Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
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.
Letavic
Michael A
MA
Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. mletavic@prdus.jnj.com
Aluisio
Leah
L
Atack
John R
JR
Bonaventure
Pascal
P
Carruthers
Nicholas I
NI
Dugovic
Christine
C
Everson
Anita
A
Feinstein
Mark A
MA
Fraser
Ian C
IC
Hoey
Kenway
K
Jiang
Xiaohui
X
Keith
John M
JM
Koudriakova
Tatiana
T
Leung
Perry
P
Lord
Brian
B
Lovenberg
Timothy W
TW
Ly
Kiev S
KS
Morton
Kirsten L
KL
Motley
S Timothy
ST
Nepomuceno
Diane
D
Rizzolio
Michele
M
Rynberg
Raymond
R
Sepassi
Kia
K
Shelton
Jonathan
J
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
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