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Spiro-piperidine azetidinones as potent TRPV1 antagonists |
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| Authors: | Dong Xiao Anandan Palani Robert Aslanian Brian A McKittrick Andrew T McPhail Craig C Correll P Tara Phelps John C Anthes Diane Rindgen |
| Institution: | 1. Chemical Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;2. Department of Chemistry, P.M. Gross Chemical Laboratory, Duke University, Durham, NC 27708, USA;3. Neurobiology Research Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA;4. Exploratory Drug Metabolism, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | A series of spiro-piperidine azetidinone were synthesized and evaluated as potential TRPV1 antagonists. An important issue of plasma stability was investigated and resolved. Further focused SAR study lead to the discovery of a potent antagonist with good oral pharmacokinetic profile in rat. |
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