alexa Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Neurology

Neurology

Journal of Multiple Sclerosis

Author(s): Pan S, Gray NS, Gao W, Mi Y, Fan Y, , Pan S, Gray NS, Gao W, Mi Y, Fan Y,

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Abstract A novel series of alkoxyimino derivatives as S1P1 agonists were discovered through de novo design using FTY720 as the chemical starting point. Extensive structure-activity relationship studies led to the discovery of (E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid (32, BAF312, Siponimod), which has recently completed phase 2 clinical trials in patients with relapsing-remitting multiple sclerosis.
This article was published in ACS Med Chem Lett and referenced in Journal of Multiple Sclerosis

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