Nucleoside Diphosphate or Diphosphonate Prodrugs, or Nucleoside Analogue Diphosphate or Diphosphonate Prodrugs

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

This invention describes a new class of prodrugs based on nucleoside diphosphates or diphosphonates, wherein the terminal phosphate group is modified with two covalently bound, non-bioreversible lipophilic groups (moieties A and B). These modifications enhance the ability of the compounds to enter cells, including crossing biological barriers like the cell membrane and potentially the blood-brain barrier. Upon entering the cell, these prodrugs slowly release the active drug (such as antivirals or anticancer agents), and in some cases, the prodrugs themselves are active against targets like viral enzymes.

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

• Treatment of viral infections such as HIV, hepatitis, influenza, and hemorrhagic fevers
• Antiretroviral therapy, particularly against retroviruses like HIV
• Potential therapies for cancer using nucleoside analogues with antitumoral effects
• Enhanced delivery of nucleotide-based drugs to cells with improved membrane penetration
• Treatment of central nervous system viral infections due to possible blood-brain barrier crossing
• Development of pharmaceutical compositions for slow and controlled drug release

BenefitsContent extracted from patent full text and abstract with AI.

• Improved cellular uptake of nucleoside-based drugs due to enhanced lipophilicity
• Potential to overcome issues with poor intracellular activation or enzymatic conversion of standard nucleoside analogues
• Slow intracellular release offers controlled pharmacokinetics and potentially fewer side effects
• High antiviral activity, including activity against resistant virus strains or enzyme-deficient cells
• Reduction of off-target toxicity due to slow release and high selectivity
• Versatile chemical design allows tuning for different drugs and therapeutic targets
• Simple and scalable synthesis with high yields as indicated by examples in the patent

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The invention provides a nucleoside diphosphate or nucleoside diphosphonate prodrug or a nucleoside analogue diphosphate or nucleoside analogue diphosphonate prodrug, or a pharmaceutically acceptable salt thereof, having two covalently bound lipophilic moieties A and B at the terminal phosphate group, phosphonate group or analogous phosphorus-containing group, wherein the lipophilic moieties A and B are both non-bioreversible.