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Page 1
Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.
René O, Fauber BP, Barnard A, Chapman K, Deng Y, Eidenschenk C, Everett C, Gobbi A, Johnson AR, La H, Norman M, Salmon G, Summerhill S, Wong H. René O, et al. Among authors: fauber bp. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4455-4461. doi: 10.1016/j.bmcl.2016.07.081. Epub 2016 Aug 3. Bioorg Med Chem Lett. 2016. PMID: 27524313
Identification of tertiary sulfonamides as RORc inverse agonists.
Fauber BP, René O, Burton B, Everett C, Gobbi A, Hawkins J, Johnson AR, Liimatta M, Lockey P, Norman M, Wong H. Fauber BP, et al. Bioorg Med Chem Lett. 2014 May 1;24(9):2182-7. doi: 10.1016/j.bmcl.2014.03.038. Epub 2014 Mar 21. Bioorg Med Chem Lett. 2014. PMID: 24685544
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Fauber BP, René O, de Leon Boenig G, Burton B, Deng Y, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, La H, Liimatta M, Lockey P, Norman M, Ouyang W, Wang W, Wong H. Fauber BP, et al. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3891-7. doi: 10.1016/j.bmcl.2014.06.048. Epub 2014 Jun 25. Bioorg Med Chem Lett. 2014. PMID: 25017032
A reversed sulfonamide series of selective RORc inverse agonists.
van Niel MB, Fauber BP, Cartwright M, Gaines S, Killen JC, René O, Ward SI, de Leon Boenig G, Deng Y, Eidenschenk C, Everett C, Gancia E, Ganguli A, Gobbi A, Hawkins J, Johnson AR, Kiefer JR, La H, Lockey P, Norman M, Ouyang W, Qin A, Wakes N, Waszkowycz B, Wong H. van Niel MB, et al. Among authors: fauber bp. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5769-5776. doi: 10.1016/j.bmcl.2014.10.037. Epub 2014 Oct 25. Bioorg Med Chem Lett. 2014. PMID: 25453817
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
René O, Fauber BP, Boenig Gde L, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Kiefer JR, Liimatta M, Lockey P, Norman M, Ouyang W, Wallweber HA, Wong H. René O, et al. Among authors: fauber bp. ACS Med Chem Lett. 2014 Dec 4;6(3):276-81. doi: 10.1021/ml500420y. eCollection 2015 Mar 12. ACS Med Chem Lett. 2014. PMID: 25815138 Free PMC article.
Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.
Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A, Gobbi A, Hawkins J, Johnson AR, La H, Lesch J, Lockey P, Norman M, Ouyang W, Summerhill S, Wong H. Fauber BP, et al. J Med Chem. 2015 Jul 9;58(13):5308-22. doi: 10.1021/acs.jmedchem.5b00597. Epub 2015 Jun 23. J Med Chem. 2015. PMID: 26061388
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