Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 4, Issue 3, Pages 333-337Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml300396r
Keywords
S1P receptor; S1P(1) agonist; lymphocytes
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A novel series of alkoxyimino derivatives as S1P(1), 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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