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19 results

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Page 1
Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Braybrooke E, Colclough N, Davies NL, Floc'h N, Greenwood R, Guérot C, Hargreaves D, Johnstrom P, Khurana P, Kostomiris DH, Li S, Lister A, Lorthioir O, Martin S, McCoull W, McLean NJ, McWilliams L, Orme JP, Packer MJ, Pearson S, Swaih AM, Tentarelli S, Tucker MJ, Ward RA, Wilkinson S, Winlow P, Wood IL. Thomson C, et al. Among authors: lorthioir o. J Med Chem. 2024 Sep 28. doi: 10.1021/acs.jmedchem.4c01792. Online ahead of print. J Med Chem. 2024. PMID: 39340451
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Finlay MRV, Barton P, Bickerton S, Bista M, Colclough N, Cross DAE, Evans L, Floc'h N, Gregson C, Guérot CM, Hargreaves D, Kang X, Lenz EM, Li X, Liu Y, Lorthioir O, Martin MJ, McKerrecher D, McWhirter C, O'Neill D, Orme JP, Mosallanejad A, Rahi A, Smith PD, Talbot V, Ward RA, Wrigley G, Wylot M, Xue L, Yao T, Ye Y, Zhao X. Finlay MRV, et al. Among authors: lorthioir o. J Med Chem. 2021 Sep 23;64(18):13704-13718. doi: 10.1021/acs.jmedchem.1c01055. Epub 2021 Sep 7. J Med Chem. 2021. PMID: 34491761
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: lorthioir o. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
Novel potent and selective pyrazolylpyrimidine-based SYK inhibitors.
Barlaam B, Boiko S, Boyd S, Dry H, Gingipalli L, Ikeda T, Johnson T, Kawatkar S, Lorthioir O, Pike A, Pollard H, Read J, Su Q, Wang H, Wang H, Wang L, Wang P, Edmondson SD. Barlaam B, et al. Among authors: lorthioir o. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127523. doi: 10.1016/j.bmcl.2020.127523. Epub 2020 Aug 30. Bioorg Med Chem Lett. 2020. PMID: 32877741
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors.
Holmes IP, Gaines S, Watson SP, Lorthioir O, Walker A, Baddeley SJ, Herbert S, Egan D, Convery MA, Singh OM, Gross JW, Strelow JM, Smith RH, Amour AJ, Brown D, Martin SL. Holmes IP, et al. Among authors: lorthioir o. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5760-3. doi: 10.1016/j.bmcl.2009.07.155. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19703773
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Holmes IP, Blunt RJ, Lorthioir OE, Blowers SM, Gribble A, Payne AH, Stansfield IG, Wood M, Woollard PM, Reavill C, Howes CM, Micheli F, Di Fabio R, Donati D, Terreni S, Hamprecht D, Arista L, Worby A, Watson SP. Holmes IP, et al. Bioorg Med Chem Lett. 2010 Mar 15;20(6):2013-6. doi: 10.1016/j.bmcl.2010.01.090. Epub 2010 Jan 25. Bioorg Med Chem Lett. 2010. PMID: 20153647
Identification of novel pyrazole acid antagonists for the EP1 receptor.
McKeown SC, Hall A, Giblin GM, Lorthioir O, Blunt R, Lewell XQ, Wilson RJ, Brown SH, Chowdhury A, Coleman T, Watson SP, Chessell IP, Pipe A, Clayton N, Goldsmith P. McKeown SC, et al. Among authors: lorthioir o. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4767-71. doi: 10.1016/j.bmcl.2006.06.086. Epub 2006 Jul 14. Bioorg Med Chem Lett. 2006. PMID: 16843659
The identification of novel orally active mGluR5 antagonist GSK2210875.
Pilla M, Andreoli M, Tessari M, Delle-Fratte S, Roth A, Butler S, Brown F, Shah P, Bettini E, Cavallini P, Benedetti R, Minick D, Smith P, Tehan B, D'Alessandro P, Lorthioir O, Ball C, Garzya V, Goodacre C, Watson S. Pilla M, et al. Among authors: lorthioir o. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7521-4. doi: 10.1016/j.bmcl.2010.09.120. Epub 2010 Nov 2. Bioorg Med Chem Lett. 2010. PMID: 21051228
19 results