Isoxazoline Derivatives With Extended Half-Life for Ectoparasite Control
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Solution Overview
Problem
Existing aryl isoxazoline compounds do not provide long-lasting protection against pests in companion animals and livestock, necessitating frequent reapplication to maintain efficacy.
Innovation Solution
Development of a compound of formula (I) with specific substituents and ring structures that enhance half-life, allowing for extended duration of action after a single oral administration or injection, effectively treating and controlling ectoparasites in animals.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If existing aryl isoxazoline compounds are used, then ectoparasite control is achieved, but the duration of action is short requiring frequent reapplication
Solution Approach 1:
The patent modifies the chemical structure of aryl isoxazoline compounds by changing parameters such as introducing specific substituents (e.g., fluorine atoms at positions 2 and 6 of the phenyl ring), altering the R1-R6 positions, and modifying the heterocyclic ring structure. These parameter changes in molecular structure result in compounds with extended half-life and prolonged duration of action against ectoparasites in companion animals and livestock.
2Reliability
If frequent reapplication is performed to maintain efficacy, then ectoparasite control is maintained, but productivity is reduced due to increased handling and application frequency
Solution Approach 1:
By changing the chemical parameters of the isoxazoline compounds through specific substituent modifications (fluorine substitution, altered alkyl chains, modified heterocyclic structures), the patent achieves compounds that maintain reliable ectoparasite control efficacy for extended periods, thereby reducing the frequency of reapplication and improving productivity.
3Ease of operation
If a single dose is administered, then ease of operation is improved, but duration of action is insufficient
Solution Approach 1:
The patent modifies the molecular parameters of aryl isoxazolines by introducing specific substituents (e.g., fluorine atoms, altered R1-R6 groups) that enhance bioavailability and extend half-life. This allows a single oral administration or injection to provide prolonged protection against ectoparasites for months, maintaining ease of operation while significantly extending duration of action.
Data Source
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.