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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).
Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L. Fensome A, et al. Among authors: gopalsamy a. J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16. J Med Chem. 2018. PMID: 30113844
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G, Cuozzo JW, Hall JP, Hsu S, Telliez JB, Lin LL. Gavrin LK, et al. Among authors: gopalsamy a. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. doi: 10.1016/j.bmcl.2005.08.029. Epub 2005 Sep 13. Bioorg Med Chem Lett. 2005. PMID: 16165349
Discovery of indazoles as inhibitors of Tpl2 kinase.
Hu Y, Cole D, Denny RA, Anderson DR, Ipek M, Ni Y, Wang X, Thaisrivongs S, Chamberlain T, Hall JP, Liu J, Luong M, Lin LL, Telliez JB, Gopalsamy A. Hu Y, et al. Among authors: gopalsamy a. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4758-61. doi: 10.1016/j.bmcl.2011.06.065. Epub 2011 Jun 22. Bioorg Med Chem Lett. 2011. PMID: 21742493
Identification of pyrimidine derivatives as hSMG-1 inhibitors.
Gopalsamy A, Bennett EM, Shi M, Zhang WG, Bard J, Yu K. Gopalsamy A, et al. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6636-41. doi: 10.1016/j.bmcl.2012.08.107. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23021994
Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.
Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A. Liu S, et al. Among authors: gopalsamy a. Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859. Sci Rep. 2016. PMID: 27527709 Free PMC article.
Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
Gopalsamy A, Narayanan A, Liu S, Parikh MD, Kyne RE Jr, Fadeyi O, Tones MA, Cherry JJ, Nabhan JF, LaRosa G, Petersen DN, Menard C, Foley TL, Noell S, Ren Y, Loria PM, Maglich-Goodwin J, Rong H, Jones LH. Gopalsamy A, et al. J Med Chem. 2017 Apr 13;60(7):3094-3108. doi: 10.1021/acs.jmedchem.7b00124. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28257199
Design and optimization of a series of 4-(3-azabicyclo[3.1.0]hexan-3-yl)pyrimidin-2-amines: Dual inhibitors of TYK2 and JAK1.
Fensome A, Ambler CM, Arnold E, Banker ME, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gifford RS, Gopalsamy A, Hegen M, Jussif J, Limburg DC, Lin TH, Pierce BS, Sharma R, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X. Fensome A, et al. Among authors: gopalsamy a. Bioorg Med Chem. 2020 May 15;28(10):115481. doi: 10.1016/j.bmc.2020.115481. Epub 2020 Mar 31. Bioorg Med Chem. 2020. PMID: 32253095
53 results