Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator
ACS Medicinal Chemistry Letters2013Vol. 4(3), pp. 333–337
Citations Over TimeTop 10% of 2013 papers
Shifeng Pan, Nathanael S. Gray, Wenqi Gao, Yuan Mi, Yi Fan, Xing Wang, Tove Tuntland, Jianwei Che, Sophie Lefebvre, Yu Chen, Alan Chu, Klaus Hinterding, Anne Gardin, Peter End, Peter Heining, Christian Bruns, Nigel G. Cooke, Barbara Nuesslein‐Hildesheim
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.
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