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Page 1
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: xing l. 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
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: xing l. 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
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning.
Schnute ME, Benoit SE, Buchler IP, Caspers N, Grapperhaus ML, Han S, Hotchandani R, Huang N, Hughes RO, Juba BM, Kim KH, Liu E, McCarthy E, Messing D, Miyashiro JS, Mohan S, O'Connell TN, Ohren JF, Parikh MD, Schmidt M, Selness SR, Springer JR, Thanabal V, Trujillo JI, Walker DP, Wan ZK, Withka JM, Wittwer AJ, Wood NL, Xing L, Zapf CW, Douhan J 3rd. Schnute ME, et al. Among authors: xing l. ACS Med Chem Lett. 2018 Dec 3;10(1):80-85. doi: 10.1021/acsmedchemlett.8b00461. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655951 Free PMC article.
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: xing l. 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
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Gerstenberger BS, Ambler C, Arnold EP, Banker ME, Brown MF, Clark JD, Dermenci A, Dowty ME, Fensome A, Fish S, Hayward MM, Hegen M, Hollingshead BD, Knafels JD, Lin DW, Lin TH, Owen DR, Saiah E, Sharma R, Vajdos FF, Xing L, Yang X, Yang X, Wright SW. Gerstenberger BS, et al. Among authors: xing l. J Med Chem. 2020 Nov 25;63(22):13561-13577. doi: 10.1021/acs.jmedchem.0c00948. Epub 2020 Aug 25. J Med Chem. 2020. PMID: 32787094
2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.
Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA, Weinberg RA, Stegeman RA, Wrightstone A, Christine L, Compton R, Li X. Trujillo JI, et al. Among authors: xing l. Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. doi: 10.1016/j.bmcl.2008.11.105. Epub 2008 Dec 6. Bioorg Med Chem Lett. 2009. PMID: 19097791
Design, synthesis and activity of a potent, selective series of N-aryl pyridinone inhibitors of p38 kinase.
Selness SR, Boehm TL, Walker JK, Devadas B, Durley RC, Kurumbail R, Shieh H, Xing L, Hepperle M, Rucker PV, Jerome KD, Benson AG, Marrufo LD, Madsen HM, Hitchcock J, Owen TJ, Christie L, Promo MA, Hickory BS, Alvira E, Naing W, Blevis-Bal R, Devraj RV, Messing D, Schindler JF, Hirsch J, Saabye M, Bonar S, Webb E, Anderson G, Monahan JB. Selness SR, et al. Among authors: xing l. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4059-65. doi: 10.1016/j.bmcl.2011.04.120. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21640588
3,939 results