Triazine Derivative Protects Beta Cells From Apoptosis

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Solution Overview

Problem

Current treatments for type 2 diabetes do not effectively address the progressive beta cell dysfunction that leads to insulin resistance and hyperglycemia, particularly in pre-diabetic individuals where beta cell dysfunction has not yet reached a critical point, and there is a need for a treatment that can delay the onset of the disease.

Innovation Solution

A specific triazine derivative, such as (+)-2-amino-3,6-dihydro-4-dimethylamino-6-methyl-1,3,5-triazine hydrochloride, is used to protect beta cells from cellular death, delaying the onset of type 2 diabetes by maintaining beta cell function and preventing dysfunction in at-risk populations.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current diabetes treatments are used, then glycemic control is achieved, but beta cell dysfunction progresses and cannot be reversed

Engineering Contradiction:
Improvebeta cell function maintenanceVSAvoiddisease progression duration
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent applies preliminary action by administering triazine derivatives to pre-diabetic individuals before beta cell dysfunction reaches a critical point. The compound prevents apoptosis and maintains beta cell mass in advance, thereby delaying the onset of type 2 diabetes rather than treating established disease. This is demonstrated in Example 1 where the compound was administered to pre-diabetic rats to prevent beta cell loss before diabetes developed.

Inventive Principle:
Principle #10Preliminary action

2Reliability

If beta cell mass is increased to compensate for insulin resistance, then glycemic control improves, but beta cell apoptosis increases leading to eventual failure

Engineering Contradiction:
Improveinsulin secretion capacityVSAvoidbeta cell apoptosis
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful effect of inflammatory stress and apoptosis into a beneficial outcome by using triazine derivatives to block apoptotic pathways. In Example 1, the compound treated rat islets with inflammatory stress, and surprisingly protected them from apoptosis rather than causing it, thereby maintaining beta cell mass and function under conditions that would normally be harmful.

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Loss of time

If treatment is started early in pre-diabetes, then disease onset is delayed, but treatment duration and compliance requirements increase

Engineering Contradiction:
Improvetime to disease onsetVSAvoidtreatment duration
Core Design Contradiction:
Loss of timeVSDuration of action of stationary object

Solution Approach 1:

The patent implements preliminary action by initiating treatment in the pre-diabetic stage before clinical disease manifests. Example 1 demonstrates administration to pre-diabetic rats that prevented beta cell loss and delayed diabetes onset. This approach extends the disease-free period but requires prolonged treatment commitment, creating a time-related challenge.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentEP2579880B1Prevention of type 2 diabetes
Publication Date: 2019.09.11 POXEL
  • EP2579880B1 patent drawingFigure 1

AI summary

The present invention relates to triazine derivatives of Formule I for their use in the treatment of Type 2 diabetes, and to compositions comprising said triazine derivatives.