Bis-aromatic Amide Sweeteners Receptor Binding

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Solution Overview

Problem

There is a need for new and improved flavoring agents and sweeteners that can induce sweetness at extremely low concentrations and enhance the sweetness of existing natural or artificial sweeteners, particularly to address the growing issues of weight gain and associated diseases like diabetes.

Innovation Solution

Development of bis-aromatic amide compounds that bind to T1R2/T1R3 sweet receptors at low concentrations, acting as high-intensity sweeteners or sweet flavor enhancers when combined with other sweeteners, thereby reducing the required amounts of caloric sweeteners in food and beverage compositions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If high-intensity sweeteners are used to reduce caloric sweetener amounts, then sweetness perception is improved at low concentrations, but the complexity of flavor formulation increases

Engineering Contradiction:
Improveconcentration of sweetenerVSAvoidflavor formulation complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by systematically varying molecular structures of amide compounds (changing chemical parameters) to achieve optimal sweetness intensity and receptor binding affinity. This allows formulation of high-intensity sweeteners that deliver potent sweetness at extremely low concentrations while maintaining manageable formulation complexity through structure-activity relationship optimization

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by combining bis-aromatic amide compounds with existing sweeteners or flavor compounds to create synergistic formulations. These composite flavor compositions leverage the high sweetness intensity of the amide compounds while incorporating complementary compounds to achieve balanced flavor profiles, thereby managing overall formulation complexity

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If new high-intensity sweeteners are discovered, then sweetness induction at low concentrations is improved, but the time and resources required for discovery and development increase

Engineering Contradiction:
Improvesweetness induction concentrationVSAvoiddiscovery and development time
Core Design Contradiction:
Quantity of substanceVSLoss of time

Solution Approach 1:

The patent applies preliminary action by conducting extensive in silico modeling and in vitro screening of amide compound derivatives before proceeding to in vivo testing and commercial development. This preliminary characterization of structure-activity relationships and receptor binding properties of various amide structures accelerates the discovery process by identifying promising candidates early, reducing overall development time and resource investment

Inventive Principle:
Principle #10Preliminary action

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

These bis-aromatic amide compounds effectively activate sweet receptors at micromolar concentrations, allowing for the formulation of comestible compositions with lower levels of traditional sweeteners, providing a high-intensity sweet taste while addressing health concerns related to sugar consumption.

Implementation Method 1

bis-aromatic amide compounds that bind to T1R2/T1R3 sweet receptors at low concentrations

Methodology Applied
Scientific EffectReceptor binding:

Data Source

PatentUS7842324B2Bis-aromatic amides and their uses as sweet flavor modifiers, tastants, and taste enhancers
Publication Date: 2010.11.30 SENOMYX INC
  • US7842324B2 patent drawing
  • US7842324B2 patent drawing
  • US7842324B2 patent drawing

AI summary

The inventions disclosed herein relate to man-made bi-aromatic amide compounds that, when contacted with comestible food or drinks or pharmaceutical compositions at concentrations preferably on the order of about 100 ppm or lower, serve as sweet taste modifiers, sweet flavoring agents, or sweet flavor enhancers, for use in foods, beverages, and other comestible products, or orally administered medicinal products or compositions, optionally in the presence of or in mixtures with conventional flavoring agents such as known natural saccharide sweeteners and previously known artificial sweeteners.