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

Dirk Behnke,Simona Cotesta,Samuel Hintermann,Markus Fendt,Christine E Gee,Laura H Jacobson,Grit Laue,Arndt Meyer,Trixie Wagner,Sangamesh Badiger,Vinod Chaudhari,Murali Chebrolu,Chetan Pandit,Daniel Hoyer,Claudia Betschart

Bioorganic & Medicinal Chemistry Letters（2015）

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摘要

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.

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关键词

Orexin,GPCRs,Insomnia,Antagonists

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