Ethylsulphonyl-Pyridine Derivatives for Flea and Tick Control
Solution Overview
Problem
Current insecticidal and acaricidal treatments for animals are not always effective, fast-acting, or long-lasting, and often contain hazardous chemicals with toxic side effects, and some agents are becoming ineffective due to parasitic resistance, particularly for controlling fleas and ticks.
Innovation Solution
Development of cyclopropyl-(hetero)aryl substituted ethylsulphonyl-pyridine derivatives and their pharmaceutical compositions that are more potent and efficacious against fleas and ticks, offering safer and more convenient topical and oral administration options.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current insecticidal and acaricidal treatments are used, then some parasitic control effect is achieved, but the treatments contain hazardous chemicals with toxic side effects and do not provide long-lasting efficacy
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of pyridine derivatives through systematic variation of substituents (R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20) to optimize the balance between antiparasitic efficacy and toxicity reduction. This involves changing molecular parameters such as substituent types, positions, and configurations to achieve superior potency while reducing hazardous effects.
2Speed
If current antiparasitic agents are used, then some control effect is achieved, but the speed of action and duration of action are insufficient
Solution Approach 1:
The patent employs parameter changes by optimizing molecular structure parameters of the pyridine derivative compounds to achieve both rapid onset and prolonged duration of action. The systematic modification of substituent parameters (various R groups) allows tuning of pharmacokinetic properties to simultaneously improve speed and duration of antiparasitic effect.
3Reliability
If current insecticidal treatments are used, then some parasitic control is achieved, but parasitic resistance is developing making agents ineffective
Solution Approach 1:
The patent applies composite materials principle by creating complex pyridine derivative structures with multiple substituted groups (various R1-R20 parameters) that combine different functional moieties. This composite molecular structure approach provides multi-target activity and reduces the likelihood of resistance development compared to simpler single-agent structures.
4Productivity
If current antiparasitic treatments are used, then some efficacy is achieved, but the treatments require frequent application and do not provide long-lasting protection
Solution Approach 1:
The patent utilizes parameter changes by optimizing the pharmacokinetic parameters of the pyridine derivative compounds through structural modification. The systematic variation of substituent parameters enhances the duration of action, reducing the frequency of reapplication needed to maintain effective protection levels.
Data Source
AI summary
Disclosed herein are intermediate compounds that form cyclopropyl-(hetero)aryl substituted ethylsulphonyl-pyridine derivatives, where such derivatives are useful as antiparasitic agents for the treatment, prevention and/or control of parasitic infections and/or infestations in animals.