Aryl Isoxazoline Compounds for Extended Ectoparasite Control

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Solution Overview

Problem

Current aryl isoxazoline compounds do not provide long-lasting protection against ectoparasites in companion animals and livestock, necessitating frequent administration.

Innovation Solution

Development of a compound of formula (I) with specific structural modifications that offer extended half-life and prolonged duration of action, effectively treating and controlling ectoparasites in warm-blooded animals such as dogs, cats, and cattle after a single oral administration or injection.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current aryl isoxazoline compounds are administered to companion animals and livestock, then ectoparasite control is achieved, but the duration of protection is insufficient requiring frequent administration

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

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of aryl isoxazoline compounds through systematic variation of substituents at different positions (R1-R5 on the aryl ring, Q group configurations). These structural parameter changes result in compounds with extended half-lives and prolonged duration of action, achieving months-long protection against ectoparasites after single administration, thereby resolving the contradiction between duration of protection and administration frequency

Inventive Principle:
Principle #35Parameter changes

2Reliability

If frequent administration is required to maintain ectoparasite control, then continuous protection is achieved, but animal burden and treatment complexity increase

Engineering Contradiction:
Improvecontinuous protectionVSAvoidtreatment simplicity
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent implements preliminary action by developing compounds with extremely long half-lives that provide sustained protection for months after a single administration. This preliminary extended action eliminates the need for frequent re-administration, maintaining continuous protection while dramatically simplifying the treatment regimen and reducing animal burden

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS20240287005A1Isoxazoline pesticides
Publication Date: 2024.08.29 ELANCO TIERGESUNDHEIT AG
  • US20240287005A1 patent drawing
  • US20240287005A1 patent drawing
  • US20240287005A1 patent drawing

AI summary

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