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Publication Number
US-12551499-B2
Publication Date
2026-02-17
Expiration Date
Abstract
The present invention is the use of purine nucleotide phosphoramidates or pharmaceutically acceptable salts thereof administered in an effective amount for the treatment or prevention of COVID-19, an infection caused by the SARS CoV-2 virus in a host, for example a human, in need thereof.
Core Innovation
The disclosure describes a method for treating COVID-19 caused by the SARS-CoV-2 virus in a human host in need thereof. The method administers an effective amount of a compound of Formula IIIa, IIIb, IIIc, IIId, or IIIf, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier. The claim specifies R1 as CH3, R2 as phenyl, R3 as hydrogen, R4a as hydrogen, R4b as methyl, and R5 as isopropyl.
Compound 1A demonstrates in vitro antiviral activity against SARS-CoV-1 and SARS-CoV-2 in airway epithelial cells, with no detected cytotoxicity up to tested limits. Persistent intracellular triphosphate accumulates preferentially in human lung, nasal, and bronchial cells. Pharmacokinetic analyses predict lung triphosphate metabolite levels exceeding the SARS-CoV-2 EC90 value, while specific dosing regimens are [procedural detail omitted for safety].
The disclosure also encompasses nucleoside analogs across Formulas I, II, IV, V, VI, VII, and VIII to X, including phosphoramidate stereoisomers, hemi-sulfate salts, and protected sugar intermediates. Scheme 1 illustrates metabolism of Compound 1 to the active triphosphate metabolite 1-6 with plasma surrogate 1-7. Because a background section is omitted, the problem being solved is not explicitly described in patent.
Claims Coverage
The supplied claims identify one independent claim directed to a method of treating COVID-19 in a human host with a specified Formula III compound. Two inventive features are identified, including features from the dependent claims.
Treatment of COVID-19 with specified Formula III compounds
A method for treating COVID-19 caused by the SARS-CoV-2 virus in a human host in need thereof, comprising administering an effective amount of a compound of Formula IIIa, IIIb, IIIc, IIId, or IIIf, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier. The claim specifies R1 as CH3, R2 as phenyl, R3 as hydrogen, R4a as hydrogen, R4b as methyl, and R5 as isopropyl. Dependent claims further specify depicted compound structures.
Pharmaceutically acceptable carrier in an oral dosage form
The dependent claims specify a pharmaceutically acceptable carrier in a dosage form suitable for oral administration, including a solid dosage form that is a tablet, capsule, or gelcap.
The independent claim covers treatment of COVID-19 caused by SARS-CoV-2 in a human host using the specified Formula III compound or its pharmaceutically acceptable salt, optionally in a pharmaceutically acceptable carrier. Dependent claims narrow the compounds to depicted structures and specify oral dosage forms, including tablets, capsules, or gelcaps.
Stated Advantages
Compound 1A shows reported in vitro antiviral activity against SARS-CoV-1 and SARS-CoV-2 in airway epithelial cells (EC90 of 0.64 µM for SARS-CoV-2), broader human coronavirus activity, and weaker activity against MERS-CoV.
No cytotoxicity is detected for Compound 1A up to the tested limits, and in vitro testing of the deuterated compounds reports no visual toxicity.
Persistent active intracellular triphosphate is reported in human nasal and bronchial cells, together with preferential lung accumulation.
Pharmacokinetic analyses predict lung triphosphate Compound 1-6 levels above the SARS-CoV-2 HAE-cell EC90.
The disclosure describes potential for convenient oral treatment, including treatment during early infection and prophylaxis.
The oral tablets are reported to have low impurity levels and chemical stability under the described storage conditions.
The description states outcomes that include reduced progressive respiratory insufficiency, recovery time, hospitalization, viral persistence, respiratory failure, and death.
Documented Applications
Treatment of COVID-19 caused by SARS-CoV-2 in a human host using the specified Formula III compounds or pharmaceutically acceptable salts.
Prophylaxis or prevention of COVID-19 with Formula IIIa to IIIf compounds or acceptable salts, and with the other disclosed compounds.
Treatment or prevention of SARS-CoV-2 infection or COVID-19 with Formula II nucleoside phosphoramidate compounds, Formula VII compounds, and Formula VIII to X nucleosides and related compounds.
Formula IV (including IVb, IVc, and IVd), Formula V, and Formula VI compounds and their pharmaceutically acceptable salts for treating or preventing SARS-CoV-2 infection or COVID-19.
Treatment and prophylaxis of SARS-CoV-2 infection involving drug-resistant variants, and prevention of infection or transmission.
Treatment of COVID-19 complications.
Oral administration of the compounds in a dosage form, including solid dosage forms such as tablets, capsules, or gelcaps, as specified in the dependent claims.
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