3-Amino Cyclohexanone Derivatives for Liver Cancer Treatment

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Solution Overview

Problem

Current treatments for liver cancer, such as hepatocellular carcinoma, lack effective agents that can significantly inhibit cancer cell growth, and existing compounds often have limited efficacy.

Innovation Solution

Development of novel anticancer agents, specifically 3-amino derivatives of 4-hydroxy-2,3-dimethoxy-6-methyl-5-(3,7,11-trimethyldodeca-2,6,10-trienyl)cyclohex-2-enone compounds, which exhibit superior inhibition against liver cancer cells compared to their 3-hydroxyl analogs, with some showing 10 to 20-fold better performance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing anticancer agents are used for liver cancer treatment, then treatment can be provided, but efficacy is limited and cancer cell growth inhibition is insufficient

Engineering Contradiction:
ImproveefficacyVSAvoidcancer cell growth inhibition
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of cyclohexanone derivatives, specifically changing substituents at positions 2, 3, and 4 of the cyclohexanone ring (including R1, R2, R3, R4, R5, R6 groups). These structural parameter changes result in compounds with significantly enhanced anticancer activity against liver cancer cells, achieving 10-20 fold improvement in efficacy compared to existing agents.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel 3-amino derivative compounds are developed, then inhibition of liver cancer cells is substantially improved, but compound development complexity increases

Engineering Contradiction:
Improveinhibition efficacyVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies local quality by introducing specific functional groups at particular positions of the cyclohexanone structure. The 3-amino derivative configuration with specific substituents (R1, R2, R3, R4, R5, R6) at defined positions creates localized regions of enhanced biological activity, achieving superior cancer cell inhibition without requiring complete structural redesign of the entire molecule.

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP3416630B1Compositions and methods for treating liver cancer
Publication Date: 2023.10.25 GOLDEN BIOTECHNOLOGY CORP(CN)
  • EP3416630B1 patent drawingFigure 1
  • EP3416630B1 patent drawingFigure 2
  • EP3416630B1 patent drawingFigure 3

AI summary

Provided herein are compositions and methods of treating liver cancer by novel anticancer agents.