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

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.

Item Type:	Article
Date Deposited:	13 Oct 2015 13:14
Last Modified:	13 Oct 2015 13:14
URI:	https://oak.novartis.com/id/eprint/8865