Retinylamine Derivatives for Ocular Disorder Treatment
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Solution Overview
Problem
Current treatments for retinal degenerative diseases such as Stargardt disease and age-related macular degeneration are ineffective in preventing or slowing disease progression, and existing therapeutic agents like retinylamine have limitations in stability and side effects.
Innovation Solution
Development of retinylamine derivatives chemically modified with amino acids and peptides to enhance stability, bioavailability, and minimize side effects, including the formation of amide bonds to improve chemical stability and absorption, and the use of biocompatible polymers for controlled release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If retinylamine is used to sequester all-trans-retinal and prevent retinal degeneration, then therapeutic efficacy is improved, but chemical stability and side effect profile worsen
Solution Approach 1:
The patent introduces amino acids and peptides as intermediary molecules that form stable amide bonds with retinylamine. This intermediary structure acts as a protective carrier that maintains the therapeutic activity of retinylamine while improving its chemical stability and reducing side effects through controlled release mechanisms
Solution Approach 2:
The invention creates composite molecular structures by combining retinylamine with amino acids and peptides to form retinylamine derivatives. These composite molecules integrate the therapeutic properties of retinylamine with the stability and biocompatibility of amino acid/peptide backbones, achieving both efficacy and stability simultaneously
2Reliability
If retinylamine is administered to reduce toxic atRAL levels, then retinal protection is improved, but bioavailability and absorption worsen
Solution Approach 1:
The patent modifies the physicochemical parameters of retinylamine by conjugating it with amino acids and peptides of varying molecular weights, hydrophobicities, and structural configurations. These parameter changes enhance the compound's solubility, membrane permeability, and overall bioavailability while maintaining its retinal protective function
Solution Approach 2:
Amino acids and peptides serve as intermediary carriers that facilitate the absorption and delivery of retinylamine across biological membranes. These intermediaries improve gastrointestinal absorption and ocular bioavailability through their inherent transport mechanisms and compatibility with biological systems
3Productivity
If retinylamine is used to inhibit RPE65 isomerase, then atRAL clearance is improved, but side effects increase
Solution Approach 1:
The patent implements periodic controlled release of retinylamine through the degradation of peptide bonds in the conjugated structure. This periodic action provides sustained therapeutic levels while avoiding peak concentrations that cause side effects, maintaining effective atRAL clearance with improved safety
Solution Approach 2:
By modifying the peptide sequence and molecular weight parameters, the patent tunes the release kinetics and specificity of RPE65 inhibition. These parameter changes enhance therapeutic selectivity and reduce off-target effects while maintaining productive atRAL clearance
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 modified retinylamine derivatives effectively prevent light-induced retinal degeneration by sequestering toxic all-trans-retinal, reducing side effects, and providing sustained therapeutic levels, thereby preserving retinal function and structure.
Implementation Method 1
R1 is an amino acid residue, a dipeptide or a tripeptide that is linked to the retinylamine by an amide bond
Implementation Method 2
sequestration of atRAL can reduce the accumulation of A2E-like derivatives, prevent retinal degeneration and preserve vision
Implementation Method 3
The oligopeptide spacer can be degradable by intestinal enzymes during digestion of the composition to provide delayed, and/or sustained delivery
Data Source
AI summary
A pharmaceutical composition includes a retinylamine derivative having the following formula:where R1 is an amino acid residue, a dipeptide or a tripeptide that is linked to the retinylamine by an amide bond.