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Page 1
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: altman md. 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: altman md. 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-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: altman md. J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26. J Med Chem. 2011. PMID: 21942426
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: altman md. 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: altman md. 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
Overcoming mutagenicity and ion channel activity: optimization of selective spleen tyrosine kinase inhibitors.
Ellis JM, Altman MD, Bass A, Butcher JW, Byford AJ, Donofrio A, Galloway S, Haidle AM, Jewell J, Kelly N, Leccese EK, Lee S, Maddess M, Miller JR, Moy LY, Osimboni E, Otte RD, Reddy MV, Spencer K, Sun B, Vincent SH, Ward GJ, Woo GH, Yang C, Houshyar H, Northrup AB. Ellis JM, et al. Among authors: altman md. J Med Chem. 2015 Feb 26;58(4):1929-39. doi: 10.1021/jm5018169. Epub 2015 Feb 16. J Med Chem. 2015. PMID: 25625541
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. Among authors: altman md. 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.
Identification of N-(1H-pyrazol-4-yl)carboxamide inhibitors of interleukin-1 receptor associated kinase 4: Bicyclic core modifications.
Lim J, Altman MD, Baker J, Brubaker JD, Chen H, Chen Y, Kleinschek MA, Li C, Liu D, Maclean JK, Mulrooney EF, Presland J, Rakhilina L, Smith GF, Yang R. Lim J, et al. Among authors: altman md. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5384-8. doi: 10.1016/j.bmcl.2015.09.028. Epub 2015 Sep 11. Bioorg Med Chem Lett. 2015. PMID: 26403930
Optimization of microtubule affinity regulating kinase (MARK) inhibitors with improved physical properties.
Sloman DL, Noucti N, Altman MD, Chen D, Mislak AC, Szewczak A, Hayashi M, Warren L, Dellovade T, Wu Z, Marcus J, Walker D, Su HP, Edavettal SC, Munshi S, Hutton M, Nuthall H, Stanton MG. Sloman DL, et al. Among authors: altman md. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4362-6. doi: 10.1016/j.bmcl.2016.02.003. Epub 2016 Feb 6. Bioorg Med Chem Lett. 2016. PMID: 27491711
53 results