Title of article :
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists
Author/Authors :
Torsten Hoffmann، نويسنده , , Michael B?s، نويسنده , , Heinz Stadler، نويسنده , , Patrick Schnider، نويسنده , , Walter Hunkeler، نويسنده , , Thierry Godel، نويسنده , , Guido Galley، نويسنده , , Theresa M. Ballard، نويسنده , , Guy A. Higgins، نويسنده , , Sonia M. Poli، نويسنده , , Andrew J. Sleight، نويسنده ,
Abstract :
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.
