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Page 1
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: saiah e. 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
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: saiah e. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
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: saiah e. 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
Diazine indole acetic acids as potent, selective, and orally bioavailable antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Huang A, Moretto A, Follows B, Janz K, Lowe M, Thomason J, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. Among authors: saiah e. J Med Chem. 2012 Jun 14;55(11):5088-109. doi: 10.1021/jm300007n. Epub 2012 May 31. J Med Chem. 2012. PMID: 22651823
Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.
Kaila N, Follows B, Leung L, Thomason J, Huang A, Moretto A, Janz K, Lowe M, Mansour TS, Hubeau C, Page K, Morgan P, Fish S, Xu X, Williams C, Saiah E. Kaila N, et al. Among authors: saiah e. J Med Chem. 2014 Feb 27;57(4):1299-322. doi: 10.1021/jm401509e. Epub 2014 Feb 10. J Med Chem. 2014. PMID: 24512187
Discovery of potent and selective matrix metalloprotease 12 inhibitors for the potential treatment of chronic obstructive pulmonary disease (COPD).
Wu Y, Li J, Wu J, Morgan P, Xu X, Rancati F, Vallese S, Raveglia L, Hotchandani R, Fuller N, Bard J, Cunningham K, Fish S, Krykbaev R, Tam S, Goldman SJ, Williams C, Mansour TS, Saiah E, Sypek J, Li W. Wu Y, et al. Among authors: saiah e. Bioorg Med Chem Lett. 2012 Jan 1;22(1):138-43. doi: 10.1016/j.bmcl.2011.11.046. Epub 2011 Nov 20. Bioorg Med Chem Lett. 2012. PMID: 22153340
Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes.
Wan ZK, Chenail E, Li HQ, Ipek M, Xiang J, Suri V, Hahm S, Bard J, Svenson K, Xu X, Tian X, Wang M, Li X, Johnson CE, Qadri A, Panza D, Perreault M, Mansour TS, Tobin JF, Saiah E. Wan ZK, et al. Among authors: saiah e. ACS Med Chem Lett. 2012 Nov 23;4(1):118-23. doi: 10.1021/ml300352x. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900572 Free PMC article.
Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model.
Xiang J, Wan ZK, Li HQ, Ipek M, Binnun E, Nunez J, Chen L, McKew JC, Mansour TS, Xu X, Suri V, Tam M, Xing Y, Li X, Hahm S, Tobin J, Saiah E. Xiang J, et al. Among authors: saiah e. J Med Chem. 2008 Jul 24;51(14):4068-71. doi: 10.1021/jm8004948. Epub 2008 Jun 26. J Med Chem. 2008. PMID: 18578516
Small molecules that target protein misfolding.
Gavrin LK, Denny RA, Saiah E. Gavrin LK, et al. Among authors: saiah e. J Med Chem. 2012 Dec 27;55(24):10823-43. doi: 10.1021/jm301182j. Epub 2012 Nov 1. J Med Chem. 2012. PMID: 23075044
32 results