Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
A series of novel spiroketal-based NK(1) antagonists is described. The effect of modifications to the spiroether ring and aromatic substituents are discussed, leading to the identification of compounds with high affinity and excellent CNS penetration.
Seward
Eileen M
EM
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex, UK. eileen_seward@merck.com
Carlson
Emma
E
Harrison
Timothy
T
Haworth
Karen R
KR
Herbert
Richard
R
Kelleher
Fintan J
FJ
Kurtz
Marc M
MM
Moseley
Jonathan
J
Owen
Simon N
SN
Owens
Andrew P
AP
Sadowski
Sharon J
SJ
Swain
Christopher J
CJ
Williams
Brian J
BJ
D064729:Neurokinin-1 Receptor Antagonists; D013141:Spiro Compounds / Q000494:pharmacology*
D064729:Neurokinin-1 Receptor Antagonists; D013141:Spiro Compounds