Crystalline Polymorphs of Anti-RSV Compound I

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Solution Overview

Problem

There is currently no safe and effective treatment available for treating RSV infection, which poses a significant unmet medical need, especially in infants, children, immune-compromised individuals, and the elderly.

Innovation Solution

The development of crystalline polymorphs of Compound I, a potent non-fusion inhibitor of RSV-A and RSV-B, which can be used to create pharmaceutical compositions for treating or preventing RSV infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If Compound I is developed as a treatment for RSV infection, then therapeutic effectiveness is improved, but solubility and stability are insufficient

Engineering Contradiction:

Improvetherapeutic effectivenessVSAvoidsolubility and stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies parameter changes by developing multiple polymorphic forms (Form A, Form B, Form C, etc.) of Compound I, each with distinct crystal structures and physical properties. These different polymorphic forms exhibit varying solubility and stability characteristics, allowing optimization of the drug's therapeutic performance while maintaining its antiviral effectiveness against RSV infection.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent creates composite pharmaceutical compositions that combine Compound I in specific polymorphic forms with pharmaceutically acceptable excipients and carriers. This composite approach enhances the solubility and stability of Compound I while preserving its therapeutic effectiveness, enabling safe and effective RSV treatment formulations.

Inventive Principle:

Principle #40Composite materials

2Adaptability or versatility

If no treatment is available for RSV infection, then the unmet medical need remains, but developing new treatments requires overcoming formulation challenges

Engineering Contradiction:

Improvetreatment availabilityVSAvoidformulation development

Core Design Contradiction:

Adaptability or versatilityVSEase of manufacture

Solution Approach 1:

The patent segments the complex formulation development into distinct polymorphic forms (Form A, Form B, Form C, etc.), each with characterized properties. This segmentation allows systematic evaluation and selection of the most suitable polymorphic form for pharmaceutical formulation, simplifying the overall drug development process for RSV treatment.

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

By changing the physical and chemical parameters of Compound I through polymorphism, the patent creates multiple formulation options with different solubility, stability, and bioavailability characteristics. This enables selection of optimal formulation parameters to overcome manufacturing challenges and bring effective RSV treatments to market.

Inventive Principle:

Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The crystalline polymorphs of Compound I provide a stable and effective form of the compound, enhancing its solubility and stability, thereby offering a promising treatment option for RSV infections.

Implementation Method 1

The present invention provides crystalline polymorphs of Compound I

Methodology Applied

Scientific EffectCrystallization: Crystallisation

Data Source

PatentUS20250145603A1Crystal forms of an Anti-RSV agent

Publication Date: 2025.05.08 ENANTA PHARM INC

AI summary

The present invention features crystalline forms of Compound I having characteristic peaks in the XRPD pattern as shown in one of FIGS. 1-9 and Tables 2-5.