Compositions and methods for ameliorating pain and reducing fever
Inventors
Bazan, Nicolas • BAZAN, Hernan • Gomez, Julio Alvarez-Builla • Paul, Dennis • Garcia, Carolina Burgos
Assignees
Alcala De Hernares, University of • South Rampart Pharma LLC • Louisiana State University
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Publication Number
US-11007199-B2
Publication Date
2021-05-18
Expiration Date
Abstract
This invention is directed to compositions, methods and kits that can be used for the treatment or amelioration of pain and fever.
Core Innovation
The patent describes analgesic and antipyretic treatment of pain and fever using non-narcotic acetaminophen (ApAP)-analog compounds, including compounds of formula (I), a “DFA salt,” and related formula (II). It focuses on a DEA salt form, 2-[[2-(4-hydroxyanilino)-2-oxo-ethyl]sulfamoyl]benzoate diethylammonium salt, proposed to retain analgesia and antipyresis comparable to ApAP while avoiding metabolism to the toxic ApAP metabolite NAPQI, i.e., not being metabolized to NAPQI in vivo.
The patent states the problem addressed by the invention as ApAP hepatotoxicity linked to formation of NAPQI and associated glutathione (GSH) depletion, with consequences relating to hepatotoxicity. It therefore describes compounds intended to reduce hepatotoxicity by reducing NAPQI generation, while maintaining comparable therapeutic effects for pain and fever relative to ApAP.
The document includes example pharmacological assays for analgesic effects and antipyretic effects, together with hepatotoxicity-related measurements including LDH, GSH assessment, CYP450 metabolism profiling, and NAPQI levels. The reported findings include that the DEA salt is comparable to ApAP for pain and fever and shows decreased hepatotoxicity and less NAPQI generation.
Claims Coverage
The patent provides multiple independent claims covering structurally defined analgesic compounds, structurally defined antipyretic compounds, and methods of treating pain and fever by administering a therapeutically effective amount of the compounds. Across these claims, the inventive features emphasize comparative in vivo performance versus acetaminophen, including comparable analgesic effects and reduced hepatotoxicity risk upon same-amount administration.
Analgesic compound defined by a chemical structure
An analgesic compound having the following chemical structure.
Comparable analgesic effect to acetaminophen at the same administered amount
The analgesic compound exhibits analgesic effects comparable to acetaminophen when administered in vivo at the same amount.
Reduced hepatotoxicity risk comparable to acetaminophen at the same administered amount
The analgesic compound exhibits reduced hepatotoxicity risk comparable to acetaminophen when administered in vivo at the same amount.
Antipyretic compound defined by a chemical structure
An antipyretic compound having the following chemical structure.
Reduced hepatotoxicity risk comparable to acetaminophen upon in vivo administration in the same amount
The antipyretic compound, when administered in vivo in the same amount as acetaminophen, has reduced risk of hepatotoxicity comparable to acetaminophen.
Treating pain by administering a therapeutically effective amount of a structurally defined compound
A method of treating pain in a patient comprising administering to the patient a therapeutically effective amount of a compound having the following chemical structure.
Treating fever by administering a therapeutically effective amount of a structurally defined compound
A method of treating fever in a patient comprising administering to the patient a therapeutically effective amount of a compound having the following chemical structure.
Overall claim coverage centers on structurally defined analgesic and antipyretic compounds, and on methods for treating pain and fever by administering therapeutically effective amounts. Dependent claim refinements further require comparable analgesic effects to acetaminophen and reduced hepatotoxicity risk while remaining comparable to acetaminophen.
Stated Advantages
Retains analgesia and antipyresis comparable to acetaminophen.
Not metabolized to the toxic ApAP metabolite NAPQI in vivo.
Reduced hepatotoxicity risk compared with acetaminophen, while remaining comparable in performance.
Decreased NAPQI generation.
Documented Applications
Analgesic and antipyretic treatment of pain and fever using non-narcotic acetaminophen (ApAP)-analog compounds.
Pharmaceutical compositions and combination concepts for medical use, including possible combination with opioids and NSAIDs, and inclusion in a medical kit.
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