Novel benzothiophene H1-antihistamines for the treatment of insomnia.


SAR of lead benzothiophene H(1)-antihistamine 2 was explored to identify backup candidates with suitable pharmacokinetic profiles for an insomnia program. Several potent and selective H(1)-antihistamines with a range of projected half-lives in humans were identified. Compound 16d had a suitable human half-life as demonstrated in a human microdose study, but… (More)
DOI: 10.1016/j.bmcl.2010.01.134