Halogen-Substituted Heterocyclic Compounds for Arthropod Control

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Solution Overview

Problem

Modern crop protection compositions face challenges in efficacy, persistence, spectrum of action, toxicity, combinability, and resistance, necessitating the development of novel compounds with improved properties.

Innovation Solution

Development of halogen-substituted compounds and their salts with specific structural features, exhibiting insecticidal, acaricidal, and parasiticidal activities, which can be used in agrochemical and animal health sectors, including formulations for seed treatment and vector control.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional pesticides are used, then pest control is achieved, but resistance develops and efficacy decreases

Engineering Contradiction:
Improvepest control efficacyVSAvoidresistance development time
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of pesticide compounds through halogen substitution patterns and heterocyclic ring variations. This creates novel compounds with altered biological properties that maintain efficacy while reducing resistance development, directly addressing the contradiction between maintaining pest control reliability and preventing resistance over time

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention employs composite materials by combining multiple heterocyclic rings (triazole, pyrimidine, pyridine) with halogen-substituted alkyl chains in a single molecular structure. This composite molecular architecture enables the compound to interact with multiple pest targets simultaneously, improving efficacy while delaying resistance development through multi-mode of action

Inventive Principle:
Principle #40Composite materials

2Adaptability or versatility

If broad-spectrum pesticides are used, then spectrum of action is improved, but toxicity to non-target organisms increases

Engineering Contradiction:
Improvespectrum of actionVSAvoidtoxicity to non-target organisms
Core Design Contradiction:
Adaptability or versatilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by introducing specific halogen substitutions at particular positions on the heterocyclic rings and alkyl chains. These localized structural modifications tune the compound's selectivity, allowing broad-spectrum activity against target pests while reducing toxicity to non-target organisms through optimized local chemical properties

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The invention uses parameter changes by systematically varying the heterocyclic ring types (triazole, pyrimidine, pyridine) and halogen substitution patterns to optimize the balance between spectrum of action and selectivity. This enables tuning of biological activity to achieve broad pest control with reduced non-target toxicity

Inventive Principle:
Principle #35Parameter changes

3Reliability

If complex pesticide formulations are used, then efficacy is improved, but manufacturing cost and complexity increase

Engineering Contradiction:
Improvepest control efficacyVSAvoidsynthesis complexity
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies segmentation by dividing the complex pesticide molecule into modular heterocyclic components (triazole ring, pyrimidine ring, pyridine ring) that can be synthesized separately and then assembled. This modular approach maintains the efficacy of complex formulations while simplifying manufacturing through standardized intermediate building blocks

Inventive Principle:
Principle #1Segmentation

Data Source

PatentUS10836732B2Compounds for combating arthropods
Publication Date: 2020.11.17 ELANCO ANIMAL HEALTH GMBH
  • US10836732B2 patent drawing
  • US10836732B2 patent drawing
  • US10836732B2 patent drawing

AI summary

The invention relates inter alia to novel compounds of the general formula (I)in which the A1-A4, T, W, Q, R1 and B1-B4 radicals are each as defined in the description. Also described are processes for preparing the compounds of the formula (I). The inventive compounds are especially suitable for controlling insects, arachnids and nematodes in agriculture, and ectoparasites in veterinary medicine.