1,2-Naphthoquinone Derivative for Leukemia Treatment

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Solution Overview

Problem

Current treatments for acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) are limited by drug resistance and side effects, with existing anticancer drugs failing to achieve complete treatment and causing harm to normal cells, necessitating the development of novel therapies.

Innovation Solution

A pharmaceutical composition containing a 1,2-naphthoquinone derivative compound, which can be formulated into various dosage forms, is used to treat drug-resistant or refractory AML and ALL, offering an effective cell-killing effect without significant harm to normal cells.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapy drugs are used to treat acute leukemia, then cancer cell killing activity is achieved, but drug resistance develops and normal cells are harmed

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

Solution Approach 1:

The patent modifies the chemical structure of naphthoquinone compounds by introducing specific substituents (e.g., at positions 3, 4, 5, 6, 7, or 8) to change the pharmacological parameters of the drug, thereby improving selectivity between cancer cells and normal cells while maintaining cytotoxic activity against leukemia cells

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes the inherent cytotoxicity of naphthoquinone compounds against cancer cells and redirects this harmful effect toward selective cancer cell killing by structural modification, converting a non-selective toxin into a selective anticancer agent that spares normal cells

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

2Productivity

If existing anticancer drugs are administered, then some cancer cells are killed, but complete treatment is not achieved due to drug resistance

Engineering Contradiction:
Improvecell killing rateVSAvoidcomplete treatment achievement
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent divides the treatment approach by creating multiple structurally distinct naphthoquinone derivatives (compounds 1-10 with different substitution patterns), allowing combination therapy or sequential treatment to overcome resistance mechanisms that affect individual drugs

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent combines naphthoquinone core structure with various functional groups and substituents to create composite molecular structures with enhanced and diversified anticancer activities, improving the overall treatment efficacy against resistant leukemia cells

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3782620B1Pharmaceutical composition comprising 1,2-naphthoquinone derivative for use in preventing or treating acute myeloid or lymphoblastic leukemia
Publication Date: 2023.12.20 HUEN CO LTD
  • EP3782620B1 patent drawingFigure 1
  • EP3782620B1 patent drawingFigure 2
  • EP3782620B1 patent drawingFigure 3

AI summary

The present invention relates to a pharmaceutical composition for preventing or treating solid cancer and blood cancers such as acute leukemia and chronic leukemia, comprising a derivative compound of 1,2-naphthoquinone or a pharmaceutically acceptable salt thereof as an effective component. The derivative compound of 1,2-naphthoquinone is highly effective in killing cancer cells of various solid cancers, acute leukemia, and chronic leukemia, and thus can be beneficially used as a pharmaceutical composition for preventing or treating cancers, especially solid cancers, acute leukemia, and chronic leukemia.