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Page 1
Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes.
DeNinno MP, Wright SW, Etienne JB, Olson TV, Rocke BN, Corbett JW, Kung DW, DiRico KJ, Andrews KM, Millham ML, Parker JC, Esler W, van Volkenburg M, Boyer DD, Houseknecht KL, Doran SD. DeNinno MP, et al. Among authors: rocke bn. Bioorg Med Chem Lett. 2012 Sep 1;22(17):5721-6. doi: 10.1016/j.bmcl.2012.06.079. Epub 2012 Jul 6. Bioorg Med Chem Lett. 2012. PMID: 22858141
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization.
Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, Liu S, McClure LD, McPherson RK, Olson TV, Orena SJ, Parker JC, Rocke BN, Soeller WC, Soglia CB, Treadway JL, Vanvolkenburg MA, Zhao Z, Cox ED. Wright SW, et al. Among authors: rocke bn. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5638-42. doi: 10.1016/j.bmcl.2007.07.081. Epub 2007 Aug 22. Bioorg Med Chem Lett. 2007. PMID: 17822893
1,5-Substituted nipecotic amides: selective PDE8 inhibitors displaying diastereomer-dependent microsomal stability.
DeNinno MP, Wright SW, Visser MS, Etienne JB, Moore DE, Olson TV, Rocke BN, Andrews MP, Zarbo C, Millham ML, Boscoe BP, Boyer DD, Doran SD, Houseknecht KL. DeNinno MP, et al. Among authors: rocke bn. Bioorg Med Chem Lett. 2011 May 15;21(10):3095-8. doi: 10.1016/j.bmcl.2011.03.022. Epub 2011 Mar 11. Bioorg Med Chem Lett. 2011. PMID: 21459572
Discovery of 2-(6-(5-Chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999): A Highly Selective Mechanism-Based Myeloperoxidase Inhibitor for the Treatment of Cardiovascular Diseases.
Ruggeri RB, Buckbinder L, Bagley SW, Carpino PA, Conn EL, Dowling MS, Fernando DP, Jiao W, Kung DW, Orr ST, Qi Y, Rocke BN, Smith A, Warmus JS, Zhang Y, Bowles D, Widlicka DW, Eng H, Ryder T, Sharma R, Wolford A, Okerberg C, Walters K, Maurer TS, Zhang Y, Bonin PD, Spath SN, Xing G, Hepworth D, Ahn K, Kalgutkar AS. Ruggeri RB, et al. Among authors: rocke bn. J Med Chem. 2015 Nov 12;58(21):8513-28. doi: 10.1021/acs.jmedchem.5b00963. Epub 2015 Oct 28. J Med Chem. 2015. PMID: 26509551
One-Step Synthesis of Sulfonamides from N-Tosylhydrazones.
Tsai AS, Curto JM, Rocke BN, Dechert-Schmitt AM, Ingle GK, Mascitti V. Tsai AS, et al. Among authors: rocke bn. Org Lett. 2016 Feb 5;18(3):508-11. doi: 10.1021/acs.orglett.5b03545. Epub 2016 Jan 15. Org Lett. 2016. PMID: 26771228
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