GPR40 Agonist Oral Diabetes Treatment

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Solution Overview

Problem

Current diabetes treatments, such as sulfonylureas and incretin-related drugs, have side effects like hypoglycemia, liver issues, and weight gain, and require injection, necessitating a new mechanism for insulin secretion that avoids these drawbacks.

Innovation Solution

Development of novel compounds acting as GPR40 receptor agonists, which stimulate insulin secretion in a blood glucose concentration-dependent manner, formulated into pharmaceutical compositions for oral administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If sulfonylureas are used to promote insulin secretion, then insulin secretion is improved, but hypoglycemia occurs

Engineering Contradiction:

Improveinsulin secretionVSAvoidhypoglycemia

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the mechanism parameter from direct insulin secretion stimulation (sulfonylureas) to GPR40 receptor-mediated glucose-dependent insulin secretion. The compound of Formula (1) acts on GPR40 receptors to stimulate insulin secretion only when glucose is present, eliminating hypoglycemia while maintaining insulin secretion efficacy.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If incretin-related drugs are used, then insulin secretion is improved, but injection administration is required

Engineering Contradiction:

Improveinsulin secretionVSAvoidadministration method

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the injection administration route (mechanical delivery system) with an orally administrable small molecule compound that acts on GPR40 receptors. The compound of Formula (1) can be administered orally and still effectively stimulate insulin secretion through GPR40-mediated mechanisms, eliminating the need for injection.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

3Reliability

If existing diabetes treatments are used, then blood glucose control is improved, but side effects such as liver failure and weight gain occur

Engineering Contradiction:

Improveblood glucose controlVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and utilizes the beneficial GPR40 receptor-mediated insulin secretion mechanism while excluding the harmful side effects associated with existing diabetes treatments. By targeting specifically the GPR40 pathway, the compound of Formula (1) achieves blood glucose control without the liver failure, weight gain, and other side effects of conventional therapies.

Inventive Principle:

Principle #2Taking out (Extraction)

Data Source

PatentUS9988379B2GPR40 receptor agonist, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent

Publication Date: 2018.06.05 LG CHEM LTD

AI summary

The present invention relates to a novel compound having GPR40 receptor agonist activity that promotes insulin secretion and inhibits blood sugar rise after glucose loading, and is thereby useful for the treatment of diabetes and complications thereof, the preparation method thereof and pharmaceutical composition containing them as an active ingredient.