Oxatriazolium-5-olate Activates Soluble Guanylate Cyclase for Endothelial Dysfunction

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Solution Overview

Problem

Current pharmaceutical agents for treating sexual disorders do not effectively promote local NO production or provide a hypotensive effect, making them ineffective for addressing endothelial dysfunction-related issues such as erectile dysfunction.

Innovation Solution

The use of 3-(3-[1,2,4]-triazolo)-oxatriazolium-5-olate as an active ingredient in pharmaceutical compositions to treat sexual disorders, which activates soluble guanylate cyclase and increases cGMP synthesis, thereby improving endothelial function and sexual potency.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current pharmaceutical agents are used to treat sexual disorders, then sexual dysfunction symptoms may be temporarily addressed, but they fail to promote local NO production and do not provide hypotensive effect, making them ineffective for addressing endothelial dysfunction

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidability to address endothelial dysfunction
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical structure parameter by using oxatriazolium-5-olate derivatives instead of conventional agents. These compounds activate soluble guanylate cyclase and increase cGMP levels, producing both hypotensive effects and improved endothelial function, thereby simultaneously addressing multiple parameters (blood pressure, NO production, endothelial health) that conventional agents fail to modify

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The oxatriazolium-5-olate derivative serves multiple functions: it acts as a vasodilator by activating soluble guanylate cyclase, promotes local NO production, provides hypotensive effect, and improves endothelial function. This multi-functionality resolves the contradiction by making a single agent capable of addressing both sexual dysfunction symptoms and underlying endothelial dysfunction

Inventive Principle:
Principle #6Universality (Multi-functionality)

2Ease of operation

If conventional pharmaceutical agents are administered, then some sexual dysfunction symptoms may be relieved, but local nitric oxide production remains insufficient and blood pressure remains elevated

Engineering Contradiction:
Improvesymptom reliefVSAvoidlocal NO production
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent introduces oxatriazolium-5-olate as an intermediary substance that activates soluble guanylate cyclase, which in turn increases cGMP levels. This intermediary mechanism indirectly promotes NO production and vasodilation, achieving both symptom relief and increased local NO production through a mediating biochemical pathway rather than direct NO administration

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If traditional treatments for sexual disorders are used, then erectile dysfunction may be partially managed, but endothelial dysfunction and hypertension persist

Engineering Contradiction:
Improvesexual function improvementVSAvoidendothelial dysfunction and hypertension
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies preliminary action by using oxatriazolium-5-olate to pre-condition the vascular system through soluble guanylate cyclase activation and cGMP increase. This preliminary vasodilatory and endothelial-protective action creates a favorable physiological state that enhances subsequent sexual function and prevents endothelial damage, addressing both sexual dysfunction and cardiovascular risk factors in advance

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 compound provides a dose-dependent activation of soluble guanylate cyclase, leading to significant improvements in endothelial function and sexual activity parameters, including reduced blood pressure, increased nitric oxide production, and enhanced sexual performance in animal models.

Implementation Method 1

The compound provides a dose-dependent activation of soluble guanylate cyclase, leading to significant improvements in endothelial function

Methodology Applied
Scientific EffectSoluble guanylate cyclase activation: Enzyme

Implementation Method 2

increased nitric oxide production

Methodology Applied
Scientific EffectNitric oxide synthesis: Chemical Bonding

Data Source

PatentEP3165223B1Use of 3-(3-[1,2,4]-triazolo)-oxatriazolium-5-olate for treating sexual disorders
Publication Date: 2019.06.26 OBSHCHESTVO S OGRANICHENNOJ OTVETABTVENNOSTJU KONSORTSIUM - PIK
  • EP3165223B1 patent drawingFigure 1
  • EP3165223B1 patent drawingFigure 2
  • EP3165223B1 patent drawingFigure 3

AI summary

The invention belongs to the chemical and pharmaceutical industry, including the creation of a new medicinal agent intended to treat sexual disorders, and can be used in the biochemistry, physiology and medicine.