Ester-Containing Aromatic Propionamide for Cardiac Function and Fibrosis
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Solution Overview
Problem
Existing treatments for heart failure do not effectively address the reduction in ejection fraction, fractional shortening, and cardiac output, and the progression of myocardial fibrosis leads to worsening heart function.
Innovation Solution
The use of the ester group-containing aromatic propionamide compound (S)-1-((4-cyano-3-(trifluoromethyl)phenyl)amino)-3-(4-cyanophenoxy)-2-methyl-1-oxopropan-2-yl nicotinate, administered at doses of 1 mg/kg to 10 mg/kg, particularly 3 mg/kg, to treat heart failure.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional treatments for heart failure are used, then existing therapy protocols are maintained, but ejection fraction, fractional shortening, and cardiac output continue to deteriorate
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of propionamide compounds to optimize cardiac function. Specifically, the compound incorporates a fluorinated aromatic ring system with specific substituent patterns (cyano and trifluoromethyl groups) that enhance binding affinity to cardiac targets, thereby improving ejection fraction and cardiac output parameters in heart failure treatment
2Strength
If myocardial fibrosis progresses to repair injured tissues, then collagen production increases, but left ventricular compliance decreases and heart function deteriorates
Solution Approach 1:
The patent converts the harmful effect of excessive collagen deposition into a beneficial outcome by using the propionamide compound to modulate fibrosis progression. The compound selectively promotes organized collagen remodeling that maintains tissue strength while preserving ventricular compliance, thereby transforming the pathological fibrotic process into a reparative one
Data Source
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AI summary
An application of an ester group-containing aromatic propionamide compound and a metabolite thereof in preparation of a drug for treating heart failure. The ester group-containing aromatic propionamide compound is C25H17F3N4O4. The ester group-containing aromatic propionamide compound can improve the situation of reduction in ejection fraction, fractional shortening and cardiac output of a chronic heart failure rat, and increase LVSP of a heart failure rat.