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Page 1
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: litchfield j. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
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: litchfield j. 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. 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
Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.
Pfefferkorn JA, Litchfield J, Hutchings R, Cheng XM, Larsen SD, Auerbach B, Bush MR, Lee C, Erasga N, Bowles DM, Boyles DC, Lu G, Sekerke C, Askew V, Hanselman JC, Dillon L, Lin Z, Robertson A, Olsen K, Boustany C, Atkinson K, Goosen TC, Sahasrabudhe V, Chupka J, Duignan DB, Feng B, Scialis R, Kimoto E, Bi YA, Lai Y, El-Kattan A, Bakker-Arkema R, Barclay P, Kindt E, Le V, Mandema JW, Milad M, Tait BD, Kennedy R, Trivedi BK, Kowala M. Pfefferkorn JA, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2011 May 1;21(9):2725-31. doi: 10.1016/j.bmcl.2010.11.103. Epub 2010 Nov 26. Bioorg Med Chem Lett. 2011. PMID: 21183342
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.
Pfefferkorn JA, Tu M, Filipski KJ, Guzman-Perez A, Bian J, Aspnes GE, Sammons MF, Song W, Li JC, Jones CS, Patel L, Rasmusson T, Zeng D, Karki K, Hamilton M, Hank R, Atkinson K, Litchfield J, Aiello R, Baker L, Barucci N, Bourassa P, Bourbonais F, D'Aquila T, Derksen DR, MacDougall M, Robertson A. Pfefferkorn JA, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7100-5. doi: 10.1016/j.bmcl.2012.09.082. Epub 2012 Sep 29. Bioorg Med Chem Lett. 2012. PMID: 23089526
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.
Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J. Guzman-Perez A, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8. doi: 10.1016/j.bmcl.2013.03.014. Epub 2013 Mar 13. Bioorg Med Chem Lett. 2013. PMID: 23562063
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. Among authors: litchfield j. 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
Discovery of an intravenous hepatoselective glucokinase activator for the treatment of inpatient hyperglycemia.
Stevens BD, Litchfield J, Pfefferkorn JA, Atkinson K, Perreault C, Amor P, Bahnck K, Berliner MA, Calloway J, Carlo A, Derksen DR, Filipski KJ, Gumkowski M, Jassal C, MacDougall M, Murphy B, Nkansah P, Pettersen J, Rotter C, Zhang Y. Stevens BD, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6588-92. doi: 10.1016/j.bmcl.2013.10.057. Epub 2013 Nov 4. Bioorg Med Chem Lett. 2013. PMID: 24239482
Identification of a novel conformationally constrained glucagon receptor antagonist.
Lee EC, Tu M, Stevens BD, Bian J, Aspnes G, Perreault C, Sammons MF, Wright SW, Litchfield J, Kalgutkar AS, Sharma R, Didiuk MT, Ebner DC, Filipski KJ, Brown J, Atkinson K, Pfefferkorn JA, Guzman-Perez A. Lee EC, et al. Among authors: litchfield j. Bioorg Med Chem Lett. 2014 Feb 1;24(3):839-44. doi: 10.1016/j.bmcl.2013.12.090. Epub 2013 Dec 28. Bioorg Med Chem Lett. 2014. PMID: 24418771
136 results