Prophylactic and therapeutic pharmaceutical agent for HIV infectious diseases characterized by comprising combination of integrase inhibitor and anti-HIV agent
Inventors
Yoshinaga, Tomokazu • TOMIDA, Yutaka
Assignees
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Publication Number
US-12564595-B2
Publication Date
2026-03-03
Expiration Date
Abstract
A prophylactic or therapeutic pharmaceutical agent for HIV infectious diseases, said pharmaceutical agent being characterized by comprising a combination of: (A) a compound represented by formula (I) (wherein ring A represents a non-aromatic heterocyclic ring; ring B represents a benzene ring or a pyridine ring; Q represents —NHC(O)— or the like: each R1 independently represents a halogen atom or the like: each of R2a and R2b independently represents a hydrogen atom or the like: R3 represents an alkyl group or a haloalky 1 group: R4 represents a hydrogen atom or an alkyl group: and n represents an integer from 1 to 3) or a pharmaceutically acceptable salt thereof, and (B) a compound having an anti-HIV effect or a pharmaceutically acceptable salt thereof.
Core Innovation
The invention concerns compounds defined by Formula (I) and related Formula (I′), together with pharmaceutically acceptable salts thereof, and specifies extensive sets of chemical substituents and ring systems for the compounds. It defines multiple substitution variables and optional core linkage/cyclization possibilities, and it further specifies preferred forms of the moiety Q, including moieties such as “—NHC(O)—” and certain five-member aromatic heterocycles.
The chemical framework is expanded through enumerated choices for ring A and ring B, where ring A includes various fused hetero/carbon ring motifs and ring B includes benzene or pyridine. It further specifies detailed sets of variable substituents, including labeled sets such as α, β, and other labeled variants, as well as R-group variables, and provides example preferred compounds by numbering within the document.
The patent also describes pharmaceutical agent combinations for HIV infection, including pharmaceutical compositions, kits, and methods for preventing or treating symptoms and diseases induced by HIV infection. These embodiments pair a compound selected from a specified group of compounds and pharmaceutically acceptable salts thereof with at least one compound having anti-HIV activity, or a pharmaceutically acceptable salt thereof, including embodiments where the components are provided as separate formulations.
Claims Coverage
The independent claims cover four categories: a pharmaceutical composition, a kit, a prevention method, and a treatment method. Across these independent claims, the core inventive concept is the pairing of component (A), a compound selected from a specified group, with component (B), at least one compound having anti-HIV activity, and dependent claims further refine component (B) by listing anti-HIV targets/classes and named anti-HIV agents, with some embodiments requiring separate formulations.
Pharmaceutical composition comprising compound A and anti-HIV compound B
A pharmaceutical composition comprising (A) a compound selected from the group of compounds and pharmaceutically acceptable salts thereof, and (B) at least one compound having anti-HIV activity, or a pharmaceutically acceptable salt thereof.
Kit comprising compound A and anti-HIV compound B
A kit comprising (A) a compound selected from the group of compounds and pharmaceutically acceptable salts thereof, and (B) at least one compound having anti-HIV activity, or a pharmaceutically acceptable salt thereof.
Preventing HIV-induced symptoms and diseases using compound A and anti-HIV compound B
A method for preventing symptoms, diseases, or symptoms and diseases induced by HIV infection comprising administering to a patient in need thereof (A) a compound selected from the group of compounds and pharmaceutically acceptable salts thereof, and (B) at least one compound having anti-HIV activity, or a pharmaceutically acceptable salt thereof.
Treating HIV-induced symptoms and diseases using compound A and anti-HIV compound B
A method of treating symptoms, diseases, or symptoms and diseases induced by HIV infection comprising administering to a patient in need thereof (A) a compound selected from the group of compounds and pharmaceutically acceptable salts thereof, and (B) at least one compound having anti-HIV activity, or a pharmaceutically acceptable salt thereof.
Overall, the claim coverage is centered on combining a specified compound group (A) with at least one anti-HIV activity compound (B) in four independent claim types: a pharmaceutical composition, a kit, a prevention method, and a treatment method for HIV infection-induced symptoms and diseases. Dependent claims further refine the anti-HIV component (B) by specifying inhibitory activity targets/classes and/or enumerating named anti-HIV agents, and further refine embodiments where components (A) and (B) are provided as separate formulations.
Stated Advantages
Efficacy against drug-resistant and mutated strains.
Provides therapeutic and prophylactic utility for HIV treatment.
Documented Applications
Pharmaceutical composition for anti-HIV use comprising a compound selected from the group of compounds together with at least one compound having anti-HIV activity, or pharmaceutically acceptable salts thereof.
A kit for anti-HIV use comprising a compound selected from the group of compounds together with at least one compound having anti-HIV activity, or pharmaceutically acceptable salts thereof.
Preventing symptoms, diseases, or symptoms and diseases induced by HIV infection by administering a compound selected from the group of compounds together with at least one anti-HIV compound, or pharmaceutically acceptable salts thereof.
Treating symptoms, diseases, or symptoms and diseases induced by HIV infection by administering a compound selected from the group of compounds together with at least one anti-HIV compound, or pharmaceutically acceptable salts thereof.
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