Imidazopyridine Modulators for Selective α2/3-GABAA Receptor Activity

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing compounds exhibit poor affinity and positive modulatory activity towards α2/3-GABA A receptors, leading to potential side effects associated with GABA A receptor modulators.

Innovation Solution

Development of imidazopyridine or imidazopyrazine compounds with specific structural variations to enhance affinity and positive modulatory activity for α2/3-GABA A receptors.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing GABA A receptor modulators are used, then receptor modulatory function is achieved, but affinity and positive modulatory activity towards α2/3-GABA A receptors are poor

Engineering Contradiction:

Improveaffinity and positive modulatory activityVSAvoidselectivity for α2/3-GABA A receptors

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies molecular parameters of GABA A receptor modulators by introducing specific imidazopyridine or imidazopyrazine structural motifs with defined substituents (R1-R11 groups), changing chemical parameters to achieve excellent affinity and positive modulatory activity specifically for α2/3-GABA A receptors while reducing side effects

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent applies local quality by introducing specific functional groups (imidazopyridine or imidazopyrazine cores with particular R1-R7 substituents) at specific positions in the molecule to enhance interaction with α2/3-GABA A receptors, while keeping other regions modified to optimize pharmacological properties

Inventive Principle:

Principle #3Local quality

2Reliability

If GABA A receptor modulators are used to treat various conditions, then therapeutic effect is achieved, but side effects such as sedation, addiction, drowsiness, and amnesia occur

Engineering Contradiction:

Improvetherapeutic effectVSAvoidside effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful side effects associated with conventional GABA A modulators into benefits by designing compounds that selectively target α2/3-GABA A receptors, thereby maintaining therapeutic effects while eliminating sedation, addiction, drowsiness, and amnesia side effects through reduced interaction with α1-GABA A receptors

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent segments the GABA A receptor subtypes (α1-δ, ε, ρ1-2 subunits) and designs compounds with selective affinity for α2/3 subunits, separating the therapeutic function from the harmful side effects by targeting only specific receptor segments

Inventive Principle:

Principle #1Segmentation

Data Source

PatentEP4703359A1Imidazopyridine or imidazopyrazine compound, preparation method therefor, and pharmaceutical composition and use thereof

Publication Date: 2026.03.04 SHANGHAI SIMR BIOTECHNOLOGY CO LTD

AI summary

Disclosed in the present invention are an imidazopyridine or imidazopyrazine compound, a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention provides an imidazopyridine or imidazopyrazine compound and an isotope derivative, a nitrogen oxide, a pharmaceutically acceptable salt, a solvate, or a pharmaceutically acceptable salt solvate thereof. The imidazopyridine or imidazopyrazine compound provided by the present invention has excellent affinity activity and positive regulation activity on an α2/3-GABAA receptor.