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Page 1
Synthesis, initial SAR and biological evaluation of 1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-4-amine derived inhibitors of IkappaB kinase.
Kempson J, Guo J, Das J, Moquin RV, Spergel SH, Watterson SH, Langevine CM, Dyckman AJ, Pattoli M, Burke JR, Yang X, Gillooly KM, McIntyre KW, Chen L, Dodd JH, McKinnon M, Barrish JC, Pitts WJ. Kempson J, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2009 May 15;19(10):2646-9. doi: 10.1016/j.bmcl.2009.03.159. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19376699
Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis.
Dyckman AJ, Langevine CM, Quesnelle C, Kempson J, Guo J, Gill P, Spergel SH, Watterson SH, Li T, Nirschl DS, Gillooly KM, Pattoli MA, McIntyre KW, Chen L, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Dyckman AJ, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21087862
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Watterson SH, Langevine CM, Van Kirk K, Kempson J, Guo J, Spergel SH, Das J, Moquin RV, Dyckman AJ, Nirschl D, Gregor K, Pattoli MA, Yang X, McIntyre KW, Yang G, Galella MA, Booth-Lute H, Chen L, Yang Z, Wang-Iverson D, McKinnon M, Dodd JH, Barrish JC, Burke JR, Pitts WJ. Watterson SH, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7006-12. doi: 10.1016/j.bmcl.2011.09.111. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22018461
Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.
Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST. Duan JJ, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24. Bioorg Med Chem Lett. 2014. PMID: 25453808
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Hart AC, Schroeder GM, Wan H, Grebinski J, Inghrim J, Kempson J, Guo J, Pitts WJ, Tokarski JS, Sack JS, Khan JA, Lippy J, Lorenzi MV, You D, McDevitt T, Vuppugalla R, Zhang Y, Lombardo LJ, Trainor GL, Purandare AV. Hart AC, et al. Among authors: pitts wj. ACS Med Chem Lett. 2015 Jul 10;6(8):845-9. doi: 10.1021/acsmedchemlett.5b00225. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288682 Free PMC article.
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1).
Guo J, Watterson SH, Spergel SH, Kempson J, Langevine CM, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ. Guo J, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2016 May 15;26(10):2470-2474. doi: 10.1016/j.bmcl.2016.03.105. Epub 2016 Apr 1. Bioorg Med Chem Lett. 2016. PMID: 27055941
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.
Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST. Hynes J Jr, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15. Bioorg Med Chem Lett. 2017. PMID: 28539220
Discovery of highly potent, selective, covalent inhibitors of JAK3.
Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ. Kempson J, et al. Among authors: pitts wj. Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11. Bioorg Med Chem Lett. 2017. PMID: 28927786
59 results