title: FFA4/GPR120 agonists: a survey of the recent patent literature.
abstract: FFA4/GPR120, a member of the rhodopsin family of G-protein-coupled receptors (GPCRs), is becoming an important target for therapeutic intervention in several areas of disease, including metabolic diseases, inflammation and cancer. In the last few years several patents on original chemotypes have been generated by different companies. In this review an analysis of the patents in the FFA4 agonism field is presented, with an emphasis on the documents published between 2013 and mid-2015. A discussion of the biological methods used in the patents is included. The general interest in this area is growing fast as half of the existing patents on FFA4 agonists have been issued after 2013. There is, however, a need of further diversifying new chemical classes away form the current substrate-like, carboxylic acid-containing agonists.
authors.affiliation: Axxam Discovery Chemistry, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Rosa
authors.initials: R
authors.lastname: Formicola
authors.affiliation: Axxam Discovery Chemistry, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Pevarello
authors.affiliation: Axxam Discovery Biology, Via Meucci, 3, 20091 Bresso (MI), Italy.
authors.forename: Christina
authors.initials: C
authors.lastname: Kuhn
authors.affiliation: Axxam Discovery Biology, Via Meucci, 3, 20091 Bresso (MI), Italy.
authors.forename: Chiara
authors.initials: C
authors.lastname: Liberati
authors.affiliation: Axxam Discovery Chemistry, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: Piscitelli
authors.affiliation: Axxam Discovery Chemistry, Via Castellino, 111, 80100 Napoli, Italy.
authors.forename: Mariangela
authors.initials: M
authors.lastname: Sodano
mesh_terms: D000818:Animals; D001681:Biological Assay; D006801:Humans; D010330:Patents as Topic; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*
chemical_list: C519853:FFAR4 protein, human; D043562:Receptors, G-Protein-Coupled