Isoxazoline Compounds for Parasite Control

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Solution Overview

Problem

Current pesticidal and parasiticidal compounds are ineffective against certain ectoparasites and endoparasites that infest animals, and there is a need for compounds that can also control invertebrate pests damaging crops and plants, as resistance to existing agents is a significant issue.

Innovation Solution

Development of novel isoxazoline compounds of formula (I) that are biologically active against parasites harming animals and pests damaging crops, plants, and wood-derived materials, formulated with pharmaceutically or agriculturally acceptable carriers for administration to animals, plants, or soil.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing pesticidal and parasiticidal compounds are used, then some parasites and pests can be controlled, but resistance development occurs and effectiveness decreases against certain ectoparasites and endoparasites

Engineering Contradiction:
Improveeffectiveness against parasites and pestsVSAvoidresistance development
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs parameter changes by modifying the chemical structure of isoxazoline compounds through various substitutions at positions B1, B2, B3, P1, P2, Y, and Q. These structural parameter changes create novel compounds with improved biological activity and reduced resistance development while maintaining effectiveness against multiple parasite and pest types

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pesticidal and parasiticidal compounds by combining the isoxazoline core structure with various substituent groups and linkers. This composite approach generates molecules with enhanced versatility and effectiveness against both ectoparasites and endoparasites while overcoming resistance issues

Inventive Principle:
Principle #40Composite materials

2Reliability

If existing compounds are used to control parasites, then some parasitic infections can be treated, but they are ineffective against certain ectoparasites and endoparasites

Engineering Contradiction:
Improveparasite control effectivenessVSAvoidspectrum of parasite coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent achieves universality by designing isoxazoline compounds with a core structure that can target multiple parasite types simultaneously. The compounds demonstrate broad-spectrum activity against ectoparasites (fleas, ticks, mites, lice) and endoparasites (nematodes, cestodes, trematodes) through their versatile molecular architecture and multiple interaction sites

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

3Productivity

If existing pesticidal agents are used, then some invertebrate pests can be controlled, but resistance to existing agents is a significant issue

Engineering Contradiction:
Improvepest control efficiencyVSAvoidresistance development
Core Design Contradiction:
ProductivityVSReliability

Solution Approach 1:

The patent applies parameter changes by systematically varying the chemical parameters of isoxazoline compounds including substituents at B1, B2, B3 positions and linkers Q1, Q2, Q3. These parameter modifications produce compounds with novel mechanisms of action that maintain high pest control efficiency while minimizing resistance development

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS10653144B2Pesticidal and parasiticidal vinyl isoxazoline compounds
Publication Date: 2020.05.19 BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC
  • US10653144B2 patent drawing
  • US10653144B2 patent drawing
  • US10653144B2 patent drawing

AI summary

The present invention relates to pesticidal and parasiticidal isoxazoline of formula (I) and salts thereof:wherein variables B1, B2, B3, R1, P1, P2, Y and Q are described herein are as defined in the description. The invention also relates to parasiticidal and pesticidal compositions comprising the isoxazoline compounds of formula (I), processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.