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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: flick 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
Synthetic Approaches to New Drugs Approved During 2016.
Flick AC, Ding HX, Leverett CA, Fink SJ, O'Donnell CJ. Flick AC, et al. J Med Chem. 2018 Aug 23;61(16):7004-7031. doi: 10.1021/acs.jmedchem.8b00260. Epub 2018 Apr 19. J Med Chem. 2018. PMID: 29620889 Review.
Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G. Schnute ME, et al. Among authors: flick ac. J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9. J Med Chem. 2018. PMID: 30130103
Synthetic Approaches to the New Drugs Approved During 2017.
Flick AC, Leverett CA, Ding HX, McInturff E, Fink SJ, Helal CJ, O'Donnell CJ. Flick AC, et al. J Med Chem. 2019 Aug 22;62(16):7340-7382. doi: 10.1021/acs.jmedchem.9b00196. Epub 2019 Apr 15. J Med Chem. 2019. PMID: 30939001 Review.
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: flick 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
Synthetic Approaches to New Drugs Approved during 2018.
Flick AC, Leverett CA, Ding HX, McInturff E, Fink SJ, Helal CJ, DeForest JC, Morse PD, Mahapatra S, O'Donnell CJ. Flick AC, et al. J Med Chem. 2020 Oct 8;63(19):10652-10704. doi: 10.1021/acs.jmedchem.0c00345. Epub 2020 May 22. J Med Chem. 2020. PMID: 32338902
Synthetic Approaches to the New Drugs Approved during 2019.
Flick AC, Leverett CA, Ding HX, McInturff E, Fink SJ, Mahapatra S, Carney DW, Lindsey EA, DeForest JC, France SP, Berritt S, Bigi-Botterill SV, Gibson TS, Liu Y, O'Donnell CJ. Flick AC, et al. J Med Chem. 2021 Apr 8;64(7):3604-3657. doi: 10.1021/acs.jmedchem.1c00208. Epub 2021 Mar 30. J Med Chem. 2021. PMID: 33783211 Review.
Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.
Casimiro-Garcia A, Allais C, Brennan A, Choi C, Dower G, Farley KA, Fleming M, Flick A, Frisbie RK, Hall J, Hepworth D, Jones H, Knafels JD, Kortum S, Lovering FE, Mathias JP, Mohan S, Morgan PM, Parng C, Parris K, Pullen N, Schlerman F, Stansfield J, Strohbach JW, Vajdos FF, Vincent F, Wang H, Wang X, Webster R, Wright SW. Casimiro-Garcia A, et al. Among authors: flick a. J Med Chem. 2022 Jan 13;65(1):757-784. doi: 10.1021/acs.jmedchem.1c01849. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967602
Synthetic Approaches to the New Drugs Approved During 2020.
Flick AC, Leverett CA, Ding HX, McInturff EL, Fink SJ, Mahapatra S, Carney DW, Lindsey EA, DeForest JC, France SP, Berritt S, Bigi-Botterill SV, Gibson TS, Watson RB, Liu Y, O'Donnell CJ. Flick AC, et al. J Med Chem. 2022 Jul 28;65(14):9607-9661. doi: 10.1021/acs.jmedchem.2c00710. Epub 2022 Jul 14. J Med Chem. 2022. PMID: 35833579 Review.
77 results