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Page 1
Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors.
Van Huis CA, Bigge CF, Casimiro-Garcia A, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Narasimhan LS, Schaum RP, Zhang E, Bryant JW, Haarer S, Janiczek N, Leadley RJ Jr, McClanahan T, Thomas Peterson J, Welch KM, Edmunds JJ. Van Huis CA, et al. Among authors: filipski kj. Chem Biol Drug Des. 2007 Jun;69(6):444-50. doi: 10.1111/j.1747-0285.2007.00520.x. Chem Biol Drug Des. 2007. PMID: 17581239
The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor.
Kohrt JT, Bigge CF, Bryant JW, Casimiro-Garcia A, Chi L, Cody WL, Dahring T, Dudley DA, Filipski KJ, Haarer S, Heemstra R, Janiczek N, Narasimhan L, McClanahan T, Peterson JT, Sahasrabudhe V, Schaum R, Van Huis CA, Welch KM, Zhang E, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: filipski kj. Chem Biol Drug Des. 2007 Aug;70(2):100-12. doi: 10.1111/j.1747-0285.2007.00539.x. Chem Biol Drug Des. 2007. PMID: 17683371
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
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.
Van Huis CA, Casimiro-Garcia A, Bigge CF, Cody WL, Dudley DA, Filipski KJ, Heemstra RJ, Kohrt JT, Leadley RJ Jr, Narasimhan LS, McClanahan T, Mochalkin I, Pamment M, Peterson JT, Sahasrabudhe V, Schaum RP, Edmunds JJ. Van Huis CA, et al. Among authors: filipski kj. Bioorg Med Chem. 2009 Mar 15;17(6):2501-11. doi: 10.1016/j.bmc.2009.01.063. Epub 2009 Feb 3. Bioorg Med Chem. 2009. PMID: 19231206
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
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
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
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
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
32 results