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Page 1
Pyridazine-derived γ-secretase modulators.
Wan Z, Hall A, Jin Y, Xiang JN, Yang E, Eatherton A, Smith B, Yang G, Yu H, Wang J, Ye L, Lau LF, Yang T, Mitchell W, Cai W, Zhang X, Sang Y, Wang Y, Tong Z, Cheng Z, Hussain I, Elliott JD, Matsuoka Y. Wan Z, et al. Among authors: eatherton a. Bioorg Med Chem Lett. 2011 Jul 1;21(13):4016-9. doi: 10.1016/j.bmcl.2011.04.143. Epub 2011 May 13. Bioorg Med Chem Lett. 2011. PMID: 21636276
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
Giblin GM, O'Shaughnessy CT, Naylor A, Mitchell WL, Eatherton AJ, Slingsby BP, Rawlings DA, Goldsmith P, Brown AJ, Haslam CP, Clayton NM, Wilson AW, Chessell IP, Wittington AR, Green R. Giblin GM, et al. Among authors: eatherton aj. J Med Chem. 2007 May 31;50(11):2597-600. doi: 10.1021/jm061195+. Epub 2007 May 4. J Med Chem. 2007. PMID: 17477516
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
Mitchell WL, Giblin GM, Naylor A, Eatherton AJ, Slingsby BP, Rawlings AD, Jandu KS, Haslam CP, Brown AJ, Goldsmith P, Clayton NM, Wilson AW, Chessell IP, Green RH, Whittington AR, Wall ID. Mitchell WL, et al. Among authors: eatherton aj. Bioorg Med Chem Lett. 2009 Jan 1;19(1):259-63. doi: 10.1016/j.bmcl.2008.10.118. Epub 2008 Nov 5. Bioorg Med Chem Lett. 2009. PMID: 19010671
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: eatherton aj. J Med Chem. 2009 Oct 8;52(19):5785-8. doi: 10.1021/jm9009857. J Med Chem. 2009. PMID: 19743867
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Allan AC, Billinton A, Brown SH, Chowdhury A, Eatherton AJ, Fieldhouse C, Giblin GM, Goldsmith P, Hall A, Hurst DN, Naylor A, Rawlings DA, Sime M, Scoccitti T, Theobald PJ. Allan AC, et al. Among authors: eatherton aj. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4343-8. doi: 10.1016/j.bmcl.2011.05.047. Epub 2011 May 23. Bioorg Med Chem Lett. 2011. PMID: 21676612
Orally bioavailable and brain-penetrant pyridazine and pyridine-derived γ-secretase modulators reduced amyloidogenic Aβ peptides in vivo.
Huang Y, Li T, Eatherton A, Mitchell WL, Rong N, Ye L, Yang XJ, Jin S, Ding Y, Zhang J, Li Y, Wu Y, Jin Y, Sang Y, Cheng Z, Browne ER, Harrison DC, Hussain I, Wan Z, Hall A, Lau LF, Matsuoka Y. Huang Y, et al. Among authors: eatherton a. Neuropharmacology. 2013 Jul;70:278-86. doi: 10.1016/j.neuropharm.2013.02.003. Epub 2013 Feb 26. Neuropharmacology. 2013. PMID: 23485401
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors.
Ding X, Dai X, Long K, Peng C, Andreotti D, Bamborough P, Eatherton AJ, Edge C, Jandu KS, Nichols PL, Philps OJ, Stasi LP, Wan Z, Xiang JN, Dong K, Dossang P, Ho MH, Li Y, Mensah L, Guan X, Reith AD, Ren F. Ding X, et al. Among authors: eatherton aj. Bioorg Med Chem Lett. 2017 Sep 1;27(17):4034-4038. doi: 10.1016/j.bmcl.2017.07.052. Epub 2017 Jul 21. Bioorg Med Chem Lett. 2017. PMID: 28774425
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Harlfinger S, Hanson L, Howard M, Howells R, Jackson A, Kemmitt P, Kingston JK, Lamont S, Lewis HJ, Li S, Liu L, Ogg D, Phillips C, Polanski R, Robb G, Robinson D, Ross S, Smith JM, Tonge M, Whiteley R, Yang J, Zhang L, Zhao X. Kettle JG, et al. Among authors: eatherton a. J Med Chem. 2020 May 14;63(9):4468-4483. doi: 10.1021/acs.jmedchem.9b01720. Epub 2020 Feb 13. J Med Chem. 2020. PMID: 32023060
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Cumming IA, Degorce SL, Aagaard A, Braybrooke EL, Davies NL, Diène CR, Eatherton AJ, Felstead HR, Groombridge SD, Lenz EM, Li Y, Nai Y, Pearson S, Robb GR, Scott JS, Steward OR, Wu C, Xue Y, Zhang L, Zhang Y. Cumming IA, et al. Among authors: eatherton aj. Bioorg Med Chem. 2022 Jun 1;63:116729. doi: 10.1016/j.bmc.2022.116729. Epub 2022 Apr 2. Bioorg Med Chem. 2022. PMID: 35439688
Identification of Novel, Selective Ataxia-Telangiectasia Mutated Kinase Inhibitors with the Ability to Penetrate the Blood-Brain Barrier: The Discovery of AZD1390.
Pike KG, Hunt TA, Barlaam B, Benstead D, Cadogan E, Chen K, Cook CR, Colclough N, Deng C, Durant ST, Eatherton A, Goldberg K, Johnström P, Liu L, Liu Z, Nissink JWM, Pang C, Pass M, Robb GR, Roberts C, Schou M, Steward O, Sykes A, Yan Y, Zhai B, Zheng L. Pike KG, et al. Among authors: eatherton a. J Med Chem. 2024 Feb 22;67(4):3090-3111. doi: 10.1021/acs.jmedchem.3c02277. Epub 2024 Feb 2. J Med Chem. 2024. PMID: 38306388
14 results