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Publication Number
US-12377079-B2
Publication Date
2025-08-05
Expiration Date
Abstract
Provided herein are compositions and methods for the treatment of infections resulting from antibiotic-resistant strains of bacteria.
Core Innovation
The invention relates to a pharmaceutical composition for the treatment of an antibiotic-resistant bacterial infection, comprising a therapeutically effective amount of a compound of Formula II and a pharmaceutically acceptable carrier. The disclosure further includes stereoisomers, tautomers, and pharmaceutically acceptable salts of the Formula II compounds, together with a therapeutically effective amount of an efflux pump inhibitor.
The Formula II compounds are defined by substituent variables R8–R12 and R13–R14, where the substituents are independently selected from hydrogen, alkyl, aryl, heteroaryl, heteroalkyl, cycloalkyl, heterocyclyl, acyl, allyl, OH, alkoxy, cyano, carboxy, CF3, halide, NH(alkyl), NH(aryl), or NH2, with optional substitutions and optional oxo substitution for certain ring classes.
An efflux pump inhibitor is identified as phenylalanyl arginyl β-naphthylamide (PAβN), and embodiments describe combination therapy in which the efflux pump inhibitor is administered concurrently, simultaneously, or sequentially with the Formula II compound. The disclosed applications include antibiotic-resistant bacterial infections and antibiotic-resistant pathogens including carbapenem-resistant Klebsiella pneumoniae, Pseudomonas aeruginosa, MRSA, and related antibiotic-resistant bacteria.
Claims Coverage
The independent claim coverage includes 3 inventive features: a Formula II pharmaceutical composition with defined substituent variables, inclusion of an efflux pump inhibitor, and identification of PAβN as the efflux pump inhibitor.
Formula II compound pharmaceutical composition
A pharmaceutical composition for treating an antibiotic-resistant bacterial infection comprising a therapeutically effective amount of a compound of Formula II, including stereoisomers, tautomers, or pharmaceutically acceptable salts, together with a pharmaceutically acceptable carrier, with R8–R12 and R13–R14 defined by specified group selections and optional substitutions.
Efflux pump inhibitor inclusion
The composition further comprising a therapeutically effective amount of an efflux pump inhibitor.
Phenylalanyl arginyl β-naphthylamide (PAβN)
The efflux pump inhibitor is phenylalanyl arginyl β-naphthylamide (PAβN).
The claim coverage centers on a Formula II pharmaceutical composition for antibiotic-resistant bacterial infection treatment, combined with an efflux pump inhibitor, with dependent coverage specifying PAβN.
Stated Advantages
Effectiveness is enhanced by co-administering an efflux pump inhibitor.
Documented Applications
Treatment of antibiotic-resistant bacterial infection.
Treatment of subjects with antibiotic-resistant bacterial infections, including Gram-negative carbapenem-resistant Enterobacteriaceae.
Use against antibiotic-resistant pathogens including carbapenem-resistant Klebsiella pneumoniae, Pseudomonas aeruginosa, and MRSA.
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