Amido-pyridyl ether compounds for broad-spectrum antiparasitic treatment

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Solution Overview

Problem

Current antiparasitic formulations are not effective against a wide range of parasites, particularly ectoparasites and endoparasites, due to resistance issues and require frequent treatment, and there is a need for a formulation that can be easily applied to animals of various sizes and coat types without needing to be sprinkled over the entire body.

Innovation Solution

Development of 2-amido-pyridyl ether compounds and compositions thereof, which are effective against ectoparasites and endoparasites, allowing for targeted application and treatment of parasitic infestations in animals, including mammals, birds, and fish.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current antiparasitic formulations are used, then treatment of parasites is achieved, but effectiveness is reduced due to resistance development and limited spectrum

Engineering Contradiction:
Improveeffectiveness against parasitesVSAvoidspectrum of parasite coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The pyridyl ether compound of formula I is designed to provide broad-spectrum activity against multiple parasite types simultaneously, including ectoparasites (fleas, ticks, mites, lice) and endoparasites (nematodes, cestodes, trematodes). This multi-functional approach replaces the need for multiple separate treatments with a single compound that addresses diverse parasitic threats.

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

Solution Approach 2:

The patent employs specific molecular structure modifications in the pyridyl ether compound, including variations in substituents R1-R6 and ring structures, to optimize biological activity and overcome resistance mechanisms. These chemical parameter changes enable the compound to maintain effectiveness against resistant parasite populations.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If frequent treatment is applied, then parasite infestations are controlled, but treatment burden and resource consumption increase

Engineering Contradiction:
Improvecontrol of parasite infestationsVSAvoidfrequency of treatment required
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The pyridyl ether compound provides sustained antiparasitic activity that maintains protective levels over extended periods. The formulation is designed to deliver continuous therapeutic effect, reducing the frequency of re-treatment compared to conventional antiparasitic agents and thereby decreasing time loss and treatment burden.

Inventive Principle:
Principle #20Continuity of useful action

3Reliability

If traditional formulations are used, then parasite treatment is achieved, but application complexity increases for animals of various sizes and coat types

Engineering Contradiction:
Improvetreatment efficacyVSAvoidapplication convenience
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The composition is formulated to provide universal applicability across different animal species, sizes, and coat types. The formulation design enables easy application regardless of the specific animal characteristics, eliminating the need for complex application procedures or product selection based on animal type.

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

4Reliability

If complete body coverage is required, then thorough parasite treatment is achieved, but application time and complexity increase

Engineering Contradiction:
Improvethoroughness of parasite treatmentVSAvoidapplication time
Core Design Contradiction:
ReliabilityVSLoss of time

Solution Approach 1:

The formulation is designed to be applied to specific strategic locations on the animal body rather than requiring complete body coverage. The compound distributes effectively from these application sites, achieving thorough parasite treatment while significantly reducing the time and effort required for application.

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP2723716B1Amido-pyridyl ether compounds and compositions and their use against parasites
Publication Date: 2017.01.11 MERIAL LTD

AI summary

The subject matter disclosed herein is directed to amido-pyridyl ether compounds of formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, Ra, a, b and d are as described herein, compositions comprising the compounds of formula I, methods for their preparation and methods for their uses against parasites.