Spiro-azetidine Isoxazoline Antiparasitic Composition

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Solution Overview

Problem

Current parasitic treatments for animals are often ineffective due to short duration of action, toxicity concerns, and emerging parasitic resistance, necessitating a stable and long-acting antiparasitic composition.

Innovation Solution

A novel long-acting topical antiparasitic composition comprising a spiro-azetidine isoxazoline compound, a glycol ether, and a veterinarily acceptable solvent, optionally with additional synergistic agents, providing extended efficacy against ectoparasites and tick-borne diseases.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If current parasitic treatments are used, then parasitic infestation can be treated, but the duration of action is short and toxicity concerns arise

Engineering Contradiction:

Improveduration of actionVSAvoidtoxicity

Core Design Contradiction:

Duration of action of moving objectVSObject-affected harmful factors

Solution Approach 1:

The patent changes the chemical parameters by introducing a spiro-azetidine isoxazoline compound with specific molecular structure modifications. This new compound achieves extended duration of action (up to 12 months) while maintaining reduced toxicity profiles compared to conventional parasiticides, directly resolving the contradiction between duration and toxicity

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite formulation combining the spiro-azetidine isoxazoline compound with specific excipients and adjuvants. This composite composition enhances the drug's stability, extends its duration of action, and reduces toxic effects, simultaneously addressing both the duration and toxicity concerns

Inventive Principle:

Principle #40Composite materials

2Reliability

If current parasitic treatments are applied, then parasitic infestation can be controlled, but parasitic resistance develops

Engineering Contradiction:

ImproveefficacyVSAvoidparasitic resistance

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent extracts the active parasiticidal component from complex conventional formulations and isolates it as a pure spiro-azetidine isoxazoline compound. This extraction allows for precise control of the active ingredient's properties and mechanism of action, maintaining reliable efficacy while reducing the development of parasitic resistance through targeted action

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The invention fundamentally changes the chemical parameters of the active ingredient by using a novel spiro-azetidine isoxazoline structure with specific stereochemistry (S-enantiomer). This parameter change creates a new mechanism of action that is effective against resistant parasite populations, preserving reliability while overcoming adaptability issues

Inventive Principle:

Principle #35Parameter changes

3Productivity

If hazardous chemicals are used for parasitic treatment, then parasitic infestation can be treated, but serious consequences including lethality from accidental ingestion occur

Engineering Contradiction:

Improvetreatment effectivenessVSAvoidlethality

Core Design Contradiction:

ProductivityVSObject-affected harmful factors

Solution Approach 1:

The patent dramatically changes the toxicological parameters of the treatment by replacing hazardous chemicals with a spiro-azetidine isoxazoline compound that has significantly reduced lethality. The S-enantiomer form provides enhanced treatment effectiveness while the molecular structure inherently reduces toxicity, resolving the contradiction between productivity and safety

Inventive Principle:

Principle #35Parameter changes

4Ease of operation

If pet collars and tags are used, then some problems can be overcome, but chewing and ingestion by the animal occurs

Engineering Contradiction:

Improveapplication convenienceVSAvoidingestion risk

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The invention extracts the active ingredient from collar/tag delivery systems and delivers it through a controlled topical application method. This extraction from the collar matrix eliminates the chewing and ingestion risks associated with collars while maintaining ease of application through simple topical administration

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses a specially formulated topical vehicle as an intermediary carrier that delivers the spiro-azetidine isoxazoline compound to the skin without requiring ingestion or chewing. This intermediary formulation ensures safe delivery while maintaining ease of operation through simple topical application

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS20230414576A1Long-acting spiro-isoxazoline antiparasitic compositions

Publication Date: 2023.12.28 ZOETIS SERVICES LLC

AI summary

The invention describes a long-acting composition comprising a spiro-azetidine isoxazoline of Formula (1) or (2)wherein R1a, R1b, R1c and R2 are as described herein, and stereoisomers thereof. The composition is a veterinary composition and also comprises a glycol ether and at least one veterinarily acceptable solvent, and optionally, at least one precipitation inhibitor, antioxidant and additional veterinary agent, and any mixture thereof. The invention also includes a method of treating an animal with a parasitic infestation by administering the long-acting composition to the animal in need thereof.