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.
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
Eileen M
EM
Seward
Emma
E
Carlson
Timothy
T
Harrison
Karen R
KR
Haworth
Richard
R
Herbert
Fintan J
FJ
Kelleher
Marc M
MM
Kurtz
Jonathan
J
Moseley
Simon N
SN
Owen
Andrew P
AP
Owens
Sharon J
SJ
Sadowski
Christopher J
CJ
Swain
Brian J
BJ
Williams
D064729:Neurokinin-1 Receptor Antagonists; D013141:Spiro Compounds / Q000494:pharmacology*
D064729:Neurokinin-1 Receptor Antagonists; D013141:Spiro Compounds