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Deprecated: Implicit conversion from float 233.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2013 ; 4 (3): 333-7 Nephropedia Template TP
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Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator #MMPMID24900670
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 N; Nuesslein-Hildesheim B
ACS Med Chem Lett 2013[Mar]; 4 (3): 333-7 PMID24900670show ga
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.