Multi-Drug Anti-TB Compound Formula I

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Solution Overview

Problem

Current treatments for tuberculosis are hindered by the emergence of multidrug-resistant and extensively drug-resistant strains of Mycobacterium tuberculosis, necessitating the development of new drug compounds to effectively treat mycobacterial infections.

Innovation Solution

The development of compounds according to Formula (I) and their pharmaceutically acceptable salts, which are used in pharmaceutical compositions for the treatment of tuberculosis and other mycobacterial infections, targeting specific therapeutic agents to combat resistant strains.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If combination therapies of three or more drugs are used to prevent resistance, then the effectiveness of treatment is improved, but the complexity of the treatment regimen increases

Engineering Contradiction:
Improveeffectiveness of treatmentVSAvoidcomplexity of treatment regimen
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent combines multiple anti-TB drug activities into a single compound molecule (Formula I). The compound integrates structural features associated with isoniazid, rifampicin, and other first-line anti-TB drugs, allowing one molecule to exert multiple therapeutic effects simultaneously, thereby preventing resistance without requiring patients to take multiple separate medications

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The compound of Formula (I) is designed to perform multiple functions: it acts as an anti-TB agent, prevents drug resistance development, and can be used in both drug-susceptible and multidrug-resistant TB treatments. The molecule's structure allows it to target multiple bacterial mechanisms, making it a universal solution for various TB scenarios

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

2Reliability

If multiple second-line drugs are administered for MDR-TB treatment, then the treatment coverage is improved, but the duration and complexity of therapy increases

Engineering Contradiction:
Improvetreatment coverageVSAvoidduration of therapy
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the chemical structure parameters of existing anti-TB drugs by creating a novel compound (Formula I) that incorporates key pharmacophoric elements of multiple first-line drugs. This structural parameter change results in a compound with enhanced activity against MDR-TB strains, potentially reducing the need for prolonged second-line therapy

Inventive Principle:
Principle #35Parameter changes

3Reliability

If standard four-drug combination therapy is used for drug-susceptible TB, then the cure rate is improved, but the treatment duration extends to six months

Engineering Contradiction:
Improvecure rateVSAvoidtreatment duration
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The compound of Formula (I) is designed to preemptively address resistance development by incorporating structural elements of multiple first-line anti-TB drugs (isoniazid, rifampicin, pyrazinamide, ethambutol). This preliminary integration of multiple drug activities into one molecule allows for rapid bacterial killing and resistance prevention, potentially shortening the overall treatment duration while maintaining high cure rates

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS20250129084A1Compounds
Publication Date: 2025.04.24 UNIVERSITY OF DUNDEE
  • US20250129084A1 patent drawing
  • US20250129084A1 patent drawing
  • US20250129084A1 patent drawing

AI summary

The invention relates to compounds or pharmaceutically acceptable salts thereof, compositions containing them, including combinations with at least one additional therapeutic agent, and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by a mycobacterium, such as tuberculosis.