Tricyclic Nitrogen Compounds for Tuberculosis Treatment

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Solution Overview

Problem

Current antibacterial compounds are ineffective against tuberculosis and other bacterial infections, particularly in treating mammalian bacterial infections effectively.

Innovation Solution

Development of novel compounds of formula (I) or their pharmaceutically acceptable salts and N-oxides, which are used to treat bacterial infections, including tuberculosis, by administering an effective amount to mammals, utilizing a method that involves a compound with a specific chemical structure capable of targeting bacterial infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current antibacterial compounds are used, then general bacterial coverage is maintained, but effectiveness against tuberculosis is lost

Engineering Contradiction:
Improveeffectiveness against tuberculosisVSAvoidbroad bacterial coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies the chemical structure of existing antibacterial compounds by introducing specific tricyclic ring systems with nitrogen atoms at defined positions, changing the molecular parameters to achieve tuberculosis efficacy while maintaining broad-spectrum activity

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention combines multiple structural elements (tricyclic core, nitrogen-containing rings, specific substituent patterns) into a composite molecular architecture that achieves both tuberculosis specificity and broad bacterial coverage

Inventive Principle:
Principle #40Composite materials

2Reliability

If novel compounds with specific structures are developed, then tuberculosis treatment efficacy is improved, but compound complexity increases

Engineering Contradiction:
Improvetuberculosis treatment efficacyVSAvoidcompound structural complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The complex antibacterial compound is divided into distinct functional segments: a tricyclic core structure, nitrogen-containing heterocyclic rings, and specific substituent groups, each contributing to different aspects of antibacterial activity and pharmacological properties

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

Specific regions of the molecule are optimized for particular functions: the tricyclic core provides structural stability, nitrogen atoms at specific positions enhance tuberculosis targeting, and substituent groups modulate pharmacokinetic properties, creating local functional specialization within the overall molecule

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS8389524B2Tricyclic nitrogen containing compounds as antibacterial agents
Publication Date: 2013.03.05 GLAXO GROUP LTD
  • US8389524B2 patent drawing
  • US8389524B2 patent drawing
  • US8389524B2 patent drawing

AI summary

Tricyclic nitrogen containing compounds and their use as antibacterials. Z1 and Z2 are independently selected from CH and N.