Bicyclic Compounds for Pest Control with Plant Tolerance

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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

Bicyclic compounds of specific structural formulas, which exhibit insecticidal properties and are well-tolerated by plants, offering favorable toxicological and environmental profiles.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If new bicyclic compounds are developed to broaden pesticide spectrum, then effectiveness against arthropods and insects is improved, but synthesis complexity and manufacturing effort increase

Engineering Contradiction:
Improveeffectiveness against pestsVSAvoidsynthesis effort
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The bicyclic compound structure is divided into distinct functional regions (first cyclic structure with nitrogen, second cyclic structure, linker L1/L2/L3). This segmentation allows independent optimization of each module for pest effectiveness while maintaining manageable synthesis pathways for each component.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent systematically varies key structural parameters including the type of cyclic structures (saturated/unsaturated), linker compositions (L1-L3 with different atoms and bonds), and substituent patterns (R1-R6 groups). These parameter changes enable tuning of both pest effectiveness and synthesis feasibility across the compound series.

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If pesticide spectrum is broadened to address resistance issues, then duration of action is improved, but toxicity concerns may increase

Engineering Contradiction:
Improveduration of pest controlVSAvoidtoxicity
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

Different regions of the bicyclic molecule have specialized functions: the nitrogen-containing cyclic structure provides pest target interaction for effectiveness, while specific substituent groups (R1-R6) and linker compositions modulate toxicity and environmental fate. This local quality differentiation allows simultaneous optimization of duration of action and safety profile.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The bicyclic compound combines multiple structural elements (two cyclic systems, heteroatoms, variable linkers, substituents) into a composite molecular architecture. This composite structure integrates pest efficacy functions with reduced toxicity characteristics, achieving prolonged protection while minimizing harmful effects on non-target organisms.

Inventive Principle:
Principle #40Composite materials

3Object-affected harmful factors

If compound structure is optimized for plant tolerance, then environmental compatibility is improved, but spectrum of activity may be limited

Engineering Contradiction:
Improveplant toleranceVSAvoidspectrum of pesticide activity
Core Design Contradiction:
Object-affected harmful factorsVSAdaptability or versatility

Solution Approach 1:

The bicyclic compound structure is designed with universal features that provide both plant tolerance and broad-spectrum pest activity. The nitrogen-containing cyclic core offers inherent safety for cultivated plants while the variable substituents (R1-R6) and linkers (L1-L3) enable activity against diverse arthropod and insect pests across multiple taxonomic groups.

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

Data Source

PatentEP3484877B1Bicyclic compounds as pest controllers
Publication Date: 2020.07.01 BAYER CROPSCIENCE AG
  • EP3484877B1 patent drawing
  • EP3484877B1 patent drawing
  • EP3484877B1 patent drawing

AI summary

The invention relates to novel bicyclic compounds, to agents containing said compounds, to the use thereof for controlling animal pests and to methods and intermediate products for the production thereof.