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Page 1
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y. Zak M, et al. Among authors: labadie s. J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22698084
Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.
Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S. Goldstein DM, et al. Among authors: labadie ss. J Med Chem. 2006 Mar 9;49(5):1562-75. doi: 10.1021/jm050736c. J Med Chem. 2006. PMID: 16509574
A novel series of IKKβ inhibitors part II: description of a potent and pharmacologically active series of analogs.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Browner MF, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Jaen JC. Cushing TD, et al. Among authors: labadie ss. Bioorg Med Chem Lett. 2011 Jan 1;21(1):423-6. doi: 10.1016/j.bmcl.2010.10.125. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074992
A novel series of IKKβ inhibitors part I: Initial SAR studies of a HTS hit.
Cushing TD, Baichwal V, Berry K, Billedeau R, Bordunov V, Broka C, Cardozo M, Cheng P, Clark D, Dalrymple S, DeGraffenreid M, Gill A, Hao X, Hawley RC, He X, Jaen JC, Labadie SS, Labelle M, Lehel C, Lu PP, McIntosh J, Miao S, Parast C, Shin Y, Sjogren EB, Smith ML, Talamas FX, Tonn G, Walker KM, Walker NP, Wesche H, Whitehead C, Wright M, Browner MF. Cushing TD, et al. Among authors: labadie ss. Bioorg Med Chem Lett. 2011 Jan 1;21(1):417-22. doi: 10.1016/j.bmcl.2010.10.126. Epub 2010 Oct 29. Bioorg Med Chem Lett. 2011. PMID: 21074993
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Labadie S, Dragovich PS, Barrett K, Blair WS, Bergeron P, Chang C, Deshmukh G, Eigenbrot C, Ghilardi N, Gibbons P, Hurley CA, Johnson A, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Mendonca R, Murray JM, Pulk R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward S, Zak M. Labadie S, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7627-33. doi: 10.1016/j.bmcl.2012.10.008. Epub 2012 Oct 11. Bioorg Med Chem Lett. 2012. PMID: 23107482
Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Malek S, Pan B, Peterson D, Pitts K, Purkey HE, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X. Dragovich PS, et al. Among authors: labadie s. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3186-94. doi: 10.1016/j.bmcl.2013.04.001. Epub 2013 Apr 10. Bioorg Med Chem Lett. 2013. PMID: 23628333
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Zak M, Hurley CA, Ward SI, Bergeron P, Barrett K, Balazs M, Blair WS, Bull R, Chakravarty P, Chang C, Crackett P, Deshmukh G, DeVoss J, Dragovich PS, Eigenbrot C, Ellwood C, Gaines S, Ghilardi N, Gibbons P, Gradl S, Gribling P, Hamman C, Harstad E, Hewitt P, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Labadie S, Lee WP, Liao J, Liimatta M, Mendonca R, Narukulla R, Pulk R, Reeve A, Savage S, Shia S, Steffek M, Ubhayakar S, van Abbema A, Aliagas I, Avitabile-Woo B, Xiao Y, Yang J, Kulagowski JJ. Zak M, et al. Among authors: labadie s. J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31. J Med Chem. 2013. PMID: 23659214
Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.
Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Liu Y, Malek S, Peterson D, Pitts K, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Yen I, Yue Q. Fauber BP, et al. Among authors: labadie s. Bioorg Med Chem Lett. 2013 Oct 15;23(20):5533-9. doi: 10.1016/j.bmcl.2013.08.060. Epub 2013 Aug 22. Bioorg Med Chem Lett. 2013. PMID: 24012183
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.
Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M. Labadie S, et al. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27. Bioorg Med Chem Lett. 2013. PMID: 24042009
Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A. Dragovich PS, et al. Among authors: labadie s. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1. Bioorg Med Chem Lett. 2014. PMID: 25037916
32 results