N-heteroaryl compounds for broad-spectrum anthelmintic treatment

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Solution Overview

Problem

Current anthelmintic agents face challenges such as evolutionary resistance, limited spectrum of activity, and the need for repeated treatments, making them less effective over time for treating parasitic helminth infections in animals.

Innovation Solution

Development of novel N-heteroaryl compounds that can be used as medicaments, specifically designed to treat a wide range of helminth infections by targeting specific molecular structures, providing a broader spectrum of activity and potentially overcoming resistance issues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If known anthelmintic agents are used to treat helminth infections, then parasitic infections can be treated, but evolutionary resistance develops rendering drugs obsolete over time

Engineering Contradiction:

Improveeffectiveness of anthelmintic agentsVSAvoidduration of drug efficacy

Core Design Contradiction:

ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent modifies the chemical structure of known anthelmintic agents by introducing heteroaryl groups at the R1 position of the piperidine ring, creating novel compounds with altered pharmacological properties that overcome resistance mechanisms while maintaining anthelmintic activity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention combines heteroaryl moieties with piperidine-amide scaffolds to create composite molecular structures that exhibit enhanced biological activity and expanded spectrum against resistant helminth populations

Inventive Principle:

Principle #40Composite materials

2Adaptability or versatility

If known anthelmintic agents are used, then specific parasite types can be treated, but the spectrum of activity is limited

Engineering Contradiction:

Improvespectrum of anthelmintic activityVSAvoideffectiveness against resistant parasites

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The novel N-heteroaryl compounds demonstrate broad-spectrum anthelmintic activity affecting multiple helminth types including nematodes, cestodes, and trematodes, making them universally effective across different parasite categories while maintaining high efficacy against resistant strains

Inventive Principle:

Principle #6Universality (Multi-functionality)

3Productivity

If known anthelmintic agents are administered, then parasitic infections are treated, but repeated treatments are needed

Engineering Contradiction:

Improvetreatment efficacyVSAvoidtime for repeated treatments

Core Design Contradiction:

ProductivityVSLoss of time

Solution Approach 1:

The patent describes compounds with prolonged duration of action that maintain anthelmintic activity over extended periods, reducing the frequency of administration and eliminating the need for repeated treatments while持续 effective against helminth infections

Inventive Principle:

Principle #20Continuity of useful action

Data Source

PatentEP2621903B1N-heteroaryl compounds

Publication Date: 2017.03.01 INTERVET INT BV

AI summary

This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to novel N-heteroaryl compounds and the preparation of said compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.