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Page 1
Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.
Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP Jr, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. Focken T, et al. Among authors: chang e, chang jh. J Med Chem. 2018 Jun 14;61(11):4810-4831. doi: 10.1021/acs.jmedchem.7b01826. Epub 2018 May 23. J Med Chem. 2018. PMID: 29737846
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.
Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A. Hu H, et al. Among authors: chang jh. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30. Bioorg Med Chem Lett. 2015. PMID: 26459208
Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.
Focken T, Liu S, Chahal N, Dauphinais M, Grimwood ME, Chowdhury S, Hemeon I, Bichler P, Bogucki D, Waldbrook M, Bankar G, Sojo LE, Young C, Lin S, Shuart N, Kwan R, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP Jr, Dehnhardt CM, Mansour TS, Oballa RM, Cohen CJ, Robinette CL. Focken T, et al. Among authors: chang jh. ACS Med Chem Lett. 2016 Jan 19;7(3):277-82. doi: 10.1021/acsmedchemlett.5b00447. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985315 Free PMC article.
Discovery of 5-Azaindazole (GNE-955) as a Potent Pan-Pim Inhibitor with Optimized Bioavailability.
Wang X, Kolesnikov A, Tay S, Chan G, Chao Q, Do S, Drummond J, Ebens AJ, Liu N, Ly J, Harstad E, Hu H, Moffat J, Munugalavadla V, Murray J, Slaga D, Tsui V, Volgraf M, Wallweber H, Chang JH. Wang X, et al. Among authors: chang jh. J Med Chem. 2017 May 25;60(10):4458-4473. doi: 10.1021/acs.jmedchem.7b00418. Epub 2017 May 5. J Med Chem. 2017. PMID: 28445037
Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain.
Bankar G, Goodchild SJ, Howard S, Nelkenbrecher K, Waldbrook M, Dourado M, Shuart NG, Lin S, Young C, Xie Z, Khakh K, Chang E, Sojo LE, Lindgren A, Chowdhury S, Decker S, Grimwood M, Andrez JC, Dehnhardt CM, Pang J, Chang JH, Safina BS, Sutherlin DP, Johnson JP Jr, Hackos DH, Robinette CL, Cohen CJ. Bankar G, et al. Among authors: chang e, chang jh. Cell Rep. 2018 Sep 18;24(12):3133-3145. doi: 10.1016/j.celrep.2018.08.063. Cell Rep. 2018. PMID: 30231997 Free article.
Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity.
Sun S, Jia Q, Zenova AY, Wilson MS, Chowdhury S, Focken T, Li J, Decker S, Grimwood ME, Andrez JC, Hemeon I, Sheng T, Chen CA, White A, Hackos DH, Deng L, Bankar G, Khakh K, Chang E, Kwan R, Lin S, Nelkenbrecher K, Sellers BD, DiPasquale AG, Chang J, Pang J, Sojo L, Lindgren A, Waldbrook M, Xie Z, Young C, Johnson JP, Robinette CL, Cohen CJ, Safina BS, Sutherlin DP, Ortwine DF, Dehnhardt CM. Sun S, et al. J Med Chem. 2019 Jan 24;62(2):908-927. doi: 10.1021/acs.jmedchem.8b01621. Epub 2018 Dec 21. J Med Chem. 2019. PMID: 30499663
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ. Wang X, et al. Among authors: chang jh. J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20. J Med Chem. 2019. PMID: 30715878
Unexpected equivalent potency of a constrained chromene enantiomeric pair rationalized by co-crystal structures in complex with estrogen receptor alpha.
Zhang B, Kiefer JR, Blake RA, Chang JH, Hartman S, Ingalla ER, Kleinheinz T, Mody V, Nannini M, Ortwine DF, Ran Y, Sambrone A, Sampath D, Vinogradova M, Zhong Y, Nwachukwu JC, Nettles KW, Lai T, Liao J, Zheng X, Chen H, Wang X, Liang J. Zhang B, et al. Among authors: chang jh. Bioorg Med Chem Lett. 2019 Apr 1;29(7):905-911. doi: 10.1016/j.bmcl.2019.01.036. Epub 2019 Feb 1. Bioorg Med Chem Lett. 2019. PMID: 30732944
2,242 results