Pyrazolopyridine-diamides for Broad-Spectrum Insecticidal Control

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Solution Overview

Problem

Existing anthranilic acid derivatives and fused bicyclic anthranilic diamides exhibit a narrow spectrum of insecticidal and acaricidal activity and have unsatisfactory environmental and biological properties.

Innovation Solution

Development of novel pyrazolopyridine-diamides with specific structural formulas that offer improved insecticidal and acaricidal activity, broader application spectrum, and enhanced plant compatibility, which can be used in combination with other biologically active compounds.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing anthranilic acid derivatives and fused bicyclic anthranilic diamides are used, then insecticidal and acaricidal activity is achieved, but the spectrum of application remains narrow and environmental and biological properties are unsatisfactory

Engineering Contradiction:

Improvespectrum of applicationVSAvoidenvironmental and biological properties

Core Design Contradiction:

Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies parameter changes by systematically modifying the chemical structure of anthranilic acid derivatives, specifically introducing a pyrazolopyridine-diamide core with variable substituents R1-R6 at different positions. This structural parameter optimization enables broader pest spectrum coverage while improving environmental and biological properties through precise molecular design

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures by combining the pyrazolopyridine-diamide core with diverse substituent groups (R1-R6) that can be independently selected from multiple chemical categories. This composite approach allows simultaneous optimization of insecticidal activity, acaricidal activity, and environmental compatibility through tailored molecular composition

Inventive Principle:

Principle #40Composite materials

2Reliability

If existing anthranilic acid derivatives are used, then some insecticidal activity is achieved, but the activity against difficult-to-control insect species is insufficient

Engineering Contradiction:

Improveinsecticidal and acaricidal activityVSAvoideffectiveness against difficult-to-control species

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent enhances insecticidal and acaricidal activity by optimizing molecular parameters including the introduction of electron-withdrawing and electron-donating groups at specific positions (R1-R6), which modulates the compound's binding affinity to target sites in pest organisms, thereby achieving superior efficacy against resistant and difficult-to-control species

Inventive Principle:

Principle #35Parameter changes

3Object-affected harmful factors

If existing compounds are used, then basic insecticidal function is provided, but plant compatibility and environmental properties are unsatisfactory

Engineering Contradiction:

Improveplant compatibilityVSAvoidenvironmental and biological properties

Core Design Contradiction:

Object-affected harmful factorsVSReliability

Solution Approach 1:

The patent applies local quality by introducing specific substituent groups at designated positions (R1-R6) on the pyrazolopyridine-diamide core structure. These localized structural modifications enhance plant compatibility and environmental safety without compromising the overall insecticidal and acaricidal activity, allowing the compound to selectively target pests while being safe for plants and the environment

Inventive Principle:

Principle #3Local quality

Data Source

PatentEP3728256B1Pyrazolopyridine-diamides, their use as insecticide and processes for preparing the same

Publication Date: 2024.10.02 PI IND LTD

AI summary

The present invention provides novel pyrazolopyridine-diamides of Formula (I), wherein, the definition of W1, W2, A1, A2, A3, B1, B2, D, Z1, E, R1, R2, R3, R4, m and n is as described in the description. The present invention also relates to the composition, combination, use and method of application of the compounds of Formula (I).