2. Academic Validation
  3. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists

Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists

  • Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. doi: 10.1016/j.bmcl.2005.11.047.
Torsten Hoffmann 1,  Michael Bös,  Heinz Stadler,  Patrick Schnider,  Walter Hunkeler,  Thierry Godel,  Guido Galley,  Theresa M Ballard,  Guy A Higgins,  Sonia M Poli,  Andrew J Sleight
Affiliations

Affiliation

  • 1 F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland. torsten.hoffmann@roche.com
PMID: 16332435 DOI: 10.1016/j.bmcl.2005.11.047
Abstract

The discovery of a novel, achiral pyridine class of potent and orally active neurokinin-1 (NK(1)) receptor antagonists is described. The evaluation of this class is briefly outlined, leading to the identification of netupitant 21 and befetupitant 29, two new proprietary chemical entities with high affinity and excellent CNS penetration.

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