Bicyclic Derivatives for Heartworm Control
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Solution Overview
Problem
Current treatments for heartworm infections in warm-blooded animals, particularly those using macrocyclic lactones, are often ineffective due to developing resistance and require cumbersome, time-consuming arsenic-based compounds, necessitating the need for new compounds that can effectively control or kill heartworms.
Innovation Solution
Development of compounds of formula (I′) and (I) that target heartworms, which include specific structural elements allowing for effective treatment and control of endoparasites by administering these compounds to the animals or their environment.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If macrocyclic lactones are used for heartworm control, then heartworm control is achieved, but resistance develops making the treatment ineffective
Solution Approach 1:
The patent modifies the chemical structure of macrocyclic lactones by changing molecular parameters - specifically introducing a 6- to 10-membered heteroaryl group at the C-1 position and a 4- to 7-membered heterocycloalkyl group at the C-6 position. These structural parameter changes create new compounds with different biological properties that overcome resistance while maintaining heartworm control effectiveness.
2Reliability
If arsenic-based compounds are used to treat adult heartworm infections, then heartworms are killed, but the treatment becomes time consuming and cumbersome
Solution Approach 1:
The patent develops new compounds that act as short-acting, highly effective heartworm killers. The compounds are designed to provide rapid and durable kill with reduced treatment duration compared to traditional arsenic-based compounds, making the treatment more convenient while maintaining high reliability in heartworm elimination.
3Reliability
If new compounds are developed to overcome resistance, then heartworm control effectiveness is improved, but the complexity of compound structure increases
Solution Approach 1:
The patent segments the molecular structure into distinct functional components: a core macrocyclic lactone framework combined with specific heteroaryl and heterocycloalkyl groups at defined positions. This segmentation allows systematic design and optimization of each component's contribution to resistance overcoming while managing overall structural complexity through modular assembly.
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.