Ectonucleotidase inhibitors

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

This invention covers a new class of chemical compounds known as ectonucleotidase (NTPDase) inhibitors. These are small-molecule nucleotide mimetics designed to selectively block NTPDase enzymes without directly affecting P2 receptors. By inhibiting NTPDases, these compounds can increase the extracellular concentrations of nucleotides such as ATP, amplifying the signaling through purinergic P2 receptors. The invention describes the chemical structures, synthesis methods, pharmaceutical compositions, and uses of these inhibitors for treating various diseases linked to ectonucleotidase activity.

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

• Treating dry eye disease via topical or systemic administration to increase nucleotide levels.
• Managing respiratory diseases (such as asthma or cystic fibrosis) by modulating nucleotide signaling.
• Therapy for inflammatory and autoimmune diseases by altering immune responses through purinergic signaling.
• Cancer treatment, exploiting the role of nucleotide signaling in tumor progression and immune environment.
• Neurological diseases (like brain inflammation or neurodegeneration), by targeting NTPDase activity in the central nervous system.
• Gastrointestinal disorders and kidney diseases where nucleotide concentration regulation is beneficial.
• Diagnostic tools, for example, improved luciferase-based ATP assays that require stable NTPDase inhibition.
• Pharmacological research tools for studying purinergic signaling and ATP metabolism.

BenefitsContent extracted from patent full text and abstract with AI.

• High selectivity for NTPDases, minimizing unwanted effects on P2 receptors.
• Increased metabolic stability compared to existing nucleotide-based inhibitors; less prone to enzymatic degradation.
• Potential for oral bioavailability due to neutral, less polar structures.
• Capability to selectively target specific NTPDase subtypes for site- and event-specific therapy.
• Amplification of endogenous purinergic signaling, potentially leading to more physiological modulation of disease.
• No interference with standard ATP detection assays (e.g., luciferase assays), making them excellent tools for research and diagnostics.
• Versatility for both therapeutic and diagnostic uses.

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Inventors & Applicants

Patent Abstract

Present invention provides ectonucleotidase (ecto-nucleotide triphosphate diphosphohydrolase, NTPDase) inhibitors represented by the following formula, namely nucleotide mimetics as selective NTPDase inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P2 receptors.