Use of physiological cooling active ingredients, and agents containing such active ingredients
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Solution Overview
Problem
Existing TRPM8 modulators have limitations in terms of strength, duration of effect, skin/mucosa irritation, odor, taste, solubility, and volatility, which restrict their applications in cosmetics, nutrition, textiles, OTC products, and pharmaceuticals.
Innovation Solution
Development of novel TRPM8 receptor modulators with specific structural types 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.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If known cooling active ingredient menthane-3-carboxylic acid-N-ethyl amide (WS3) is used, then cooling effect is achieved, but duration of cooling effect is short
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of TRPM8 modulators through systematic variation of R1-R6 substituents in formulas (I), (II), and (III). This structural parameter optimization enables the discovery of compounds with enhanced duration of action while maintaining reliable cooling effects, directly resolving the limitation of short-acting known agents like WS3.
2Temperature
If elevated menthol concentrations are used, then cooling effect is enhanced, but irritation and anaesthetic effect occur
Solution Approach 1:
The patent employs copying by developing novel TRPM8 modulator structures (formulas I, II, III) that replicate and optimize the cooling mechanism of menthol while eliminating its harmful effects. These structurally distinct compounds copy the beneficial TRPM8 activation pathway without producing irritation or anaesthetic side effects, even at effective concentrations.
Solution Approach 2:
The patent uses parameter changes by systematically varying molecular structures (R1-R6 substituents) to optimize the balance between cooling efficacy and irritation potential. This structural parameter optimization identifies compounds that achieve strong TRPM8 activation with minimal harmful effects, resolving the contradiction between cooling intensity and skin tolerance.
3Adaptability or versatility
If traditional cooling agents are used, then cooling effect is achieved, but solubility limitations restrict applications
Solution Approach 1:
The patent applies parameter changes by systematically modifying molecular properties (R1-R6 substituents including hydrophilic groups like OH, OCH3, and ionic groups like COOH) to enhance solubility parameters. This enables the TRPM8 modulators to be effectively formulated in diverse media (aqueous, alcoholic, oily) for expanded applications in cosmetics, nutrition, textiles, and pharmaceuticals.
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 superior cooling effect that is both rapid and long-lasting, reducing irritation and improving solubility, making them suitable for diverse applications beyond traditional cooling agents.
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.
Data Source
AI summary
The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.