Compounds and compositions having knock-down or blood feed inhibition activity against insect pests

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Solution Overview

Problem

Current insecticides, such as pyrethroids, are becoming ineffective due to resistance in dipteran insect pests like mosquitoes and flies, which are vectors of diseases and cause nuisance, and there is a need for new active compounds that can knockdown or inhibit blood feeding without relying on oral administration.

Innovation Solution

The use of 4-(trifluoromethyl)pyridine compounds that can be picked up by target insects, causing rapid knockdown or blood feed inhibition, including those resistant to traditional insecticides, without the need for oral consumption, and are integrated into various products and management solutions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If traditional insecticides like pyrethroids are used, then initial control effectiveness is achieved, but resistance develops making them ineffective over time

Engineering Contradiction:
Improveinsecticide effectivenessVSAvoidduration of resistance
Core Design Contradiction:
ReliabilityVSDuration of action of stationary object

Solution Approach 1:

The patent introduces new chemical compounds with different molecular structures (4-(trifluoromethyl)pyridine compounds) that differ fundamentally from traditional pyrethroids. This structural parameter change allows the new compounds to bypass resistance mechanisms developed against older insecticides, restoring effectiveness against resistant insect populations.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent combines multiple active ingredients including 4-(trifluoromethyl)pyridine compounds with other insecticidal substances to create composite formulations. This composite approach provides synergistic effects and reduces the likelihood of resistance development by targeting multiple physiological pathways simultaneously.

Inventive Principle:
Principle #40Composite materials

2Reliability

If oral administration is required for insecticide effectiveness, then control is achieved, but application complexity and animal compliance become problematic

Engineering Contradiction:
Improveinsecticide control effectivenessVSAvoidapplication method simplicity
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the mechanical/oral administration system with a transdermal delivery system. The insecticide is applied topically to the animal's skin and absorbed through the cutaneous route, eliminating the need for oral dosing while maintaining effective blood concentrations. This substitution simplifies application and ensures compliance without requiring animal cooperation.

Inventive Principle:
Principle #28Mechanics substitution (Replace mechanical system)

Solution Approach 2:

The patent uses the animal's skin and bloodstream as intermediary pathways to deliver the insecticide systemically. The 4-(trifluoromethyl)pyridine compounds are absorbed through the skin and distributed via the circulatory system to reach target insects, serving as an effective intermediary delivery mechanism that avoids direct oral administration.

Inventive Principle:
Principle #24Intermediary (Mediator)

3Reliability

If new active compounds are developed to overcome resistance, then effectiveness against resistant strains is improved, but knowledge of their mode of action and safety profile is limited

Engineering Contradiction:
Improveeffectiveness against resistant strainsVSAvoidknowledge of mode of action
Core Design Contradiction:
ReliabilityVSLoss of information

Solution Approach 1:

The patent incorporates comprehensive toxicological and pharmacological testing protocols to gather feedback on the safety and efficacy of the new compounds. Extensive studies on mode of action, metabolism, and toxicology are conducted to build a knowledge base that informs safe and effective usage guidelines, gradually reducing the information gap through systematic research.

Inventive Principle:
Principle #23Feedback

Data Source

PatentUS20190350203A1Compounds and compositions having knock-down or blood feed inhibition activity against insect pests
Publication Date: 2019.11.21 SYNGENTA CROP PROTECITON AG
  • US20190350203A1 patent drawing
  • US20190350203A1 patent drawing
  • US20190350203A1 patent drawing

AI summary

With the present invention it has now been found that certain 4-(trifluoromethyl)pyridine compounds and active compound compositions comprising such compounds are suitable for controlling nuisance, disease carrying or haematophagous (blood feeding) insects pests incl. dipteran, 5 triatominae and cimicidae insect pests by knockdown or by or blood feed inhibition. In one embodiment, dipteran pests are selected from flies and mosquitoes, including insecticide-resistant flies and mosquitoes, as well as fly and mosquito vectors of pathogenic disease. Target cimicidae insect pests are selected from bed bugs. Target triatominae pests are selected from kissing bugs Other aspects of the present invention will also be apparent in the detailed description which 10 follows.