Inhibitors of influenza virus replication
Inventors
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Assignees
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Cocrystal PharmaCocrystal Pharma is a clinical-stage biotechnology company specializing in the discovery and development of novel antiviral therapeutics for serious and chronic viral diseases such as influenza, COVID-19, hepatitis C, norovirus, and other respiratory viruses. The company leverages structure-based drug discovery technology and expertise in structural biology to design direct viral replication inhibitors with broad-spectrum activity. Its pipeline includes candidates in preclinical and clinical development, addressing unmet needs in antiviral medicine.
Cocrystal Pharma is a clinical-stage biotechnology company specializing in the discovery and development of novel antiviral therapeutics for serious and chronic viral diseases such as influenza, COVID-19, hepatitis C, norovirus, and other respiratory viruses. The company leverages structure-based drug discovery technology and expertise in structural biology to design direct viral replication inhibitors with broad-spectrum activity. Its pipeline includes candidates in preclinical and clinical development, addressing unmet needs in antiviral medicine.
Publication Number
US-12565488-B2
Publication Date
2026-03-03
Expiration Date
Abstract
Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient a safe and effective amount of a compound represented by Formula I, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
Core Innovation
The invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, defined by a heteroaryl framework with multiple independently varying substituents including Y, A, B, L, Ar, and R groups. Within Formula I, Y is selected from O, S, SO2, or NR1, A and B are independently null, C6-10 aryl, or a 5-7 membered heteroaryl containing 1-3 ring heteroatoms selected from N, O, and S, and the aryl or heteroaryl is optionally substituted. The Formula I definition further allows a range of heteroatom selections, optional substitutions, and sub-formulas and representative chemical structures with variations in substituents and motifs.
The disclosed compounds are associated with inhibiting influenza polymerase PA endonuclease activity, binding free virus and/or PB2-associated complexes, and thereby inhibiting influenza replication. The compounds are described in connection with reducing influenza viral amount or titer in biological samples and in patients. The document also discloses pharmaceutical compositions and pharmaceutically acceptable salts of the Formula I compounds together with formulation concepts and administration options.
The framework further incorporates provisos that restrict structural elements under specific parameter conditions. When z is 0, then Y is NR1, A is null, and L is NR3, and when x is 0, L is NR3; x and z are each 0 or 1.
Claims Coverage
The document includes one independent claim directed to a compound, or a pharmaceutically acceptable salt, defined by a Formula I structural framework with multiple independently varying substituent parameters, plus provisos that constrain the structure when x and/or z take specific values. The claim coverage also includes at least one method-of-use claim for reducing influenza virus in a biological sample or in a patient.
Formula I compound or pharmaceutically acceptable salt
A compound of Formula I, or a pharmaceutically acceptable salt thereof, wherein Y is O, S, SO2, or NR1; A and B are each independently null, C6-10 aryl, or 5-7 membered heteroaryl having 1-3 ring heteroatoms selected from N, O, and S, with optional substitution; L is a bond, NR3, or C(R4)2; and the remaining variable substituent groups are defined according to the stated ranges and substituent rules.
Provisos tying z and x to structural elements
When z is 0, then Y is NR1, A is null, and L is NR3, and when x is 0, L is NR3, while x is 0 or 1 and z is 0 or 1.
Reducing influenza virus in a biological sample or in a patient
A method of reducing the amount of influenza virus in a biological sample or in a patient by administering a safe and effective amount of the compound or salt.
The independent claim coverage is centered on a broad Formula I scaffold with extensive variable substitution across Y, A, B, L, and the various R groups on aryl and heteroaryl moieties, further limited by specific provisos that enforce structural assignments when z and/or x are set to 0. The provided claim set also includes method coverage for reducing influenza virus in a biological sample or in a patient.
Stated Advantages
Inhibits influenza replication by inhibiting influenza polymerase PA endonuclease activity.
Inhibits influenza virus replication by binding free virus and/or PB2-associated complexes.
Reduces influenza viral amount or titer in a biological sample or in a patient.
Provides a basis for treatment and prevention of influenza infection.
Documented Applications
Treatment and prevention of influenza infection in a patient by administering a therapeutically or prophylactically effective amount of a Formula I compound or a pharmaceutically acceptable salt thereof.
Reducing the amount of influenza virus in a biological sample or in a patient by administering a safe and effective amount of the compound or salt.
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