Antimicrobial compounds, compositions, and uses thereof
Inventors
Sleet, Randolph B. • Kates, Steven A. • Parkinson, Steven
Assignees
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Publication Number
US-12030908-B2
Publication Date
2024-07-09
Expiration Date
Abstract
A method of treating an infection of a lung in a patient in need thereof according to an embodiment includes administering to the patient an effective amount of a compound having the formula: or a pharmaceutically acceptable salt thereof.
Core Innovation
The disclosure provides a compound having Formula (I) and pharmaceutically acceptable salts thereof, including a sodium salt. The compound is described with a defined nucleoside-like structure that includes a ribose-like moiety, a cytosine-like ring, two phosphate groups, and two butyl groups.
The document discloses phosphonate/phosphodiester-containing bisphosphonate prodrug/derivative compounds and their preparation through protected intermediate chemistry, including phosphitylation, coupling, oxidation to bis-phosphonate, amino/Boc deprotection, and phosphodiester hydrolysis. The work provides intermediates and final compound forms, including conversion to ammonium and free acid forms and salts, including a sodium salt.
The document further describes biological and cytological comparisons using bacterial cytological profiling, including membrane/permeability and DNA condensation impacts, and reports rapid viability reduction for Nu-8. It also reports antimicrobial activity expressed via MIC comparisons across pH values and activity against slow-growing bacteria, with higher potency/biological activity at a pH greater than about 3.
The disclosed therapeutic use is framed as treating infection or lung infection by administration of the disclosed compound having a formula, or a pharmaceutically acceptable salt, to a patient in need thereof. The document includes treatment of bacterial and fungal lung infections and emphasizes lung infection treatment settings aligned with bacterial pathogens referenced in the document.
Claims Coverage
The provided claim coverage centers on treating a lung infection by administering an effective amount of a compound having the specified formula, or a pharmaceutically acceptable salt thereof. The independent claim and dependent claims present six inventive features, with refinement for inhalation administration, dose range, infection etiology, and sodium salt form.
Treating a lung infection with a formula compound or salt
A method of treating a lung infection in a patient in need thereof by administering to the patient an effective amount of a compound having the formula, or a pharmaceutically acceptable salt thereof.
Inhalation administration
The method of treating a lung infection where the administering is performed by inhalation.
Dosage in about 0.1 to about 1000 mg/kg
The method where the patient is administered a dose of about 0.1 to about 1000 mg per kg of body weight.
Dosage in about 0.1 to about 500 mg/kg
The method where the patient is administered a dose of about 0.1 to about 500 mg per kg of patient body weight.
Infection caused by Pseudomonas aeruginosa or Acinetobacter baumannii
The method where the lung infection is caused by Pseudomonas aeruginosa, Acinetobacter baumannii, or their combination.
Sodium salt form
The method where the pharmaceutically acceptable salt is a sodium salt.
Overall, the coverage centers on treating a lung infection by administering an effective amount of the disclosed formula compound or a pharmaceutically acceptable salt, with dependent refinement for inhalation delivery, mg/kg dosage ranges, infections caused by Pseudomonas aeruginosa and/or Acinetobacter baumannii, and the sodium salt form.
Stated Advantages
Higher potency/biological activity at less acidic pH (pH > about 3).
Compatibility with inhalation administration.
Activity against slow-growing bacteria.
Documented Applications
Treatment of lung infections in patients, including bacterial and fungal lung infections.
Treatment use against Pseudomonas aeruginosa lung infection.
Treatment use against Acinetobacter baumannii lung infection.
Treatment use against Aspergillus fumigatus lung infection.
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