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Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs)

Behnke, Dirk and Cotesta, Simona and Hintermann, Samuel and Fendt, Markus and Gee, Christine and Jacobson, Laura and Laue, Grit and Meyer, Arndt and Wagner, Beatrix and Badiger, Sangamesh and Chaudhari, Vinod and Chebrolu, Murali and Pandit, Chetan and Hoyer, Daniel and Betschart, Claudia (2015) Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs). Bioorganic and Medicinal Chemistry Letters, 25 (23). pp. 5555-5560. ISSN 0960-894X

Abstract

Compound rac-1 was identified by high throughput screening. Here we report SAR studies and MedChem optimization towards the highly potent dual orexin receptor antagonists (S)-2 and (S)-3. Furthermore, strategies to overcome the suboptimal physicochemical properties are highlighted and the pharmacokinetic profiles of representative compounds is presented.

Item Type: Article
Keywords: Orexin, GPCRs, insomnia, antagonists
Date Deposited: 14 Nov 2015 00:45
Last Modified: 14 Nov 2015 00:45
URI: https://oak.novartis.com/id/eprint/26372

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