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Page 1
Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
Gerspacher M, Fairhurst RA, Mah R, Roehn-Carnemolla E, Furet P, Fritsch C, Guthy DA. Gerspacher M, et al. Among authors: fairhurst ra. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3582-4. doi: 10.1016/j.bmcl.2015.06.077. Epub 2015 Jun 30. Bioorg Med Chem Lett. 2015. PMID: 26164189
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.
Arnold NJ, Arnold R, Beer D, Bhalay G, Collingwood SP, Craig S, Devereux N, Dodds M, Dunstan AR, Fairhurst RA, Farr D, Fullerton JD, Glen A, Gomez S, Haberthuer S, Hatto JD, Howes C, Jones D, Keller TH, Leuenberger B, Moser HE, Muller I, Naef R, Nicklin PA, Sandham DA, Turner KL, Tweed MF, Watson SJ, Zurini M. Arnold NJ, et al. Among authors: fairhurst ra. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2376-9. doi: 10.1016/j.bmcl.2006.11.019. Epub 2006 Nov 10. Bioorg Med Chem Lett. 2007. PMID: 17337182
7-Azaindole-3-acetic acid derivatives: potent and selective CRTh2 receptor antagonists.
Sandham DA, Adcock C, Bala K, Barker L, Brown Z, Dubois G, Budd D, Cox B, Fairhurst RA, Furegati M, Leblanc C, Manini J, Profit R, Reilly J, Stringer R, Schmidt A, Turner KL, Watson SJ, Willis J, Williams G, Wilson C. Sandham DA, et al. Among authors: fairhurst ra. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4794-8. doi: 10.1016/j.bmcl.2009.06.042. Epub 2009 Jun 14. Bioorg Med Chem Lett. 2009. PMID: 19592244
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: fairhurst ra. 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
An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.
Beattie D, Beer D, Bradley ME, Bruce I, Charlton SJ, Cuenoud BM, Fairhurst RA, Farr D, Fozard JR, Janus D, Rosethorne EM, Sandham DA, Sykes DA, Trifilieff A, Turner KL, Wissler E. Beattie D, et al. Among authors: fairhurst ra. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6280-5. doi: 10.1016/j.bmcl.2012.07.096. Epub 2012 Aug 4. Bioorg Med Chem Lett. 2012. PMID: 22932315
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: fairhurst ra. 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
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors.
Fairhurst RA, Gerspacher M, Imbach-Weese P, Mah R, Caravatti G, Furet P, Fritsch C, Schnell C, Blanz J, Blasco F, Desrayaud S, Guthy DA, Knapp M, Arz D, Wirth J, Roehn-Carnemolla E, Luu VH. Fairhurst RA, et al. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3575-81. doi: 10.1016/j.bmcl.2015.06.067. Epub 2015 Jun 26. Bioorg Med Chem Lett. 2015. PMID: 26199119
33 results