4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
A series of novel 4,4-disubstituted cyclohexylamines as NK(1) receptor antagonists is described: modifications to the amine moiety retain NK(1) receptor binding affinity whilst disrupting I(Kr) affinity.
Cooper
Laura C
LC
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. laura_cooper@merck.com
Carlson
Emma J
EJ
Castro
Jose L
JL
Chicchi
Gary G
GG
Dinnell
Kevin
K
Di Salvo
Jerry
J
Elliott
Jason M
JM
Hollingworth
Gregory J
GJ
Kurtz
Marc M
MM
Ridgill
Mark P
MP
Rycroft
Wayne
W
Tsao
Kwei-Lan
KL
Swain
Christopher J
CJ
D000588:Amines / Q000737:chemistry; D000818:Animals; D001578:Benzopyrans / Q000737:chemistry; D001665:Binding Sites; D016466:CHO Cells; D027682:Cation Transport Proteins; D002999:Clone Cells; D006224:Cricetinae; D003514:Cyclohexylamines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051638:Ether-A-Go-Go Potassium Channels; D005849:Gerbillinae; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D008968:Molecular Conformation; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000737:chemistry; D015221:Potassium Channels / Q000187:drug effects / Q000378:metabolism; D024642:Potassium Channels, Voltage-Gated; D011869:Radioligand Assay; D018040:Receptors, Neurokinin-1 / Q000737:chemistry / Q000187:drug effects; D013329:Structure-Activity Relationship; D013997:Time Factors
D000588:Amines; D001578:Benzopyrans; D027682:Cation Transport Proteins; D003514:Cyclohexylamines; D051638:Ether-A-Go-Go Potassium Channels; C092509:KCNH6 protein, human; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; D015221:Potassium Channels; D024642:Potassium Channels, Voltage-Gated; D018040:Receptors, Neurokinin-1; C087257:L 706000