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Page 1
Pyrimidone-based series of glucokinase activators with alternative donor-acceptor motif.
Filipski KJ, Guzman-Perez A, Bian J, Perreault C, Aspnes GE, Didiuk MT, Dow RL, Hank RF, Jones CS, Maguire RJ, Tu M, Zeng D, Liu S, Knafels JD, Litchfield J, Atkinson K, Derksen DR, Bourbonais F, Gajiwala KS, Hickey M, Johnson TO, Humphries PS, Pfefferkorn JA. Filipski KJ, et al. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4571-8. doi: 10.1016/j.bmcl.2013.06.036. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23831135
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Rapundalo ST, Saiya-Cork K, Leadley RJ, Narasimhan L, Zhang E, Whitlow M, Adler M, McLean K, Chou YL, McKnight C, Arnaiz DO, Shaw KJ, Light DR, Edmunds JJ. Kohrt JT, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4752-6. doi: 10.1016/j.bmcl.2005.07.059. Bioorg Med Chem Lett. 2005. PMID: 16125385
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Narasimhan LS, Zhang E, Rapundalo ST, Saiya-Cork K, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1060-4. doi: 10.1016/j.bmcl.2005.10.076. Epub 2005 Nov 11. Bioorg Med Chem Lett. 2006. PMID: 16289811
The discovery of glycine and related amino acid-based factor Xa inhibitors.
Kohrt JT, Filipski KJ, Cody WL, Bigge CF, La F, Welch K, Dahring T, Bryant JW, Leonard D, Bolton G, Narasimhan L, Zhang E, Peterson JT, Haarer S, Sahasrabudhe V, Janiczek N, Desiraju S, Hena M, Fiakpui C, Saraswat N, Sharma R, Sun S, Maiti SN, Leadley R, Edmunds JJ. Kohrt JT, et al. Among authors: filipski kj. Bioorg Med Chem. 2006 Jul 1;14(13):4379-92. doi: 10.1016/j.bmc.2006.02.040. Epub 2006 Mar 10. Bioorg Med Chem. 2006. PMID: 16529937
Pyrazole inhibitors of HMG-CoA reductase: an attempt to dramatically reduce synthetic complexity through minimal analog re-design.
Larsen SD, Poel TJ, Filipski KJ, Kohrt JT, Pfefferkorn JA, Sorenson RJ, Tait BD, Askew V, Dillon L, Hanselman JC, Lu GH, Robertson A, Sekerke C, Kowala MC, Auerbach BJ. Larsen SD, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5567-72. doi: 10.1016/j.bmcl.2007.08.004. Epub 2007 Aug 11. Bioorg Med Chem Lett. 2007. PMID: 17764936
Pyridones as glucokinase activators: identification of a unique metabolic liability of the 4-sulfonyl-2-pyridone heterocycle.
Pfefferkorn JA, Lou J, Minich ML, Filipski KJ, He M, Zhou R, Ahmed S, Benbow J, Perez AG, Tu M, Litchfield J, Sharma R, Metzler K, Bourbonais F, Huang C, Beebe DA, Oates PJ. Pfefferkorn JA, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2009 Jun 15;19(12):3247-52. doi: 10.1016/j.bmcl.2009.04.107. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19435665
Intrinsic electrophilicity of the 4-methylsulfonyl-2-pyridone scaffold in glucokinase activators: role of glutathione-S-transferases and in vivo quantitation of a glutathione conjugate in rats.
Litchfield J, Sharma R, Atkinson K, Filipski KJ, Wright SW, Pfefferkorn JA, Tan B, Kosa RE, Stevens B, Tu M, Kalgutkar AS. Litchfield J, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6262-7. doi: 10.1016/j.bmcl.2010.08.095. Epub 2010 Aug 21. Bioorg Med Chem Lett. 2010. PMID: 20829042
A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.
Filipski KJ, Bian J, Ebner DC, Lee EC, Li JC, Sammons MF, Wright SW, Stevens BD, Didiuk MT, Tu M, Perreault C, Brown J, Atkinson K, Tan B, Salatto CT, Litchfield J, Pfefferkorn JA, Guzman-Perez A. Filipski KJ, et al. Bioorg Med Chem Lett. 2012 Jan 1;22(1):415-20. doi: 10.1016/j.bmcl.2011.10.113. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22119466
Novel and selective spiroindoline-based inhibitors of Sky kinase.
Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA. Powell NA, et al. Among authors: filipski kj. Bioorg Med Chem Lett. 2012 Jan 1;22(1):190-3. doi: 10.1016/j.bmcl.2011.11.036. Epub 2011 Nov 16. Bioorg Med Chem Lett. 2012. PMID: 22119469
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: filipski kj. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
32 results