Benzene- and Azine-Amide Compounds for Resistant Pest Control

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Solution Overview

Problem

Existing pesticides are ineffective against certain animal pests, particularly insects and arthropods, and there is a need for new compounds that can effectively control these pests without causing harm to the environment.

Innovation Solution

Development of benzene- and azine-amide compounds with specific structural features, including various substituents and stereoisomers, which form salts and hydrates, providing pesticidal activity against insects and arthropods.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing pesticides are used to control insect and arthropod pests, then pest control is attempted, but the pesticides are ineffective against certain animal pests

Engineering Contradiction:
Improvepest control effectivenessVSAvoidineffectiveness against certain pests
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent modifies the chemical structure of existing amide compounds by changing molecular parameters - specifically introducing heteroaryl groups (pyridine, pyrimidine, pyrazine, pyridazine rings) at the R2 position and various heterocyclic Q groups. These structural parameter changes create new pesticidal compounds with enhanced activity against previously resistant insect and arthropod pests while maintaining environmental safety.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If new pesticidal compounds are developed to improve pest control effectiveness, then resistance to pests is reduced, but the complexity of compound structure increases

Engineering Contradiction:
Improvepest control effectivenessVSAvoidcompound structure complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent segments the amide molecule into distinct functional regions: the Q group (heterocyclic ring), the R1-R4 substituent positions, and the core amide structure. This segmentation allows systematic variation of specific moieties (particularly Q and R2 groups) to optimize pest control activity while maintaining overall molecular manageability through established chemical nomenclature and structure-activity relationships.

Inventive Principle:
Principle #1Segmentation

3Reliability

If compounds with multiple substituents and stereoisomers are synthesized to enhance pesticidal activity, then pest control performance improves, but the difficulty of manufacturing and purification increases

Engineering Contradiction:
Improvepesticidal activityVSAvoidmanufacturing and purification difficulty
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs preliminary action by establishing clear structure-activity relationships before full synthesis. Key findings from preliminary studies identified heteroaryl groups at R2 and specific Q groups as critical for activity. This allows prioritization of synthesizing compounds with these active moieties first, while deferring or simplifying the synthesis of less active variants, thereby reducing overall manufacturing complexity.

Inventive Principle:
Principle #10Preliminary action

Data Source

PatentUS12528788B2Pesticidally active benzene- and azine-amide compounds
Publication Date: 2026.01.20 SYNGENTA CROP PROTECITON AG
  • US12528788B2 patent drawing
  • US12528788B2 patent drawing
  • US12528788B2 patent drawing

AI summary

Compounds of formula (I) 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.