867035-87-8Relevant academic research and scientific papers
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia
Moree, Wilna J.,Li, Bin-Feng,Jovic, Florence,Coon, Timothy,Yu, Jinghua,Gross, Raymond S.,Tucci, Fabio,Marinkovic, Dragan,Zamani-Kord, Said,Malany, Siobhan,Bradbury, Margaret J.,Hernandez, Lisa M.,O'Brien, Zhihong,Wen, Jianyun,Wang, Hua,Hoare, Samuel R. J.,Petroski, Robert E.,Sacaan, Aida,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
supporting information; experimental part, p. 5307 - 5310 (2010/06/13)
Analogues of the known H1-antihistamine R-dimethindene were profiled as potential agents for the treatment of insomnia. Several highly selective compounds were efficacious in rodent sleep models. On the basis of overall profile, indene 1d and benzothiophene 2a had pharmacokinetic properties suitable for evaluation in night time dosing. Compound 2a did not show an in vivo cardiovascular effect from weak hERG channel inhibition.
SLEEP INDUCING COMPOUNDS AND METHODS RELATING THERETO
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Page/Page column 34-37, (2010/02/14)
Compounds having the following structure: (I) including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2a, R2b, R3, R4, R5a, R5b, L1, L2 and n are as defined herein. Pharmaceutical compositions containing one or more compounds of structure (I), as well as methods relating to the use thereof, including methods for treating insomnia, inducing sleep or inducing sedation or hypnosis, are also disclosed.
