5-membered heteroaryl carboxamide compounds for treatment of HBV
Inventors
Heckrodt, Thilo • Walker, Michael • Zhong, Min
Assignees
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Publication Number
US-12655130-B2
Publication Date
2026-06-16
Expiration Date
Abstract
The present disclosure relates to 5-membered heteroaryl carboxamide compounds, which may disrupt Hepatitis B (HBV) core protein assembly. The present disclosure further relates to pharmaceutical compositions comprising 5-membered heteroaryl carboxamide compounds which may disrupt HBV core protein assembly. The present disclosure further relates to uses of 5-membered heteroaryl carboxamide compounds and pharmaceutical compositions thereof in methods of treating Hepatitis B (HBV) infection.
Core Innovation
The disclosure describes substituted octahydropentalenyl carboxamides and compounds of Formula I, including five-membered heteroaryl carboxamide derivatives with oxazole, thiazole, imidazole, and pyrazole variants, and their pharmaceutically acceptable salts. These compounds, which encompass stereochemical variants and selected example compounds, disrupt Hepatitis B virus core protein assembly. Pharmaceutical compositions comprising a compound or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient are also described.
Methods for treating Hepatitis B infection utilize the compounds, pharmaceutically acceptable salts, or pharmaceutical compositions, including combination therapy with antiviral and immune-modulating agents. Documented embodiments include characterization by proton nuclear magnetic resonance, mass spectrometry, and X-ray crystallography, with reported screening results in a HepAD38 viral-production assay. Enteric formulations and dosage-form kits are also provided.
Claims Coverage
The claims define four inventive features directed to Formula I compounds, selected listed examples, additional compound forms, and a diastereomer, each with pharmaceutically acceptable salts.
Formula I compounds and pharmaceutically acceptable salts
Claim 1 covers a compound of Formula I or a pharmaceutically acceptable salt thereof, with specified alternatives for linkers, ring structures, and substituents.
Compounds selected from listed examples
Claim 20 covers a compound selected from a listed set of examples, or a pharmaceutically acceptable salt thereof.
Compound or pharmaceutically acceptable salt
Claims 21 and 22 cover a compound or a pharmaceutically acceptable salt thereof, wherein specific compound structures are not visible in the supplied claim text.
Diastereomer of a compound
Claim 23 covers a diastereomer of a compound or a pharmaceutically acceptable salt thereof.
The independent claims encompass Formula I compound genera, specifically listed example compounds, unspecified compound forms, and diastereomers, each with pharmaceutically acceptable salts. Dependent claims further specify pharmaceutical compositions comprising a pharmaceutically acceptable excipient and methods of treating Hepatitis B infection.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment of Hepatitis B (HBV) infection by administering a therapeutically effective amount of a claimed compound, pharmaceutically acceptable salt, or pharmaceutical composition.
Combination therapy for Hepatitis B (HBV) treatment with antiviral and immune-modulating agents.
Pharmaceutical compositions for multiple administration routes, including enteric formulations and dosage-form kits.
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