Azatricyclic Antibacterial Compounds Broad-Spectrum Activity

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Solution Overview

Problem

Current antibacterial compounds lack effectiveness against a wide range of bacterial infections, particularly in treating Gram-negative and Gram-positive organisms, and there is a need for new pharmaceutical agents that can target various bacterial infections effectively.

Innovation Solution

Development of novel compounds of formula (I) or their pharmaceutically acceptable salts, solvates, and N-oxides, which are specifically designed to target bacterial infections, comprising a compound with a unique structural formula that includes specific substituents and heterocyclic rings, allowing for effective antibacterial activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibacterial compounds are used, then existing bacterial infections can be treated, but effectiveness against a wide range of bacterial infections (particularly Gram-negative and Gram-positive organisms) is insufficient

Engineering Contradiction:
Improveantibacterial effectivenessVSAvoidbroad-spectrum coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent modifies molecular parameters of antibacterial compounds by introducing specific heterocyclic ring systems (azatricyclic core with nitrogen-containing six-membered rings) and varying substituent groups (R1-R14 positions) to achieve broad-spectrum effectiveness against both Gram-positive and Gram-negative bacteria while maintaining reliability of action

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining a azatricyclic core framework with diverse heterocyclic substituents (pyridine, pyrimidine, triazine, quinoline, isoquinoline, naphthyridine derivatives) to achieve both broad-spectrum coverage and reliable antibacterial activity through synergistic structural elements

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP2041145B1Azatricyclic compounds and their use
Publication Date: 2010.10.27 GLAXO GROUP LTD
  • EP2041145B1 patent drawing
  • EP2041145B1 patent drawing
  • EP2041145B1 patent drawing

AI summary

Tricyclic nitrogen containing compounds),of formula (I) or a pharmaceutically, acceptable salt, solvate and/or N-oxide thereof: and their use as antibacterials.