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
  • 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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