Diazaheterobicyclic Compounds for Selective TASK Channel Blockade

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Solution Overview

Problem

Current treatments for breathing disorders such as obstructive sleep apnea, central sleep apnea, and snoring lack effective and selective blockers for TASK-1 and TASK-3 channels, which are crucial for regulating breathing and have implications in various diseases beyond respiratory issues.

Innovation Solution

Development of (imidazo[1,2-a]pyridin-3-yl)methyl-substituted diazaheterobicyclic compounds that act as potent and selective blockers of TASK-1 and TASK-3 channels, capable of stabilizing upper airways and modulating cellular responses.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current treatments for breathing disorders are used, then existing therapeutic options are available, but effective and selective blockers for TASK-1 and TASK-3 channels are lacking

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidselectivity for TASK-1 and TASK-3 channels
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of compounds to achieve selective blockade of TASK-1 and TASK-3 channels. The invention introduces specific molecular parameters (substituted diazaheterobicyclic structures with imidazo[1,2-a]pyridin-3-yl)methyl groups) that optimize binding affinity and selectivity for these channels, thereby improving treatment effectiveness while maintaining channel selectivity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent segments the therapeutic approach by developing compounds with specific structural divisions: the diazaheterobicyclic core structure is separated and optimized independently, then combined with the (imidazo[1,2-a]pyridin-3-yl)methyl substituent. This segmentation allows independent optimization of each structural element to achieve both effectiveness and selectivity for TASK channels

Inventive Principle:
Principle #1Segmentation

2Reliability

If TASK-1 and TASK-3 channels are blocked, then breathing disorders can be treated, but potential side effects in other systems may occur

Engineering Contradiction:
Improvetreatment efficacyVSAvoidpotential side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds with specific structural features that confer selective action on TASK-1 and TASK-3 channels while sparing other potassium channel families. The substituted diazaheterobicyclic structure with its specific spatial arrangement and electronic properties creates localized interaction with TASK channel binding sites, enabling effective treatment with minimized off-target effects

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP3487856B1Substituted diazahetero-bicyclic compounds and their use
Publication Date: 2025.01.22 BAYER AG
  • EP3487856B1 patent drawing
  • EP3487856B1 patent drawing
  • EP3487856B1 patent drawing

AI summary

The present invention relates to novel (imidazo[1,2-a]pyridine-3-yl)methyl-substituted diazahetero-bicyclic compounds, to methods for preparing same, to their use alone or in combinations for the treatment and/or prevention of diseases, as well as to their use for producing drugs for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of breathing disorders, including sleep-related breathing disorders such as obstructive and central sleep apnea and snoring. The present invention further relates to a method for detecting a compound having TASK-1 and/or TASK-3 blocking properties.