867038-24-2Relevant academic research and scientific papers
Selectivity profiling of novel indene H1-antihistamines for the treatment of insomnia
Li, Bin-Feng,Moree, Wilna J.,Yu, Jinghua,Coon, Timothy,Zamani-Kord, Said,Malany, Siobhan,Jalali, Kayvon,Wen, Jianyun,Wang, Hua,Yang, Chun,Hoare, Samuel R.J.,Petroski, Robert E.,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
, p. 2629 - 2633 (2010)
A series of indene analogs of the H1-antihistamine (-)-R-dimethindene was evaluated for selectivity in the search for potentially improved sedative-hypnotics. Variation of the 6-substitutent in the indene core in combination with a pendant electron rich heterocycle led to the identification of several potent H1-antihistamines with desirable selectivity over CYP enzymes, the M1 muscarinic receptor and the hERG channel. These compounds were candidates for further ADME profiling and in vivo evaluation.
SLEEP INDUCING COMPOUNDS AND METHODS RELATING THERETO
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Page/Page column 61-62, (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.
