial epithelial cells, and animal data show preferential lung accumulation, supporting respiratory targeting.
Antiviral activity of Compound 1A against SARS-CoV-2 and other coronaviruses is reported.
Chemical stability of formulated Compound 2A tablets is reported.
Documented Applications
Treatment of 2019 coronavirus disease (COVID-19) caused by SARS-CoV-2 in a human.
Prophylaxis of COVID-19.
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