Taxane Compounds for Resistant Tuberculosis Strains

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Solution Overview

Problem

Current treatments for tuberculosis are hindered by increasing drug resistance in Mycobacterium tuberculosis strains, necessitating the development of novel compounds with effective anti-tuberculosis activity against both sensitive and resistant strains.

Innovation Solution

Development of taxane compounds with specific structural formulas (I, II, and III) that incorporate carbocyclic or heterocyclic aromatic rings, capable of targeting Mycobacterium tuberculosis, including administration methods and pharmaceutical compositions for therapeutic efficacy.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional antibiotics are used to treat tuberculosis, then treatment is effective against sensitive strains, but drug resistance develops in resistant strains

Engineering Contradiction:
Improveanti-tuberculosis efficacyVSAvoideffectiveness against resistant strains
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of taxane compounds by changing parameters such as substituting aromatic rings at specific positions (R1-R8), adjusting side chain lengths (n=1-3), and modifying functional groups (R9, R10, R11). These structural parameter changes create novel compounds that bypass resistance mechanisms while maintaining anti-tuberculosis efficacy against both sensitive and resistant strains.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures by combining taxane core structures with various aromatic ring systems (carbocyclic or heterocyclic) and different side chain configurations. This composite approach generates a diverse library of compounds (formulas I, II, and III) that collectively address the challenge of drug resistance through multiple structural variants.

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If taxane compounds are developed for anti-tuberculosis activity, then effectiveness against resistant strains improves, but compound structure and synthesis complexity increases

Engineering Contradiction:
Improveeffectiveness against resistant strainsVSAvoidcompound structure complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent segments the taxane molecule into distinct functional regions with specific substituents (R1-R11) that can be independently modified. This segmentation allows systematic variation of structural elements (aromatic rings at different positions, different side chains) to optimize activity against resistant strains while managing synthesis complexity through modular approaches.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The taxane core structure serves as a universal platform that can accommodate multiple different aromatic ring systems and side chain configurations. This multi-functionality allows a single core structure to generate multiple active compounds against different strain types, reducing the need to develop entirely new molecular frameworks for each application.

Inventive Principle:
Principle #6Universality (Multi-functionality)

Data Source

PatentUS7615653B2Anti-tuberculosis taxane compounds
Publication Date: 2009.11.10 THE RES FOUND OF STATE UNIV OF NEW YORK
  • US7615653B2 patent drawing
  • US7615653B2 patent drawing
  • US7615653B2 patent drawing

AI summary

The present invention relates to compounds having the formula (I):