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Page 1
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: oakman h. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
Arnold N, Beattie D, Bradley M, Brearley A, Brown L, Charlton SJ, Fairhurst RA, Farr D, Fozard J, Fullerton J, Gosling M, Hatto J, Janus D, Jones D, Jordan L, Lewis C, Maas J, McCarthy C, Mercer M, Oakman H, Press N, Profit R, Schuerch F, Sykes D, Taylor RJ, Trifilieff A, Tuffnell A. Arnold N, et al. Among authors: oakman h. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4341-7. doi: 10.1016/j.bmcl.2014.06.014. Epub 2014 Jun 26. Bioorg Med Chem Lett. 2014. PMID: 25065493
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Arnold N, Beer D, Brown L, Cheung R, Christie J, Denholm A, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Oakman H, Sahri H, Tuffnell AR, Tweed M, Tyler JW, Wagner T, Fozard JR, Trifilieff A. Press NJ, et al. Among authors: oakman h. J Med Chem. 2012 Sep 13;55(17):7472-9. doi: 10.1021/jm300459a. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22889281
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Beattie D, Brearley A, Brown Z, Charlton SJ, Cox B, Fairhurst RA, Fozard JR, Gedeck P, Kirkham P, Meja K, Nanson L, Neef J, Oakman H, Spooner G, Taylor RJ, Turner RJ, West R, Woodward H. Beattie D, et al. Among authors: oakman h. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1219-24. doi: 10.1016/j.bmcl.2009.11.131. Epub 2009 Dec 1. Bioorg Med Chem Lett. 2010. PMID: 20031406
Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Arnold N, Beer D, Brown L, Cheung R, Christie J, Denholm A, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Oakman H, Sahri H, Tuffnell AR, Tweed M, Trifilieff A. Press NJ, et al. Among authors: oakman h. J Med Chem. 2015 Sep 10;58(17):6747-52. doi: 10.1021/acs.jmedchem.5b00902. Epub 2015 Aug 28. J Med Chem. 2015. PMID: 26288344
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.
Beattie D, Bradley M, Brearley A, Charlton SJ, Cuenoud BM, Fairhurst RA, Gedeck P, Gosling M, Janus D, Jones D, Lewis C, McCarthy C, Oakman H, Stringer R, Taylor RJ, Tuffnell A. Beattie D, et al. Among authors: oakman h. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5302-7. doi: 10.1016/j.bmcl.2010.06.136. Epub 2010 Jul 1. Bioorg Med Chem Lett. 2010. PMID: 20655218