TRPM8 Modulator Composition for Long-Lasting Skin Cooling

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Solution Overview

Problem

Existing TRPM8 modulators have deficiencies in strength of effect, duration of effect, skin/mucosa irritation, odor, taste, solubility, and volatility, limiting their applications in cosmetics, nutrition, pharmaceuticals, and other fields.

Innovation Solution

Development of novel TRPM8 receptor modulators with specific chemical structures that induce a longer-lasting cooling effect, suitable for various applications including cosmetics, pharmaceuticals, and textiles, by modulating the TRPM8 receptor to create a sensation of coldness without the drawbacks of existing compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If existing TRPM8 modulators (e.g., menthol, WS-23) are used to produce cooling effects, then the cooling sensation is achieved, but the duration of effect is insufficient and irritation occurs

Engineering Contradiction:
Improveduration of cooling effectVSAvoidskin/mucosa irritation
Core Design Contradiction:
Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of TRPM8 modulators through variations in molecular weight, lipophilicity (logP), and functional groups. These parameter changes result in compounds with extended duration of action and reduced irritation compared to existing modulators like menthol and WS-23

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by designing molecules that combine hydrophobic regions (for membrane interaction and prolonged action) with hydrophilic regions (for reduced irritation and improved solubility). The compounds integrate multiple functional elements within a single molecular structure to achieve both extended duration and reduced harmful effects

Inventive Principle:
Principle #40Composite materials

2Strength

If higher concentrations of existing TRPM8 modulators are applied to strengthen cooling effect, then the sensation of coldness is enhanced, but irritation and anaesthetic effects increase

Engineering Contradiction:
Improvestrength of cooling effectVSAvoidirritation and anaesthetic effect
Core Design Contradiction:
StrengthVSObject-affected harmful factors

Solution Approach 1:

The patent utilizes parameter changes by optimizing the potency-to-toxicity ratio through molecular structure modification. The new modulators achieve strong cooling effects at lower concentrations due to improved receptor affinity and selectivity, thereby avoiding the irritation and anaesthetic effects associated with higher concentrations of existing modulators

Inventive Principle:
Principle #35Parameter changes

3Adaptability or versatility

If existing TRPM8 modulators are used in cosmetics and pharmaceuticals, then cooling sensation is provided, but deficiencies in solubility, volatility, and odor limit their applications

Engineering Contradiction:
Improveapplication range in cosmetics and pharmaceuticalsVSAvoidsolubility, volatility, and odor properties
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies parameter changes by systematically adjusting molecular properties including solubility through functional group selection, volatility through molecular weight optimization, and odor characteristics through structural modification. These changes expand the adaptability of the modulators for various cosmetic and pharmaceutical applications while maintaining reliable physical and chemical properties

Inventive Principle:
Principle #35Parameter changes

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 novel modulators provide a longer-lasting cooling effect with reduced irritation and improved properties, expanding their application in cosmetics, pharmaceuticals, and textiles while maintaining effectiveness and safety.

Implementation Method 1

TRPM8 is activated, which brings about a Ca2+ influx into the cold-sensitive neurons. The electrical signal produced as a result is ultimately perceived as a sensation of coldness.

Methodology Applied
Scientific EffectReceptor activation:

Data Source

PatentUS8927605B2Use of physiological cooling active ingredients, and agents containing such active ingredients
Publication Date: 2015.01.06 SYMRISE GMBH & CO KG
  • US8927605B2 patent drawing
  • US8927605B2 patent drawing
  • US8927605B2 patent drawing

AI summary

The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.