Formula I Anthelmintic Compounds for Resistant Parasites

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Solution Overview

Problem

Current anthelmintic agents face challenges such as the development of resistance by parasites, limited spectrum of activity, and the need for repeated treatments, necessitating the development of new compounds to effectively treat a wide range of endoparasitic infections in humans and animals.

Innovation Solution

The development of compounds corresponding to Formula I, which include specific structural elements like various alkyl, alkenyl, cycloalkyl, phenyl, and heteroaryl groups, along with linkers and nitrogen-containing chains, to create effective anthelmintic agents.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If known anthelmintic drugs are used to treat endoparasitic infections, then current parasitic infections can be treated, but parasites develop resistance rendering the drugs obsolete over time

Engineering Contradiction:
Improveeffectiveness of anthelmintic treatmentVSAvoidlong-term efficacy of drug
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent applies parameter changes by developing compounds with novel molecular structures (Formula I) that differ from existing anthelmintic classes. The specific structural parameters including the heteroaryl group, linker chain with nitrogen atoms, and substituted alkyl groups create a new chemical space that parasites have not developed resistance against, thereby maintaining long-term treatment effectiveness

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining multiple functional elements: a heteroaryl group (X1), a linker chain (X3) with nitrogen atoms, and various substituted groups (X4-X9). This composite structural approach generates a new class of anthelmintic agents with potentially enhanced and sustained efficacy against resistant parasite populations

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If existing anthelmintic agents are used, then treatment can be provided, but the spectrum of activity is limited and repeated treatments are needed

Engineering Contradiction:
Improvespectrum of activityVSAvoidfrequency of repeated treatments
Core Design Contradiction:
Adaptability or versatilityVSLoss of time

Solution Approach 1:

The patent achieves universality through the versatile Formula I structure that can target multiple parasite types simultaneously. The molecular framework with variable substituents (X1-X9) allows the compound to interact with conserved biological targets across different endoparasite species, providing broad-spectrum activity in a single treatment

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

Solution Approach 2:

The invention modifies key molecular parameters including the introduction of nitrogen-containing linker chains and specific heteroaryl groups that enhance the compound's ability to bind to diverse parasite targets, thereby expanding the spectrum of activity and reducing the need for repeated treatments

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9096524B2Anthelmintic agents and their use
Publication Date: 2015.08.04 INTERVET INT BV
  • US9096524B2 patent drawing
  • US9096524B2 patent drawing
  • US9096524B2 patent drawing

AI summary

This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.