Phospholipid Carba-Nucleoside Formulation for Antiviral Stability

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Solution Overview

Problem

There is a lack of effective vaccine or post-exposure treatment modalities for preventing or managing viral infections caused by Arenaviridae, Coronaviridae, Filoviridae, Flaviviridae, Orthomyxoviridae, Pneumoviridae, and Paramyxoviridae viruses, with patients often receiving only supportive therapy.

Innovation Solution

Pharmaceutical formulations comprising phospholipids, a compound of Formula I or its pharmaceutically acceptable salt, and sucrose, where the phospholipids include phosphatidyl choline and an anionic phospholipid, are developed for treating these viral infections.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If the compound of Formula Ia is administered alone, then the antiviral activity is achieved, but the bioavailability and stability are insufficient

Engineering Contradiction:

Improveantiviral activityVSAvoidbioavailability and stability

Core Design Contradiction:

ReliabilityVSStability of the object's composition

Solution Approach 1:

The patent applies composite materials by formulating the compound of Formula Ia with phospholipids (including phosphatidyl choline and anionic phospholipids) and sucrose to create a liposomal formulation. This composite structure enhances the bioavailability and stability of the antiviral compound while maintaining its antiviral activity, directly resolving the contradiction between achieving antiviral effect and improving stability.

Inventive Principle:

Principle #40Composite materials

2Ease of operation

If supportive therapy is provided to patients with viral infections, then the immediate treatment needs are met, but the underlying viral infection is not effectively treated

Engineering Contradiction:

Improvetreatment simplicityVSAvoideffectiveness against viral infection

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent employs parameter changes by modifying the physical and chemical properties of the compound of Formula Ia through formulation with phospholipids and sucrose. This changes the pharmacokinetic parameters (bioavailability, half-life, stability) of the drug, transforming it from a compound with insufficient bioavailability to one that can effectively treat viral infections while maintaining ease of administration.

Inventive Principle:

Principle #35Parameter changes

Data Source

PatentEP4346772B1Phospholipid formulations of 1'-cyano substituted carba-nucleoside analogs

Publication Date: 2026.04.01 GILEAD SCIENCES INC

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AI summary

The disclosure provides pharmaceutical formulations of the compound of Formula (I) : Formula (I) or a pharmaceutically acceptable salt thereof.