Polycyclic carbamoylpyridone derivative
Inventors
Assignees
Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12139489-B2
Publication Date
2024-11-12
Expiration Date
Abstract
The present invention provides a compound represented by Formula (I): wherein ring A is a substituted or unsubstituted heterocycle; ring C is a benzene ring or the like; R1 is halogen or the like; R2a and R2b are each independently hydrogen or the like; R3 is substituted or unsubstituted alkyl or the like; R4 is hydrogen or the like; and n is an integer of 1 to 3.
Core Innovation
The invention relates to polycyclic carbamoylpyridone derivatives and selected compounds represented by structural formulae and chemical structure depictions with defined ring variants and substituent options. The disclosure provides multiple structural sub-formulas and structural definitions, including ring A configurations, variable groups, and specific compound selections associated with the defined structural variants.
The compounds share a common chemical scaffold with aromatic or heteroaromatic rings, fused bicyclic or polycyclic motifs, and variable substituents including halogens such as fluorine and chlorine, hydroxyl groups, carbonyl groups, and nitrogen-containing motifs. The specification identifies numerous numbered compound members and uses these structural entries to define the compound selection in the claimed methods.
The invention is directed to using the selected compounds, or pharmaceutically acceptable salts thereof, in methods for treating and preventing HIV infection. The disclosure emphasizes HIV integrase inhibitory medicaments, including long-acting integrase inhibitor use, and frames the compounds as useful against resistant HIV virus with favorable pharmacokinetic, solubility, and tolerability attributes for prophylactic or therapeutic application.
Claims Coverage
The independent claims collectively cover method formulations for HIV management, with three inventive features recurring across the items: selecting a compound or pharmaceutically acceptable salt from the disclosed group, administering that compound, and using the method to treat and, in one claim, prevent HIV infection.
Administering a selected compound or pharmaceutically acceptable salt for HIV treatment and prevention
A method for treating and preventing HIV infection comprising administering a compound or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of the disclosed compounds.
Administering a selected compound for treating HIV infection
A method of treating HIV infection comprising administering a compound selected from the group consisting of the disclosed compounds.
Selecting a compound defined by a specific chemical structure identifier
Dependent claims narrow the administered compound to specific depicted structures identified in the disclosure, including II-31 and II-42.
Overall, the claim coverage centers on administering selected compounds, or pharmaceutically acceptable salts, from the disclosed chemical structure groups to treat HIV infection and, in one claim, to treat and prevent HIV infection. The dependent claims further constrain the selection to specific depicted structure identifiers within the specification.
Stated Advantages
Improved resistance profile for use against resistant HIV virus.
Useful as a long-acting integrase inhibitor for prophylactic or therapeutic application.
Favorable pharmacokinetic attributes.
Favorable solubility attributes.
Favorable tolerability attributes.
Treating HIV infection.
Preventing HIV infection.
Anti-HIV integrase inhibition.
Use in combination therapy.
Documented Applications
Medicinal use as an integrase inhibitor medicament for treating and preventing HIV infection.
Use as a long-acting integrase inhibitor medicament for prophylactic or therapeutic application, including against resistant HIV virus.
Treating HIV infection by administering the depicted structurally defined compounds.
Preventing HIV infection by administering the depicted structurally defined compounds.
Antiviral integrase inhibitor activity.
Anti-HIV integrase activity testing with EC50 values and resistance evaluation against HIV mutants using fold change.
Pharmaceutical formulation/administration contexts.
Evaluation including CYP inhibition/MBI assays and in vivo pharmacokinetic and stability findings, together with in vitro safety/functional assays and solubility-related tests.
Interested in licensing this patent?