Method of treating COVID-19
Inventors
Hoffman, Robert Louis • Kania, Robert Steven • Owen, Dafydd Rhys • Pettersson, Martin Youngjin • Sammons, Matthew Forrest • Tuttle, Jamison Bryce
Assignees
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Publication Number
US-12485157-B2
Publication Date
2025-12-02
Expiration Date
Abstract
The invention relates to methods of treating COVID-19 in a patient by administering therapeutically effective amounts of certain SARS-CoV-2 inhibitor compounds or pharmaceutical compositions containing them to a patient in need thereof. The invention also relates to inhibiting SARS-CoV-2 coronavirus viral replication activity comprising contacting SARS-CoV-2-related coronavirus protease with a therapeutically effective amount of a SARS-Cov-2 protease inhibitor, such as a SARS-Cov-2 3CL protease inhibitor and compositions comprising the same.
Core Innovation
The invention relates to treating COVID-19 by administering to a patient in need thereof a therapeutically effective amount of a compound selected from a group of stereochemically defined (3S)-3-({N-[(4-methoxy-1H-indol-2-yl)carbonyl]-L-leucyl}amino)-2-oxo-4-[(3S)-2-oxopyrrolidin-3-yl]butyl acetate, pivalate, benzoate derivatives, including substituted benzoate esters, or pharmaceutically acceptable salts thereof. The compounds are defined by stereochemistry and specific leucyl-indole-pyrrolidinyl butyl ester forms as part of the treatment method for COVID-19.
The described therapeutic approach includes administration as a pharmaceutical composition containing a therapeutically effective amount of the selected compound, together with pharmaceutically acceptable salts. The disclosed embodiments include oral, inhalation, intranasal, and sublingual administration, and they specify a dosing frequency of one to four times within a 24-hour period.
The document links coronavirus replication to 3CL protease inhibition and discusses structural homology and active-site features, including catalytic dyad/triad components such as Cys/His. In this context, the leucyl-indole-pyrrolidinyl butyl acetate/pivalate/benzoate derivatives are positioned as therapeutically effective compounds used to inhibit viral replication associated with coronavirus 3CL protease.
Claims Coverage
Two independent claims are present, covering treating COVID-19 by administering a therapeutically effective amount of specified stereochemically defined leucyl-indole-pyrrolidinyl butyl acetate/pivalate/benzoate derivatives, or pharmaceutically acceptable salts, and treating COVID-19 by administering a pharmaceutical composition containing such compounds. The described dependent claims further cover administration routes, dosing frequency, and combination therapy with additional therapeutic agents.
Treating covid-19 by administering stereochemically defined leucyl-indole-pyrrolidinyl butyl acetate/pivalate/benzoate derivatives
A method of treating COVID-19 in a patient by administering to a patient in need thereof a therapeutically effective amount of a compound selected from (3S)-3-({N-[(4-methoxy-1H-indol-2-yl)carbonyl]-L-leucyl}amino)-2-oxo-4-[(3S)-2-oxopyrrolidin-3-yl]butyl acetate, pivalate, benzoate derivatives including substituted benzoate esters, or a pharmaceutically acceptable salt thereof.
Treating covid-19 with a pharmaceutical composition comprising the selected stereochemically defined leucyl-indole-pyrrolidinyl butyl derivatives
A method of treating COVID-19 in a patient by administering to a patient in need thereof a pharmaceutical composition comprising a therapeutically effective amount of a compound selected from the same stereochemically defined leucyl-indole-pyrrolidinyl butyl acetate, pivalate, and benzoate derivatives including substituted benzoate esters, or a pharmaceutically acceptable salt thereof.
Route-specific administration of the selected compound or salt
The compound or a pharmaceutically acceptable salt thereof is administered orally, by inhalation, intranasally, or sublingually.
Dosing frequency within a 24-hour period
The compound or a pharmaceutically acceptable salt of it is administered one to four times within a 24-hour period.
Combination therapy with one or more additional therapeutic agents
The method further includes administering one or more additional therapeutic agents, including remdesivir, dexamethasone, and other listed agents.
The claim coverage centers on COVID-19 treatment using therapeutically effective amounts of defined (3S)-configured leucyl-indole-pyrrolidinyl butyl acetate/pivalate/benzoate derivatives, or salts, either directly or as a pharmaceutical composition. The dependent claim coverage further emphasizes route and dosing refinements and supports combination therapy with one or more additional therapeutic agents.
Stated Advantages
Documented Applications
No documented applications found
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