Design and synthesis of new tricyclic indoles as potent modulators of the S1P sub(1) receptor

Design and synthesis of new tricyclic indoles as potent modulators of the S1P sub(1) receptor

Modulators of S1P sub(1) have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P sub(1) chemotypes were designed and optimized for potency and oral bioavailability. These new agent...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-02, Vol.25 (3), p.659-663
Hauptverfasser: Buzard, Daniel J, Schrader, Thomas O, Zhu, Xiuwen, Lehmann, Juerg, Johnson, Ben, Kasem, Michelle, Kim, Sun Hee, Kawasaki, Andrew, Lopez, Luis, Moody, Jeanne, Han, Sangdon, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Thatte, Jayant, Gatlin, Joel, Jones, Robert M
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Sprache:eng
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Zusammenfassung:Modulators of S1P sub(1) have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P sub(1) chemotypes were designed and optimized for potency and oral bioavailability. These new agents are characterized by a 'tricyclic fused indole array' and are highly potent agonists of the S1P sub(1) receptor.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2014.11.089