Quinolone Derivative Composition for Vascular and Cancer Cell Proliferation

Solution Overview

Problem

Current treatments for hyperproliferative vascular disorders such as arteriosclerosis and restenosis, as well as cancers, are inadequate in effectively inhibiting the proliferation of vascular smooth muscle cells and cancer cells, leading to suboptimal prevention and treatment outcomes.

Innovation Solution

Development of a pharmaceutical composition containing specific compounds represented by Formula 1, which inhibit the proliferation of smooth muscle cells and cancer cells, thereby preventing or treating hyperproliferative vascular disorders and cancers, administered in conjunction with a pharmaceutically acceptable carrier.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional chemotherapeutics (alkylating agents, metabolic antagonists, antibiotics) are used to treat cancers and hyperproliferative disorders, then some anticancer effect is achieved, but the inhibition of cell proliferation is insufficient and treatment outcomes are suboptimal

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidcell proliferation inhibition rate

Core Design Contradiction:

ReliabilityVSProductivity

Solution Approach 1:

The patent applies parameter changes by developing a series of quinolone derivative compounds with varying substituent groups (R1-R6) at different positions on the quinolone core structure. By systematically modifying chemical parameters (substituent types, positions, and combinations), the invention achieves enhanced inhibition of vascular smooth muscle cell and cancer cell proliferation, with IC50 values reaching less than 0.03 µM and 0.16 µM respectively, thereby resolving the insufficient proliferation inhibition problem of conventional therapies

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite material principles by creating complex quinolone derivative molecules that combine the core quinolone structure with various functional substituent groups (halo, hydroxyl, cyano, amino, nitro, alkyl, alkoxy, aryl, heteroaryl groups). This composite molecular architecture integrates multiple pharmacophoric elements that work synergistically to achieve superior anticancer and anti-proliferative activity compared to single-function conventional chemotherapeutics

Inventive Principle:

Principle #40Composite materials

2Productivity

If existing substances (heparin, polyanionic benzylglycoside, cyclodextrin) are used to inhibit vascular smooth muscle cell proliferation, then some inhibition effect is observed, but the prevention and treatment outcomes for arteriosclerosis and restenosis remain inadequate

Engineering Contradiction:

Improvesmooth muscle cell proliferation inhibition rateVSAvoidprevention and treatment outcome

Core Design Contradiction:

ProductivityVSReliability

Solution Approach 1:

The patent applies parameter changes by developing a series of quinolone derivative compounds with varying substituent groups (R1-R6) at different positions on the quinolone core structure. By systematically modifying chemical parameters (substituent types, positions, and combinations), the invention achieves enhanced inhibition of vascular smooth muscle cell and cancer cell proliferation, with IC50 values reaching less than 0.03 µM and 0.16 µM respectively, thereby resolving the insufficient proliferation inhibition problem of conventional therapies

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent applies inversion by developing a completely new chemical scaffold (quinolone derivatives) instead of modifying existing anti-proliferative substances. This paradigm shift from optimizing known compounds to creating novel molecular structures with specific anti-proliferative mechanisms enables the achievement of superior therapeutic outcomes for arteriosclerosis and restenosis prevention

Inventive Principle:

Principle #13The other way round (Inversion)

Data Source

PatentEP2124948B1Compositions for treating hyperproliferative vascular disorders and cancers

Publication Date: 2017.07.26 NC BIT INC

Figure 1a~1c

AI summary

The present invention relates to a pharmaceutical composition for preventing or treating hyperproliferative vascular disorders, and a pharmaceutical anticancer composition comprising the compound represented by the Formula 1. The present compounds exhibit IC50 values of less than 0.16 µM for vascular smooth muscle cells and cancer cells to effectively prevent proliferation of vascular smooth muscle cells and cancer cells, thereby ensuring prevention or treatment of hyperproliferative vascular disorders such as arteriosclerosis and restenosis, and cancers.