N-acyldipeptide Derivatives for Skin Thickness and Elasticity

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Solution Overview

Problem

Current treatments for aging-related skin changes are inadequate in effectively addressing intrinsic and extrinsic aging symptoms, such as wrinkles, age spots, and skin thinning, as they often fail to improve skin thickness and elasticity.

Innovation Solution

Compositions comprising gluconolactone and N-acyldipeptide derivatives, specifically represented by the generic Formula (I): R1-AAB-AAC-R2, where R1 is an acyl radical with up to 19 carbon atoms, AAB and AAC are specific amino acids, and R2 includes various functional groups, are administered topically or systemically to alleviate aging-related skin changes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional treatments for aging-related skin changes are used, then treatment simplicity is maintained, but skin thickness improvement and elasticity enhancement are insufficient

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidcomposition complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines gluconolactone with specific N-acyldipeptide derivatives (N-Ac-Tyr-Tyr-OH, N-Ac-Val-Ala-OH) to create a composite composition that synergistically improves skin thickness and elasticity. This composite approach addresses the limitation of conventional single-agent treatments by integrating multiple active components with complementary mechanisms of action.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent specifies precise concentration parameters for each component (gluconolactone at 0.01-10%, N-acyldipeptide derivatives at 0.01-5%) to optimize therapeutic effectiveness. By controlling these compositional parameters, the invention achieves reliable improvement in skin thickness and elasticity while maintaining manageable formulation complexity.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If N-acyldipeptide derivatives are used to improve skin thickness and elasticity, then therapeutic effectiveness increases, but formulation complexity increases

Engineering Contradiction:
Improveskin thickness improvementVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent selects specific N-acyldipeptide derivatives with particular amino acid sequences (Tyr-Tyr and Val-Ala) that have demonstrated efficacy for skin thickness improvement. This targeted selection of specific peptide structures rather than using any dipeptide derivative allows for optimized therapeutic effect while simplifying the formulation approach by focusing on proven active components.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP3777876B1N-acyldipeptide derivatives and their uses
Publication Date: 2023.08.09 NEOSTRATA CO INC

AI summary

N-acyldipeptide derivatives are described. Compositions comprising the N-acyldipeptide derivatives are therapeutically effective for topical or systemic administration to alleviate or improve conditions, disorders, diseases, symptoms or syndromes associated with a tumor, cancer, immune, nervous, vascular, musculoskeletal or cutaneous system, or other tissue or system in a subject.