635701-98-3Relevant academic research and scientific papers
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.
PROCESS FOR MAKING AZETIDINE-3-CARBOXYLIC ACID
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Page 48, (2010/02/06)
The present invention is directed to an improved process for synthesizing azetidine-3-carboxylic acid, comprising triflating diethylbis(hydroxymethyl)malonate followed by azetidine ring-formation by intramolecular cyclization using an amine, decarboxylation to give the mono acid azetidine and hydrogenation to give the title compound. Azetidine-3-carboxylic acid is useful as an intermediate for making certain S1P?1#191/Edg1 receptor agonists, which are immunosupressive agents.
1-((5-ARYL-1,2,4-OXADIAZOL-3-YL)BENZYL)AZETIDINE-3-CARBOXYLATES AND 1-((5-ARYL-1,2,4-OXADIAZOL-3-YL)BENZYL)PYRROLIDINE-3-CARBOXYLATES AS EDG RECEPTOR AGONISTS
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Page 42, (2010/02/06)
The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.
