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Page 1
Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.
Hurley CA, Blair WS, Bull RJ, Chang C, Crackett PH, Deshmukh G, Dyke HJ, Fong R, Ghilardi N, Gibbons P, Hewitt PR, Johnson A, Johnson T, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Maxey RJ, Mendonca R, Narukulla R, Pulk R, Ubhayakar S, van Abbema A, Ward SI, Waszkowycz B, Zak M. Hurley CA, et al. Among authors: deshmukh g. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3592-8. doi: 10.1016/j.bmcl.2013.04.018. Epub 2013 Apr 17. Bioorg Med Chem Lett. 2013. PMID: 23642482
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: deshmukh g. J Med Chem. 2013 Jun 13;56(11):4764-85. doi: 10.1021/jm4004895. Epub 2013 May 31. J Med Chem. 2013. PMID: 23659214
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. Among authors: deshmukh g. 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 imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Kulagowski JJ, Blair W, Bull RJ, Chang C, Deshmukh G, Dyke HJ, Eigenbrot C, Ghilardi N, Gibbons P, Harrison TK, Hewitt PR, Liimatta M, Hurley CA, Johnson A, Johnson T, Kenny JR, Bir Kohli P, Maxey RJ, Mendonca R, Mortara K, Murray J, Narukulla R, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Waszkowycz B, Zak M. Kulagowski JJ, et al. Among authors: deshmukh g. J Med Chem. 2012 Jun 28;55(12):5901-21. doi: 10.1021/jm300438j. Epub 2012 Jun 11. J Med Chem. 2012. PMID: 22591402
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: deshmukh g. J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22698084
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. Among authors: deshmukh g. 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
Lung-restricted inhibition of Janus kinase 1 is effective in rodent models of asthma.
Dengler HS, Wu X, Peng I, Rinderknecht CH, Kwon Y, Suto E, Kohli PB, Liimatta M, Barrett K, Lloyd J, Cain G, Briggs M, Addo S, Salmon G, Ubhayakar S, Deshmukh G, Shahidi-Latham SK, Quiason-Huynh CM, Jackman J, Liu J, Ray NC, Goodacre SC, Johnson A, McKenzie BS, Lee WP, Zak M, Kenny JR, Ghilardi N. Dengler HS, et al. Among authors: deshmukh g. Sci Transl Med. 2018 Nov 21;10(468):eaao2151. doi: 10.1126/scitranslmed.aao2151. Sci Transl Med. 2018. PMID: 30463918
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Hamilton GL, Chen H, Deshmukh G, Eigenbrot C, Fong R, Johnson A, Kohli PB, Lupardus PJ, Liederer BM, Ramaswamy S, Wang H, Wang J, Xu Z, Zhu Y, Vucic D, Patel S. Hamilton GL, et al. Among authors: deshmukh g. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1497-1501. doi: 10.1016/j.bmcl.2019.04.014. Epub 2019 Apr 11. Bioorg Med Chem Lett. 2019. PMID: 31000154
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M. Patel S, et al. Among authors: deshmukh g. J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23. J Med Chem. 2015. PMID: 25341110
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Patel S, Harris SF, Gibbons P, Deshmukh G, Gustafson A, Kellar T, Lin H, Liu X, Liu Y, Liu Y, Ma C, Scearce-Levie K, Ghosh AS, Shin YG, Solanoy H, Wang J, Wang B, Yin J, Siu M, Lewcock JW. Patel S, et al. Among authors: deshmukh g. J Med Chem. 2015 Oct 22;58(20):8182-99. doi: 10.1021/acs.jmedchem.5b01072. Epub 2015 Oct 2. J Med Chem. 2015. PMID: 26431428
105 results