- Novel Potent Dopamine-Norepinephrine and Triple Reuptake Uptake Inhibitors Based on Asymmetric Pyran Template and Their Molecular Interactions with Monoamine Transporters
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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
- Santra, Soumava,Kortagere, Sandhya,Vedachalam, Seenuvasan,Gogoi, Sanjib,Antonio, Tamara,Reith, Maarten E.A.,Dutta, Aloke K.
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p. 1406 - 1418
(2021/05/10)
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- HEAT SHOCK PROTEIN 90 INHIBITORS
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Substituted aromatic compounds of formula (I) shown below: (formula I) The definition of each variable in formula (I) appears in the Specification. Also disclosed is a pharmaceutical composition containing one of the substituted aromatic compounds. Further disclosed is a method of using one of these compounds for treating a medical condition associated with HSP90.
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Page/Page column 32; 33; 35
(2018/10/19)
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- Substituted Pyran Derivatives
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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
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Paragraph 0135; 0136
(2014/10/29)
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- Antagonists of the human A2A adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines
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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.
- 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.
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experimental part
p. 33 - 47
(2011/04/19)
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- Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors
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Previously, we developed a strategy to develop a novel class of histone deacetylase (HDAC) inhibitors by tethering short-chain fatty acids with Zn 2+-chelating motifs, which led to N-hydroxy-4-(4-phenylbutyryl-amino) benzamide (HTPB), a hydroxa
- Lu, Qiang,Wang, Da-Sheng,Chen, Chang-Shi,Hu, Yuan-Dong,Chen, Ching-Shih
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p. 5530 - 5535
(2007/10/03)
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- QUINOLINE-DERIVED AMIDE MODULATORS OF VANILLOID VR1 RECEPTOR
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This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to quinoline-derived amides that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.
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