Triaryl Compounds Stimulating Beta-Cell Mass via Telomerase

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Solution Overview

Problem

Current treatments for diabetes lack a cure and effective methods to stimulate or increase pancreatic beta-cell mass, which is crucial for managing insulin levels and glucose regulation.

Innovation Solution

The use of specific tri-phenyl compounds that activate or enhance telomerase expression or activity, leading to the stimulation or increase of pancreatic beta-cell mass in diabetic subjects, thereby improving glucose tolerance and reducing insulin resistance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If conventional diabetes treatments are used, then blood glucose levels can be managed, but pancreatic beta-cell mass cannot be stimulated or increased

Engineering Contradiction:
Improvepancreatic beta-cell massVSAvoidcure effectiveness
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent uses telomerase activators as intermediary substances to indirectly stimulate pancreatic beta-cell mass. Instead of directly targeting beta cells, the compounds activate telomerase, which then promotes beta-cell proliferation and survival through telomere maintenance, resolving the contradiction by introducing a mediating biological pathway

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the biological parameter of telomerase activity to achieve beta-cell mass increase. By administering telomerase activators that modify the telomerase activity parameter, the treatment indirectly increases beta-cell mass, transforming the approach from direct beta-cell targeting to parameter-mediated stimulation

Inventive Principle:
Principle #35Parameter changes

2Reliability

If no new treatment approaches are developed, then current diabetes management continues, but a cure remains unavailable

Engineering Contradiction:
Improvediabetes cureVSAvoidtreatment mechanism
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent extracts and targets a specific biological mechanism (telomerase activity) that is distinct from conventional diabetes treatments. By isolating and activating this specific pathway, the invention creates a novel cure mechanism that differs fundamentally from existing insulin-based or glucose-lowering therapies, thereby achieving a cure while maintaining manageable complexity

Inventive Principle:
Principle #2Taking out (Extraction)

3Quantity of substance

If telomerase activity is not activated, then pancreatic beta-cell mass remains stable, but glucose tolerance deteriorates in diabetic subjects

Engineering Contradiction:
Improvepancreatic beta-cell massVSAvoidglucose tolerance impairment
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by activating telomerase before significant beta-cell loss occurs or to prevent further deterioration. The telomerase activators work prophylactically to maintain telomere length and prevent beta-cell apoptosis, thereby preserving beta-cell mass and preventing glucose tolerance impairment before it worsens

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

The compounds significantly reduce blood glucose levels, increase pancreatic beta-cell mass, and improve glucose tolerance, demonstrating therapeutic potential in managing diabetes and its complications.

Implementation Method 1

the compound can activate or enhance telomerase expression or activity

Methodology Applied
Scientific EffectTelomerase activation:

Data Source

PatentEP3065723B1Compounds for the treatment of diabetes and disease complications arising from same
Publication Date: 2020.09.23 BEN GURION UNIVERSITY OF THE NEGEV
  • EP3065723B1 patent drawingFigure 1A~1B
  • EP3065723B1 patent drawingFigure 2A
  • EP3065723B1 patent drawingFigure 2B

AI summary

The present invention is directed to use of a series of tri-aryl compounds and compositions comprising the same for the treatment of diabetes and disease conditions arising as a consequence of the same.