Multi-Kinase Compounds for Neuroinflammation and Neurodegeneration

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Solution Overview

Problem

Current therapies are inadequate for conditions involving RIPK1/3 kinases, RIPK2, c-abl, and LRRK2, which contribute to inflammatory and neurodegenerative diseases such as stroke, myocardial infarction, retinal injuries, chronic inflammation, and neuroinflammation diseases like Crohn's disease, Parkinson's disease, and multiple sclerosis.

Innovation Solution

Development of compounds with inhibitory activity against RIPK2, c-abl, and LRRK2 kinases, formulated into pharmaceutical compositions to modulate their activity and treat associated diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapies are used for conditions involving RIPK1/3 kinases, RIPK2, c-abl, and LRRK2, then treatment is provided for some symptoms, but the therapies are inadequate for effectively treating inflammatory and neurodegenerative diseases

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidapplicability to multiple disease conditions
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops compound (I) that simultaneously inhibits multiple kinase targets (RIPK2, c-abl, and LRRK2) with a single molecular structure. This multi-target inhibition approach allows one compound to address multiple inflammatory and neurodegenerative disease conditions, achieving versatility across different pathological mechanisms while maintaining reliable therapeutic effectiveness in each indication

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

2Reliability

If kinase inhibition is achieved to treat neurodegenerative diseases, then therapeutic benefits are provided, but the complexity of targeting multiple kinases increases

Engineering Contradiction:
Improvetherapeutic benefitVSAvoidmolecular structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges the inhibitory functions for three distinct kinases (RIPK2, c-abl, and LRRK2) into a single integrated molecular structure (compound I). This consolidation achieves therapeutic benefits across multiple disease mechanisms without requiring separate compounds for each target, thereby reducing overall treatment complexity while maintaining reliable therapeutic effectiveness

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP4200299B1Compounds for prevention or treatment of neurodegenerative disorders
Publication Date: 2026.03.18 1ST BIOTHERAPEUTICS INC
  • EP4200299B1 patent drawing
  • EP4200299B1 patent drawing
  • EP4200299B1 patent drawing

AI summary

The present disclosure provides a compound of Formula (I) or pharmaceutically acceptable salt, stereoisomers thereof, a pharmaceutical composition comprising the compound, and a method to treat or prevent inflammatory and autoimmune diseases, especially neuroinflammation diseases using the compound.