Imidazopyridine LSD1 Inhibitors With Higher Selectivity

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Solution Overview

Problem

Current LSD1 inhibitors lack sufficient selectivity and cause side effects such as drug resistance and toxicity to normal cells, limiting their effectiveness in treating cancer and neoplastic diseases.

Innovation Solution

Development of a novel imidazopyridine derivative compound represented by Formula 1, or its tautomer, stereoisomer, solvate, or pharmaceutically acceptable salt, which effectively inhibits Lysine-specific histone demethylase-1 (LSD1) to treat diseases caused by its abnormal activation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional LSD1 inhibitors are used, then LSD1 inhibition is achieved, but selectivity is insufficient and side effects occur

Engineering Contradiction:

ImproveLSD1 inhibition effectivenessVSAvoidtoxicity to normal cells and drug resistance

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent modifies the chemical structure parameters of LSD1 inhibitors by introducing specific substituents at defined positions (e.g., R1-R6 groups, heterocyclic moieties) to optimize the balance between inhibition potency and selectivity, thereby reducing off-target effects on normal cells

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining imidazopyridine core with various heterocyclic groups and substituents, forming a series of compound analogs (Formulas 1-3) that achieve enhanced selectivity and reduced side effects through structural complexity

Inventive Principle:

Principle #40Composite materials

2Productivity

If existing LSD1 inhibitors are applied, then cancer treatment is attempted, but drug resistance develops

Engineering Contradiction:

Improvecancer treatment effectivenessVSAvoiddrug resistance

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent systematically varies chemical parameters including substituent types, positions, and configurations to generate diverse inhibitor analogs that can overcome resistance mechanisms by targeting different binding modes or affinities

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentUS12479845B2Imidazopyridine derivative compounds and use of same

Publication Date: 2025.11.25 HANMI PHARM CO LTD

AI summary

Provided is a compound selected from a compound of chemical formula 1 having lysine-specific demethylase-1 (LSD1) inhibitory activity, and a tautomer, a stereoisomer, and a solvate thereof, and pharmaceutically acceptable salts of the aforementioned components. The compound is effective in the prevention or treatment of diseases caused by abnormal activation of LSD1. Also disclosed is a composition containing the compound as an active ingredient and its uses in preventing and/or treating diseases caused by abnormal activation of LSD1.