Triazine derivatives and methods of use thereof
Inventors
Assignees
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Publication Number
US-11702406-B1
Publication Date
2023-07-18
Expiration Date
Abstract
Certain antiviral compounds, pharmaceutical compositions, and methods related thereto are disclosed.
Core Innovation
The disclosure provides compounds of formula (I), including pharmaceutically acceptable salts, esters, stereoisomers, tautomers, deuterium substitutes, and prodrugs. The compounds are defined within a core formula framework with variable substituents and related variants.
The therapeutic context is antiviral treatment by inhibiting a coronavirus 3C-like protease, including 3CLpro/3C1pro and 3CLpro/3Lpro. The disclosed compounds are positioned for use against coronaviruses, including SARS-CoV-2 and MERS-CoV, in the context of viral infection treatment.
The disclosure also includes pharmaceutical composition content describing use with a pharmaceutically acceptable excipient, along with formulation discussion. Biological evaluation includes an antiviral in vitro assay against SARS-CoV-2 Omicron variants B.1.1.529 and BA.5.2 using Calu-3 cells, and in vivo pharmacokinetics in rats and crab-eating monkeys.
Claims Coverage
The independent claims are directed to compound variants and pharmaceutical compositions, with methods for treating viral infection and inhibiting a coronavirus 3C-like protease. Across the provided claims, six inventive features are identified.
Compound or variant of formula (I)
A compound or pharmaceutically acceptable salts thereof, or deuterium substitutes thereof, or isomers thereof, or prodrugs thereof.
Pharmaceutical composition with a pharmaceutically acceptable excipient
A pharmaceutical composition that includes the compound, or its pharmaceutically acceptable salt, deuterium substitute, isomer, or prodrug, together with a pharmaceutically acceptable excipient.
Treating viral infection by administration
Treating a patient’s viral infection by administering an effective amount of the pharmaceutical composition.
Virus selection from a defined group
Performing the method using a virus selected from a specified group of named viruses.
Inhibiting coronavirus 3C-like protease by administration
Inhibiting a coronavirus 3C-like protease (3CLpro/3Lpro) in a patient by administering an effective amount of the pharmaceutical composition.
Selected compound group
A compound, or pharmaceutically acceptable salts thereof, or deuterium substitutes thereof, or isomers thereof, or prodrugs thereof, wherein the compound is selected from the group consisting of [not provided in the partial text].
The claims tie the compound variants to a pharmaceutical composition with a pharmaceutically acceptable excipient, administration of an effective amount to treat viral infection, and narrower claims to virus selection from an enumerated group and inhibition of a coronavirus 3C-like protease (3CLpro/3Lpro).
Stated Advantages
Antiviral treatment by inhibiting coronavirus 3C-like protease.
Treatment of a patient’s viral infection.
Documented Applications
Inhibiting a coronavirus 3C-like protease (3CLpro/3Lpro) in a patient.
Treating a patient’s viral infection by administering an effective amount of the pharmaceutical composition.
Therapeutic targeting of coronaviruses including SARS-CoV-2 and MERS-CoV in the context of viral infection treatment.
Antiviral in vitro assay against SARS-CoV-2 Omicron variants B.1.1.529 and BA.5.2 using Calu-3 cells.
In vivo pharmacokinetics in rats and crab-eating monkeys.
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