126645-52-1Relevant articles and documents
Discovery of novel and selective tertiary alcohol containing inhibitors of the norepinephrine transporter
Cases-Thomas, Manuel J.,Masters, John J.,Walter, Magnus W.,Campbell, Gordon,Haughton, Louise,Gallagher, Peter T.,Dobson, David R.,Mancuso, Vincent,Bonnier, Benjamin,Giard, Thierry,Defrance, Thierry,Vanmarsenille, Michel,Ledgard, Andrew,White, Craig,Ouwerkerk-Mahadevan, Sivi,Brunelle, Francoise J.,Dezutter, Nancy A.,Herbots, Camy A.,Lienard, Joel Y.,Findlay, Jeremy,Hayhurst, Lorna,Boot, John,Thompson, Linda K.,Hemrick-Luecke, Susan
, p. 2022 - 2025 (2006)
A novel series of tertiary alcohol containing 2-substituted benzyl morpholines have been discovered as potent and selective inhibitors of the norepinephrine transporter. Efficient synthetic routes were developed featuring a highly diastereoselective nucleophilic addition of benzyl Grignard reagents to enantiopure (4-benzylmorpholin-2-yl)phenylmethanone (11) as the key synthetic step. In vitro binding affinity for the norepinephrine, dopamine and serotonin transporters and in vivo examination of a select compound (16) in a pharmacodynamic animal model for norepinephrine reuptake inhibition are presented.
SUBSTITUTED [1,2,4] TRIAZOLO [1,5-A] PYRIMIDIN-7-YL COMPOUNDS AS PDE2 INHIBITORS
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Page/Page column 48, (2015/11/10)
The invention provides a chemical entity of Formula (I): wherein R1, R2, X, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of
DIHYDROPTERIDINONE DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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, (2012/07/28)
Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defined as in the description, their preparation process, pharmaceutical compositions comprising said derivatives and their use as therapeutical agents, especially as Plk kinase inhibitors are disclosed.
