title: 4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
abstract: 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.
authors.affiliation: 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
authors.forename: Laura C
authors.initials: LC
authors.lastname: Cooper
authors.forename: Emma J
authors.initials: EJ
authors.lastname: Carlson
authors.forename: Jose L
authors.initials: JL
authors.lastname: Castro
authors.forename: Gary G
authors.initials: GG
authors.lastname: Chicchi
authors.forename: Kevin
authors.initials: K
authors.lastname: Dinnell
authors.forename: Jerry
authors.initials: J
authors.lastname: Di Salvo
authors.forename: Jason M
authors.initials: JM
authors.lastname: Elliott
authors.forename: Gregory J
authors.initials: GJ
authors.lastname: Hollingworth
authors.forename: Marc M
authors.initials: MM
authors.lastname: Kurtz
authors.forename: Mark P
authors.initials: MP
authors.lastname: Ridgill
authors.forename: Wayne
authors.initials: W
authors.lastname: Rycroft
authors.forename: Kwei-Lan
authors.initials: KL
authors.lastname: Tsao
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Swain
mesh_terms: 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
chemical_list: 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