Polyglycerol Derivative and a Method for Manufacturing the Same

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

This invention describes a new class of polyglycerol derivatives featuring a dendritic (highly branched) polyglycerol backbone with one or more negatively charged substituents (such as sulfate, sulfonate, phosphate, etc.) attached via cleavable linkers (including ester, amide, carbamate, etc.). These cleavable "shells" allow the polymers to degrade under certain conditions, leading to improved biocompatibility and biodistribution compared to non-cleavable analogs. The invention covers both the derivatives themselves and methods for their synthesis.

Use CasesContent extracted from patent full text and abstract with AI.

• Treatment of acute or chronic inflammatory diseases by inhibiting leukocyte adhesion and complement activation.
• Development of anti-inflammatory or anti-complement drugs with improved safety profiles.
• Carrier platforms for targeted drug delivery to inflamed tissues (e.g., by attaching pharmaceuticals or diagnostic probes).
• Imaging agents for diagnosing inflammatory conditions (by conjugating with probes for fluorescence, MRI, etc.).
• Research tools for studying inflammation, immune cell recruitment, or drug delivery processes.

BenefitsContent extracted from patent full text and abstract with AI.

• Improved biodegradability and reduced accumulation in vital organs (liver, kidney, spleen) compared to existing polymers like dendritic polyglycerol sulfate (dPGS).
• Enhanced biocompatibility and lower risk of long-term toxicity or side effects.
• Tunable degradation rates by choosing appropriate linker chemistries, enabling controlled release profiles.
• Strong inhibition of L-selectin and complement system, leading to potent anti-inflammatory effects with minimal anticoagulant side effects (lower bleeding risk than heparin).
• Versatility to attach various negatively charged groups and functional probes or drugs, opening a wide range of biomedical and diagnostic applications.
• Potential for safer, longer-term treatment of inflammatory diseases without the drawbacks of current polysulfated drugs.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention relates to a polyglycerol derivative, comprising a dendritic polyglycerol backbone and at least one substituent in the nature of a covalently bound negatively charged group chosen from the group consisting of sulfates, sulfonates, phosphates, phosphonates, bisphosphonates, carboxylates and combinations thereof. The polyglycerol derivative is characterized in that the substituent is bound to the polyglycerol backbone via a linker, the linker being chosen from the group consisting of moieties being or comprising a carbamate group, an ester group, an orthoester group, an amide group, a disulfide bridge group, an acetal group, an imine group and combinations thereof. The invention also relates to uses of such a polyglycerol derivative and to a method of manufacturing the same.