Novel Anthelmintic Compounds Broad-Spectrum Parasite Control

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Solution Overview

Problem

Current anthelmintic compounds have limitations in efficacy, bioavailability, and spectrum of coverage for treating and preventing parasitic infections in animals, particularly against endoparasites and ectoparasites, necessitating the development of new active agents and veterinary compositions.

Innovation Solution

Development of novel anthelmintic compounds of specific formulae (IA), (IA-1), and (IA-2) along with their compositions, which include racemic mixtures, stereoisomers, tautomeric forms, and salt forms, combined with pharmaceutically acceptable carriers, offering broad-spectrum coverage against internal and external parasites.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current anthelmintic compounds are used, then treatment is provided for parasitic infections, but efficacy and spectrum of coverage are limited

Engineering Contradiction:
ImproveefficacyVSAvoidspectrum of coverage
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent develops novel anthelmintic compounds with broad-spectrum activity against multiple parasite types including nematodes, cestodes, and trematodes. The compounds are designed to perform multiple functions: treating existing infections, providing prophylaxis, and covering diverse parasite species with a single agent, thereby resolving the limitation of narrow spectrum of coverage while maintaining high efficacy

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

Solution Approach 2:

The patent employs systematic modification of chemical parameters including molecular structure, stereochemistry (R and S enantiomers), and physical properties to optimize compound performance. By varying structural parameters and evaluating bioavailability, the invention achieves improved efficacy across different parasite types while overcoming the limitations of existing compounds

Inventive Principle:
Principle #35Parameter changes

2Reliability

If current anthelmintic compounds are used, then treatment is provided, but bioavailability is insufficient

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidbioavailability
Core Design Contradiction:
ReliabilityVSUse of energy by moving object

Solution Approach 1:

The patent systematically modifies chemical and physical parameters of the anthelmintic compounds including molecular weight, lipophilicity, and stereochemical configuration to enhance bioavailability. The evaluation of R and S enantiomers and optimization of physical properties enables improved absorption and distribution while maintaining treatment effectiveness

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent develops compositions that may combine multiple compounds or formulations to achieve synergistic effects and improved bioavailability. By creating composite anthelmintic preparations with optimized delivery systems and combinations of active ingredients, the invention overcomes the bioavailability limitations of single compounds while enhancing overall treatment effectiveness

Inventive Principle:
Principle #40Composite materials

Data Source

PatentEP3247701B1Anthelmintic compounds, compositions and method of using thereof
Publication Date: 2021.09.22 BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC
  • EP3247701B1 patent drawing
  • EP3247701B1 patent drawing
  • EP3247701B1 patent drawing

AI summary

The present invention relates to novel anthelmintic compounds of formula (IA) below: wherein, Y is selected from the group consisting of -H, aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl; and Z is selected from the group consisting of aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocyclyl, alkyl, haloalkyl, and alkoxyalkyl. Variables Ring A, Ring B, Ring C, X1, X6, and X8 are as defined herein. The invention also relates to parasiticidal compositions comprising the compounds, and methods and uses of the compounds for treating and preventing parasitic infections and infestations in animals.