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Page 1
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: haberthuer s. J Med Chem. 2012 Sep 13;55(17):7472-9. doi: 10.1021/jm300459a. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22889281
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Brown L, Cheung R, Christie J, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Press NE, Sahri H, Tuffnell AR, Tweed M, Fozard JR. Press NJ, et al. Among authors: haberthuer s. Bioorg Med Chem Lett. 2005 Jun 15;15(12):3081-5. doi: 10.1016/j.bmcl.2005.04.021. Bioorg Med Chem Lett. 2005. PMID: 15876531
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: haberthuer s. 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
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: haberthuer s. 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 solid-phase approach towards the synthesis of PDE5 inhibitors.
Beer D, Bhalay G, Dunstan A, Glen A, Haberthuer S, Moser H. Beer D, et al. Among authors: haberthuer s. Bioorg Med Chem Lett. 2002 Aug 5;12(15):1973-6. doi: 10.1016/s0960-894x(02)00296-2. Bioorg Med Chem Lett. 2002. PMID: 12113821
8-Aryl xanthines potent inhibitors of phosphodiesterase 5.
Arnold R, Beer D, Bhalay G, Baettig U, Collingwood SP, Craig S, Devereux N, Dunstan A, Glen A, Gomez S, Haberthuer S, Howe T, Jelfs S, Moser H, Naef R, Nicklin P, Sandham D, Stringer R, Turner K, Watson S, Zurini M. Arnold R, et al. Among authors: haberthuer s. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2587-90. doi: 10.1016/s0960-894x(02)00480-8. Bioorg Med Chem Lett. 2002. PMID: 12182866
Synthesis and biological properties of novel glucocorticoid androstene C-17 furoate esters.
Sandham DA, Barker L, Beattie D, Beer D, Bidlake L, Bentley D, Butler KD, Craig S, Farr D, Ffoulkes-Jones C, Fozard JR, Haberthuer S, Howes C, Hynx D, Jeffers S, Keller TH, Kirkham PA, Maas JC, Mazzoni L, Nicholls A, Pilgrim GE, Schaebulin E, Spooner GM, Stringer R, Tranter P, Turner KL, Tweed MF, Walker C, Watson SJ, Cuenoud BM. Sandham DA, et al. Among authors: haberthuer s. Bioorg Med Chem. 2004 Oct 1;12(19):5213-24. doi: 10.1016/j.bmc.2004.06.027. Bioorg Med Chem. 2004. PMID: 15351404
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity.
Alikhani V, Beer D, Bentley D, Bruce I, Cuenoud BM, Fairhurst RA, Gedeck P, Haberthuer S, Hayden C, Janus D, Jordan L, Lewis C, Smithies K, Wissler E. Alikhani V, et al. Among authors: haberthuer s. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4705-10. doi: 10.1016/j.bmcl.2004.06.086. Bioorg Med Chem Lett. 2004. PMID: 15324892