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Page 1
Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR. Lim J, et al. Among authors: dinsmore cj. J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26. J Med Chem. 2011. PMID: 21942426
The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead.
Siu T, Kozina ES, Jung J, Rosenstein C, Mathur A, Altman MD, Chan G, Xu L, Bachman E, Mo JR, Bouthillette M, Rush T, Dinsmore CJ, Marshall CG, Young JR. Siu T, et al. Among authors: dinsmore cj. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7421-5. doi: 10.1016/j.bmcl.2010.10.031. Epub 2010 Oct 12. Bioorg Med Chem Lett. 2010. PMID: 21044843
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q. Katz JD, et al. Among authors: dinsmore cj. J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24. J Med Chem. 2011. PMID: 21608528
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ. Northrup AB, et al. Among authors: dinsmore cj. J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18. J Med Chem. 2013. PMID: 23379595
The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: lead optimization.
Siu T, Kumarasinghe SE, Altman MD, Katcher M, Northrup A, White C, Rosenstein C, Mathur A, Xu L, Chan G, Bachman E, Bouthillette M, Dinsmore CJ, Marshall CG, Young JR. Siu T, et al. Among authors: dinsmore cj. Bioorg Med Chem Lett. 2014 Mar 15;24(6):1466-71. doi: 10.1016/j.bmcl.2014.02.011. Epub 2014 Feb 15. Bioorg Med Chem Lett. 2014. PMID: 24582987
The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.
Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, Mampreian DM, Shi F, Liu D, Fradera X, Johnson K, Bays N, Kadic E, He F, Goldenblatt P, Shaffer L, Patel SB, Lesburg CA, Alpert C, Dorosh L, Deshmukh SV, Yu H, Klappenbach J, Elwood F, Dinsmore CJ, Fernandez R, Moy L, Young JR. Siu T, et al. Among authors: dinsmore cj. J Med Chem. 2017 Dec 14;60(23):9676-9690. doi: 10.1021/acs.jmedchem.7b01135. Epub 2017 Dec 4. J Med Chem. 2017. PMID: 29156136
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ. Pan BS, et al. Among authors: dinsmore cj. Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9. Cancer Res. 2010. PMID: 20145145
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Beshore DC, Liverton NJ, McIntyre CJ, Claiborne CF, Libby B, Culberson JC, Salata JJ, Regan CP, Lynch JJ, Kiss L, Spencer RH, Kane SA, White RB, Yeh S, Hartman GD, Dinsmore CJ. Beshore DC, et al. Among authors: dinsmore cj. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6. doi: 10.1016/j.bmcl.2010.03.005. Epub 2010 Mar 4. Bioorg Med Chem Lett. 2010. PMID: 20304642
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S. Lin J, et al. J Med Chem. 2019 Jul 25;62(14):6575-6596. doi: 10.1021/acs.jmedchem.9b00362. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31199148
52 results