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Page 1
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Among authors: joseph sb. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: joseph sb. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.
Phillips DP, Gao W, Yang Y, Zhang G, Lerario IK, Lau TL, Jiang J, Wang X, Nguyen DG, Bhat BG, Trotter C, Sullivan H, Welzel G, Landry J, Chen Y, Joseph SB, Li C, Gordon WP, Richmond W, Johnson K, Bretz A, Bursulaya B, Pan S, McNamara P, Seidel HM. Phillips DP, et al. Among authors: joseph sb. J Med Chem. 2014 Apr 24;57(8):3263-82. doi: 10.1021/jm401731q. Epub 2014 Apr 4. J Med Chem. 2014. PMID: 24666203
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Among authors: joseph sb. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B. Tully DC, et al. Among authors: joseph sb. J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29148806
Tropifexor-Mediated Abrogation of Steatohepatitis and Fibrosis Is Associated With the Antioxidative Gene Expression Profile in Rodents.
Hernandez ED, Zheng L, Kim Y, Fang B, Liu B, Valdez RA, Dietrich WF, Rucker PV, Chianelli D, Schmeits J, Bao D, Zoll J, Dubois C, Federe GC, Chen L, Joseph SB, Klickstein LB, Walker J, Molteni V, McNamara P, Meeusen S, Tully DC, Badman MK, Xu J, Laffitte B. Hernandez ED, et al. Among authors: joseph sb. Hepatol Commun. 2019 May 17;3(8):1085-1097. doi: 10.1002/hep4.1368. eCollection 2019 Aug. Hepatol Commun. 2019. PMID: 31388629 Free PMC article.
Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis.
Chianelli D, Rucker PV, Roland J, Tully DC, Nelson J, Liu X, Bursulaya B, Hernandez ED, Wu J, Prashad M, Schlama T, Liu Y, Chu A, Schmeits J, Huang DJ, Hill R, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Liu B, Richmond W, Sancho-Martinez I, Phimister A, Seidel HM, Badman MK, Joseph SB, Laffitte B, Molteni V. Chianelli D, et al. Among authors: joseph sb. J Med Chem. 2020 Apr 23;63(8):3868-3880. doi: 10.1021/acs.jmedchem.9b01621. Epub 2020 Feb 5. J Med Chem. 2020. PMID: 31940200
Discovery of CMX990: A Potent SARS-CoV-2 3CL Protease Inhibitor Bearing a Novel Warhead.
Dayan Elshan NGR, Wolff KC, Riva L, Woods AK, Grabovyi G, Wilson K, Pedroarena J, Ghorai S, Nazarian A, Weiss F, Liu Y, Mazumdar W, Song L, Okwor N, Malvin J, Bakowski MA, Beutler N, Kirkpatrick MG, Gebara-Lamb A, Huang E, Nguyen-Tran VTB, Chi V, Li S, Rogers TF, McNamara CW, Gupta AK, Rahimi A, Chen JJ, Joseph SB, Schultz PG, Chatterjee AK. Dayan Elshan NGR, et al. Among authors: joseph sb. J Med Chem. 2024 Feb 22;67(4):2369-2378. doi: 10.1021/acs.jmedchem.3c01938. Epub 2024 Feb 9. J Med Chem. 2024. PMID: 38335279 Free PMC article.
100 results