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Page 1
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP, Gobbi A, Savy P, Burton B, Deng Y, Everett C, La H, Johnson AR, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: la h. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4109-13. doi: 10.1016/j.bmcl.2015.08.028. Epub 2015 Aug 14. Bioorg Med Chem Lett. 2015. PMID: 26321361
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. Among authors: la h. 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: la h. 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
Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Fauber BP, Gobbi A, Robarge K, Zhou A, Barnard A, Cao J, Deng Y, Eidenschenk C, Everett C, Ganguli A, Hawkins J, Johnson AR, La H, Norman M, Salmon G, Summerhill S, Ouyang W, Tang W, Wong H. Fauber BP, et al. Among authors: la h. Bioorg Med Chem Lett. 2015 Aug 1;25(15):2907-12. doi: 10.1016/j.bmcl.2015.05.055. Epub 2015 May 28. Bioorg Med Chem Lett. 2015. PMID: 26048793
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. Among authors: la h. 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
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: la h. 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
Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.
Huestis MP, Dela Cruz D, DiPasquale AG, Durk MR, Eigenbrot C, Gibbons P, Gobbi A, Hunsaker TL, La H, Leung DH, Liu W, Malek S, Merchant M, Moffat JG, Muli CS, Orr CJ, Parr BT, Shanahan F, Sneeringer CJ, Wang W, Yen I, Yin J, Siu M, Rudolph J. Huestis MP, et al. Among authors: la h. J Med Chem. 2021 Apr 8;64(7):3940-3955. doi: 10.1021/acs.jmedchem.0c02085. Epub 2021 Mar 29. J Med Chem. 2021. PMID: 33780623
Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).
Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ. Flygare JA, et al. Among authors: la h. J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28. J Med Chem. 2012. PMID: 22413863 Free PMC article.
216 results