Linear Polyglycerol Derivatives, a Method for Manufacturing and Applications

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes new linear polyglycerol compounds, which are polymers with a backbone of glycerol units linked in a straight line, to which multiple sugars or sugar derivatives—especially sialic acid or its analogs—are chemically attached. These materials have a high degree of functionalization (10–100%), resulting in a multivalent glycopolymer. The invention covers their synthesis, use as antiviral, antibacterial, and anti-inflammatory agents, and combinations with neuraminidase inhibitors (such as Tamiflu) for enhanced therapeutic effect against viruses like influenza. The compounds exhibit strong virus-binding and blocking effects, especially against influenza viruses, with low toxicity.

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• Prophylactic or therapeutic agent against influenza and other respiratory viruses by blocking virus entry into host cells.
• Combination therapy with neuraminidase inhibitors (e.g., Tamiflu or Relenza) to enhance antiviral efficacy and reduce resistance development.
• Broad-spectrum antiviral applications, potentially including other pathogens that use glycan-mediated entry.
• Antibacterial or anti-inflammatory treatments, given the biocompatibility and functional versatility of the polymer backbone.
• Use as a non-toxic drug delivery platform by leveraging its multivalent sugar presentation for targeted binding to specific pathogens or cells.
• Development of diagnostic tools leveraging specific virus or bacteria binding properties.

BenefitsContent extracted from patent full text and abstract with AI.

• Greater antiviral potency compared to current gold-standard drugs like Tamiflu, particularly in preventing virus binding and entry.
• Broad-spectrum potential against multiple strains of influenza and possibly other viruses, depending on sugar moieties used.
• Low to negligible toxicity, making the compounds suitable for prophylactic use and for vulnerable populations.
• Synergistic effect when combined with neuraminidase inhibitors, potentially lowering the required dosage and reducing the risk of resistance.
• Customizable degree of substitution and molecular weight for tuning pharmacological and pharmacokinetic properties.
• Scalable and reproducible manufacturing methods allowing precise control over polymer structure and functionality.
• Biocompatibility and water solubility, facilitating formulation and delivery in various pharmaceutical products.

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Patent Abstract

The invention relates to a linear polyglycerol compound, comprising an optionally terminally substituted backbone of linearly linked glycerol units. This linear polyglycerol compound is characterized in that it carries a plurality of substituents in the nature of covalently bound residues chosen from the group consisting of sugars and sugar derivatives, wherein a degree of substitution of the backbone is between 10 and 100 %. The invention also relates to uses of this linear polyglycerol compound, to a combination preparation of this linear polyglycerol compound and a neuraminidase inhibitor, to uses of this combination preparation and to a manufacturing method of the linear polyglycerol compound.