Novel imidazobenzazepine derivatives as dual H 1/5-HT 2A antagonists for the treatment of sleep disorders

…, S Delle Fratte, R Di Fabio, CP Leslie, F Pavone…

Index: Gianotti, Massimo; Corti, Corrado; Fratte, Sonia Delle; Di Fabio, Romano; Leslie, Colin P.; Pavone, Francesca; Piccoli, Laura; Stasi, Luigi; Wigglesworth, Mark J. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 17 p. 5069 - 5073

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Citation Number: 9

Abstract

A novel imidazobenzazepine template (5a) with potent dual H1/5-HT2A antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R1-2- R-5H-imidazo [1, 2-b][2] benzazepin-11-yl)-1-piperazinyl]-2, 2-dimethylpropanoic acids (eg, 9, 19, 20, and 21), characterized by potent and balanced H1/5-HT2A receptor antagonist ...