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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: aspnes g. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Trifluoromethylpyrimidine-based inhibitors of proline-rich tyrosine kinase 2 (PYK2): structure-activity relationships and strategies for the elimination of reactive metabolite formation.
Walker DP, Bi FC, Kalgutkar AS, Bauman JN, Zhao SX, Soglia JR, Aspnes GE, Kung DW, Klug-McLeod J, Zawistoski MP, McGlynn MA, Oliver R, Dunn M, Li JC, Richter DT, Cooper BA, Kath JC, Hulford CA, Autry CL, Luzzio MJ, Ung EJ, Roberts WG, Bonnette PC, Buckbinder L, Mistry A, Griffor MC, Han S, Guzman-Perez A. Walker DP, et al. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6071-7. doi: 10.1016/j.bmcl.2008.10.030. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18951788
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. 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
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.
Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X. Bhattacharya SK, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23153798
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. 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. 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
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: aspnes g. 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
Discovery and Optimization of Imidazopyridine-Based Inhibitors of Diacylglycerol Acyltransferase 2 (DGAT2).
Futatsugi K, Kung DW, Orr ST, Cabral S, Hepworth D, Aspnes G, Bader S, Bian J, Boehm M, Carpino PA, Coffey SB, Dowling MS, Herr M, Jiao W, Lavergne SY, Li Q, Clark RW, Erion DM, Kou K, Lee K, Pabst BA, Perez SM, Purkal J, Jorgensen CC, Goosen TC, Gosset JR, Niosi M, Pettersen JC, Pfefferkorn JA, Ahn K, Goodwin B. Futatsugi K, et al. Among authors: aspnes g. J Med Chem. 2015 Sep 24;58(18):7173-85. doi: 10.1021/acs.jmedchem.5b01006. J Med Chem. 2015. PMID: 26349027
35 results