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Page 1
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: traeger sc. 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
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Shan W, Balog A, Nation A, Zhu X, Chen J, Cvijic ME, Geng J, Rizzo CA, Spires T Jr, Attar RM, Obermeier M, Traeger S, Dai J, Zhang Y, Galella M, Trainor G, Vite GD, Gavai AV. Shan W, et al. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5707-5711. doi: 10.1016/j.bmcl.2016.10.059. Epub 2016 Oct 21. Bioorg Med Chem Lett. 2016. PMID: 27836399
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: traeger sc. 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: traeger sc. 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 and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: traeger sc. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Discovery of Imidazopyridines as Potent Inhibitors of Indoleamine 2,3-Dioxygenase 1 for Cancer Immunotherapy.
Zhang L, Cherney EC, Zhu X, Lin TA, Gullo-Brown J, Maley D, Johnston-Allegretto K, Kopcho L, Fereshteh M, Huang C, Li X, Traeger SC, Dhar G, Anandam A, Mahankali S, Padmanabhan S, Rajanna P, Murali V, Mariappan T, Borzilleri R, Vite G, Hunt JT, Balog A. Zhang L, et al. Among authors: traeger sc. ACS Med Chem Lett. 2021 Mar 2;12(3):494-501. doi: 10.1021/acsmedchemlett.1c00014. eCollection 2021 Mar 11. ACS Med Chem Lett. 2021. PMID: 33738077 Free PMC article.
Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases.
Cheng PTW, Kaltenbach RF 3rd, Zhang H, Shi J, Tao S, Li J, Kennedy LJ, Walker SJ, Shi Y, Wang Y, Dhanusu S, Reddigunta R, Kumaravel S, Jusuf S, Smith D, Krishnananthan S, Li J, Wang T, Heiry R, Sum CS, Kalinowski SS, Hung CP, Chu CH, Azzara AV, Ziegler M, Burns L, Zinker BA, Boehm S, Taylor J, Sapuppo J, Mosure K, Everlof G, Guarino V, Zhang L, Yang Y, Ruan Q, Xu C, Apedo A, Traeger SC, Cvijic ME, Lentz KA, Tirucherai G, Sivaraman L, Robl J, Ellsworth BA, Rosen G, Gordon DA, Soars MG, Gill M, Murphy BJ. Cheng PTW, et al. Among authors: traeger sc. J Med Chem. 2021 Nov 11;64(21):15549-15581. doi: 10.1021/acs.jmedchem.1c01256. Epub 2021 Oct 28. J Med Chem. 2021. PMID: 34709814
alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.
Magnin DR, Biller SA, Chen Y, Dickson JK Jr, Fryszman OM, Lawrence RM, Logan JV, Sieber-McMaster ES, Sulsky RB, Traeger SC, Hsieh DC, Lan SJ, Rinehart JK, Harrity TW, Jolibois KG, Kunselman LK, Rich LC, Slusarchyk DA, Ciosek CP Jr. Magnin DR, et al. Among authors: traeger sc. J Med Chem. 1996 Feb 2;39(3):657-60. doi: 10.1021/jm9507340. J Med Chem. 1996. PMID: 8576905 No abstract available.
29 results