Benzazepinone Nav1.7 blockers: potential treatments for neuropathic pain.
A series of benzazepinones were synthesized and evaluated as hNa(v)1.7 sodium channel blockers. Several compounds from this series displayed good oral bioavailability and exposure and were efficacious in a rat model of neuropathic pain.
Hoyt
Scott B
SB
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. scott_hoyt@merck.com
London
Clare
C
Ok
Hyun
H
Gonzalez
Edward
E
Duffy
Joseph L
JL
Abbadie
Catherine
C
Dean
Brian
B
Felix
John P
JP
Garcia
Maria L
ML
Jochnowitz
Nina
N
Karanam
Bindhu V
BV
Li
Xiaohua
X
Lyons
Kathryn A
KA
McGowan
Erin
E
Macintyre
D Euan
DE
Martin
William J
WJ
Priest
Birgit T
BT
Smith
McHardy M
MM
Tschirret-Guth
Richard
R
Warren
Vivien A
VA
Williams
Brande S
BS
Kaczorowski
Gregory J
GJ
Parsons
William H
WH
D000818:Animals; D001570:Benzodiazepinones / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001682:Biological Availability; D004195:Disease Models, Animal; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D015394:Molecular Structure; D062556:NAV1.7 Voltage-Gated Sodium Channel; D009437:Neuralgia / Q000188:drug therapy*; D051381:Rats; D026941:Sodium Channel Blockers / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D015222:Sodium Channels / Q000737:chemistry / Q000187:drug effects*
D001570:Benzodiazepinones; D062556:NAV1.7 Voltage-Gated Sodium Channel; C503480:Scn9a protein, rat; D026941:Sodium Channel Blockers; D015222:Sodium Channels