title: Antagonists at the neurokinin receptors--recent patent literature.
abstract: This review describes the patent applications and relevant scientific literature published during 2002 in the field of novel neurokinin receptor antagonists, with an emphasis on the medicinal chemistry of recent patent publications. A brief update on the development status of compounds including: the neurokinin-1 receptor antagonists aprepitant (Merck & Co Inc), vofopitant, ezlopitant (Pfizer Inc), R-673 (F Hoffmann-La Roche Ltd); the neurokinin-2 receptor antagonists nepadutant (Menarini Ricerche SpA), saredutant (Sanofi-Synthelabo), SR-144190 (Sanofi-Synthelabo) and UK-290795 (Pfizer Inc); and the neurokinin-3 receptor antagonists osanetant (Sanofi-Synthelabo) and talnetant (GlaxoSmithKline plc) will be given. The review also reports the recent published patent literature in the area of novel therapeutic uses and novel formulations and combinations claimed for neurokinin receptor antagonists.
authors.affiliation: NiKem Research Srl, Via Zambeletti 25, 20021-Baranzate di Bollate, Milan, Italy. giuseppe.giardina@nikemresearch.com
authors.forename: Giuseppe A M
authors.initials: GA
authors.lastname: Giardina
authors.forename: Stefania
authors.initials: S
authors.lastname: Gagliardi
authors.forename: Marisa
authors.initials: M
authors.lastname: Martinelli
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D004338:Drug Combinations; D006801:Humans; D064729:Neurokinin-1 Receptor Antagonists; D010455:Peptides / Q000494:pharmacology; D018041:Receptors, Neurokinin-2 / Q000037:antagonists & inhibitors*; D018042:Receptors, Neurokinin-3 / Q000037:antagonists & inhibitors*
chemical_list: D004338:Drug Combinations; D064729:Neurokinin-1 Receptor Antagonists; D010455:Peptides; D018041:Receptors, Neurokinin-2; D018042:Receptors, Neurokinin-3