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

The discovery of a novel, achiral pyridine class of potent and orally active neurokinin-1 (NK1) 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.

Graphical abstractThe discovery of netupitant 21 and befetupitant 29 is described.Figure optionsDownload full-size imageDownload as PowerPoint slide