Substituted Aromatic Compounds for Tissue Regeneration
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Solution Overview
Problem
Current treatments for tissue self-repair and regeneration, particularly in injured organs, are inadequate in effectively stimulating tissue growth and modulating key markers such as metalloproteinases and growth factors, leading to insufficient repair and regeneration outcomes.
Innovation Solution
The development of compounds represented by Formula I and their pharmaceutically acceptable salts, which are administered to subjects to stimulate tissue self-repair, regeneration, and modulate the expression of markers like HGF, LOX, MMPs, AAT, and ILK, promoting tissue growth and repair in organs such as the kidney, heart, liver, skin, and cartilage.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments are used for tissue self-repair and regeneration, then the treatment process is simple, but the effectiveness in stimulating tissue growth and modulating key markers is insufficient
Solution Approach 1:
The patent modifies the basic aromatic compound structure by systematically varying substituents at different positions (R1-R6 groups including halogens, alkyl chains, functional groups) to optimize biological activity. This allows tuning of pharmacological properties to enhance tissue repair effectiveness while maintaining a manageable structural framework based on the core aromatic ring system.
Solution Approach 2:
The invention creates composite molecular structures by combining the aromatic core with multiple different substituent types (halogen atoms, alkyl groups, functional groups like carboxylic acids and esters). This composite approach at the molecular level generates compounds with enhanced and multifaceted biological activities for tissue regeneration.
2Reliability
If compounds of Formula I are administered to stimulate tissue regeneration, then tissue growth and marker expression are enhanced, but the risk of off-target effects and toxicity increases
Solution Approach 1:
The patent introduces specific substituent patterns at defined positions on the aromatic ring (such as halogen atoms at positions 3 and 5, specific alkyl chains at position 4) to create localized chemical characteristics that direct the compound's action toward desired biological targets while minimizing interactions with off-target proteins and receptors.
Solution Approach 2:
The invention utilizes the potential reactivity of functional groups (such as carboxylic acids and esters) that could otherwise cause toxicity by designing them to specifically modulate metalloproteinase and growth factor activity. These same functional groups that might be harmful are converted into beneficial agents that regulate tissue repair processes through controlled modulation of key biological markers.
3Reliability
If compounds are designed to modulate multiple markers simultaneously, then comprehensive tissue repair is achieved, but the difficulty of optimizing compound structure increases
Solution Approach 1:
The patent designs the aromatic compound core with multiple substituent positions that can independently or collectively interact with different biological targets. The core structure serves multiple functions: the aromatic ring provides structural stability, while various substituent groups (halogens, alkyl chains, functional groups) can simultaneously or sequentially modulate different markers including metalloproteinases and growth factors, achieving comprehensive tissue repair through a single multifunctional molecule.
Solution Approach 2:
The invention divides the molecule into distinct functional segments: the core aromatic ring provides structural framework, while separate substituent groups (R1-R6) are positioned to interact with different biological targets. This segmentation allows each part to contribute to specific marker modulation while the overall structure works synergistically to achieve comprehensive tissue repair effects.
Data Source
AI summary
Described herein are compounds of Formula I, or pharmaceutically acceptable salts thereof, or combinations thereof, as well as uses thereof. Such uses include promoting tissue self-repair or tissue regeneration of an organ, stimulating the generation of tissue growth, modulating (e.g., increasing) the level of a tissue-repair marker, treating physical injury in an organ, tissue or cell, promoting wound healing, as well as anti-aging applications. Corresponding compositions, methods, kits, and uses are also described. Formula I wherein A is C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R1 is H, F of OH; R2 is H, F, OH, C5 alkyl, C6 alkyl, C5 alkenyl, C6 alkenyl, C(O)—(CH2)n—CH3 or CH(OH)—(CH2)n—CH3 wherein n is 3 or 4; R3 is H, F, OH, or CH2Ph; R4 is H, F or OH; Q is 1) (CH2), C(O)OH wherein m is 1 or 2 2) CH(CH3)C(O)OH, 3) C(CH3)2C(O)OH, 4) CH(F)—C(O)OH, 5) CF2—C(O)OH or 6) C(O)—C(O)OH.