Quinoline Compound Combination Therapy for Metastatic Ewing's Sarcoma

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Solution Overview

Problem

Current treatments for Ewing's sarcoma, including surgery, radiotherapy, and single-drug chemotherapy, are inadequate in preventing metastasis and result in significant toxic side effects, with a low 5-year survival rate and limited effectiveness against advanced or metastatic cases.

Innovation Solution

A quinoline compound, 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine, or its pharmaceutically acceptable salts, is administered in various forms and routes to treat Ewing's sarcoma, particularly in combination with other therapeutic agents to enhance efficacy and reduce side effects.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If multi-drug combination chemotherapy is used to improve survival rate, then the 5-year survival rate is remarkably improved, but long-term chemotherapy results in toxic and side effects on multiple body systems

Engineering Contradiction:
Improve5-year survival rateVSAvoidtoxic and side effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters of the treatment by introducing a novel quinoline compound with specific molecular structure (1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine) that has different pharmacological properties from conventional chemotherapeutic agents, aiming to achieve similar or better anti-tumor efficacy with reduced toxicity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs a composite treatment approach by combining the quinoline compound with other therapeutic agents (radiotherapy, surgery, or conventional chemotherapy drugs), creating a multi-modal treatment regimen that leverages the synergistic effects of different treatment modalities to improve outcomes while potentially reducing the burden of each individual treatment

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional chemotherapy drugs are used to treat Ewing's sarcoma, then tumor growth is inhibited, but the treatment is inadequate against advanced or metastatic cases and causes significant side effects

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidside effects
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces a novel chemical compound with a unique quinoline core structure and specific substituents (fluoro group, methoxy group, indole moiety, cyclopropylamine group) that fundamentally changes the pharmacological parameters of the treatment, providing improved efficacy against advanced and metastatic Ewing's sarcoma while reducing toxicity to normal tissues

Inventive Principle:
Principle #35Parameter changes

3Ease of operation

If surgery, radiotherapy or single-drug chemotherapy is used for treatment, then the treatment process is simple, but the effect is not ideal and the 5-year survival rate is no more than 10%

Engineering Contradiction:
Improvetreatment simplicityVSAvoid5-year survival rate
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent merges multiple treatment modalities by combining the quinoline compound with radiotherapy, surgery, or conventional chemotherapy in a comprehensive treatment regimen, thereby integrating the advantages of different approaches to achieve superior outcomes compared to any single modality alone

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP3957631B1Quinoline compound or pharmaceutically acceptable salt thereof for treating ewing's sarcoma
Publication Date: 2025.09.10 CHIA TAI TIANQING PHARMA GRP CO LTD
  • EP3957631B1 patent drawing
  • EP3957631B1 patent drawing
  • EP3957631B1 patent drawing

AI summary

The present invention belongs to the field of medicine, and provides a quinoline compound or a pharmaceutically acceptable salt thereof for treating Ewing's sarcoma, and particularly relates to use of compound I or a pharmaceutically acceptable salt thereof in the preparation of a medicament for treating Ewing's sarcoma and use of compound I or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent in the preparation of a combination medicament for treating Ewing's sarcoma. The chemical name of compound I is 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropanamine.