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Page 1
The discovery of the benzazepine class of histamine H3 receptor antagonists.
Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Briggs MA, Calver AR, Crook B, Davis RP, Davis S, Dean DK, Harris L, Heightman TD, Panchal T, Parr CA, Quashie N, Steadman JG, Schogger J, Sehmi SS, Stean TO, Takle AK, Trail BK, White T, Witherington J, Worby A, Medhurst AD. Wilson DM, et al. Among authors: worby a. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6897-901. doi: 10.1016/j.bmcl.2013.09.089. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24161834
Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD. Wilson DM, et al. Among authors: worby a. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6890-6. doi: 10.1016/j.bmcl.2013.09.090. Epub 2013 Oct 5. Bioorg Med Chem Lett. 2013. PMID: 24269482
GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models.
Medhurst AD, Atkins AR, Beresford IJ, Brackenborough K, Briggs MA, Calver AR, Cilia J, Cluderay JE, Crook B, Davis JB, Davis RK, Davis RP, Dawson LA, Foley AG, Gartlon J, Gonzalez MI, Heslop T, Hirst WD, Jennings C, Jones DN, Lacroix LP, Martyn A, Ociepka S, Ray A, Regan CM, Roberts JC, Schogger J, Southam E, Stean TO, Trail BK, Upton N, Wadsworth G, Wald JA, White T, Witherington J, Woolley ML, Worby A, Wilson DM. Medhurst AD, et al. Among authors: worby a. J Pharmacol Exp Ther. 2007 Jun;321(3):1032-45. doi: 10.1124/jpet.107.120311. Epub 2007 Feb 27. J Pharmacol Exp Ther. 2007. PMID: 17327487
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part 2: [g]-fused and hetero-fused systems.
Micheli F, Bonanomi G, Braggio S, Capelli AM, Damiani F, Di Fabio R, Donati D, Gentile G, Hamprecht D, Perini O, Petrone M, Tedesco G, Terreni S, Worby A, Heidbreder C. Micheli F, et al. Among authors: worby a. Bioorg Med Chem Lett. 2008 Feb 1;18(3):908-12. doi: 10.1016/j.bmcl.2007.12.042. Epub 2008 Jan 4. Bioorg Med Chem Lett. 2008. PMID: 18178090
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.
Micheli F, Bonanomi G, Braggio S, Capelli AM, Celestini P, Damiani F, Di Fabio R, Donati D, Gagliardi S, Gentile G, Hamprecht D, Petrone M, Radaelli S, Tedesco G, Terreni S, Worby A, Heidbreder C. Micheli F, et al. Among authors: worby a. Bioorg Med Chem Lett. 2008 Feb 1;18(3):901-7. doi: 10.1016/j.bmcl.2007.12.066. Epub 2008 Jan 3. Bioorg Med Chem Lett. 2008. PMID: 18248991
Studies towards the identification of a new generation of atypical antipsychotic agents.
Garzya V, Forbes IT, Gribble AD, Hadley MS, Lightfoot AP, Payne AH, Smith AB, Douglas SE, Cooper DG, Stansfield IG, Meeson M, Dodds EE, Jones DN, Wood M, Reavill C, Scorer CA, Worby A, Riley G, Eddershaw P, Ioannou C, Donati D, Hagan JJ, Ratti EA. Garzya V, et al. Among authors: worby a. Bioorg Med Chem Lett. 2007 Jan 15;17(2):400-5. doi: 10.1016/j.bmcl.2006.10.036. Epub 2006 Oct 19. Bioorg Med Chem Lett. 2007. PMID: 17084080
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Bromidge SM, Arban R, Bertani B, Bison S, Borriello M, Cavanni P, Dal Forno G, Di-Fabio R, Donati D, Fontana S, Gianotti M, Gordon LJ, Granci E, Leslie CP, Moccia L, Pasquarello A, Sartori I, Sava A, Watson JM, Worby A, Zonzini L, Zucchelli V. Bromidge SM, et al. Among authors: worby a. J Med Chem. 2010 Aug 12;53(15):5827-43. doi: 10.1021/jm100482n. J Med Chem. 2010. PMID: 20590088
Dopamine D(3) receptor antagonists: The quest for a potentially selective PET ligand. Part two: Lead optimization.
Micheli F, Holmes I, Arista L, Bonanomi G, Braggio S, Cardullo F, Di Fabio R, Donati D, Gentile G, Hamprecht D, Terreni S, Heidbreder C, Savoia C, Griffante C, Worby A. Micheli F, et al. Among authors: worby a. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4011-3. doi: 10.1016/j.bmcl.2009.06.028. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19553113
1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines: a series of potent and selective dopamine D(3) receptor antagonists.
Micheli F, Bonanomi G, Blaney FE, Braggio S, Capelli AM, Checchia A, Curcuruto O, Damiani F, Fabio RD, Donati D, Gentile G, Gribble A, Hamprecht D, Tedesco G, Terreni S, Tarsi L, Lightfoot A, Stemp G, Macdonald G, Smith A, Pecoraro M, Petrone M, Perini O, Piner J, Rossi T, Worby A, Pilla M, Valerio E, Griffante C, Mugnaini M, Wood M, Scott C, Andreoli M, Lacroix L, Schwarz A, Gozzi A, Bifone A, Ashby CR Jr, Hagan JJ, Heidbreder C. Micheli F, et al. Among authors: worby a. J Med Chem. 2007 Oct 18;50(21):5076-89. doi: 10.1021/jm0705612. Epub 2007 Sep 15. J Med Chem. 2007. PMID: 17867665
33 results