Bicyclic Pesticide Compounds Broadening Activity Spectrum

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Solution Overview

Problem

Current plant protection products face challenges such as limited spectrum of activity, resistance issues, toxicity concerns, and synthesis complexity, necessitating the development of new compounds with improved properties.

Innovation Solution

The development of new bicyclic compounds, specifically those of the formula (I), which include various substituents and functional groups, to broaden the spectrum of pesticides and enhance their efficacy and safety profiles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing plant protection products are used, then current pesticide needs are met, but the spectrum of activity is limited and resistance occurs

Engineering Contradiction:
Improvespectrum of pesticide activityVSAvoidresistance issues
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of pesticide compounds through systematic variation of substituents (R1, R2, R3, R4, R5, R6, R7, R8) at positions on the core heterocyclic ring system. This structural parameter optimization enables broadening of the spectrum of pesticide activity while maintaining efficacy and reducing resistance development through novel molecular configurations that differ from existing products

Inventive Principle:
Principle #35Parameter changes

2Productivity

If new bicyclic compounds are developed, then the spectrum of pesticides is broadened and efficacy is improved, but synthesis complexity increases

Engineering Contradiction:
Improveefficacy and spectrum of activityVSAvoidsynthesis complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by dividing the complex bicyclic compound synthesis into modular stages: (1) preparation of substituted heterocyclic compounds with specific substituents, (2) formation of the bicyclic core structure, and (3) introduction of functional groups. This segmented approach allows systematic optimization of each synthesis stage independently, managing complexity while achieving the desired spectral breadth and efficacy

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies universality by developing a core bicyclic compound structure that serves multiple pesticidal functions and can be adapted to target different pest types and resistance mechanisms. The versatile core structure with variable substituents enables a single synthetic platform to produce multiple active ingredients with different spectra of activity, reducing overall synthesis complexity across the pesticide portfolio

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

3Productivity

If plant protection products are optimized for efficacy, then pest control improves, but toxicity concerns arise

Engineering Contradiction:
Improvepest control efficacyVSAvoidtoxicity
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by introducing specific substituent patterns (R1-R8) at localized positions on the heterocyclic ring system that enhance pesticidal activity at the target site while minimizing systemic toxicity. The localized modification of molecular properties at specific positions allows differential effects: high affinity for pest targets versus low affinity for non-target organisms, thereby improving efficacy while reducing harmful effects

Inventive Principle:
Principle #3Local quality

Data Source

PatentEP3152216B1Bicyclic compounds as pesticides
Publication Date: 2019.07.24 BAYER CROPSCIENCE AG
  • EP3152216B1 patent drawing
  • EP3152216B1 patent drawing
  • EP3152216B1 patent drawing

AI summary

The application relates to new bicyclic compounds of formula (I) where Het is a group from the set consisting of (a), (b), (c), (d), (e), A is oxygen or sulfur, Q is nitrogen or C-R3, V is a group from the set consisting of oxygen, sulfur and NR4, and R1 - R4, A2, G1 and T are as defined in claim 1, the use of said compounds for controlling animal pests, and methods and intermediate products for the synthesis thereof.