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Novel, broad-spectrum anticonvulsants containing a sulfamide group: advancement of N-((benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into human clinical studies.
Parker MH, Smith-Swintosky VL, McComsey DF, Huang Y, Brenneman D, Klein B, Malatynska E, White HS, Milewski ME, Herb M, Finley MF, Liu Y, Lubin ML, Qin N, Iannucci R, Leclercq L, Cuyckens F, Reitz AB, Maryanoff BE. Parker MH, et al. J Med Chem. 2009 Dec 10;52(23):7528-36. doi: 10.1021/jm801432r. J Med Chem. 2009. PMID: 19388676
2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.
Baxter EW, Conway KA, Kennis L, Bischoff F, Mercken MH, Winter HL, Reynolds CH, Tounge BA, Luo C, Scott MK, Huang Y, Braeken M, Pieters SM, Berthelot DJ, Masure S, Bruinzeel WD, Jordan AD, Parker MH, Boyd RE, Qu J, Alexander RS, Brenneman DE, Reitz AB. Baxter EW, et al. Among authors: parker mh. J Med Chem. 2007 Sep 6;50(18):4261-4. doi: 10.1021/jm0705408. Epub 2007 Aug 8. J Med Chem. 2007. PMID: 17685503
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.
Huang Y, Strobel ED, Ho CY, Reynolds CH, Conway KA, Piesvaux JA, Brenneman DE, Yohrling GJ, Moore Arnold H, Rosenthal D, Alexander RS, Tounge BA, Mercken M, Vandermeeren M, Parker MH, Reitz AB, Baxter EW. Huang Y, et al. Among authors: parker mh. Bioorg Med Chem Lett. 2010 May 15;20(10):3158-60. doi: 10.1016/j.bmcl.2010.03.097. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20399652
Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112).
McComsey DF, Smith-Swintosky VL, Parker MH, Brenneman DE, Malatynska E, White HS, Klein BD, Wilcox KS, Milewski ME, Herb M, Finley MF, Liu Y, Lubin ML, Qin N, Reitz AB, Maryanoff BE. McComsey DF, et al. Among authors: parker mh. J Med Chem. 2013 Nov 27;56(22):9019-30. doi: 10.1021/jm400894u. Epub 2013 Nov 11. J Med Chem. 2013. PMID: 24205976 Free PMC article.
Design and synthesis of a series of bioavailable fatty acid synthase (FASN) KR domain inhibitors for cancer therapy.
Lu T, Schubert C, Cummings MD, Bignan G, Connolly PJ, Smans K, Ludovici D, Parker MH, Meyer C, Rocaboy C, Alexander R, Grasberger B, De Breucker S, Esser N, Fraiponts E, Gilissen R, Janssens B, Peeters D, Van Nuffel L, Vermeulen P, Bischoff J, Meerpoel L. Lu T, et al. Among authors: parker mh. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2159-2164. doi: 10.1016/j.bmcl.2018.05.014. Epub 2018 May 8. Bioorg Med Chem Lett. 2018. PMID: 29779975
131 results