title: Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
abstract: We describe the generation of novel EP(1) receptor antagonists by investigation of thiophene isosteres. In addition, we disclose preliminary in vitro and in vivo DMPK for selected compounds.
authors.affiliation: Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. adrian.2.hall@gsk.com
authors.forename: Adrian
authors.initials: A
authors.lastname: Hall
authors.forename: Rino A
authors.initials: RA
authors.lastname: Bit
authors.forename: Susan H
authors.initials: SH
authors.lastname: Brown
authors.forename: Helene M
authors.initials: HM
authors.lastname: Chaignot
authors.forename: Iain P
authors.initials: IP
authors.lastname: Chessell
authors.forename: Tanya
authors.initials: T
authors.lastname: Coleman
authors.forename: Gerard M P
authors.initials: GM
authors.lastname: Giblin
authors.forename: David N
authors.initials: DN
authors.lastname: Hurst
authors.forename: Ian R
authors.initials: IR
authors.lastname: Kilford
authors.forename: Xiao Q
authors.initials: XQ
authors.lastname: Lewell
authors.forename: Anton D
authors.initials: AD
authors.lastname: Michel
authors.forename: Shiyam
authors.initials: S
authors.lastname: Mohamed
authors.forename: Alan
authors.initials: A
authors.lastname: Naylor
authors.forename: Riccardo
authors.initials: R
authors.lastname: Novelli
authors.forename: Lee
authors.initials: L
authors.lastname: Skinner
authors.forename: David J
authors.initials: DJ
authors.lastname: Spalding
authors.forename: Sac P
authors.initials: SP
authors.lastname: Tang
authors.forename: Richard J
authors.initials: RJ
authors.lastname: Wilson
mesh_terms: D000818:Animals; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D066298:In Vitro Techniques; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype
chemical_list: D006571:Heterocyclic Compounds; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype