P2X7 antagonists for CNS indications: recent patent disclosures
Paolo Pevarello1, Silvia Bovolenta2, Paola Tarroni2
1Axxam Discovery Research, Via Castellino, 111, 80100 Napoli, Italy.
Pharmaceutical Patent Analyst
|March 2, 2017
Summary
Pharmaceutical companies are developing P2X7 receptor antagonists for inflammation. This review focuses on patents from 2008-2016, particularly those targeting CNS-penetrant compounds for neurological conditions.
Area of Science:
- Pharmacology
- Medicinal Chemistry
- Neuroscience
Background:
- The P2X7 receptor, a purinergic ion channel, is a key target in inflammation research.
- Recent years have seen significant pharmaceutical interest in P2X7 antagonists.
- Focus has shifted towards developing centrally acting (CNS) compounds targeting this receptor.
Purpose of the Study:
- To review patent literature concerning P2X7 receptor modulators from 2008 to 2016.
- To identify and analyze patents claiming CNS-penetrant compounds.
- To assess the physicochemical properties, assays, and claimed uses of these compounds.
Main Methods:
- Systematic patent literature search (2008-2016).
- Analysis of patent physicochemical properties to predict CNS penetration.
- Evaluation of in vitro/in vivo assays and therapeutic indications described in patents.
Main Results:
- Numerous patents filed by pharmaceutical companies detail P2X7 modulators.
- A subset of these patents specifically focuses on compounds with predicted CNS penetration.
- Identified trends in chemical scaffolds, assay methodologies, and therapeutic targets.
Conclusions:
- The P2X7 receptor remains a significant target for drug development, especially for CNS disorders.
- Patent activity indicates a growing trend towards developing orally available, CNS-penetrant P2X7 inhibitors.
- Further research into these patented compounds could yield novel treatments for inflammatory and neurological diseases.
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