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Page 1
Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.
Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin-Bertrand M, Weigelt CA, Khandelwal P, Vishwakrishnan S, Selvakumar K, Karmakar A, Gupta AK, Basha M, Ramlingam S, Manjunath N, Vanteru S, Karmakar S, Maddala N, Vetrichelvan M, Gupta A, Rampulla RA, Mathur A, Yip S, Li P, Wu DR, Khan J, Ruzanov M, Sack JS, Wang J, Yarde M, Cvijic ME, Li S, Shuster DJ, Borowski V, Xie JH, McIntyre KW, Obermeier MT, Fura A, Stefanski K, Cornelius G, Hynes J Jr, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM. Marcoux D, et al. Among authors: beaudoin bertrand m. J Med Chem. 2019 Nov 14;62(21):9931-9946. doi: 10.1021/acs.jmedchem.9b01369. Epub 2019 Oct 31. J Med Chem. 2019. PMID: 31638797
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: beaudoin bertrand m. 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
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: beaudoin bertrand m. 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
Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.
Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA. Liu Q, et al. Among authors: beaudoin bertrand m. J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5. J Med Chem. 2017. PMID: 28541707
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: beaudoin bertrand m. 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
Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG, Beaudoin-Bertrand M, Xiao Z, Marcoux D, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Karmakar A, Basha M, Babu V, Gupta AK, Mathur A, Salter-Cid L, Denton R, Zhao Q, Dhar TGM. Yang MG, et al. Among authors: beaudoin bertrand m. J Med Chem. 2021 Mar 11;64(5):2714-2724. doi: 10.1021/acs.jmedchem.0c01992. Epub 2021 Feb 16. J Med Chem. 2021. PMID: 33591748