2. Academic Validation
  3. Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes

  • Bioorg Med Chem Lett. 2010 Feb 1;20(3):1109-13. doi: 10.1016/j.bmcl.2009.12.024.
Patrizio Mattei 1,  Markus Boehringer,  Patrick Di Giorgio,  Holger Fischer,  Michael Hennig,  Joerg Huwyler,  Buelent Koçer,  Bernd Kuhn,  Bernd M Loeffler,  Alexander Macdonald,  Robert Narquizian,  Etienne Rauber,  Elena Sebokova,  Urs Sprecher
Affiliations

Affiliation

  • 1 F Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland. patrizio.mattei@roche.com
PMID: 20031405 DOI: 10.1016/j.bmcl.2009.12.024
Abstract

Design, synthesis, and SAR are described for a class of DPP-IV inhibitors based on aminobenzo[a]quinolizines with non-aromatic substituents in the S1 specificity pocket. One representative thereof, carmegliptin (8p), was chosen for clinical development. Its X-ray structure in complex with the Enzyme and early efficacy data in animal models of type 2 diabetes are also presented.

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