Cyclic urea derivatives as potent NK1 selective antagonists.
A series of novel five- and six-membered ring urea derivatives have been described as potent and selective NK1 receptor antagonists. Several compounds in this series exhibited good oral activity and brain penetration. Syntheses of these compounds are also described herein.
Shue
Ho-Jane
HJ
Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
Chen
Xiao
X
Shih
Neng-Yang
NY
Blythin
David J
DJ
Paliwal
Sunil
S
Lin
Ling
L
Gu
Danlin
D
Schwerdt
John H
JH
Shah
Sapna
S
Reichard
Gregory A
GA
Piwinski
John J
JJ
Duffy
Ruth A
RA
Lachowicz
Jean E
JE
Coffin
Vicki L
VL
Liu
Fei
F
Nomeir
Amin A
AA
Morgan
Cynthia A
CA
Varty
Geoffrey B
GB
D000818:Animals; D001682:Biological Availability; D004305:Dose-Response Relationship, Drug; D005849:Gerbillinae; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D009043:Motor Activity / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology
D006571:Heterocyclic Compounds; D064729:Neurokinin-1 Receptor Antagonists; D014508:Urea