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
Synthesis and evaluation of fluorinated analogues of monoamine reuptake inhibitors
Philippe, Christine,Kaffy, Julia,Milcent, Thierry,Bonnet-Delpon, Danile
experimental part, p. 136 - 145 (2012/03/08)
The synthesis of two series of fluorinated analogues of monoamines reuptake inhibitors based on tertiary alcohols 2-substituted morpholines scaffold has been achieved through the incorporation of fluorinated substituent into 2-substituted morpholino ketones. Their binding affinities have been measured on different monoamine transporters.