Bicyclic Derivatives for Heartworm Resistance Control
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Solution Overview
Problem
Current treatments for heartworm infections, such as those using macrocyclic lactones, face challenges due to developing resistance in Dirofilaria immitis, necessitating the need for new compounds that effectively control or kill heartworms.
Innovation Solution
Development of bicyclic derivatives represented by formula (I), which can be administered to treat or control endoparasites like heartworms in warm-blooded animals, including compositions and methods involving these compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If macrocyclic lactones are used for heartworm control, then heartworm infections are controlled, but resistance develops in Dirofilaria immitis
Solution Approach 1:
The patent applies parameter changes by developing compounds with a novel bicyclic chemical structure (formula I) that differs fundamentally from macrocyclic lactones. This structural parameter change creates a new chemical class with different mechanisms of action, thereby overcoming resistance while maintaining heartworm control effectiveness.
Solution Approach 2:
The patent employs composite materials by combining specific bicyclic core structures with various substituent groups (R1-R6, G, M, Y1, Y2, Z1-Z4) to create a series of derivative compounds. This composite approach allows optimization of pharmacological properties and activity against resistant heartworm strains while maintaining the core structural framework.
2Reliability
If adult heartworm infections are treated with arsenic-based compounds, then heartworms are killed, but treatment is time consuming and cumbersome
Solution Approach 1:
The patent replaces the mechanical/administrative complexity of multi-step arsenic-based treatments with a simplified pharmaceutical compound (formula I). This substitution transforms a cumbersome treatment protocol into a more manageable drug administration regimen, reducing time and operational complexity while maintaining efficacy.
3Adaptability or versatility
If new compounds are developed to overcome resistance, then alternative therapeutic options are provided, but compound complexity increases
Solution Approach 1:
The patent applies segmentation by dividing the complex molecular structure into distinct functional components: a core bicyclic framework (X1-X6, G, M) and variable substituent groups (R1-R6, Y1, Y2, Z1-Z4). This segmentation allows systematic exploration of structure-activity relationships while managing complexity through modular design principles.
Data Source
AI summary
The present invention provides compounds of formula (I):which are useful in the control of endoparasites, for example heartworms, in warm-blooded animals.