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Interplay of dissolution, solubility, and nonsink permeation determines the oral absorption of the Hedgehog pathway inhibitor GDC-0449 in dogs: an investigation using preclinical studies and physiologically based pharmacokinetic modeling.
Wong H, Theil FP, Cui Y, Marsters JC Jr, Khojasteh SC, Vernillet L, La H, Song X, Wang H, Morinello EJ, Deng Y, Hop CE. Wong H, et al. Among authors: la h. Drug Metab Dispos. 2010 Jul;38(7):1029-38. doi: 10.1124/dmd.110.032680. Epub 2010 Apr 20. Drug Metab Dispos. 2010. PMID: 20406853
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
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
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
Cyclodextrin Reduces Intravenous Toxicity of a Model Compound.
Mantik P, Xie M, Wong H, La H, Steigerwalt RW, Devanaboyina U, Ganem G, Shih D, Flygare JA, Fairbrother WJ, Chakravarty P, Russell D, Fernandez GE, Narang AS. Mantik P, et al. Among authors: la h. J Pharm Sci. 2019 Jun;108(6):1934-1943. doi: 10.1016/j.xphs.2019.01.004. Epub 2019 Jan 11. J Pharm Sci. 2019. PMID: 30639736
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
216 results