Halogen-Substituted Compounds for Broad-Spectrum Pest 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

The development of halogen-substituted compounds and their N-oxides and salts, defined by a specific general formula, which exhibit biological properties suitable for controlling animal pests, particularly in the agrochemical and animal health sectors.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If known halogen-substituted compounds are used for crop protection, then herbicidal or insecticidal activity is achieved, but the spectrum of action is limited and resistance develops

Engineering Contradiction:
Improvespectrum of pesticide actionVSAvoidresistance development
Core Design Contradiction:
Adaptability or versatilityVSReliability

Solution Approach 1:

The patent applies parameter changes by systematically varying the halogen substitution patterns (different positions, types and numbers of halogen atoms), the heteroaryl group structures, and the substituent combinations in the general formula (I) to create compounds with diverse biological activities against different pest types including insects, mites, nematodes and fungi, thereby expanding the spectrum of action while reducing resistance development

Inventive Principle:
Principle #35Parameter changes

2Reliability

If novel halogen-substituted compounds are synthesized to improve efficacy and spectrum, then biological activity against animal pests is enhanced, but synthesis expense increases

Engineering Contradiction:
Improvebiological activity and efficacyVSAvoidsynthesis expense
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent achieves universality by designing a core heteroaryl compound structure (general formula I) that can perform multiple functions: it exhibits activity against various insect orders (Lepidoptera, Coleoptera, Diptera, Hymenoptera), mites, nematodes, and fungi through appropriate selection of halogen substituents and heteroaryl groups, reducing the need for multiple separate pesticides and thereby lowering overall synthesis and application expenses

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

3Duration of action of stationary object

If crop protection compositions are designed for improved persistence, then duration of action is extended, but toxicity concerns increase

Engineering Contradiction:
Improvepersistence of pesticideVSAvoidtoxicity
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The patent applies local quality by strategically placing specific halogen atoms (fluorine, chlorine, bromine) at particular positions on the heteroaryl ring structure and combining them with specific heteroaryl groups and substituents to achieve localized enhancement of persistence through metabolic stability while maintaining selective toxicity against target pests and reducing harm to non-target organisms

Inventive Principle:
Principle #3Local quality

Data Source

PatentUS9675070B2Halogen-substituted compounds
Publication Date: 2017.06.13 ELANCO ANIMAL HEALTH GMBH
  • US9675070B2 patent drawing
  • US9675070B2 patent drawing
  • US9675070B2 patent drawing

AI summary

The invention relates inter alia to halogen-substituted compounds of the general formula (I)in which the radicals A1-A4, T, n, W, Q, R1 and Z1-Z3 have the meanings given in the description. Also described are processes for preparing the compounds of the formula (I). The compounds according to the invention are particularly suitable for controlling insects, arachnids and nematodes in agriculture and ectoparasites in veterinary medicine.