Anti-SARS-CoV-2 Crystal Forms for Stability and Drug Compatibility

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Solution Overview

Problem

There is a need for novel therapeutic agents that can effectively treat, ameliorate, or prevent SARS-CoV-2 infection, as existing compounds targeting the 3CLpro enzyme have not been approved as coronavirus therapies.

Innovation Solution

Development of polymorphic and pseudopolymorphic forms of Compound I, a potent 3CL Protease inhibitor, which are characterized by differential scanning calorimetry, powder X-ray diffraction, and Fourier-transform infrared spectroscopy, providing improved physicochemical properties and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Stability of the object's composition

If polymorphic forms of Compound I are developed, then stability and solid-state properties are improved, but manufacturing complexity increases

Engineering Contradiction:

ImprovestabilityVSAvoidmanufacturing complexity

Core Design Contradiction:

Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by developing multiple polymorphic forms (different crystal structures) of Compound I, each with distinct physical and chemical properties. By changing the crystalline arrangement parameters, the invention achieves improved stability and solubility characteristics while maintaining the same chemical composition, thereby resolving the contradiction between stability improvement and manufacturing complexity.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention utilizes phase transitions between different polymorphic forms of Compound I to achieve desired stability profiles. Each polymorphic form represents a different solid phase with unique stability characteristics, allowing selection of the most appropriate form for specific pharmaceutical applications while managing manufacturing considerations through controlled crystallization processes.

Inventive Principle:

Principle #36Phase transitions

2Adaptability or versatility

If multiple polymorphic forms are characterized and produced, then pharmaceutical compatibility is improved, but production time and complexity increase

Engineering Contradiction:

Improvepharmaceutical compatibilityVSAvoidproduction time

Core Design Contradiction:

Adaptability or versatilityVSLoss of time

Solution Approach 1:

The patent employs preliminary action by pre-characterizing multiple polymorphic forms of Compound I with respect to their pharmaceutical compatibility, stability, and physicochemical properties. This advance preparation allows selection of the most suitable polymorphic form for specific pharmaceutical applications, reducing the need for extensive testing and optimization during later production stages, thereby managing production time effectively.

Inventive Principle:

Principle #10Preliminary action

Data Source

PatentUS12570663B2Crystal forms of an anti-sars CoV-2 agent

Publication Date: 2026.03.10 ENANTA PHARM INC

AI summary

The present invention features crystalline forms of Compound I,including polymorphs and pseudopolymorphs, which are useful in the preparation of pharmaceutical compositions.