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Page 1
Discovery and Preclinical Evaluation of BMS-986242, a Potent, Selective Inhibitor of Indoleamine-2,3-dioxygenase 1.
Cherney EC, Zhang L, Nara S, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, Darienzo C, Discenza L, Ranasinghe A, Grubb M, Ziemba T, Traeger SC, Li X, Johnston K, Kopcho L, Fereshteh M, Foster K, Stefanski K, Fargnoli J, Swanson J, Brown J, Delpy D, Seitz SP, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: discenza l. ACS Med Chem Lett. 2021 Jan 28;12(2):288-294. doi: 10.1021/acsmedchemlett.0c00668. eCollection 2021 Feb 11. ACS Med Chem Lett. 2021. PMID: 33603977 Free PMC article.
Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors.
Cherney EC, Zhang L, Guo W, Huang A, Williams D, Seitz S, Shan W, Zhu X, Gullo-Brown J, Maley D, Lin TA, Hunt JT, Huang C, Yang Z, D'Arienzo CJ, Discenza LN, Ranasinghe A, Grubb MF, Traeger SC, Li X, Johnston KA, Kopcho L, Fereshteh M, Foster KA, Stefanski K, Delpy D, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan TT, Pattasseri S, Nimje RY, Hong Z, Kempson J, Rampulla R, Mathur A, Gupta A, Borzilleri R, Vite G, Balog A. Cherney EC, et al. Among authors: discenza ln. ACS Med Chem Lett. 2021 Jun 16;12(7):1143-1150. doi: 10.1021/acsmedchemlett.1c00236. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267885 Free PMC article.
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: discenza ln. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770
Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Watterson SH, Liu Q, Beaudoin Bertrand M, Batt DG, Li L, Pattoli MA, Skala S, Cheng L, Obermeier MT, Moore R, Yang Z, Vickery R, Elzinga PA, Discenza L, D'Arienzo C, Gillooly KM, Taylor TL, Pulicicchio C, Zhang Y, Heimrich E, McIntyre KW, Ruan Q, Westhouse RA, Catlett IM, Zheng N, Chaudhry C, Dai J, Galella MA, Tebben AJ, Pokross M, Li J, Zhao R, Smith D, Rampulla R, Allentoff A, Wallace MA, Mathur A, Salter-Cid L, Macor JE, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. Among authors: discenza l. J Med Chem. 2019 Apr 11;62(7):3228-3250. doi: 10.1021/acs.jmedchem.9b00167. Epub 2019 Mar 29. J Med Chem. 2019. PMID: 30893553
Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development.
Wittman MD, Carboni JM, Yang Z, Lee FY, Antman M, Attar R, Balimane P, Chang C, Chen C, Discenza L, Frennesson D, Gottardis MM, Greer A, Hurlburt W, Johnson W, Langley DR, Li A, Li J, Liu P, Mastalerz H, Mathur A, Menard K, Patel K, Sack J, Sang X, Saulnier M, Smith D, Stefanski K, Trainor G, Velaparthi U, Zhang G, Zimmermann K, Vyas DM. Wittman MD, et al. Among authors: discenza l. J Med Chem. 2009 Dec 10;52(23):7360-3. doi: 10.1021/jm900786r. J Med Chem. 2009. PMID: 19778024
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA. De Lucca GV, et al. Among authors: discenza l. J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27531604
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
Srivastava AS, Ko S, Watterson SH, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Yip S, Li P, Sun D, Wu DR, Dai J, Wang C, Zhang Y, Wang B, Pawluczyk J, Kempson J, Zhao R, Hou X, Rampulla R, Mathur A, Galella MA, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Srivastava AS, et al. Among authors: discenza ln. ACS Med Chem Lett. 2020 Sep 16;11(11):2195-2203. doi: 10.1021/acsmedchemlett.0c00335. eCollection 2020 Nov 12. ACS Med Chem Lett. 2020. PMID: 33214829 Free PMC article.
21 results