Merged Ion Channel Modulating Compounds for Arrhythmia Treatment

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Solution Overview

Problem

Current multiple drug therapies for conditions like arrhythmia require high dosing levels, leading to increased physiological stress and adverse side effects due to drug interactions, and are burdensome for patients both financially and in terms of lifestyle.

Innovation Solution

Development of merged compounds that combine the pharmacophores of ion channel modulating compounds and additional therapeutic agents, such as beta-blockers, into a single compound to selectively inhibit cardiac ionic currents, thereby reducing dosing levels and minimizing side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multiple drug therapies are used to treat arrhythmia, then therapeutic effectiveness is improved, but physiological stress and adverse side effects increase due to high dosing levels and drug interactions

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidphysiological stress and adverse side effects

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent merges multiple pharmacophores from different therapeutic agents into a single merged compound. This combines the therapeutic effects of multiple drugs while eliminating the need for high dosing levels and reducing drug interactions, thereby maintaining therapeutic effectiveness while decreasing physiological stress and adverse side effects

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The merged compound performs multiple therapeutic functions simultaneously by incorporating multiple pharmacophores. A single compound can target different ion channels and provide complementary physiological responses, replacing the need for multiple separate drugs and reducing overall physiological stress

Inventive Principle:

Principle #6Universality (Multi-functionality)

2Adaptability or versatility

If multiple therapeutic agents are prescribed in tandem, then comprehensive treatment coverage is improved, but patient burden and cost increase

Engineering Contradiction:

Improvetreatment coverageVSAvoidpatient burden and cost

Core Design Contradiction:

Adaptability or versatilityVSEase of operation

Solution Approach 1:

Multiple therapeutic agents are merged into a single compound formulation. This maintains comprehensive treatment coverage by incorporating multiple pharmacophores while simplifying the patient regimen to a single dose, thereby reducing patient burden and cost

Inventive Principle:

Principle #5Merging (Combining)

3Reliability

If high dosing levels of individual therapeutic agents are used, then desired physiological response is improved, but drug interactions and adverse side effects increase

Engineering Contradiction:

Improvephysiological responseVSAvoiddrug interactions and adverse side effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

Multiple pharmacophores are combined in a single merged compound that achieves the desired physiological response at lower dosing levels. This reduces the concentration of individual drugs in the system, thereby minimizing drug interactions and adverse side effects while maintaining therapeutic effectiveness

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The patent changes the dosing parameter from high levels of individual agents to lower levels of a merged compound. The merged compound's multiple pharmacophores work synergistically to achieve the same physiological response at reduced doses, thereby decreasing the risk of drug interactions and side effects

Inventive Principle:

Principle #35Parameter changes

4Adaptability or versatility

If multiple separate therapeutic agents are administered, then therapeutic versatility is improved, but ease of patient care deteriorates

Engineering Contradiction:

Improvetherapeutic versatilityVSAvoidease of patient care

Core Design Contradiction:

Adaptability or versatilityVSEase of operation

Solution Approach 1:

Multiple therapeutic agents are merged into a single compound formulation. This maintains therapeutic versatility by incorporating multiple pharmacophores with different mechanisms of action while simplifying patient care to a single administration, thereby improving ease of patient care

Inventive Principle:

Principle #5Merging (Combining)

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 merged compounds effectively treat and prevent arrhythmias by reducing the need for high dosing levels, decreasing adverse side effects, and simplifying patient care by providing multiple therapeutic agents in a single formulation.

Implementation Method 1

Merged compounds comprising a pharmacophore of an ion channel modulating compound and a pharmacophore of an additional therapeutic agent

Methodology Applied

Scientific EffectIon channel modulation:

Data Source

PatentUS8058304B2Merged ion channel modulating compounds and uses thereof

Publication Date: 2011.11.15 CORREVIO INT SARL

AI summary

Merged compounds of ion channel modulating compounds, including, for example, merged compounds of the ion channel modulating compound of the following formula: (I) are described herein, as well as methods of making and using such merged compounds and pharmaceutical compositions containing such merged compounds.