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Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Wan H, Schroeder GM, Hart AC, Inghrim J, Grebinski J, Tokarski JS, Lorenzi MV, You D, Mcdevitt T, Penhallow B, Vuppugalla R, Zhang Y, Gu X, Iyer R, Lombardo LJ, Trainor GL, Ruepp S, Lippy J, Blat Y, Sack JS, Khan JA, Stefanski K, Sleczka B, Mathur A, Sun JH, Wong MK, Wu DR, Li P, Gupta A, Arunachalam PN, Pragalathan B, Narayanan S, K C N, Kuppusamy P, Purandare AV. Wan H, et al. Among authors: li p. ACS Med Chem Lett. 2015 Jul 12;6(8):850-5. doi: 10.1021/acsmedchemlett.5b00226. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288683 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: li p. 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 Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design.
Xiao HY, Watterson SH, Langevine CM, Srivastava AS, Ko SS, Zhang Y, Cherney RJ, Guo WW, Gilmore JL, Sheppeck JE 2nd, Wu DR, Li P, Ramasamy D, Arunachalam P, Mathur A, Taylor TL, Shuster DJ, McIntyre KW, Shen DR, Yarde M, Cvijic ME, Marino AM, Balimane PV, Yang Z, Banas DM, Cornelius G, D'Arienzo CJ, Warrack BM, Lehman-McKeeman L, Salter-Cid LM, Xie J, Barrish JC, Carter PH, Dyckman AJ, Dhar TG. Xiao HY, et al. Among authors: li p. J Med Chem. 2016 Nov 10;59(21):9837-9854. doi: 10.1021/acs.jmedchem.6b01099. Epub 2016 Oct 20. J Med Chem. 2016. PMID: 27726358
Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.
Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ. Yang MG, et al. Among authors: li yw, li p. J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7. J Med Chem. 2016. PMID: 28002964
Development of the Large-Scale Synthesis of Tetrahydropyran Glycine, a Precursor to the HCV NS5A Inhibitor BMS-986097.
Mathur A, Wang B, Smith D, Li J, Pawluczyk J, Sun JH, Wong MK, Krishnananthan S, Wu DR, Sun D, Li P, Yip S, Chen BC, Baran PS, Chen Q, Lopez OD, Yong Z, Bender JA, Nguyen VN, Romine JL, Laurent DRS, Wang G, Kadow JF, Meanwell NA, Belema M, Zhao R. Mathur A, et al. Among authors: li j, li p. J Org Chem. 2017 Oct 6;82(19):10376-10387. doi: 10.1021/acs.joc.7b01852. Epub 2017 Sep 14. J Org Chem. 2017. PMID: 28877441
Identification of Imidazo[1,2-b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors.
Liu C, Lin J, Moslin R, Tokarski JS, Muckelbauer J, Chang C, Tredup J, Xie D, Park H, Li P, Wu DR, Strnad J, Zupa-Fernandez A, Cheng L, Chaudhry C, Chen J, Chen C, Sun H, Elzinga P, D'arienzo C, Gillooly K, Taylor TL, McIntyre KW, Salter-Cid L, Lombardo LJ, Carter PH, Aranibar N, Burke JR, Weinstein DS. Liu C, et al. Among authors: li p. ACS Med Chem Lett. 2019 Feb 21;10(3):383-388. doi: 10.1021/acsmedchemlett.9b00035. eCollection 2019 Mar 14. ACS Med Chem Lett. 2019. PMID: 30891145 Free PMC article.
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: li s, li p. 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
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