Inhibitors for coronavirus
Inventors
BOHMANN, Jonathan A. • GUTIERREZ, Nadean M. • McDonough, Joseph A. • Campbell, Robert Francis • Joyce, Michael Gordon • Panchal, Rekha • SANKHALA, Rajeshwer • DUPLANTIER, Allen
Assignees
Southwest Research Institute SwRI • Henry M Jackson Foundation for Advancedment of Military Medicine Inc • United States Department of the Army
Publication Number
US-11963959-B2
Publication Date
2024-04-23
Expiration Date
2042-08-12
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Abstract
Inhibitors against SARS-COV-1, SARS-CoV-2 (Covid-19), MERS-CoV, and variants within each, including methods of treating a subject suffering from such respiratory disease.
Core Innovation
The invention provides inhibitors against SARS-CoV-1, SARS-CoV-2 (Covid-19), MERS-CoV, and their variants, including novel drug compositions and methods of treating subjects suffering from these respiratory diseases. The described inhibitors mainly comprise pyrroloquinazolines and thiazoles or their pharmaceutically acceptable salts, which target the coronavirus main protease (Mpro), a critical enzyme required for viral replication.
The problem addressed is the urgent need for effective antiviral therapies targeting coronaviruses, specifically COVID-19 and related viruses, as current options are limited. The main protease Mpro has been identified as a promising target since its inhibition prevents viral replication, providing a potential anticoronaviral strategy.
The invention describes the screening and identification of small molecule inhibitors that effectively inhibit viral replication by targeting Mpro. Representative compounds, particularly from pyrroloquinazoline and thiazole families, show efficacy against multiple coronavirus species in vitro, and pharmacokinetic studies in animals indicate that these compounds achieve effective drug levels in both blood plasma and lungs. Therapeutic methods described include various routes of administration and dosage forms for treatment and prophylaxis of coronavirus infections.
Claims Coverage
There is one independent claim covering the main inventive feature of the method for treating coronavirus infections using pyrroloquinazoline compounds.
Method for treatment of COVID-19 and related coronavirus infections using specific pyrroloquinazoline compounds
The invention covers: - A method for treatment of COVID-19 caused by SARS-COV-1, SARS-CoV-2 (Covid-19), MERS-CoV, and their variants in a mammalian subject. - The method comprises administering to the subject an effective amount of a pyrroloquinazoline compound of the following structural formulae, as explicitly recited in the claim and specification. - The pyrroloquinazoline compounds specifically include 7-(2-(trifluoromethyl)benzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine, 7-(2-methylbenzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine, 4-((1,3-diamino-8-methyl-7H-pyrrolo[3,2-f]quinazolin-7-yl)methyl)benzonitrile, 7-allyl-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine, and other explicitly named derivatives. - The scope includes methods utilizing these compounds or their pharmaceutically acceptable salts and administering them in effective amounts for anti-coronaviral therapy.
The inventive feature focuses on administering effective amounts of specified pyrroloquinazoline compounds for treating SARS-CoV-1, SARS-CoV-2, MERS-CoV, and their variants in mammalian subjects.
Stated Advantages
The inhibitors target a conserved region of the viral main protease (Mpro), preventing viral replication across multiple coronavirus species.
Compounds provide a reduction in viral load and improvement in clinical status or symptoms associated with coronavirus infection.
The described compounds are relatively well-tolerated and achieve concentration levels for a significant percentage of time above EC90 in both blood plasma and the lung.
Documented Applications
Treatment of mammalian subjects, particularly humans, suffering from COVID-19, SARS, MERS, and their variants using the described pyrroloquinazoline and thiazole compounds.
Administration of the compounds for prophylactic or therapeutic intervention to prevent, inhibit, arrest the development of, relieve, or cause regression of coronavirus-associated respiratory diseases.
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