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.
Hoffmann, Torsten,Boes, Michael,Stadler, Heinz,Schnider, Patrick,Hunkeler, Walter,Godel, Thierry,Galley, Guido,Ballard, Theresa M.,Higgins, Guy A.,Poli, Sonia M.,Sleight, Andrew J.
p. 1362 - 1365
(2007/10/03)
4-phenyl-pyridine derivatives
The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.
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(2008/06/13)
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