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  • 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.

Bioorganic & medicinal chemistry letters (2005-12-08)
Torsten Hoffmann, Michael Bös, Heinz Stadler, Patrick Schnider, Walter Hunkeler, Thierry Godel, Guido Galley, Theresa M Ballard, Guy A Higgins, Sonia M Poli, Andrew J Sleight
PMID16332435
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.