1085386-52-2Relevant academic research and scientific papers
Design and synthesis of selective and potent orally active S1P5 agonists
Mattes, Henri,Dev, Kumlesh Kumar,Bouhelal, Rochdi,Barske, Carmen,Gasparini, Fabrizio,Guerini, Danilo,Mir, Anis Khusro,Orain, David,Osinde, Maribel,Picard, Anne,Dubois, Celine,Tasdelen, Engin,Haessig, Samuel
, p. 1693 - 1696 (2012/01/02)
Putting the brakes on demyelination: Fingolimod (FTY720) was recently shown to significantly decrease relapse rates in patients with multiple sclerosis. This drug attenuates the trafficking of harmful T-cells entering the brain by regulating sphingosine-1-phosphate (S1P) receptors. We designed, synthesized, evaluated 2H-phthalazin-1-one derivatives (e.g., 1L) as selective S1P5 receptor agonists; these compounds are highly potent and selective, with good PK properties, and significant activity in oligodendrocytes. (Chemical Presented).
BENZAMIDES USEFUL AS S1P RECEPTOR MODULATORS
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Page/Page column 21, (2009/01/20)
The invention relates to novel aromatic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
