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Page 1
Carboxylate bioisosteres of gabapentin.
Burgos-Lepley CE, Thompson LR, Kneen CO, Osborne SA, Bryans JS, Capiris T, Suman-Chauhan N, Dooley DJ, Donovan CM, Field MJ, Vartanian MG, Kinsora JJ, Lotarski SM, El-Kattan A, Walters K, Cherukury M, Taylor CP, Wustrow DJ, Schwarz JB. Burgos-Lepley CE, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2333-6. doi: 10.1016/j.bmcl.2005.05.016. Epub 2005 Jun 8. Bioorg Med Chem Lett. 2006. PMID: 15946842
Carboxylate bioisosteres of pregabalin.
Schwarz JB, Colbry NL, Zhu Z, Nichelson B, Barta NS, Lin K, Hudack RA, Gibbons SE, Galatsis P, DeOrazio RJ, Manning DD, Vartanian MG, Kinsora JJ, Lotarski SM, Li Z, Dickerson MR, El-Kattan A, Thorpe AJ, Donevan SD, Taylor CP, Wustrow DJ. Schwarz JB, et al. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3559-63. doi: 10.1016/j.bmcl.2006.03.083. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621528
Oxadiazolone bioisosteres of pregabalin and gabapentin.
Wustrow DJ, Belliotti TR, Capiris T, Kneen CO, Bryans JS, Field MJ, Williams D, El-Kattan A, Buchholz L, Kinsora JJ, Lotarski SM, Vartanian MG, Taylor CP, Donevan SD, Thorpe AJ, Schwarz JB. Wustrow DJ, et al. Bioorg Med Chem Lett. 2009 Jan 1;19(1):247-50. doi: 10.1016/j.bmcl.2008.10.101. Epub 2008 Oct 25. Bioorg Med Chem Lett. 2009. PMID: 19010672
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. 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
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.
Duplantier AJ, Becker SL, Bohanon MJ, Borzilleri KA, Chrunyk BA, Downs JT, Hu LY, El-Kattan A, James LC, Liu S, Lu J, Maklad N, Mansour MN, Mente S, Piotrowski MA, Sakya SM, Sheehan S, Steyn SJ, Strick CA, Williams VA, Zhang L. Duplantier AJ, et al. J Med Chem. 2009 Jun 11;52(11):3576-85. doi: 10.1021/jm900128w. J Med Chem. 2009. PMID: 19438227
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. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
How modeling and simulation have enhanced decision making in new drug development.
Miller R, Ewy W, Corrigan BW, Ouellet D, Hermann D, Kowalski KG, Lockwood P, Koup JR, Donevan S, El-Kattan A, Li CS, Werth JL, Feltner DE, Lalonde RL. Miller R, et al. J Pharmacokinet Pharmacodyn. 2005 Apr;32(2):185-97. doi: 10.1007/s10928-005-0074-7. Epub 2005 Nov 7. J Pharmacokinet Pharmacodyn. 2005. PMID: 16283534 Review.
70 results