Isoxazoline Insecticides Overcoming Parasite Resistance
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Solution Overview
Problem
Current methods for controlling invertebrate pests and animal parasites are inadequate due to resistance issues, requiring new compounds that are more effective, less toxic, and environmentally safer with different modes of action.
Innovation Solution
Development of isoxazoline compounds with specific structural features, including geometric and stereoisomers, N-oxides, and salts, for use in compositions that target invertebrate pests and parasites, offering a biologically effective solution for pest control and parasite management.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing parasiticides are used for animal parasite control, then current treatment methods are compromised due to growing resistance, but developing new compounds increases research and development costs and time
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of isoxazoline compounds through systematic variation of substituents at different positions (R1-R6 groups). This structural parameter optimization enables the development of new compounds with improved efficacy against resistant parasites while following established medicinal chemistry frameworks, thus balancing innovation with development efficiency
Solution Approach 2:
The patent implements local quality by introducing specific substituent groups (halogens, alkyl chains, aromatic rings) at targeted positions within the isoxazoline molecular framework. This localized structural modification allows precise tuning of biological activity and resistance-breaking properties without requiring complete redesign of the entire molecule, thereby reducing development time while maintaining reliability
2Reliability
If new isoxazoline compounds are developed to overcome resistance, then effectiveness against invertebrate pests improves, but structural complexity and synthesis difficulty increase
Solution Approach 1:
The patent applies segmentation by dividing the isoxazoline molecule into distinct functional modules (R1-R6 substituent groups) that can be independently optimized. Each substituent position represents a modular unit that can be selectively modified to address specific resistance mechanisms or target different invertebrate pests, allowing complex effectiveness to be achieved through systematic combination of simpler structural elements
Solution Approach 2:
The patent implements universality by designing the isoxazoline core structure with multiple substitutable positions that can accommodate various functional groups. This universal framework allows a single base compound to be adapted for multiple applications against different invertebrate pests and resistance profiles, reducing the need for entirely new molecular designs and thereby managing structural complexity
3Productivity
If conventional insecticides are used for crop protection, then productivity is maintained, but environmental safety and toxicity concerns worsen
Solution Approach 1:
The patent applies the blessing in disguise principle by converting the historical harm of pesticide resistance and environmental toxicity into beneficial outcomes through isoxazoline compounds. These compounds are designed with inherent selectivity and reduced non-target toxicity, transforming the challenge of overcoming resistance into an opportunity to develop safer, more effective pest control solutions that protect both crop productivity and environmental health
Solution Approach 2:
The patent implements mechanics substitution by replacing conventional insecticide mechanisms with a novel isoxazoline mode of action that targets specific invertebrate pest pathways. This substitution reduces reliance on broad-spectrum toxic chemicals and replaces them with more selective compounds that maintain crop protection efficacy while minimizing environmental harm and non-target species impact
Data Source
AI summary
Disclosed are compounds of Formula I, including all geometric and stereoisomers, N-oxides, and salts thereof. Also disclosed are compositions containing the compounds of Formula I and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.