Inositol Derivatives for Use in Pathological Crystallization

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

This patent describes modified inositol compounds, specifically inositol derivatives covalently linked with one or more solubility-enhancing groups such as polyethylene glycol (PEG) chains. These compounds are designed to prevent or treat pathological calcium crystallization in the body, which underlies conditions like cardiovascular calcification, kidney stones, and other tissue calcifications. The invention shows that these PEGylated inositol derivatives are more effective at inhibiting the conversion of amorphous calcium-phosphate complexes to crystalline forms than current compounds, making them useful for various medical disorders where unwanted calcification occurs.

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

• Treatment and prevention of vascular calcification in patients with chronic kidney disease (CKD)
• Reducing or preventing kidney stones (nephrolithiasis)
• Treating calcification of heart valves (valvular calcification)
• Therapy for calcinosis cutis (calcification of skin tissues)
• Management of nephrocalcinosis (calcium deposits in kidneys)
• Prevention or treatment of chondrocalcinosis (cartilage calcification/pseudogout)
• Therapy for osteoporosis and conditions involving bone demineralization
• Support for patients undergoing hemodialysis or peritoneal dialysis
• Reducing cardiovascular risk and events related to arterial calcification (e.g., atherosclerosis, myocardial infarction)

BenefitsContent extracted from patent full text and abstract with AI.

• Enhanced solubility and improved bioavailability of inositol derivatives for medical use due to PEGylation
• Greater effectiveness than traditional inositol phosphates at preventing pathological crystallization, as shown in validated human serum assays
• Potential for tailored pharmacokinetics and dosing schedules through modification of PEG chain length
• Reduction of cardiovascular and renal calcifications reduces morbidity and mortality in high-risk groups, such as CKD and transplant patients
• Applicable to a wide range of calcification-related disorders, increasing clinical utility
• May be incorporated directly into dialysis solutions for patients with renal failure
• Non-protein small molecule with broad safety potential

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to inositol derivatives covalently modified with one, two or three solubility functions, particularly polyethylene glycol moieties, for use in therapy or prevention of conditions related to pathological calcium crystallization, such as cardiovascular calcifications, nephrocalcinosis, calcinosis cutis, chondrocalcinosis and kidney stones.