Isoxazoline Pesticide Compounds with Extended Half-Life

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Solution Overview

Problem

Current veterinary and agricultural treatments for ectoparasites in companion animals and livestock often require frequent administration and have limited duration of action, which can be inconvenient and costly.

Innovation Solution

Development of a compound of formula (I) with extended half-life that provides long-lasting protection against ectoparasites in warm-blooded animals, such as dogs, cats, and cattle, after a single oral administration or injection, effectively treating and controlling ectoparasites for months.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current veterinary and agricultural treatments for ectoparasites are used, then ectoparasite control is achieved, but frequent administration is required and duration of action is limited

Engineering Contradiction:
Improveduration of actionVSAvoidfrequency of administration
Core Design Contradiction:
Duration of action of moving objectVSLoss of time

Solution Approach 1:

The patent modifies the chemical structure of isoxazoline compounds by changing parameters such as introducing fluorine atoms at specific positions (R2 and/or R4), modifying the heteroaryl group (X), and adjusting substituents (R5-R10, W1-W6). These structural parameter changes result in compounds with extended half-life and prolonged duration of action against ectoparasites, allowing for less frequent administration while maintaining effective control.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If frequent administration of ectoparasite treatments is performed, then ectoparasite control is maintained, but convenience and cost increase

Engineering Contradiction:
Improveectoparasite controlVSAvoidconvenience
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

By modifying the chemical parameters of the isoxazoline compounds (introducing fluorine atoms, modifying heteroaryl groups, adjusting substituents), the patent creates compounds that maintain reliable ectoparasite control over extended periods. This prolonged duration of action reduces the frequency of administration, thereby improving convenience for animal owners while maintaining effective pest control reliability.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If current ectoparasite treatments are used, then pest control is achieved, but treatment cost increases due to frequent administration

Engineering Contradiction:
Improvepest controlVSAvoidtreatment frequency
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of isoxazoline compounds by introducing fluorine atoms at specific positions and adjusting heteroaryl groups and substituents. These parameter changes result in compounds with extended half-life that provide prolonged pest control duration. Consequently, fewer treatments are required over time, reducing the total quantity of substance administered and lowering overall treatment costs while maintaining reliable pest control effectiveness.

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS20240270729A1(THI)oxazoline pesticides
Publication Date: 2024.08.15 ELANCO TIERGESUNDHEIT AG
  • US20240270729A1 patent drawing
  • US20240270729A1 patent drawing
  • US20240270729A1 patent drawing

AI summary

The present invention provides compounds of formula (I):which are useful for long-lasting treatment and control of pests, optionally fleas and ticks, in companion animals and livestock, and pharmaceutical compositions and methods of using the same.