Indole Compound Therapy for Multiple Sclerosis Recurrence Prevention

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Solution Overview

Problem

Existing therapeutic drugs for multiple sclerosis (MS) are insufficient in treating or preventing the recurrence and progression of the disease, particularly in relapsing-remitting, primary progressive, and secondary progressive MS, and do not effectively manage symptoms such as weakness, ataxia, sensory neuropathy, dysuria, dyschezia, mental disorders, and memory disorders.

Innovation Solution

Compound A, N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide, and its pharmaceutically acceptable salts, particularly the monohydrochloride, are used to treat or prevent MS, including its recurrence and progression, by reducing disease severity and managing symptoms through oral or parenteral administration.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing therapeutic drugs for multiple sclerosis are used, then treatment of MS is provided, but treatment effect is insufficient for preventing recurrence and progression

Engineering Contradiction:
Improvetreatment effectVSAvoidprevention of recurrence and progression
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of indole compounds to create Compound A with optimized ITK inhibitory activity. This structural modification results in enhanced therapeutic efficacy for preventing MS recurrence and progression while maintaining acceptable side effect profiles, directly addressing the insufficiency of existing treatments

Inventive Principle:
Principle #35Parameter changes

2Reliability

If FTY-720 is used for treating multiple sclerosis, then some treatment effect is achieved, but it is insufficient for certain cases

Engineering Contradiction:
Improvetreatment effectVSAvoideffectiveness across different MS cases
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by developing Compound A with modified chemical parameters compared to FTY-720. This creates a new therapeutic agent with enhanced ITK inhibitory activity and improved adaptability to different MS cases including relapsing-remitting, primary progressive, and secondary progressive MS, overcoming the limitations of FTY-720

Inventive Principle:
Principle #35Parameter changes

3Quantity of substance

If low molecular ITK inhibitors are used, then ITK inhibition is achieved, but treatment of MS is not effectively described

Engineering Contradiction:
ImproveITK inhibitionVSAvoidMS treatment efficacy
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The patent applies parameter changes by optimizing the molecular structure of indole compounds to achieve Compound A, which maintains low molecular weight for ITK inhibition while significantly improving MS treatment efficacy. The specific chemical modifications enhance both the quantity of ITK inhibition and the reliability of MS treatment outcomes

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating Compound A as a sophisticated indole compound structure that combines multiple functional groups (indole, indazole, morpholine) to achieve both ITK inhibition and enhanced MS treatment efficacy, surpassing simple low molecular ITK inhibitors

Inventive Principle:
Principle #40Composite materials

Data Source

PatentUS12458646B2Therapeutic or preventing agent for multiple sclerosis including indole compound
Publication Date: 2025.11.04 SHIONOGI & CO LTD
  • US12458646B2 patent drawing
  • US12458646B2 patent drawing
  • US12458646B2 patent drawing

AI summary

The present invention provides a therapeutic agent or prophylactic agent for multiple sclerosis, containing N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide or a pharmaceutically acceptable salt thereof.