Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor

Abstract Modulators of S1P 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 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 1 receptor.