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Piperidine-based renin inhibitors: Upper chain optimization |
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| Authors: | Olivier Corminboeuf Olivier Bezençon ?ubo? Remeň Corinna Grisostomi Sylvia Richard-Bildstein Daniel Bur Lars Prade Panja Strickner Patrick Hess Walter Fischli Beat Steiner Alexander Treiber |
| Institution: | Drug Discovery Chemistry & Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland |
| Abstract: | The optimization of the 4-position of recently described new 3,4-disubstituted piperidine-based renin inhibitors is reported herein. The synthesis and characterization of compounds leading to the discovery of 11 (ACT-178882, MK-1597), a renin inhibitor with a suitable profile for development is described. |
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