Pyrrolo[2,3-B]pyridin derivatives as 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-12357631-B2
Publication Date
2025-07-15
Expiration Date
Abstract
Provided herein are compounds of Formula A, B or C that can inhibit the replication of influenza viruses, reduce the amount of influenza viruses, and/or treat influenza.
Core Innovation
The invention relates to compounds of Formula A and pharmaceutically acceptable salts thereof. In Formula A, Z1 is halogen, Z2 and Z3 are each H, X is C6-C10 aryl or a 5-10-membered heteroaryl comprising 1-3 ring heteroatoms selected from O, N, and S, R1 and R2 are H, R3 is halogen, R4 is H, each R5 independently is H or C1-C6 alkyl, and R9 is H.
A further core element is the L linker and associated Rz group. In Formula A, L is C1-C14 alkyl-OC(O)NH-C1-C14 alkyl-Rz, and each Rz is independently selected from H, C1-C6 alkyl, C1-C6 alkyl-CO2R5, and Y, where Y is independently C6-C10 aryl. The alkyl portion is optionally substituted with halogen, cyano, hydroxy, oxo, amino, carboxy, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 aminoalkoxy, C1-C6 cyanoalkoxy, C1-C6 hydroxyalkoxy, and C2-C6 alkoxyalkoxy.
The patent further presents Table A compounds as specific exemplified structures within the Formula A class, including listed compound numbers and their pharmaceutically acceptable salts. The disclosed subject matter also describes influenza virus replication inhibitors, pharmaceutical compositions, and administration, and it references compounds capable of inhibiting influenza replication, reducing influenza viral amount or titer, and treating or preventing influenza.
Claims Coverage
The consolidated claims coverage includes two independent claim types: a broad Formula A compound claim and a Table A compound claim. Across these claims, the inventive features center on the Formula A scaffold with defined Z1-Z3, X, R1-R5, R9, L, and Rz variables, together with specific Table A-listed compounds and pharmaceutically acceptable salts.
Formula A compound scaffold with defined substituents
A compound of Formula A wherein Z1 is halogen, Z2 is H, Z3 is H, X is C6-C10 aryl or a 5-10-membered heteroaryl comprising 1-3 ring heteroatoms selected from O, N, and S, R1 is H, R2 is H, R3 is halogen, R4 is H, each R5 is independently H or C1-C6 alkyl, R9 is H, and L is C1-C14 alkyl-OC(O)NH-C1-C14 alkyl-Rz, with each Rz independently selected from H, C1-C6 alkyl, C1-C6 alkyl-CO2R5, and Y, where each Y is independently C6-C10 aryl, or a pharmaceutically acceptable salt thereof.
Optional alkyl substitution on the L group
The alkyl portion of L is optionally substituted with one or more substituents independently selected from halogen, cyano, hydroxy, oxo, amino, carboxy, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 aminoalkoxy, C1-C6 cyanoalkoxy, C1-C6 hydroxyalkoxy, and C2-C6 alkoxyalkoxy.
Table A compounds and pharmaceutically acceptable salts
A compound as recited in Table A, or a pharmaceutically acceptable salt thereof.
Pharmaceutical composition with pharmaceutically acceptable carrier
A pharmaceutical composition that includes the compound or its salt together with a pharmaceutically acceptable carrier, adjuvant, or vehicle.
Overall, the claim coverage is directed to the Formula A structural definition with specified halogen, aryl/heteroaryl, and L/Rz variable options, and to compounds specifically recited in Table A together with pharmaceutically acceptable salts and a pharmaceutical composition using a pharmaceutically acceptable carrier, adjuvant, or vehicle.
Stated Advantages
Inhibiting influenza replication.
Reducing influenza viral amount or titer.
Treating or preventing influenza.
Documented Applications
Influenza treatment using therapeutically effective amounts.
Influenza prophylaxis using prophylactically effective amounts.
Influenza virus replication inhibition and reduction of influenza viral amount or titer.
Pharmaceutical compositions for manufacture of a medicament.
Pulmonary delivery using inhalable powders, sprays or aerosols, intranasal sprays, and nebulization.
Administration routes including oral, parenteral, rectal/vaginal, topical/transdermal, ophthalmic, and implanted reservoir contexts.
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