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Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Liu J, et al. Among authors: fischmann to. ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985298 Free PMC article.
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
Dwyer MP, Keertikar K, Paruch K, Alvarez C, Labroli M, Poker C, Fischmann TO, Mayer-Ezell R, Bond R, Wang Y, Azevedo R, Guzi TJ. Dwyer MP, et al. Among authors: fischmann to. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6178-82. doi: 10.1016/j.bmcl.2013.08.110. Epub 2013 Sep 7. Bioorg Med Chem Lett. 2013. PMID: 24091081
Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.
Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ. Paruch K, et al. ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12. ACS Med Chem Lett. 2010. PMID: 24900195 Free PMC article.
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
McElroy WT, Tan Z, Ho G, Paliwal S, Li G, Seganish WM, Tulshian D, Tata J, Fischmann TO, Sondey C, Bian H, Bober L, Jackson J, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. McElroy WT, et al. Among authors: fischmann to. ACS Med Chem Lett. 2015 May 12;6(6):677-82. doi: 10.1021/acsmedchemlett.5b00106. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101573 Free PMC article.
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.
Lim J, Altman MD, Baker J, Brubaker JD, Chen H, Chen Y, Fischmann T, Gibeau C, Kleinschek MA, Leccese E, Lesburg C, Maclean JK, Moy LY, Mulrooney EF, Presland J, Rakhilina L, Smith GF, Steinhuebel D, Yang R. Lim J, et al. ACS Med Chem Lett. 2015 Apr 20;6(6):683-8. doi: 10.1021/acsmedchemlett.5b00107. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101574 Free PMC article.
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X. Seganish WM, et al. Among authors: fischmann to. ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288698 Free PMC article.
Discovery of novel BTK inhibitors with carboxylic acids.
Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA. Gao X, et al. Among authors: fischmann to. Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25. Bioorg Med Chem Lett. 2017. PMID: 28254166
51 results