172353-84-3Relevant academic research and scientific papers
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
AMINOSTYRYLBENZOFURAN DERIVATIVES AS INHIBITORS AGAINST BETA-AMYLOID FIBRIL FORMATION, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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, (2015/03/16)
The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptabl
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
AMINOSTYRYLBENZOFURAN DERIVATIVES AS INHIBITORS AGAINST BETA-AMYLOID FIBRIL FORMATION, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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, (2013/10/21)
The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptabl
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.
Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation
Byun, Ji Hun,Kim, HyeYun,Kim, YoungSoo,Mook-Jung, Inhee,Kim, Dong Jin,Lee, Won Koo,Yoo, Kyung Ho
scheme or table, p. 5591 - 5593 (2009/06/18)
The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.
Probe for diseases with amyloid accumulation, amyloid-staining agent, remedy and preventive for diseases with amyloid accumulation and diagnostic probe and staining agent for neurofibrillary change
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Page/Page column 16, (2010/02/15)
The present invention provides compounds having high affinity for amyloid β-protein which are for the diagnosis of diseases in which amyloid β-protein accumulates, for agents for specifically staining amyloid β-protein, and for the treatment and/or prophy
