172353-84-3Relevant articles and documents
Novel Potent Dopamine-Norepinephrine and Triple Reuptake Uptake Inhibitors Based on Asymmetric Pyran Template and Their Molecular Interactions with Monoamine Transporters
Santra, Soumava,Kortagere, Sandhya,Vedachalam, Seenuvasan,Gogoi, Sanjib,Antonio, Tamara,Reith, Maarten E.A.,Dutta, Aloke K.
, p. 1406 - 1418 (2021/05/10)
We have carried out a structural exploration of (2S,4R,5R)-2-(bis(4-fluorophenyl)methyl)-5-((4-methoxybenzyl)amino)tetrahydro-2H-pyran-4-ol (D-473) to investigate the influence of various functional groups on its aromatic ring, the introduction of heteroc
Substituted Pyran Derivatives
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, (2014/10/29)
Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter system
Antagonists of the human A2A adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines
Gillespie, Roger J.,Bamford, Samantha J.,Botting, Ruth,Comer, Mike,Denny, Sarah,Gaur, Suneel,Griffin, Michael,Jordan, Allan M.,Knight, Anthony R.,Lerpiniere, Joanne,Leonardi, Stefania,Lightowler, Sean,McAteer, Steven,Merrett, Angela,Misra, Anil,Padfield, Antony,Reece, Mark,Saadi, Mona,Selwood, Daniel L.,Stratton, Gemma C.,Surry, Dominic,Todd, Richard,Tong, Xin,Ruston, Vicki,Upton, Rebecca,Weiss, Scott M.
, p. 33 - 47 (2011/04/19)
Antagonism of the human A2A receptor has been implicated as a point of therapeutic intervention in the alleviation of the symptoms associated with Parkinson's disease. This is thought to occur, at least in part, by increasing the sensitivity of the dopaminergic neurons to the residual, depleted levels of striatal dopamine. We herein describe a novel series of functionalized triazolo[4,5-d]pyrimidine derivatives that display functional antagonism of the A2A receptor. Optimization of these compounds has resulted in improvements in potency, selectivity, and the pharmacokinetic properties of key derivatives. These efforts have led to the discovery of 60 (V2006/BIIB014), which demonstrates strong oral activity in commonly used models of Parkinson's disease. Furthermore, this derivative has shown excellent preclinical pharmacokinetics and has successfully completed phase I clinical studies. This compound is presently undergoing further clinical evaluation in collaboration with Biogen Idec.