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Discovery and Biological Characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a New Potent and Selective Neurokinin 1 (NK1) Receptor Antagonist Clinical Candidate

Discovery and Biological Characterization of (2R,4S)-1'-acetyl-N-{(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl}-2-(4-fluoro-2-methylphenyl)-N-methyl-4,4'-bipiperidine-1-carboxamide as a New Potent and Selective Neurokinin 1 (NK1) Receptor Antagonist Clinical Candidate

Romano Di Fabio, Giuseppe Alvaro, Cristiana Griffante, Domenica A Pizzi, Daniele Donati, Mario Mattioli, Zadeo Cimarosti, Giuseppe Guercio, Carla Marchioro, Stefano Provera, Laura Zonzini, Dino Montanari, etc.

J Med Chem. 2011 Feb 24;54(4):1071-9.

PMID: 21229983

Abstract:

A large body of compelling preclinical evidence supports the clinical use of neurokinin (NK) receptor antagonists in a plethora of CNS and non-CNS therapeutic areas. The significant investment made in this area over the past 2 decades culminated with the observation that NK(1) receptor antagonists elicited clinical efficacy in major depression disorders. In addition, aprepitant (Merck) was launched as a new drug able to prevent chemotherapy-induced nausea and vomiting (CINV). After the discovery by GlaxoSmithKline of vestipitant, a wide drug discovery program was launched aimed at identifying additional clinical candidates. New compounds were designed to maximize affinity at the NK(1) receptor binding site while retaining suitable physicochemical characteristics to ensure excellent pharmacokinetic and pharmacodynamic properties in vivo. Herein we describe the discovery process of a new NK(1) receptor antagonist (casopitant) selected as clinical candidate and progressed into clinical studies to treat major depression disorders.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP15336728	4,4′-Bipiperidine		15336-72-8	Price

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