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Page 1
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Hall A, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Hammond B, Healy MP, Johnson MR, Metcalf A, Michel AD, Naylor A, Novelli R, Spalding DJ, Sweeting J, Winyard L. Hall A, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2007 Feb 15;17(4):916-20. doi: 10.1016/j.bmcl.2006.11.059. Epub 2006 Nov 22. Bioorg Med Chem Lett. 2007. PMID: 17175160
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Gleave RJ, Hammond B, Healy MP, Johnson MR, Michel AD, Naylor A, Novelli R, Spalding DJ, Tang SP. Hall A, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3657-62. doi: 10.1016/j.bmcl.2006.04.073. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697196
1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists: Structure-activity relationships of 4- and 5-substituted benzoic acid derivatives.
Hall A, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Hammond B, Healy MP, Johnson MR, Metcalf A, Michel AD, Naylor A, Novelli R, Spalding DJ, Sweeting J. Hall A, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2007 Feb 1;17(3):732-5. doi: 10.1016/j.bmcl.2006.10.078. Epub 2006 Oct 28. Bioorg Med Chem Lett. 2007. PMID: 17098427
Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Giblin GM, Goldsmith P, Healy MP, Jandu KS, Johnson MR, Michel AD, Naylor A, Sweeting JA. Hall A, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1200-5. doi: 10.1016/j.bmcl.2006.12.021. Epub 2006 Dec 12. Bioorg Med Chem Lett. 2007. PMID: 17196385
Identification of novel glycine sulfonamide antagonists for the EP1 receptor.
McKeown SC, Hall A, Blunt R, Brown SH, Chessell IP, Chowdhury A, Giblin GM, Healy MP, Johnson MR, Lorthioir O, Michel AD, Naylor A, Lewell X, Roman S, Watson SP, Winchester WJ, Wilson RJ. McKeown SC, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1750-4. doi: 10.1016/j.bmcl.2006.12.060. Epub 2006 Dec 22. Bioorg Med Chem Lett. 2007. PMID: 17236765
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Giblin GM, Billinton A, Briggs M, Brown AJ, Chessell IP, Clayton NM, Eatherton AJ, Goldsmith P, Haslam C, Johnson MR, Mitchell WL, Naylor A, Perboni A, Slingsby BP, Wilson AW. Giblin GM, et al. Among authors: johnson mr. J Med Chem. 2009 Oct 8;52(19):5785-8. doi: 10.1021/jm9009857. J Med Chem. 2009. PMID: 19743867
Pyridine-derived γ-secretase modulators.
Wan Z, Hall A, Sang Y, Xiang JN, Yang E, Smith B, Harrison DC, Yang G, Yu H, Price HS, Wang J, Hawkins J, Lau LF, Johnson MR, Li T, Zhao W, Mitchell WL, Su X, Zhang X, Zhou Y, Jin Y, Tong Z, Cheng Z, Hussain I, Elliott JD, Matsuoka Y. Wan Z, et al. Among authors: johnson mr. Bioorg Med Chem Lett. 2011 Aug 15;21(16):4832-5. doi: 10.1016/j.bmcl.2011.06.042. Epub 2011 Jun 17. Bioorg Med Chem Lett. 2011. PMID: 21742495
Substituted thiazolylureas.
Islip PJ, Closier MD, Johnson MR, Neville MC. Islip PJ, et al. Among authors: johnson mr. J Med Chem. 1972 Jan;15(1):101-3. doi: 10.1021/jm00271a031. J Med Chem. 1972. PMID: 4331916 No abstract available.
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
McBride C, Trzoss L, Povero D, Lazic M, Ambrus-Aikelin G, Santini A, Pranadinata R, Bain G, Stansfield R, Stafford JA, Veal J, Takahashi R, Ly J, Chen S, Liu L, Nespi M, Blake R, Katewa A, Kleinheinz T, Sujatha-Bhaskar S, Ramamoorthi N, Sims J, McKenzie B, Chen M, Ultsch M, Johnson M, Murray J, Ciferri C, Staben ST, Townsend MJ, Stivala CE. McBride C, et al. J Med Chem. 2022 Nov 10;65(21):14721-14739. doi: 10.1021/acs.jmedchem.2c01250. Epub 2022 Oct 24. J Med Chem. 2022. PMID: 36279149
989 results