Quinoline Derivative Combination Therapy for Resistant Soft Tissue Sarcomas

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Solution Overview

Problem

Soft tissue sarcomas are highly malignant tumors with a short median survival time and limited treatment options, particularly for advanced, recurrent, or metastatic cases that are resistant to conventional chemotherapy and radiation therapy.

Innovation Solution

A pharmaceutical combination of a quinoline derivative (Formula I or its pharmaceutically acceptable salt) with a second therapeutic drug, such as chemotherapeutics or immunotherapeutics, is administered to treat soft tissue sarcomas, including regimens like 12 mg of Formula I with 90 mg/m² epirubicin every 3 weeks, optionally combined with radiation therapy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapy and radiation therapy are used to treat soft tissue sarcomas, then treatment options are limited, but treatment effectiveness is insufficient for advanced, recurrent, or metastatic cases

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtreatment options
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent combines the quinoline derivative (anlotinib) with a second therapeutic drug to create a combination therapy regimen. This merging of two different therapeutic agents addresses the insufficiency of single-agent conventional chemotherapy and radiation therapy, providing enhanced treatment effectiveness for advanced, recurrent, or metastatic soft tissue sarcomas while expanding treatment options.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If quinoline derivative alone is used for treatment, then treatment simplicity is maintained, but treatment response is insufficient for resistant cases

Engineering Contradiction:
Improvetreatment responseVSAvoidtreatment regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent merges the quinoline derivative with a second therapeutic drug in a coordinated combination regimen. This combination approach enhances treatment response for resistant cases while maintaining manageable complexity through structured administration protocols.

Inventive Principle:
Principle #5Merging (Combining)

3Reliability

If combination therapy with multiple drugs is used, then treatment response is enhanced, but treatment complexity increases

Engineering Contradiction:
Improvetreatment responseVSAvoidcombination regimen complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines two therapeutic agents (quinoline derivative and second therapeutic drug) in a coordinated manner to enhance treatment response. The combination is structured with defined administration protocols to manage complexity while achieving synergistic anti-tumor effects.

Inventive Principle:
Principle #5Merging (Combining)

4Reliability

If standard chemotherapy doses are used, then treatment safety is maintained, but treatment effectiveness against resistant tumors is insufficient

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent combines the quinoline derivative with a second therapeutic drug at optimized doses to enhance anti-tumor effectiveness against resistant tumors. The combination is designed to achieve synergistic effects while managing toxicity through coordinated administration and dose selection.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentUS12377089B2Quinoline derivative used for soft tissue sarcoma combination therapy
Publication Date: 2025.08.05 CHIA TAI TIANQING PHARMA GRP CO LTD
  • US12377089B2 patent drawing
  • US12377089B2 patent drawing
  • US12377089B2 patent drawing

AI summary

A quinoline derivative used for soft tissue sarcoma combination therapy, relating to a use of the quinoline derivative in combination with a second therapeutic drug to treat soft tissue sarcoma, wherein the second therapeutic drug may be a chemotherapy drug, a small molecule targeted anti-tumour drug or an immunotherapy drug. The chemical name of the quinoline derivative compound I is 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine.