1202074-00-7Relevant articles and documents
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups
Reed, Anthony B.,Lanman, Brian A.,Neira, Susana,Harrington, Paul E.,Sham, Kelvin K.C.,Frohn, Mike,Pickrell, Alexander J.,Tasker, Andrew S.,Gore, Anu,Fiorino, Mike,Itano, Andrea,McElvain, Michele,Middleton, Scot,Morrison, Henry,Xu, Han,Xu, Yang,Wong, Min,Cee, Victor J.
, p. 1779 - 1783 (2012/04/04)
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (-)-2-amino -4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo[5,4-b]pyridin-2-yl) phenyl)-2-methylbutanoic acid (8c), which possessed good in vivo efficacy and pharmacokinetic properties. A 0.3 mg/kg oral dose of 8c produced a statistically significant reduction in blood lymphocyte counts 24 h post-dosing in female Lewis rats.
