Nucleoside and Nucleoside Triphosphate Prodrugs

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

This patent introduces novel prodrugs—bioreversibly masked nucleoside diphosphates (NDPs) and nucleoside triphosphates (NTPs)—and their analogues, designed for medical use, especially for treating viral infections such as AIDS/HIV. The patented compounds improve drug delivery by enabling active nucleoside diphosphates and triphosphates to enter cells directly, bypassing the conventional need for intracellular phosphorylation. This approach can reduce side effects associated with monophosphate intermediates and enables development of more effective antiviral and antitumor medications. The patent also covers methods for synthesizing these prodrugs and preparing pharmaceutical compositions for oral or other forms of administration.

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

• Treatment of viral infections, particularly HIV/AIDS and other retrovirus-related diseases.
• Development of new antiviral drugs with improved cell uptake and efficacy.
• Creation of antitumor therapies employing nucleoside analogues.
• Improving blood-brain barrier penetration for drugs targeting neurological infections or diseases.
• Analytical applications in biochemistry for delivering phosphorylated metabolites directly into cells for research.

BenefitsContent extracted from patent full text and abstract with AI.

• Allows direct delivery of active diphosphate and triphosphate forms of drugs into cells, increasing therapeutic effectiveness.
• Reduces dependence on intracellular phosphorylation, minimizing resistance or metabolic bottlenecks in drug activation.
• Can lower drug dosages needed, thus potentially reducing toxicity and unwanted side effects.
• Improves ability of drugs to cross the blood-brain barrier, expanding treatment of viral infections in the central nervous system.
• Enables design of oral drugs and flexible pharmaceutical formulations for greater patient convenience and compliance.
• Facilitates new biochemical research protocols by enabling controlled intracellular delivery of phosphorylated metabolites.

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Patent Abstract

The invention relates to compounds that can be used as prodrugs, medicaments, pharmaceutical compositions, and pharmaceutical forms of administration produced from said compounds, and a method for producing the compounds according to the invention. The invention proposes bioreversible masked diphosphates and triphosphates, in particular nucleoside diphosphates (NDP) and nucleoside triphosphates (NTP), and corresponding analogues suitable for treating viral diseases such as AIDS, for example.