Novel lactam NK1 antagonists with anti-emetic activity.
Hollingworth GJ,
Carlson EJ,
Castro JL,
Chicchi GG,
Clark N,
Cooper LC,
Dirat O,
Salvo JD,
Elliott JM,
Kilburn R,
Kurtz MM,
Rycroft W,
Tattersall FD,
Tsao KL,
Swain CJ.
Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. greg_hollingworth@merck.com
A series of 4,4-disubstituted cyclohexylamine NK(1) antagonists containing a lactam ring is described. The compounds are brain penetrant and activity is demonstrated in a ferret emesis model.
PMID: 16384700 [PubMed - indexed for MEDLINE]