Cyclopropyl-(Hetero)aryl Ethylsulphonyl-Pyridines for Flea and Tick Control

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Solution Overview

Problem

Current insecticidal and acaricidal treatments for animals are not always effective, fast-acting, or long-lasting, and often contain hazardous chemicals, posing toxicity risks and facing issues with parasitic resistance, particularly for controlling fleas and ticks.

Innovation Solution

Development of cyclopropyl-(hetero)aryl-substituted ethylsulphonyl-pyridine derivatives and their pharmaceutical compositions, which are safer, more potent, and environmentally friendly, offering improved efficacy against ectoparasites like fleas and ticks.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current insecticidal and acaricidal treatments are used, then parasitic control is achieved, but toxicity and hazardous chemical exposure increase

Engineering Contradiction:
Improveparasitic control efficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent applies parameter changes by modifying the chemical structure of antiparasitic agents through specific molecular configurations (cyclopropyl, heteroaryl, ethylsulphonyl, and pyridine groups). These structural parameter changes result in compounds with improved efficacy against parasites while simultaneously reducing toxicity compared to conventional treatments

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by combining multiple functional groups and molecular components (cyclopropyl rings, heteroaryl substituents, ethylsulphonyl groups, and pyridine cores) to create novel compounds that achieve both high parasitic control efficacy and reduced toxicity, representing a composite molecular structure approach

Inventive Principle:
Principle #40Composite materials

2Reliability

If current treatments are applied, then parasitic infestations are controlled, but parasitic resistance develops

Engineering Contradiction:
Improveparasitic control efficacyVSAvoidparasitic resistance
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent addresses parasitic resistance by changing the chemical parameters of antiparasitic compounds through novel molecular structures. The specific configurations of cyclopropyl-(hetero)aryl-substituted ethylsulphonyl-pyridine derivatives represent parameter changes that differentiate these compounds from existing treatments, thereby overcoming resistance mechanisms that have developed against conventional agents

Inventive Principle:
Principle #35Parameter changes

3Reliability

If conventional antiparasitic agents are used, then treatment is achieved, but speed of action and duration of action are insufficient

Engineering Contradiction:
Improveantiparasitic activityVSAvoidduration of action
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent improves speed of action and duration of action through parameter changes in molecular structure. The novel cyclopropyl-(hetero)aryl-substituted ethylsulphonyl-pyridine derivatives possess specific structural parameters that enhance their pharmacokinetic properties, resulting in faster onset of action and prolonged duration of efficacy compared to conventional treatments

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS12435083B2Cyclopropyl-(hetero)aryl-substituted ethylsulphonyl-pyridine derivatives
Publication Date: 2025.10.07 NIHON NOHYAKU CO LTD
  • US12435083B2 patent drawing
  • US12435083B2 patent drawing
  • US12435083B2 patent drawing

AI summary

The present invention relates to cyclopropyl-(hetero)aryl substituted ethylsulphonyl-pyridine derivatives of formula (1)wherein the variables are as defined in the description and in the claims, which can be used as antiparasitic agents for the treatment, prevention and/or control of parasitic infections and/or infestations in animals.