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

Pan, Shifeng, Gray, Nathanael, Gao, Wenqi, Mi, Yuan, Fan, Yi, Wang, Xia, Tuntland, Tove, Che, Jianwei, Lefebvre, Sophie, Chen, Yu, Chu, Alan, Gardin, Anne, End, Peter, Heining, Peter, Bruns, Christian, Cooke, Nigel Graham and Nuesslein-Hildesheim, Barbara (2013) Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Medicinal Chemistry Letters, 4 (3). ISSN 1948-5875


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.

Item Type: Article
Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14


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