Quinoline derivative for treating rheumatoid arthritis

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Solution Overview

Problem

Current treatments for rheumatoid arthritis, such as traditional synthetic DMARDs and glucocorticoids, are costly and have significant side effects, while biological DMARDs are expensive and may lead to relapse or aggravate disease development, and none can prevent disease progression.

Innovation Solution

Administration of a quinoline derivative, specifically 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine, or its pharmaceutically acceptable salts, alone or in combination with other DMARDs, to treat rheumatoid arthritis, improving physical function and quality of life.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional synthetic DMARDs (methotrexate, leflunomide, hydroxychloroquine, sulfasalazine) are used to treat rheumatoid arthritis, then disease progression can be slowed and joints protected from permanent damage, but significant side effects occur including liver damage, bone marrow suppression, and serious lung infections

Engineering Contradiction:
Improvedisease progression controlVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent introduces a novel chemical compound (quinoline derivative with specific molecular structure) that changes the pharmacological parameters of treatment. This new compound aims to achieve similar or better disease control while modifying the safety profile by reducing hepatotoxicity, bone marrow suppression, and pulmonary toxicity associated with traditional DMARDs

Inventive Principle:
Principle #35Parameter changes

2Reliability

If targeted synthetic DMARDs and biological DMARDs are used to treat rheumatoid arthritis, then treatment effectiveness is improved, but treatment cost increases significantly

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtreatment cost
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent presents a small molecule quinoline derivative that can be synthesized cost-effectively compared to expensive biological DMARDs. This approach uses a chemically synthesizable compound rather than complex biologic products, aiming to provide effective treatment at a lower cost burden for patients

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Ease of operation

If glucocorticoids are used alone or in large doses over a long period to control RA symptoms, then rapid symptom relief is achieved, but disease relapse occurs and disease development is aggravated

Engineering Contradiction:
Improvesymptom relief speedVSAvoiddisease progression prevention
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent introduces the quinoline derivative as an intermediary therapeutic agent that can control disease progression and symptoms without the harmful rebound effects of glucocorticoids. This new compound acts as a mediator between symptomatic relief and disease modification, aiming to provide sustained benefit without aggravating disease development upon withdrawal

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS12508258B2Quinoline derivative for treating rheumatoid arthritis
Publication Date: 2025.12.30 CHIA TAI TIANQING PHARMA GRP CO LTD
  • US12508258B2 patent drawing
  • US12508258B2 patent drawing
  • US12508258B2 patent drawing

AI summary

A quinoline derivative for treating rheumatoid arthritis and a use thereof in preparing a pharmaceutical composition for treating rheumatoid arthritis. In particular, a use of the quinoline derivative 1-[[[4-(4-Fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropanamine in treating rheumatoid arthritis.