Fused Ring Anthranilate Derivatives for Anti-Fibrotic Therapy
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Solution Overview
Problem
Current treatments for tissue fibrosis, such as those using tranilast, have limitations due to side effects and genetic susceptibility issues, necessitating the development of alternative compounds with improved anti-fibrotic, anti-inflammatory, and anti-proliferative properties.
Innovation Solution
Development of fused ring derivatives of 2-{[(2E)-3-(3,4-dimethoxyphenyl)prop-2-enoyl]amino}benzoic acid and their pharmaceutical compositions, which can inhibit fibrosis and inflammation by targeting specific molecular pathways.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If tranilast is used to treat fibrotic conditions, then anti-fibrotic efficacy is improved, but side effects and genetic susceptibility issues worsen
Solution Approach 1:
The patent divides the molecular structure of tranilast into distinct functional segments and modifies specific portions. By segmenting the molecule and selectively modifying particular groups (such as changing the anthranilic acid core to fused ring systems), the invention maintains the anti-fibrotic active segments while removing or modifying segments responsible for harmful effects and genetic interactions.
Solution Approach 2:
The patent systematically changes molecular parameters including chemical structure, stereochemistry, and physical properties. By altering parameters such as replacing hydrogen atoms with different groups, changing bond configurations, and modifying molecular weight, the invention creates derivatives that maintain therapeutic efficacy while reducing harmful effects and genetic susceptibility issues.
2Reliability
If existing anti-fibrotic agents are used, then fibrosis treatment is achieved, but treatment limitations due to side effects occur
Solution Approach 1:
The patent identifies harmful factors in the original tranilast structure (such as specific functional groups causing side effects) and converts them into beneficial features. By modifying these problematic segments into different chemical groups, the invention transforms potential harmful elements into components that enhance safety profile while preserving anti-fibrotic activity.
Solution Approach 2:
The patent creates composite molecular structures by combining different chemical moieties in fused ring systems. These composite structures integrate the beneficial anti-fibrotic properties of tranilast with the safety advantages of alternative chemical groups, resulting in molecules that achieve effective fibrosis treatment with reduced side effects.
Data Source
AI summary
The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.


