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Design and optimization of new piperidines as renin inhibitors |
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| Authors: | Olivier Corminboeuf Olivier Bezençon Corinna Grisostomi Ľuboš Remeň Sylvia Richard-Bildstein Daniel Bur Lars Prade Patrick Hess Panja Strickner Walter Fischli Beat Steiner Alexander Treiber |
| Affiliation: | Drug Discovery Chemistry & Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland |
| Abstract: | The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41, two bioavailable renin inhibitors orally active at low doses in a transgenic rat model of hypertension. |
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