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19 results

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Page 1
The discovery of a potent Nav1.3 inhibitor with good oral pharmacokinetics.
Pryde DC, Swain NA, Stupple PA, West CW, Marron B, Markworth CJ, Printzenhoff D, Lin Z, Cox PJ, Suzuki R, McMurray S, Waldron GJ, Payne CE, Warmus JS, Chapman ML. Pryde DC, et al. Among authors: stupple pa. Medchemcomm. 2017 Apr 28;8(6):1255-1267. doi: 10.1039/c7md00131b. eCollection 2017 Jun 1. Medchemcomm. 2017. PMID: 30108836 Free PMC article.
Non-benzimidazole containing inhibitors of respiratory syncytial virus.
Pryde DC, Tran TD, Gardner I, Bright H, Stupple P, Galan S, Alsop L, Watson L, Middleton DS, Dayal S, Platts M, Murray EJ, Parkinson T, Webster R. Pryde DC, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):827-33. doi: 10.1016/j.bmcl.2012.11.062. Epub 2012 Nov 29. Bioorg Med Chem Lett. 2013. PMID: 23265891
Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels.
McCormack K, Santos S, Chapman ML, Krafte DS, Marron BE, West CW, Krambis MJ, Antonio BM, Zellmer SG, Printzenhoff D, Padilla KM, Lin Z, Wagoner PK, Swain NA, Stupple PA, de Groot M, Butt RP, Castle NA. McCormack K, et al. Among authors: stupple pa. Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32. doi: 10.1073/pnas.1220844110. Epub 2013 Jul 1. Proc Natl Acad Sci U S A. 2013. PMID: 23818614 Free PMC article.
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.
Alexandrou AJ, Brown AR, Chapman ML, Estacion M, Turner J, Mis MA, Wilbrey A, Payne EC, Gutteridge A, Cox PJ, Doyle R, Printzenhoff D, Lin Z, Marron BE, West C, Swain NA, Storer RI, Stupple PA, Castle NA, Hounshell JA, Rivara M, Randall A, Dib-Hajj SD, Krafte D, Waxman SG, Patel MK, Butt RP, Stevens EB. Alexandrou AJ, et al. Among authors: stupple pa. PLoS One. 2016 Apr 6;11(4):e0152405. doi: 10.1371/journal.pone.0152405. eCollection 2016. PLoS One. 2016. PMID: 27050761 Free PMC article.
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.
Swain NA, Batchelor D, Beaudoin S, Bechle BM, Bradley PA, Brown AD, Brown B, Butcher KJ, Butt RP, Chapman ML, Denton S, Ellis D, Galan SRG, Gaulier SM, Greener BS, de Groot MJ, Glossop MS, Gurrell IK, Hannam J, Johnson MS, Lin Z, Markworth CJ, Marron BE, Millan DS, Nakagawa S, Pike A, Printzenhoff D, Rawson DJ, Ransley SJ, Reister SM, Sasaki K, Storer RI, Stupple PA, West CW. Swain NA, et al. Among authors: stupple pa. J Med Chem. 2017 Aug 24;60(16):7029-7042. doi: 10.1021/acs.jmedchem.7b00598. Epub 2017 Aug 10. J Med Chem. 2017. PMID: 28682065
An imidazopiperidine series of CCR5 antagonists for the treatment of HIV: the discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1-yl)-8-azabicyclo[3.2.1]oct-8-yl]propyl}acetamide (PF-232798).
Stupple PA, Batchelor DV, Corless M, Dorr PK, Ellis D, Fenwick DR, Galan SR, Jones RM, Mason HJ, Middleton DS, Perros M, Perruccio F, Platts MY, Pryde DC, Rodrigues D, Smith NN, Stephenson PT, Webster R, Westby M, Wood A. Stupple PA, et al. J Med Chem. 2011 Jan 13;54(1):67-77. doi: 10.1021/jm100978n. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128663
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
Mowbray CE, Burt C, Corbau R, Perros M, Tran I, Stupple PA, Webster R, Wood A. Mowbray CE, et al. Among authors: stupple pa. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5599-602. doi: 10.1016/j.bmcl.2009.08.039. Epub 2009 Aug 13. Bioorg Med Chem Lett. 2009. PMID: 19709880
Pyrazole NNRTIs 3: optimisation of physicochemical properties.
Mowbray CE, Corbau R, Hawes M, Jones LH, Mills JE, Perros M, Selby MD, Stupple PA, Webster R, Wood A. Mowbray CE, et al. Among authors: stupple pa. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5603-6. doi: 10.1016/j.bmcl.2009.08.043. Epub 2009 Aug 14. Bioorg Med Chem Lett. 2009. PMID: 19717303
Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.
Mowbray CE, Burt C, Corbau R, Gayton S, Hawes M, Perros M, Tran I, Price DA, Quinton FJ, Selby MD, Stupple PA, Webster R, Wood A. Mowbray CE, et al. Among authors: stupple pa. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5857-60. doi: 10.1016/j.bmcl.2009.08.080. Epub 2009 Aug 27. Bioorg Med Chem Lett. 2009. PMID: 19748778
19 results