76) (1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis. Dossetter AG, Beeley H, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, Macfaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M. J Med Chem. 2012, 55(14), 6363-6374.

77) Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition. Dossetter AG, Bowyer J, Cook CR, Crawford JJ, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Krapp S, Macfaul PA, McGuire TM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C. Bioorg Med Chem Lett. 2012, 22(17), 5563-5568.

78) A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds – identification of those isosteres more likely to have beneficial effects, Alexander G. Dossetter, Adam Douglas and Charles O’Donnell, Med. Chem. Commun., 2012,3, 1164-1169.

79) A matched molecular pair analysis of in-vitro human microsomal metabolic stability measurements for methylene substitution or replacements – identification of those transforms more likely to have beneficial effects. Alexander G. Dossetter, Med. Chem. Commun., 2012, 3, 1518.

80) Pharmacokinetic Benefits of 3,4-Dimethoxy Substitution of a Phenyl ring and Design of Isosteres yielding orally available Cathepsin K Inhibitors., Crawford JJ, Bowyer J, Cook CR, Finlayson JE, Heron NM, Heyes C, Highton AJ, Hudson JA, Jestel A, Kenny PW, Krapp S, Martin S, Macfaul PA, McGuire TM, Gutierrez PM, Morley AD, Morris JJ, Page KM, Ribeiro LR, Sawney H, Steinbacher S, Smith C, Vickers M, Dossetter AG. J Med Chem. 2012, 55, 8827.

81) Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity. McCoull W, Barton P, Broo A, Brown A, Clarke D, Coope G, Davies RDM, Dossetter AG , Kelly E,  Knerr L, Macfaul P, Holmes J,  Martin N,  Moore JE, Morgan D, Newton C, Osterlund K, Robb G, Rosevere E, Selmi N, Stokes S, Svensson T, Ullah V, Williams, E. Med. Chem. Commun., 2012, Accepted Manuscript

82) “Investigation of the Origins of Regiochemical Control in [4+2] Cycloadditions of 2-Pyrones and Alkynylboronates”
Kirkham, J. D.; Leach, A. G.; Row, E. C.; Harrity, J. P. A. Synthesis, 2012, 44, 1964-1973.

83) Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors
Frederick W. Goldberg, Andrew G. Leach, James S. Scott, Wendy L. Snelson, Sam D. Groombridge, Craig S. Donald, Stuart N. L. Bennett, Cristian Bodin, Pablo Morentin Gutierrez, and Amy C. Gyte. J. Med. Chem., 2012, 55 (23), pp 10652–10661

84) Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists
James S. Scott, Alan M. Birch, Katy J. Brocklehurst, Hayley S. Brown, Kristin Goldberg, Sam D. Groombridge, Julian A. Hudson, Andrew G. Leach, Philip A. MacFaul, Darren McKerrecher, Ruth Poultney, Paul Schofield and Per H. Svensson Med. Chem. Commun., 2013,4, 95-100

85) Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1
Alleyn T. Plowright, Peter Barton, Stuart Bennett, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Robert D. M. Davies, Anne Ertan, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Per H. Svensson, Andrew V. Turnbull and Michael J. Waring Med. Chem. Commun., 2013,4, 151-158

86) A monomeric form of iNOS can rationalise observed SAR for inhibitors of dimerisation: quantum mechanics and docking compared
Andrew G. Leach, Lise-Lotte Olsson and Daniel J. Warner Med. Chem. Commun., 2013,4, 180-186

87) Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353
Michael J. Waring, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Leonie Campbell, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Philip A. MacFaul, Charles O’Donnell and Andrew V. Turnbull Med. Chem. Commun., 2013,4, 159-164

88) Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors
Frederick W. Goldberg, Alan M. Birch, Andrew G. Leach, Sam D. Groombridge, Wendy L. Snelson, Pablo Morentin Gutierrez, Clare D. Hammond, Susan Birtles and Linda K. Buckett Med. Chem. Commun., 2013,4, 165-174.

89) Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases Addie, M.; Ballard, P.; Buttar, D.; Crafter, C.; Currie, G.; Davies, B. R.; Debreczeni, J.; Dry, H.; Dudley, P.; Greenwood, R.; Johnson, P. D.; Kettle, J. G.; Lane, C.; Lamont, G.; Leach, A. G.; Luke, R. W. A.; Morris, J.; Ogilvie, D.; Page, K.; Pass, M.; Pearson, S.; Ruston, L. J. Med. Chem., 2013, 56 (5), pp 2059–2073.

90) Experimental testing of quantum mechanical predictions of mutagenicity: aminopyrazoles. Leach, A.G.; McCoull, W.; Bailey, A.; Barton, P. J.; Mee, C. D.; Rosevere, E.; Chem Res. Toxicol. 2013, 26, 703.

91)Matched Molecular Pair Analysis in Drug Discovery, Dossetter, A.G.; Griffen,E.J.; Leach,A.G.; Drug Disco. Today. http://dx.doi.org/10.1016/j.drudis.2013.03.003

92) Highly diastereoselective radical cyclisations of chiral sulfinimines. Rochette EM, Lewis W, Dossetter AG, Stockman RA. Chem Commun (Camb). 2013 Oct 21;49(82):9395-7. doi: 10.1039/c3cc45452e.

93) Predicting the activity and toxicity of new psychoactive substances: a pharmaceutical industry perspective. Leach AG. Drug Test Anal. 2013 Dec 19. doi: 10.1002/dta.1593.

94) Achieving improved permeability by hydrogen bond donor modulation in a series of MGAT2 inhibitors. Scott. J. S.; Berry, D. J.; Brown, H. S.; Buckett, L.; Clarke, D. S.; Goldberg, K.; Hudson, J. A.; Leach, A. G.; MacFaul, P. A.; Raubo, P.; Robb, G. R. Med. Chem. Comm. 2013, 4, 1305-1311.

95) ‘Big data’ in pharmaceutical science: challenges and opportunities Dossetter, Ecker, Laverty & Overington Future Medicinal Chemistry, May 2014, Vol. 6, No. 8 , Pages 857-864 (doi: 10.4155/fmc.14.45)

96) Optimization of Brain Penetrant 11β-Hydroxysteroid Dehydrogenase Type I Inhibitors and in Vivo Testing in Diet-Induced Obese Mice Goldberg, F.W.; Dossetter, A.G.; Scott, J.S. Robb, G.R; Boyd, S.; Groombridge, S.D.; Kemmitt, P.D.; Sjogren, T.; Morentin-Gutierrez, P.; deSchoolmeester, J.; Swales, J.G.; Turnbull, A.V.; Wild, M.J. J. Med. Chem. 2014,57 (3), pp 970-986. DOI: 10.1021/jm4016729

97) Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists McCoull, W.; Barton, P., Brown, A. J. H. ; Bowker, S.S.; Cameron, J.; Clarke, D.S.; Davies, R. D. M.; Dossetter, A.G.; Ertan, A.; Fenwick, M.; Green, C.; Holmes, J.L.; Martin, N.; Masters, D.; Moore, J.E.; Newcombe, N.J.; Newton, C.; Pointon, H.; Robb, G.R.; Sheldon, C.; Stokes, S; Morgan D. J. Med. Chem., Articles ASAP DOI: 10.1021/jm500610n

98) Cytochrome P450 substrate recognition and binding” in Drug Metabolism Prediction, Kirchmair, J., ed. Leach, A. G.*; Kidley, N. J. 2014, 103-132.

99) Predicting the activity and toxicity of new psychoactive substances: a pharmaceutical industry perspective. Leach, A. G.* Drug Test. Analysis 2014, 6, 739-745.

100) Circumventing seizure activity in a series of G Protein Coupled Receptor 119 (GPR119) agonists. Scott, J. S.; Bowker, S. S.; Brocklehurst, K. J.; Brown, H. S.; Clarke, D. S.; Easter, A.; Ertan, A.;
Goldberg, K. Hudson, J. A.; Kavanagh, S.; Laber, D.; Leach, A. G.; MacFaul, P. A.; Martin, E. A.; McKerrecher, D.; Schofield, P.; Svensson, P. H.; Teague, J. J. Med. Chem. 2014, 57, 8984-8998.