Substituted Pyrimidinium Compounds for Resistant Pest Control

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Solution Overview

Problem

Current pesticidal agents face challenges due to the development of resistance by invertebrate pests such as insects, arachnids, and nematodes, necessitating the need for new compounds with broad-spectrum activity.

Innovation Solution

Substituted pyrimidinium compounds of a specific formula, including their stereoisomers, salts, tautomers, and N-oxides, which form eight to fourteen-membered bicyclic rings systems, offering potent pesticidal activity against difficult-to-control invertebrate pests.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing pesticidal agents are used, then initial pesticidal activity is achieved, but resistance development by target pests occurs over time

Engineering Contradiction:
Improvepesticidal activityVSAvoidresistance-free control period
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent applies parameter changes by developing compounds with novel molecular structures (formula I pyrimidinium compounds) that differ fundamentally from existing pesticidal agents. This structural parameter change creates new modes of action that pests have not developed resistance against, thereby maintaining reliable pesticidal activity while extending the resistance-free control period.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent segments the pesticidal market by targeting specific pest groups (insects, arachnids, nematodes) with specialized compounds designed for each group's unique physiological characteristics. This segmentation allows for more precise mode of action development, reducing cross-resistance and extending effective control periods for each target group.

Inventive Principle:
Principle #1Segmentation

2Adaptability or versatility

If broad-spectrum pesticidal activity is pursued, then activity against multiple pest types is achieved, but specificity and selectivity may be reduced

Engineering Contradiction:
Improvebroad activity spectrumVSAvoidnon-target effects
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by designing compounds with specific molecular features (substituent patterns R1-R6, ring structures A-A6) that interact with particular pest physiological targets. This localized molecular design enables selective toxicity toward pests while sparing non-target organisms, achieving broad-spectrum activity against multiple pest types without proportionally increasing non-target effects.

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent achieves universality through the pyrimidinium core structure (formula I) that can target multiple pest types (insects, arachnids, nematodes) through different physiological mechanisms. The compound class serves multiple functions across diverse pest groups while maintaining selectivity through structure-activity relationship optimization.

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

Data Source

PatentUS9975895B2Substituted pyrimidinium compounds and derivatives for combating animal pests
Publication Date: 2018.05.22 BASF SE
  • US9975895B2 patent drawing
  • US9975895B2 patent drawing
  • US9975895B2 patent drawing

AI summary

Substituted pyrimidinium compounds of the general formula (I) and their uses for combating animal pestsThe present invention relates to substituted pyrimidinium compounds of formula (I), to the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these substituted pyrimidinium compounds and of compositions thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such substituted pyrimidinium compounds.The substituted pyrimidinium compounds of the present invention are defined by the following general formula (I):wherein X, Y, Z, R1, R2, A, A1 and A2 are defined as in the description.