Bis-indolylmethane Adjuvants Potentiate Antibiotic Activity

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Solution Overview

Problem

Current antibiotic development is hindered by the high cost and low investment returns, leading to a lack of new antibiotics and strategies to combat antibiotic resistance.

Innovation Solution

Development of antimicrobial agents and compounds that potentiate existing antimicrobial agents, specifically pharmaceutical compositions containing compounds with Formula A or B, which enhance the activity of antibiotics and overcome resistance mechanisms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If new antibiotics are developed through traditional methods, then antibiotic activity is improved, but development cost and time increase significantly

Engineering Contradiction:
Improveantibiotic activityVSAvoiddevelopment time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The patent applies preliminary action by developing adjuvant compounds that can be combined with existing antibiotics. Instead of developing entirely new antibiotics from scratch, the invention prepares auxiliary agents in advance that enhance the effectiveness of already-established antibiotics, thereby reducing development time while maintaining or improving antibiotic activity.

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent employs composite materials by creating pharmaceutical compositions that combine adjuvant compounds with existing antibiotics. These composite formulations leverage the synergistic effects between the adjuvant and the antibiotic, achieving enhanced antimicrobial activity without requiring the lengthy development process of creating a completely new antibiotic molecule.

Inventive Principle:
Principle #40Composite materials

2Productivity

If investment in antibiotic development increases, then new antibiotics are developed, but investment returns decrease

Engineering Contradiction:
Improveantibiotic development outputVSAvoidinvestment return
Core Design Contradiction:
ProductivityVSLoss of energy

Solution Approach 1:

The patent applies universality by creating adjuvant compounds that can work with multiple different antibiotic classes. A single adjuvant compound can enhance the activity of various antibiotics against different resistant pathogens, allowing pharmaceutical companies to develop one versatile agent that serves multiple therapeutic purposes, thereby improving productivity while reducing the need for extensive separate development programs.

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

Solution Approach 2:

The patent employs parameter changes by modifying the pharmacological parameters of existing antibiotics through combination with adjuvants. Rather than changing the fundamental antibiotic molecule, the invention alters the effective concentration, spectrum of activity, or resistance-breaking capability by combining with auxiliary compounds, thus achieving development output with reduced investment risk.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If adjuvant compounds are developed to overcome resistance, then antibiotic effectiveness is improved, but the number of clinically approved adjuvants remains limited

Engineering Contradiction:
Improveantibiotic effectivenessVSAvoidnumber of approved adjuvants
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent applies segmentation by dividing the resistance problem into specific mechanisms and developing targeted adjuvant compounds for each. Rather than seeking a single universal solution, the invention creates multiple specialized adjuvants that address different resistance mechanisms (e.g., efflux pumps, beta-lactamases, membrane permeability), thereby increasing the overall number of approved adjuvants through focused development programs.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs intermediary compounds that mediate between the antibiotic and the resistant pathogen. These adjuvant compounds act as intermediaries that either inhibit resistance mechanisms or enhance antibiotic penetration, providing a bridge that restores antibiotic effectiveness without requiring direct modification of the antibiotic molecule itself.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS12285407B2Bis-indolylmethane derivatives and uses thereof
Publication Date: 2025.04.29 UNIVERSITY OF THE WEST INDIES
  • US12285407B2 patent drawing
  • US12285407B2 patent drawing
  • US12285407B2 patent drawing

AI summary

A pharmaceutical composition is described herein, including an antimicrobial agent and a compound having Formula A, or Formula B. Methods of using the pharmaceutical compositions to treat microbial infection are also described.