title: P2X7 antagonists for CNS indications: recent patent disclosures.
abstract: P2X7, a ligand-gated purinergic ion channel, has been at the center of intense efforts in the pharmaceutical industry in the last 15 years due to the growing appreciation of its role in inflammation. Since 2008-2009, increased focus on CNS available compounds has led to the publication of various patents on behalf of several pharmaceutical companies. This patent review aims at analyzing the recent patent literature (2008-2016) with a particular emphasis on those patents that are thought to deal with CNS penetrant compounds on the basis of their physicochemical features, the assays described in the patents and the uses these compounds are claimed for.
authors.affiliation: Axxam Discovery Research, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Pevarello
authors.affiliation: Via Meucci, 3, 20091 Bresso (MI), Italy.
authors.forename: Silvia
authors.initials: S
authors.lastname: Bovolenta
authors.affiliation: Via Meucci, 3, 20091 Bresso (MI), Italy.
authors.forename: Paola
authors.initials: P
authors.lastname: Tarroni
authors.affiliation: Via Meucci, 3, 20091 Bresso (MI), Italy.
authors.forename: Lorena
authors.initials: L
authors.lastname: Za
authors.affiliation: Axxam Discovery Research, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Elda
authors.initials: E
authors.lastname: Severi
authors.affiliation: Axxam Discovery Research, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Domenica
authors.initials: D
authors.lastname: Torino
authors.affiliation: Axxam Discovery Research, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Rocco
authors.initials: R
authors.lastname: Vitalone
mesh_terms: D000818:Animals; D002460:Cell Line; D002493:Central Nervous System Diseases / Q000188:drug therapy* / Q000378:metabolism; D002986:Clinical Trials as Topic; D004195:Disease Models, Animal; D006801:Humans; D015394:Molecular Structure; D019636:Neurodegenerative Diseases / Q000188:drug therapy / Q000378:metabolism; D010330:Patents as Topic; D058920:Purinergic P2X Receptor Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use*; D058469:Receptors, Purinergic P2X / Q000378:metabolism
chemical_list: D058920:Purinergic P2X Receptor Antagonists; D058469:Receptors, Purinergic P2X
keywords: BzATP; EAE; FLIPR assay; P2X7; PBMC; QPatch; THP-1; YO-PRO® or YO-PRO-1; interleukin-1