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

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Pan S, Gray NS, Gao W, Mi Y, Fan Y, Wang X, Tuntland T, Che J, Lefebvre S, Chen Y, Chu A, Hinterding K, Gardin A, End P, Heining P, Bruns C, Cooke NG, Nuesslein-Hildesheim B

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

ACS Med Chem Lett. 2013 Jan 4;4(3):333-7. doi: 10.1021/ml300396r. eCollection 2013 Mar 14.

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24900670 [ View in PubMed

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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-ethylben zyl)azetidine-3-carboxylic acid (32, BAF312, Siponimod), which has recently completed phase 2 clinical trials in patients with relapsing-remitting multiple sclerosis.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Siponimod	Sphingosine 1-phosphate receptor 1	Protein	Humans	Unknown	Not Available	Details