2. Academic Validation
  3. Piperidine-based renin inhibitors: upper chain optimization

Piperidine-based renin inhibitors: upper chain optimization

  • Bioorg Med Chem Lett. 2010 Nov 1;20(21):6291-6. doi: 10.1016/j.bmcl.2010.08.087.
Olivier Corminboeuf 1,  Olivier Bezençon,  Luboš Remeň,  Corinna Grisostomi,  Sylvia Richard-Bildstein,  Daniel Bur,  Lars Prade,  Panja Strickner,  Patrick Hess,  Walter Fischli,  Beat Steiner,  Alexander Treiber
Affiliations

Affiliation

  • 1 Drug Discovery Chemistry & Biochemistry, Actelion Pharmaceuticals Ltd, Gewerbestrasse 16, 4123 Allschwil, Switzerland.
PMID: 20843690 DOI: 10.1016/j.bmcl.2010.08.087
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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