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 Henares, University of • South Rampart Pharma LLC • Louisiana State University
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Publication Number
US-11529355-B2
Publication Date
2022-12-20
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 document describes novel acetaminophen (ApAP/paracetamol) analogs as analgesic and antipyretic agents. The compounds are presented as pharmaceutical compositions and are defined by specific chemical structures, including “DEA salt” and an additional compound of a further formula. The invention is framed around retaining analgesia and antipyresis while addressing hepatotoxicity concerns associated with acetaminophen.
The problem addressed in the background is the hepatotoxicity risk associated with acetaminophen, which is tied in the document to metabolism leading to N-acetyl-benzoquinoneimine (NAPQI). The described approach focuses on minimizing formation of the toxic metabolite NAPQI, with the document discussing reduced hepatotoxic risk as a result of avoiding metabolism to NAPQI.
In vivo comparisons are described for pain and fever effects, where DEA salt is reported to be comparable to acetaminophen for analgesic and antipyretic outcomes while showing decreased toxicity. The document reports lower NAPQI generation and reduced hepatotoxicity versus acetaminophen, supported by biochemical and toxicity-related rationales and assays.
Claims Coverage
The document provides three independent claims covering a pharmaceutical composition for an analgesic compound, a method of treating pain, and a method of treating fever. Across these independent claims, the inventive features include the specific chemical structure of an analgesic compound, formulation with a pharmaceutically acceptable carrier or excipient, and therapeutic use for pain or fever treatment with a therapeutically effective amount.
Analgesic compound pharmaceutical composition with a specific chemical structure and pharmaceutically acceptable carrier
A pharmaceutical composition comprising an analgesic compound having the chemical structure defined in the claim and a pharmaceutically acceptable carrier or excipient.
Treating pain by administering a therapeutically effective amount of a pharmaceutical composition with a specific chemical structure
A method of treating pain in a patient comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising a compound having the chemical structure defined in the claim and a pharmaceutically acceptable carrier or excipient.
Treating fever by administering a therapeutically effective amount of a pharmaceutical composition with a specific chemical structure
A method of treating fever in a patient comprising administering to the patient a therapeutically effective amount of a pharmaceutical composition comprising a compound having the chemical structure defined in the claim and a pharmaceutically acceptable carrier or excipient.
Overall claim coverage centers on pharmaceutical compositions containing an analgesic compound defined by a specified chemical structure, formulated with a pharmaceutically acceptable carrier or excipient, and on methods for treating pain and treating fever by administering therapeutically effective amounts. The document’s dependent claim refinements emphasize comparative analgesia at the same amount versus acetaminophen, reduced risk of hepatotoxicity versus acetaminophen at the same amount, and antipyresis when administered in vivo.
Stated Advantages
Retains analgesia and antipyresis effects while minimizing hepatotoxicity.
Decreased hepatotoxicity versus acetaminophen.
Lower NAPQI generation compared with acetaminophen.
Comparable analgesic effects to acetaminophen when administered in vivo at the same amount.
Reduced risk of hepatotoxicity versus acetaminophen when administered in vivo at the same amount.
Antipyresis when administered in vivo.
Documented Applications
Medical use for treatment of pain in a patient.
Medical use for treatment of fever in a patient.
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