885706-06-9Relevant academic research and scientific papers
2-(ARYL)AZACYCLYLMETHYL CARBOXYLATES, SULFONATES, PHOSPHONATES, PHOSPHINATES AND HETEROCYCLES AS S1P RECEPTOR AGONISTS
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Page/Page column 44, (2008/06/13)
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by mo
Discovery of potent 3,5-diphenyl-1,2,4-oxadiazole sphingosine-1-phosphate-1 (S1P1) receptor agonists with exceptional selectivity against S1P2 and S1P3
Li, Zhen,Chen, Weirong,Hale, Jeffrey J.,Lynch, Christopher L.,Mills, Sander G.,Hajdu, Richard,Keohane, Carol Ann,Rosenbach, Mark J.,Milligan, James A.,Shei, Gan-Ju,Chrebet, Gary,Parent, Stephen A.,Bergstrom, James,Card, Deborah,Forrest, Michael,Quackenbush, Elizabeth J.,Wickham, L. Alexandra,Vargas, Hugo,Evans, Rose M.,Rosen, Hugh,Mandala, Suzanne
, p. 6169 - 6173 (2007/10/03)
A class of 3,5-diphenyl-1,2,4-oxadiazole based compounds have been identified as potent sphingosine-1-phosphate-1 (S1P1) receptor agonists with minimal affinity for the S1P2 and S1P3 receptor subtypes. Analogue 26 (S1P1 IC50 = 0.6 nM) has an excellent pharmacokinetics profile in the rat and dog and is efficacious in a rat skin transplant model, indicating that S1P3 receptor agonism is not a component of immunosuppressive efficacy.
