Novel imidazobenzazepine derivatives as dual H1/5-HT2A antagonists for the treatment of sleep disorders |
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| Authors: | Massimo Gianotti Corrado Corti Sonia Delle Fratte Romano Di Fabio Colin P. Leslie Francesca Pavone Laura Piccoli Luigi Stasi Mark J. Wigglesworth |
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| Affiliation: | 1. Neurosciences CEDD, GlaxoSmithKline, Medicines Research Centre, Via A. Fleming 4, 37135 Verona, Italy;2. GlaxoSmithKline Medicines Research Centre, NFSP, Harlow, UK |
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| 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 (e.g., 9, 19, 20, and 21), characterized by potent and balanced H1/5-HT2A receptor antagonist activities and good developability profiles. |
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