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

作者信息

Hoffmann Torsten, Bös Michael, Stadler Heinz, Schnider Patrick, Hunkeler Walter, Godel Thierry, Galley Guido, Ballard Theresa M, Higgins Guy A, Poli Sonia M, Sleight Andrew J

机构信息

F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland.

出版信息

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1362-5. doi: 10.1016/j.bmcl.2005.11.047. Epub 2005 Dec 5.

DOI:10.1016/j.bmcl.2005.11.047

PMID:16332435

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.

摘要

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