title: Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
abstract: The pre-clinical characterization of novel aryloxypyridine amides that are histamine H(3) receptor antagonists is described. These compounds are high affinity histamine H(3) ligands that penetrate the CNS and occupy the histamine H(3) receptor in rat brain. Several compounds were extensively profiled pre-clinically leading to the identification of two compounds suitable for nomination as development candidates.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mletavic@prdus.jnj.com
authors.forename: Michael A
authors.initials: MA
authors.lastname: Letavic
authors.forename: Leah
authors.initials: L
authors.lastname: Aluisio
authors.forename: John R
authors.initials: JR
authors.lastname: Atack
authors.forename: Pascal
authors.initials: P
authors.lastname: Bonaventure
authors.forename: Nicholas I
authors.initials: NI
authors.lastname: Carruthers
authors.forename: Christine
authors.initials: C
authors.lastname: Dugovic
authors.forename: Anita
authors.initials: A
authors.lastname: Everson
authors.forename: Mark A
authors.initials: MA
authors.lastname: Feinstein
authors.forename: Ian C
authors.initials: IC
authors.lastname: Fraser
authors.forename: Kenway
authors.initials: K
authors.lastname: Hoey
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Jiang
authors.forename: John M
authors.initials: JM
authors.lastname: Keith
authors.forename: Tatiana
authors.initials: T
authors.lastname: Koudriakova
authors.forename: Perry
authors.initials: P
authors.lastname: Leung
authors.forename: Brian
authors.initials: B
authors.lastname: Lord
authors.forename: Timothy W
authors.initials: TW
authors.lastname: Lovenberg
authors.forename: Kiev S
authors.initials: KS
authors.lastname: Ly
authors.forename: Kirsten L
authors.initials: KL
authors.lastname: Morton
authors.forename: S Timothy
authors.initials: ST
authors.lastname: Motley
authors.forename: Diane
authors.initials: D
authors.lastname: Nepomuceno
authors.forename: Michele
authors.initials: M
authors.lastname: Rizzolio
authors.forename: Raymond
authors.initials: R
authors.lastname: Rynberg
authors.forename: Kia
authors.initials: K
authors.lastname: Sepassi
authors.forename: Jonathan
authors.initials: J
authors.lastname: Shelton
mesh_terms: D000577:Amides / Q000737:chemistry; D000818:Animals; D001381:Azepines / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D054828:Histamine H3 Antagonists / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
chemical_list: C559587:(4-cyclobutyl-(1,4)diazepan-1-yl)-(6-(4-fluorophenoxy)pyridin-3-yl)methanone; D000577:Amides; D001381:Azepines; D054828:Histamine H3 Antagonists; D011725:Pyridines