Reversible Nitroxide Derivatives for Controlled NO Release
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Solution Overview
Problem
Current treatments for inflammation, obesity, metabolic syndrome, acute kidney disease, and chronic kidney disease lack effective pharmaceutical solutions that can induce vasodilation and address metabolic and inflammatory stress without significant side effects.
Innovation Solution
Development of reversible nitrogen oxides of nitroalkenes, which are administered to subjects, featuring an electron withdrawing group, a leaving group, and a carbon-carbon double bond, to release nitric oxide and conjugated nitro linoleic acid, providing therapeutic benefits while minimizing gastrointestinal side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments for inflammation, obesity, and kidney disease are used, then therapeutic effects are achieved, but significant side effects occur
Solution Approach 1:
The patent introduces reversible nitrogen oxides of nitroalkenes as intermediary compounds that deliver nitric oxide and conjugated nitro linoleic acid in a controlled manner. These intermediaries act as carriers that provide therapeutic benefits while minimizing direct gastrointestinal toxicity, resolving the contradiction between therapeutic effectiveness and side effects.
Solution Approach 2:
The patent modifies the chemical structure and delivery parameters of nitric oxide compounds by creating reversible nitrogen oxides of nitroalkenes with specific electron withdrawing groups and leaving groups. This structural parameter change allows controlled release of active species, improving therapeutic index by reducing harmful side effects while maintaining efficacy.
2Ease of operation
If nitric oxide releasing compounds are administered, then vasodilation is induced, but gastrointestinal side effects occur
Solution Approach 1:
The reversible nitrogen oxides of nitroalkenes serve as intermediary compounds that release nitric oxide in a controlled manner. This intermediary approach allows vasodilation induction while minimizing direct gastrointestinal contact with toxic nitric oxide compounds, thereby reducing gastrointestinal side effects.
Solution Approach 2:
The patent employs compounds that require preliminary biochemical transformation (decomposition into nitric oxide and conjugated nitro linoleic acid) before producing the therapeutic vasodilating effect. This preliminary action step allows for controlled, gradual release of active species, reducing acute gastrointestinal toxicity while maintaining vasodilation efficacy.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The reversible nitrogen oxides of nitroalkenes effectively treat inflammation, obesity, and kidney diseases by inducing vasodilation and reducing metabolic and inflammatory stress, with reduced side effects such as diarrhea, cramping, and inflammatory bowel disease.
Implementation Method 1
reversible nitrogen oxides of nitroalkenes... to release nitric oxide and conjugated nitro linoleic acid
Data Source
AI summary
Various embodiments of this invention are directed to pharmaceutical compositions and methods for treating disease. The compositions of such embodiments include reversible nitroxide derivatives of nitroalkenes. The methods of various embodiments include administering an effective amount of any of these pharmaceutical compositions to a patient in need of treatment.