Diazine-Amide Compounds for Targeted Insecticidal Efficacy

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Solution Overview

Problem

Current pesticides, particularly those for controlling insects and arthropods, lack efficacy and specificity, leading to environmental and health concerns.

Innovation Solution

Development of novel pesticidally active diazine-amide compounds, specifically those of formula I, which include various substituents and agrochemically acceptable salts, stereoisomers, and N-oxides, to enhance insecticidal activity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current pesticides are used to control insects and arthropods, then pest control function is provided, but efficacy and specificity are insufficient leading to environmental and health concerns

Engineering Contradiction:
Improvepesticidal efficacyVSAvoidenvironmental impact and health risks
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by developing a new chemical compound structure (diazine-amide with specific heteroaryl substituents) that fundamentally alters the molecular parameters of pesticides. This structural modification enables enhanced insecticidal activity through improved binding affinity to target enzymes (acetylcholinesterase) while reducing non-specific toxicity to non-target organisms, thereby resolving the contradiction between efficacy and environmental safety

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs composite material principles by creating complex heteroaryl-diazine-amide structures that combine multiple functional moieties (heteroaryl rings, diazine core, amide linkers) into a single molecular entity. This composite structure allows simultaneous optimization of pest control activity, selectivity, and environmental compatibility that cannot be achieved with simpler pesticide molecules

Inventive Principle:
Principle #40Composite materials

2Reliability

If novel diazine-amide compounds are developed to enhance insecticidal activity, then pesticidal efficacy is improved, but compound structure complexity increases

Engineering Contradiction:
Improveinsecticidal activityVSAvoidmolecular structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the pesticide molecule into distinct functional segments: a heteroaryl group (providing metabolic stability and target binding), a diazine-amide core (providing acetylcholinesterase inhibition), and substitutable positions for optimizing specificity. This modular segmentation allows systematic optimization of insecticidal activity while managing molecular complexity through defined structural domains

Inventive Principle:
Principle #1Segmentation

Data Source

PatentEP3947358B1Pesticidally active diazine-amide compounds
Publication Date: 2025.06.18 SYNGENTA CROP PROTECITON AG
  • EP3947358B1 patent drawing
  • EP3947358B1 patent drawing
  • EP3947358B1 patent drawing

AI summary

Compounds of formula I (l) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides.