WX-216 Sodium Salt Crystal Forms for Stable Influenza APIs

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Solution Overview

Problem

Current antiviral drugs for influenza, such as neuraminidase inhibitors, face challenges with emerging drug-resistant strains, necessitating the development of compounds with new action mechanisms for effective treatment and prevention of Influenza A virus.

Innovation Solution

The development of sodium salts of WX-216, specifically in various crystal forms, which exhibit good druggability and stability, providing a range of active pharmaceutical ingredients (APIs) for drug development, including crystal forms I to VIII, characterized by specific XRPD, DSC, and TGA patterns.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing antiviral drugs like neuraminidase inhibitors are used, then Influenza A virus can be treated, but drug-resistant strains emerge reducing effectiveness

Engineering Contradiction:

Improveeffectiveness of antiviral treatmentVSAvoidresistance of virus strains

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent applies parameter changes by developing new chemical compounds with different molecular structures (pyrimidine derivatives) and exploring multiple salt forms (sodium, potassium, calcium, magnesium salts) and crystal forms to alter the chemical parameters of the antiviral agent, thereby overcoming viral resistance to existing drugs

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent employs composite materials by creating salt forms of pyrimidine derivatives that combine the active pharmaceutical ingredient with different metal cations, producing multiple composite compounds (e.g., sodium salt, potassium salt) with potentially different pharmacological properties and resistance profiles

Inventive Principle:

Principle #40Composite materials

2Adaptability or versatility

If multiple salt forms and crystal forms are developed, then more API options are provided for drug development, but the complexity of screening and characterization increases

Engineering Contradiction:

Improveoptions of intermediate products and APIsVSAvoidcomplexity of salt form screening

Core Design Contradiction:

Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The patent applies segmentation by systematically dividing the salt form development into distinct categories (sodium salt, potassium salt, calcium salt, magnesium salt) and further segmenting each into specific crystal forms (Form I, Form II, etc.), allowing methodical screening and characterization of each segment rather than attempting to evaluate all possibilities simultaneously

Inventive Principle:

Principle #1Segmentation

Data Source

PatentEP3992192B1Dominant salt forms of pyrimidine derivatives, and crystal forms thereof

Publication Date: 2026.02.18 GUANGDONG RAYNOVENT BIOTECH CO LTD

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AI summary

Disclosed are sodium salts of pyrimidine derivatives, and a series of crystal forms thereof. The series of crystal forms exhibit a good druggability, such as stability, fluidity, compressibility, etc., and provide a variety of bulk drug options for subsequent drug product development.