Antiviral Solid Forms via Salt and Crystalline Parameter Changes
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Solution Overview
Problem
There is a need for effective antiviral agents and methods to treat viral infections such as those caused by paramyxoviridae, pneumoviridae, picornaviridae, flaviviridae, filoviridae, arenaviridae, orthomyxovirus, poxvirus, and coronaviridae, with a requirement for improved pharmaceutical formulations and manufacturing processes.
Innovation Solution
Development of solid forms, including salts and crystalline forms, of the compound ((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methyl isopropyl carbonate, which are used in pharmaceutical compositions and methods for treating or preventing viral infections, enhancing bioavailability, stability, and manufacturability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional antiviral agents are used, then viral infections can be treated, but bioavailability and stability are insufficient
Solution Approach 1:
The patent changes the physical and chemical parameters of the antiviral compound by creating multiple solid forms including salts (maleate, oxalate, methanesulfonate, ethanesulfonate) and crystalline forms. These parameter changes optimize bioavailability while maintaining manufacturing feasibility through established salt formation and crystallization processes
Solution Approach 2:
The patent creates composite pharmaceutical formulations by combining the antiviral compound with various counterions (maleate, oxalate, sulfonates) and excipients. These composite salt forms and crystalline structures improve stability and bioavailability while remaining manufacturable using standard pharmaceutical techniques
2Reliability
If conventional antiviral agents are used, then viral infections can be treated, but stability is insufficient
Solution Approach 1:
The patent modifies the stability parameters of the antiviral compound through salt formation and crystallization. The solid forms (maleate, oxalate, methanesulfonate, ethanesulfonate salts and crystalline forms) provide enhanced stability while maintaining compatibility with standard manufacturing processes
Solution Approach 2:
The patent uses readily available, inexpensive counterions (maleic acid, oxalic acid, methanesulfonic acid, ethanesulfonic acid) to create stable salt forms. These common chemicals provide stable pharmaceutical formulations without complicating manufacturing, as they can be easily obtained and processed
3Reliability
If solid forms are developed to improve bioavailability and stability, then pharmaceutical effectiveness is enhanced, but manufacturing complexity increases
Solution Approach 1:
The patent segments the antiviral compound into different solid forms (multiple salt forms and crystalline forms) to optimize pharmaceutical effectiveness. Each salt form and crystalline form can be manufactured separately using established processes, avoiding the need for complex single-step synthesis while maintaining high effectiveness
Solution Approach 2:
The patent achieves enhanced pharmaceutical effectiveness through parameter changes in the solid forms (different counterions, crystalline structures). These parameter variations improve bioavailability and stability while using standard pharmaceutical manufacturing techniques, avoiding excessive process complexity
Data Source
AI summary
The disclosure provides solid forms, e.g. salts and crystalline forms thereof, of the compound of Formula I and uses thereof. Also provided are the methods of making the solid forms, as well as pharmaceutical formulations and kits comprising the solid forms.