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2 results on '"Schutz N"'

1. Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.

Author

Saha AK, Yu X, Lin J, Lobera M, Sharadendu A, Chereku S, Schutz N, Segal D, Marantz Y, McCauley D, Middleton S, Siu J, Bürli RW, Buys J, Horner M, Salyers K, Schrag M, Vargas HM, Xu Y, McElvain M, and Xu H

Abstract

We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P1 agonist with >1000× selectivity over S1P3. It demonstrated a good in vitro ADME profile and excellent oral bioavailability across species. Dosed orally at 0.3 mg/kg, 18 significantly reduced blood lymphocyte counts 24 h postdose and demonstrated efficacy in a mouse EAE model of relapsing MS.

Published
2010
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2. Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1).

Author

Lanman BA, Cee VJ, Cheruku SR, Frohn M, Golden J, Lin J, Lobera M, Marantz Y, Muller KM, Neira SC, Pickrell AJ, Rivenzon-Segal D, Schutz N, Sharadendu A, Yu X, Zhang Z, Buys J, Fiorino M, Gore A, Horner M, Itano A, McElvain M, Middleton S, Schrag M, Vargas HM, Xu H, Xu Y, Zhang X, Siu J, and Bürli RW

Abstract

Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at 0.3 mg/kg, 14 significantly reduced blood lymphocyte counts 24 h postdose and attenuated a delayed type hypersensitivity (DTH) response to antigen challenge.

Published
2010
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