Heterocyclic Potassium Channel Modulators for Neurological Disorders

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Solution Overview

Problem

Current treatments for diseases involving potassium channels lack effective modulators that can specifically target voltage-dependent potassium channels to manage conditions such as epilepsy, pain, and neurological disorders.

Innovation Solution

Development of novel heterocyclic compounds that act as potassium channel modulators, specifically targeting voltage-dependent potassium channels to increase ion flow and treat central or peripheral nervous system disorders by administering effective amounts of these compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for diseases involving potassium channels are used, then existing therapeutic approaches are maintained, but effective modulators that can specifically target voltage-dependent potassium channels are lacking

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidspecificity to voltage-dependent potassium channels
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing novel heterocyclic compounds with specific molecular structures (Formula I) that have distinct chemical properties compared to existing treatments. These structural parameters (ring systems, substituents R1-R6) are optimized to achieve specific binding to voltage-dependent potassium channels, thereby improving both therapeutic effectiveness and channel specificity simultaneously

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel heterocyclic compounds are developed to specifically target voltage-dependent potassium channels, then specificity and therapeutic effectiveness are improved, but the complexity of drug development and characterization increases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidcomplexity of compound structure and testing
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the complex heterocyclic compound into distinct structural modules (core heterocyclic ring system with variable substituents R1-R6). This modular structure allows systematic optimization of specific components while maintaining overall therapeutic effectiveness, thereby managing development complexity through structured design

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies universality by creating a broad class of heterocyclic compounds (Formula I) that can target multiple voltage-dependent potassium channels (Kv1.1-Kv1.6, Kv2.1-Kv2.3, Kv3.1-Kv3.3) with a single structural framework. This multi-functional approach allows one compound class to address various neurological conditions, reducing overall development complexity compared to creating separate targeted therapies for each channel

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

Data Source

PatentEP2178373B1Heterocycles as potassium channel modulators
Publication Date: 2013.01.23 ICAGEN INC
  • EP2178373B1 patent drawing
  • EP2178373B1 patent drawing
  • EP2178373B1 patent drawing

AI summary

Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.