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Page 1
Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists.
Humphries PS, Benbow JW, Bonin PD, Boyer D, Doran SD, Frisbie RK, Piotrowski DW, Balan G, Bechle BM, Conn EL, Dirico KJ, Oliver RM, Soeller WC, Southers JA, Yang X. Humphries PS, et al. Among authors: benbow jw. Bioorg Med Chem Lett. 2009 May 1;19(9):2400-3. doi: 10.1016/j.bmcl.2009.03.082. Epub 2009 Mar 25. Bioorg Med Chem Lett. 2009. PMID: 19346127
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.
Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS. Didiuk MT, et al. Among authors: benbow jw. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19625189
1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes.
Andrews KM, Beebe DA, Benbow JW, Boyer DA, Doran SD, Hui Y, Liu S, McPherson RK, Neagu C, Parker JC, Piotrowski DW, Schneider SR, Treadway JL, VanVolkenberg MA, Zembrowski WJ. Andrews KM, et al. Among authors: benbow jw. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1810-4. doi: 10.1016/j.bmcl.2011.01.055. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21324688
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, Zawistoski M, Li J, Oliver R, Guzman-Perez A, Liu KK, Walker DP, Benbow JW, Morris J. Kalgutkar AS, et al. Among authors: benbow jw. Chem Res Toxicol. 2010 Jun 21;23(6):1115-26. doi: 10.1021/tx100137n. Chem Res Toxicol. 2010. PMID: 20507089
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. 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
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