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Conference talks on Slideshare

7th October 2016 - Pharmacophore extraction from Matched Molecular Pair Analysis

28th September 2016 - American Chemistry Society meeting Fall 2016 MedChemica - Extracting and exploiting medicinal chemistry ADMET knowledge automatically from public and large pharma data

3rd September 2013 - Cambridge Med Chemistry conference Fall 2013 Multi-Parameter Optimization of Pharmaceuticals: the Big-Data Way

Publications

140 Publications and Patents
In areas of medicinal chemistry (GPCRs, Kinases, Proteases, Enzymes), Computational chemistry (Matched Molecular Pair Analysis, Infomatices, Quantum Mechanics) and Organic Synthesis (Diels-Alder, asymmetric synthesis,  reaction modeling, polymer supported reagents).

Key Matched Molecular Pair Analysis Papers.

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

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.

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.

Enantiomeric pairs reveal that key medicinal chemistry parameters vary more than simple physical property based models can explain
Andrew G. Leach, Elizabeth A. Pilling, Alfred A. Rabow, Simone Tomasi, Nabil Asaad, Niklaas J. Buurma, Andrew Ballard and Stefania Narduolo Med. Chem. Commun., 2012,3, 528-540.

Matched Molecular Pairs as a Medicinal Chemistry Tool
Griffen, E.; Leach, A. G.*; Robb, G. R.; Warner, D. J. J. Med. Chem. 2011, 54, 7739-7750.
A statistical analysis of in vitro human microsomal metabolic stability of small phenyl group substituents, leading to improved design sets for parallel SAR exploration of a chemical series. Dossetter, Alexander G. Bioorganic & Medicinal Chemistry (2010), 18(12), 4405-4414.

WizePairZ: A Novel Algorithm to Identify, Encode, and Exploit Matched Molecular Pairs with Unspecified Cores in Medicinal Chemistry
Daniel J. Warner, Edward J. Griffen and Stephen A. St-Gallay
J. Chem. Inf. Model., 2010, 50 (8), pp 1350–1357

The rise of the intelligent machines in drug hunting? Griffen, Ed. Future Medicinal Chemistry (2009), 1(3), 405-408.

Matched Molecular Pairs as a Guide in the Optimization of Pharmaceutical Properties; a Study of Aqueous Solubility, Plasma Protein Binding and Oral Exposure
Leach, A. G.*; Jones, H. D.; Cosgrove, D. A.; Kenny, P. W.; Ruston, L.; MacFaul, P.; Wood, J. M.; Colclough, N.; Law, B. J. Med. Chem. 2006, 49, 6672-6682.

MedChemica Publication by Year
Most highly cited indicated with ‡.

2016

110) MIDA boronates are hydrolysed fast and slow by two different mechanisms. Gonzalez, J. A.; Ogba, O. M.; Morehouse, G. F.; Rosson, N.; Houk, K. N.; Leach, A. G.; Cheong, P. H.-Y.; Burke, M. D.; Lloyd-Jones, G. C. Nat. Chem. 2016, ASAP.

109) “Matched molecular pair analysis” in Comprehensive Medicinal Chemistry III, Davis, A. and Edge, C. Eds. Leach, A. G.*; Lukac, I.; Zarnecka, J. M.; Dossetter, A. G.; Griffen, E. J.

108) Protodeboronation of Heteroaromatic, Vinyl, and Cyclopropyl Boronic Acids: pH-Rate Profiles, Autocatalysis, and Disproportionation. Cox, P. A.; Leach, A. G.; Campbell, A. D.; Lloyd-Jones, G. C. J. Am. Chem. Soc. 2016, 138, 9145-9157.

2015

106) Novel N-thiazolyl piperazine-1-carboxamide CCR2 antagonists – investigation of an unexpected reaction with glutathione. Cumming, J. G.; MacFaul, P. A.; Leach, A. G.* Med. Chem. Commun. 2015, 6, 2140-2145.

105) Designing hydroxamates and reversed hydroxamates to inhibit zinc-containing proteases but not cytochrome P450s: insights from quantum mechanics and protein-ligand crystal structures. Barker, C.; Lukac, I.; Leach, A. G.* Mol. Informatics 2015, 34, 608-614.

104) A mechanistic proposal for the protodeboronation of neat boronic acids: boronic acid mediated reaction in the solid state. Noonan, G.; Leach, A. G.* Org. Biomol. Chem. 2015, 13, 2555-2560.

103) An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer. Colley, H. E.; Muthana, M.; Danson, S. J.; Jackson, L. V.; Brett, M. L.; Harrison, J.; Coole, S. F.; Mason, D. P.; Jennings, L. R.; Wong, M.; Tulasi, V.; Norman, D.; Lockey, P. M.; Williams, L.; Dossetter, A. G.; Griffen, E.J.; Thompson, M. J. Department of Chemistry, University of Sheffield , Brook Hill, Sheffield S3 7HF, U.K. J. Med. Chem. 2015, 58, 9309-33.

102) Discovery of a series of 2-(pyridinyl)pyrimidines as potent antagonists of GPR40. Waring, M. J.; Baker, D. J.; Bennett, S. N. L. Dossetter, A. G.; Fenwick, M.; Garcia, R.; Georgsson, J.; Groombridge, S.D.; Loxham, S; MacFaul, P.A.; Maskill, K. G.; Morgan, D.; Morrell, J.; Pointon, H.; Robb, G. R.; Smith, D. M.; Stokes, S.; Wilkinson, G. Med. Chem. Commun., 2015, 6, 1024-1029

101) Tactics to avoid inhibition of cytochrome P450s” in Tactics in Contemporary Drug Design, Meanwell, N., ed. Leach, A. G.* 2015, 107-158.

101) Medicinal chemistry optimisation of kinetics” in Kinetics and Thermodynamics of Drug Binding, Keseru, G. M. and Swinney, D., eds. Waring, M. J.; Leach, A. G.; Miller, D. 2015.

2014

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.

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

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

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

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

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)

2013

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.

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.

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.

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

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.

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.

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.

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

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

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

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

2012

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

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.

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

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.

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.

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.

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.

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.

75) A System for Encoding and Searching Markush Structures
Cosgrove, D. A.; Green, K. M.; Leach, A. G.; Poirrette, A.; Winter, J. J. Chem. Inf. Model. 2012, 52, 1936-1947.

74) “Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.”
McCoull, W.; Addie, M. S.; Birch, A. M.; Birtles, S.; Buckett, L. K.; Butlin, R. J.; Bowker, S. S.; Boyd, S.; Chapman, S.; Davies, R. D. M.; Donald, C. S.; Green, C. P.; Jenner, C.; Kemmitt, P. D.; Leach, A. G.; Moody, G. C.; Morentin Gutierrez, P.; Newcombe, N. J.; Nowak, T.; Packer, M. J.; Plowright, A. T.; Revill, J.; Schofield, P.; Sheldon, C.; Stokes, S.; Turnbull, A. V.; Wang, S. J. Y.; Whalley, D. P.; Wood, J. M. Bioorg. Med. Chem. Letters 2012, 22, 3873-3878.

73) “Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase.”
Norman, R. A.; Schott, A.-S.; Andrews, D. M.; Breed, J.; Foote, K. M.; Garner, A. P.; Ogg, D.; Orme, J. P; Pink, J. H.; Roberts, K.; Rudge, D. A.; Thomas, A. P.; Leach, A. G.* J. Med. Chem. 2012, 55, 5003-5012.

72) Use of Small-Molecule Crystal Structures To Address Solubility in a Novel Series of G Protein Coupled Receptor 119 Agonists: Optimization of a Lead and in Vivo Evaluation
Scott, J. S.; Birch, A. M.; Brocklehurst, K. J.; Broo, A.; Brown, H. S.; Butlin, R. J.; Clarke, D. S.; Davidsson, O.; Ertan, A.; Goldberg, K.; Groombridge, S. D.; Hudson, J. A.; Laber, D.; Leach, A. G.; MacFaul, P. A.; McKerrecher, D.; Pickup, A.; Schofield, P.; Svensson, P. H.; Sörme, P.; Teague, J. J. Med. Chem. 2012, 55, 5361-5379.

71) Protein–Ligand Crystal Structures Can Guide the Design of Selective Inhibitors of the FGFR Tyrosine Kinase
Richard A. Norman, Anne-Kathrin Schott, David M. Andrews, Jason Breed, Kevin M. Foote, Andrew P. Garner, Derek Ogg, Jonathon P. Orme, Jennifer H. Pink, Karen Roberts, David A. Rudge, Andrew P. Thomas, and Andrew G. Leach
J. Med. Chem., 2012, 55 (11), pp 5003–5012

70) Rationally Designing Safer Anilines: The Challenging Case of 4-Aminobiphenyls
Birch, A. M.; Groombridge, S.; Law, R.; Leach, A. G.*; Mee, C.; Schramm, C. J. Med. Chem. 2012, 55, 3923-3933.

69) Oxadiazole isomers: all bioisosteres are not created equal
Kristin Goldberg, Sam Groombridge, Julian Hudson, Andrew G. Leach, Philip A. MacFaul, Adrian Pickup, Ruth Poultney, James S. Scott, Per H. Svensson and Joseph Sweeney Med. Chem. Commun., 2012,3, 600-604.

68) Enantiomeric pairs reveal that key medicinal chemistry parameters vary more than simple physical property based models can explain
Andrew G. Leach, Elizabeth A. Pilling, Alfred A. Rabow, Simone Tomasi, Nabil Asaad, Niklaas J. Buurma, Andrew Ballard and Stefania Narduolo Med. Chem. Commun., 2012,3, 528-540.

67) “Mechanistic Studies on a Sulfoxide Transfer Reaction Mediated by Diphenyl Sulfoxide/Triflic Anhydride”
Fascione, M. A.; Adshead, S. J.; Mandal, P. K.; Kilner, C. A.; Leach, A. G.; Turnbull, W. B. Chem. Eur. J. 2012, 18, 2987-2997.

66) “Do Glycosyl Sulfonium Ions Engage in Neighbouring-Group Participation? A Study of Oxathiane Glycosyl Donors and the Basis for their Stereoselectivity”
Fascione, M. A.; Kilner, C. A.; Leach, A. G.; Turnbull, W. B. Chem. Eur. J. 2012, 18, 321-333.

2011

65) DNA-dependent protein kinase (DNA-PK) inhibitors: Structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain
Clapham, Kate M.; Bardos, Julia; Finlay, M. Raymond V.; Golding, Bernard T.; Griffen, Edward J.; Griffin, Roger J.; Hardcastle, Ian R.; Menear, Keith A.; Ting, Attilla; Turner, Paul;  et al  Bioorganic & Medicinal Chemistry Letters (2011), 21(3), 966-970.DOI: 10.1016/j.bmcl.2010.12.047

64) “Discovery, optimisation and in vivo evaluation of novel GPR119 agonists”
Brocklehurst, K. J.; Broo, A.; Butlin, R. J.; Brown, H. S.; Clarke, D. S.; Davidsson, Ö.; Goldberg, K.; Groombridge, S. D.; Kelly, E. E.; Leach, A.; McKerrecher, D.; O’Donnell, C.; Poucher, S.; Schofield, P.; Scott, J. S.; Teague, J.; Westgate, L.; Wood, M. J. M Bioorg. Med. Chem. Lett. 2011, 21, 7310-7316.

63) Matched Molecular Pairs as a Medicinal Chemistry Tool
Griffen, E.; Leach, A. G.*; Robb, G. R.; Warner, D. J. J. Med. Chem. 2011, 54, 7739-7750.

62) “The Discovery of Benzanilides as c-Met Receptor Tyrosine Kinase Inhibitors by a Directed Screening approach”
Allen, J. V.; Bardelle, C.; Blades, K.; Buttar, D.; Chapman, L.; Colclough, N.; Dossetter, A. G.; Garner, A. P.; Girdwood, A.; Lambert, C.; Leach, A. G.; Law, B.; Major, J.; Plant, H.; Slater, A. M. Bioorganic & Medicinal Chemistry Letters (2011), 21(18), 5224-5229.

61) Quantitatively Interpreted Enhanced Inhibition of Cytochrome P450s by Heteroaromatic Rings Containing Nitrogen
Leach, A. G.*; Kidley, N. J. J. Chem. Inf. Model. 2011, 51, 1048-1063.

2010

60) A statistical analysis of in vitro human microsomal metabolic stability of small phenyl group substituents, leading to improved design sets for parallel SAR exploration of a chemical series. Dossetter, Alexander G. Bioorganic & Medicinal Chemistry (2010), 18(12), 4405-4414.

59) WizePairZ: A Novel Algorithm to Identify, Encode, and Exploit Matched Molecular Pairs with Unspecified Cores in Medicinal Chemistry
Daniel J. Warner, Edward J. Griffen and Stephen A. St-Gallay
J. Chem. Inf. Model., 2010, 50 (8), pp 1350–1357
Publication Date (Web): August 6, 2010 (Article)
DOI: 10.1021/ci100084s

58) Data-mining patent literature for novel chemical reagents for use in medicinal chemistry design
Jason G. Kettle, Richard A. Ward and Ed Griffen Med. Chem. Commun., 2010,1, 331-338.

2009

57) “Neighbouring group participation vs. addition to oxacarbenium ions: studies on the synthesis of mycobacterial oligosaccharides.”
Stalford, S. A.; Kilner, C. A.; Leach, A. G.; Turnbull,  W. B. Org. Biomol. Chem. 2009, 4842-4852.

56) “Stereoselective glycosylation using oxathiane glycosyl donors.”
Fascione, M. A.; Adshead, S. J.; Stalford, S. A.; Kilner, C. A.; Leach, A. G.; Turnbull,  W. B. Chem. Commun. 2009, 5841-5843.

55) Side Chain Flexibilities in the Human Ether-a-go-go Related Gene Potassium Channel (hERG) Together with Matched-Pair Binding Studies Suggest a New Binding Mode for Channel Blockers
Zachariae, U.; Giordanetto, F.; Leach, A. G. J. Med. Chem. 2009, 52, 4266-4276.

54) The rise of the intelligent machines in drug hunting?
Griffen, Ed Future Medicinal Chemistry (2009), 1(3), 405-408. DOI: 10.4155/fmc.09.43

53) In vitro pharmacological profiles of kinase inhibitors: Comparison with other pharmaceuticals
Luke, R.W.A., Rolf, M.G., Bradbury, R.H., Griffen, E.J., Hales, N.J., Kettle, J., Thomas, A.P., Bowes, J., Valentin, J.P., Barker, A.J., Journal of Pharmacological and Toxicological Methods (2009),60 (2), 219 (2009) DOI: 10.1016/j.vascn.2009.04.052,

52) Reaction energies computed with density functional theory correspond with a whole organism effect; modelling the Ames test for mutagenicity
Andrew G. Leach, Rebecca Cann and Simone Tomasi Chem. Commun., 2009,0, 1094-1096

51) Beyond Picomolar Affinities: Quantitative Aspects of Noncovalent and Covalent Binding of Drugs to Proteins
Smith, A. J. T.; Zhang, X.; Leach, A. G.; Houk, K. N. J. Med. Chem. 2009, 52, 225-233.

2008

50) “Inhibitors of the tyrosine kinase EphB4. Part 2: Structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines.”
Bardelle, C.; Coleman, T.; Cross, D.; Davenport, S.; Kettle, J. G.; Ko, E. J.; Leach, A. G.; Mortlock, A.; Read, J.; Roberts, N. J.; Robins, P.; Williams, E. J. Bioorg. Med. Chem. Lett. 2008, 18, 5717-5721.

49) Theoretical Prediction of a Perepoxide Intermediate for the Reaction of Singlet Oxygen with trans-Cyclooctene Contrasts with the Two-Step No-Intermediate Ene Reaction for Acyclic Alkenes
Leach, A. G.; Houk, K. N.; Foote, C. S. J. Org. Chem. 2008, 73, 8511–8519.

48) “Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines.”
Bardelle, C.; Cross, D.; Davenport, S.; Kettle, J. G.; Ko, E. J.; Leach, A.G.; Mortlock, A.; Read, J.; Roberts, N. J.; Robins, P.; Williams, E. J. Bioorg. Med. Chem. Lett. 2008, 18, 2776-2780.

47) Stereoselective Construction of the Tricyclic Core of Neoliacinic Acid.      Clark, J. Stephen; Baxter, Carl A.; Dossetter, Alexander G.; Poigny, Stephane; Castro, Jose L.; Whittingham, William G. Journal of Organic Chemistry  (2008),  73(3),  1040-1055

2007

46) Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.  Arnould, Jean Claude; Delouvrie, Benedicte; Boutron, Pascal; Dossetter, Al G.; Foote, Kevin M.; Hamon, Annie; Hancox, Urs; Harris, Craig S.; Hutton, Mike; Lamorlette, Maryannick; Matusiak, Zbigniew.    Centre de Recherches, PI Pompelle,  AstraZeneca,  Reims,  Fr.    Bioorganic & Medicinal Chemistry Letters  (2007),  17(23),  6448-6454.  

45) An integrated approach to fragment-based lead generation: philosophy, strategy and case studies AstraZeneca's drug discovery programmes
Albert, Jeffrey S.; Blomberg, Niklas; Breeze, Alexander L.; Brown, Alastair J. H.; Burrows, Jeremy N.; Edwards, Philip D.; Folmer, Rutger H. A.; Geschwindner, Stefan; Griffen, Ed J.; Kenny, Peter W.;  et al  Current Topics in Medicinal Chemistry (Sharjah, United Arab Emirates) (2007), 7(16), 1600-1629. DOI: 10.2174/156802607782341091

2006

44) Matched Molecular Pairs as a Guide in the Optimization of Pharmaceutical Properties; a Study of Aqueous Solubility, Plasma Protein Binding and Oral Exposure
Leach, A. G.*; Jones, H. D.; Cosgrove, D. A.; Kenny, P. W.; Ruston, L.; MacFaul, P.; Wood, J. M.; Colclough, N.; Law, B. J. Med. Chem. 2006, 49, 6672-6682.

43) Fragment screening: an introduction
Leach, Andrew R.; Hann, Michael M.; Burrows, Jeremy N.; Griffen, Ed J.  Molecular BioSystems (2006), 2(9), 429-446. DOI: 10.1039/b610069b

42) An enantioselective desymmetrisation approach to C9-substituted trans-hydrindene rings based on a diastereotopic group-selective intramolecular Diels–Alder reaction
Nadia Azzi, Ed Griffen, Mark Light and Bruno Linclau Chem. Commun., 2006,0, 4909-4911

41) Shapes of Antibody Binding Sites:  Qualitative and Quantitative Analyses Based on a Geomorphic Classification Scheme
Lee, M.; Lloyd, P.; Zhang, X.; Schallhorn, J. M.; Sugimoto, K.; Leach, A. G.; Sapiro, G.; Houk, K. N. J. Org. Chem. 2006, 71, 5082-5092.

40) "Inhibitors of epidermal growth factor receptor tyrosine kinase: Novel C-5 substituted anilinoquinazolines designed to target the ribose pocket."
Ballard, P.; Bradbury, R. H.; Harris, C. S.; Hennequin, L. F. A.; Hickinson, M.; Johnson, P. D.; Kettle, J. G.; Klinowska, T.; Leach, A. G.; Morgentin, R.; Pass, M.; Ogilvie, D. J.; Olivier, A.; Warin, N.; Williams, E. J. Bioorg. Med. Chem. Lett. 2006, 16, 1633-1637.

39) Fragment screening: An introduction
Leach, Andrew R.; Hann, Michael M.; Burrows, Jeremy N.; Griffen, Ed J.
Edited by Hubbard, Roderick E  Structure-Based Drug Discovery (2006), 142-172.

38) Lead discovery and the concepts of complexity and lead-likeness in the evolution of drug candidates
Hann, M. M.; Leach, A. R.; Burrows, J. N.; Griffen, E.
Edited by Taylor, John B.; Triggle, David J Comprehensive Medicinal Chemistry II (2006), 4, 435-458. DOI: 10.1016/B0-08-045044-X/

37) "Energy Contour Plots: Slices through the potential energy surface that simplify quantum mechanical studies of reacting systems."
Leach, A. G.*; Goldstein, E. J. Chem. Ed. 2006, 83, 451-459.

2005

36) "The origins of periselectivity and substituent effects in electrocyclizations of o-nitrosostyrenes: a computational study."
Leach, A. G.; Houk, K. N.; Davies, I. W. Synthesis 2005, 3463-3467.

35) "Comparison of the ATP binding sites of protein kinases using conformationally diverse bisindolylmaleimides."
Bartlett, S.; Beddard, G. S.; Jackson, R. M.; Kayser, V.; Kilner, C.; Leach, A.; Nelson, A.; Oledzki, P. R.; Parker, P.; Reid, G. D.; Warriner, S. L. J. Am. Chem. Soc. 2005, 127, 11699-11708.

2004

34) Antibody-Catalyzed Oxy-Cope Rearrangement:  Mechanism and Origins of Catalysis and Stereoselectivity from DFT Quantum Mechanics and Flexible Docking
Black, K. A.; Leach, A. G.; Kalani, M. Y. S.; Houk, K. N. J. Am. Chem. Soc. 2004, 126, 9695-9708.

33) Anomalous Intramolecular C-H Insertion Reactions of Rhodium Carbenoids: Factors Influencing the Reaction Course and Mechanistic Implications. Clark, J. Stephen; Dossetter, Alexander G.; Wong, Yung-Sing; Townsend, Robert J.; Whittingham, William G.; Russell, C. Adam.    School of Chemistry,  University of Nottingham,  Nottingham,  UK. Journal of Organic Chemistry  (2004),  69(11),  3886-3898.  

32) Catalytic enantioselective intermolecular cycloadditions of 2-diazo-3,6-diketo ester-derived carbonyl ylides with alkene dipolarophiles.      Hodgson, David M.; Brueckl, Tobias; Glen, Rebecca; Labande, Agnes H.; Selden, Deborah A.; Dossetter, Alexander G.; Redgrave, Alison J.    Department of Chemistry, Chemistry Research Laboratory,  University of Oxford,  Oxford,  UK.    Proceedings of the National Academy of Sciences of the United States of America  (2004),  101(15),  5450-5454.  

31) Insertion of (E)-(1,2-dihalovinyl)lithium and (2-haloethynyl)lithium into zirconacycles
David Norton, Richard J. Whitby and Ed Griffen Chem. Commun., 2004,0, 1214-1215.

30) Theoretical Investigation of the Origins of Catalysis of a Retro-Diels−Alder Reaction by Antibody 10F11
Leach, A. G.; Houk, K. N.; Reymond, J.-L. J. Org. Chem. 2004, 69, 3683-3692.

2003

29) "Unexpected Syn Hydride Migration in the Non-aldol Aldol Reaction."
Jung, M. E.; van den Heuvel, A.; Leach, A. G.; Houk, K. N. Org. Lett. 2003, 5, 3375-3378.

‡ 28) A Standard Set of Pericyclic Reactions of Hydrocarbons for the Benchmarking of Computational Methods:  The Performance of ab Initio, Density Functional, CASSCF, CASPT2, and CBS-QB3 Methods for the Prediction of Activation Barriers, Reaction Energetics, and Transition State Geometries
Guner, V.; Khuong, K. S.; Leach, A. G.; Lee, P. S.; Bartberger, M. D.; Houk, K. N. J. Phys. Chem. A 2003, 107, 11445-11459.

27) A Cornucopia of Cycloadducts:  Theoretical Predictions of the Mechanisms and Products of the Reactions of Cyclopentadiene with Cycloheptatriene
Leach, A. G.; Goldstein, E.; Houk, K. N. J. Am. Chem. Soc. 2003, 125, 8330-8339.

26) "Theoretical Studies of Antibody Catalysis," in Catalytic Antibodies, Ehud
Keinan, ed., Weinheim, Germany:  Wiley-VCH, 2004, pp. 72-117.
Dean J. Tantillo, Andrew G. Leach, Xiyun Zhang, and K. N. Houk.

‡25) "Binding Affinities of Host-Guest, Protein-Ligand, and Protein-Transition-State Complexes."
Houk, K. N.; Leach, A. G.; Kim, S. P.; Zhang, X. Angew. Chem. Int. Ed. 2003, 42, 4872-4897.

24) "The Mechanism and Regioselectivity of the Ene Reactions of Nitroso Compounds: A Theoretical Study of Reactivity, Regioselectivity, and Kinetic Isotope Effects Establishes a Stepwise Path Involving Polarized Diradical Intermediates."
Leach, A. G.; Houk, K. N. Org. Biomol. Chem. 2003, 1, 1389-1403.

23) Synthesis and evaluation of 4,4',6,6'-tetrasubstituted binaphtholphosphate dirhodium(II) complexes as catalysts in enantioselective carbonyl ylide formation-cycloaddition reactions.      Hodgson, David M.; Selden, Deborah A.; Dossetter, Alexander G..    Department of Chemistry, Dyson Perrins Laboratory,  University of Oxford,  Oxford,  UK.    Tetrahedron: Asymmetry  (2003),  14(24),  3841-3849.  

22) Theoretical Elucidation of Kinetic and Thermodynamic Control of Radical Addition Regioselectivity
Leach, A. G.; Wang, R.; Wohlhieter, G. E.; Khan, S. I.; Jung, M. E.; Houk, K. N. J. Am. Chem. Soc. 2003, 125, 4271-4278.

‡ 21) Mechanism of Ene Reactions of Singlet Oxygen. A Two-Step No-Intermediate Mechanism
Singleton, D. A.; Hang, C.; Szymanski, M. J.; Meyer, M. P.; Leach, A. G.; Kuwata, K. T.; Chen, J. S.; Greer, A.; Foote, C. S.; Houk, K. N. J. Am. Chem. Soc. 2003, 125, 1319-1328.

2002

20) "An Unexpected Bispericyclic Transition Structure Leading to 4+2 and 2+4 Cycloadducts in the Endo Dimerization of Cyclopentadiene"
Leach, A. G.; Houk, K. N. Chemtracts-Organic Chemistry  2002, 611-616.

19) The Ene Reactions of Nitroso Compounds Involve Polarized Diradical Intermediates
Leach, A. G.; Houk, K. N. J. Am. Chem. Soc. 2002, 124, 14820-14821.

18) The Origins of Noncovalent Catalysis of Intermolecular Diels−Alder Reactions by Cyclodextrins, Self-Assembling Capsules, Antibodies, and RNAses
Kim, S. P.; Leach, A. G.; Houk, K. N. J. Org. Chem. 2002, 67, 4250-4260.

17) "Hetero-Diels-Alder and hetero-ene reactions of singlet oxygen, nitroso compounds and triazolinediones: transition states and mechanisms from contemporary theory."
Leach, A. G.; Houk, K. N. Chem. Comm. 2002, 1243-1255.

16) "Mechanism of the Forbidden [3s,5s]-Sigmatropic Shift.  Orbital Symmetry Influences Stepwise Mechanisms Involving Diradical Intermediates."
Leach, A. G.; Catak, S.; Houk, K. N. Chem. Eur. J. 2002, 8, 1290-1299.

2001

15) "New Polyethylene Glycol Polymers As Ketal Protecting Groups - A Polymer Supported Approach to Symmetrically Substituted Spiroketals"
Haag, R.; Leach, A. G.; Ley, S. V.; Nettekoven, M.; Schnaubelt, J. Synth. Comm. 2001, 31, 2965-2977.

14) Transition States and Mechanisms of the Hetero-Diels−Alder Reactions of Hyponitrous Acid, Nitrosoalkanes, Nitrosoarenes, and Nitrosocarbonyl Compounds
Leach, A. G.; Houk, K. N. J. Org. Chem. 2001, 66, 5192-5200.

‡ 13) A polymer-supported thionating reagent
Ley, S. V.; Leach, A. G.; Storer, R. I. J. Chem. Soc., Perkin Trans. 1 2001, 358-361.

2000

‡ 12) Multi-step organic synthesis using solid-supported reagents and scavengers: a new paradigm in chemical library generation
Ley, S. V.; Baxendale, I. R.; Bream, R. N.; Jackson, P. S.; Leach, A. G.; Longbottom, D. A.; Nesi, M.; Scott, J. S.; Storer, R. I.; Taylor, S. J. J. Chem. Soc., Perkin Trans. 1 2000, 3815-4195.

11. Asymmetric epoxide cyclisation route to the F-pyran fragment of the altohyrtins and key aldol studies
JC Anderson, BP McDermott, EJ Griffen Tetrahedron (2000) 56 (44), 8747-8767 DOI: /10.1016/S0040-4020(00)00804-8,

10) "The First Optically Active BINOL-BINAP Copolymer Catalyst: Highly Stereoselective Tandem Asymmetric Reactions"
Houk, K. N.; Leach, A. G. Chemtracts-Organic Chemistry 2000, 13, 633-638.

9) "Combined Application of Analytical Techniques for the Characterization of Polymer Supported Species"
Grice, P; Leach, A. G.; Ley, S. V.; Massi, A.; Mynett, D. M. J. Comb. Chem. 2000, 2, 491-495.

1995-99

8) Highly enantio- and diastereoselective hetero-Diels-Alder reactions catalyzed by new chiral tridentate chromium (III) catalysts.      Dossetter, Alexander G.; Jamison, Timothy F.; Jacobsen, Eric N.    Department of Chemistry and Chemical Biology,  Harvard University,  Cambridge,  MA,  USA.    Angewandte Chemie, International Edition  (1999),  38(16),  2398-2400. 

7) Synthesis of the functionalized core of neoliacinic acid.      Clark, Stephen J.; Dossetter, Alexander G.; Blake, Alexander J.; Li, Wan-Sheung; Whittingham, William G.    School of Chemistry,  University of Nottingham,  Nottingham,  UK.    Chemical Communications (1999), 8, 749-750

6) "Rapid conformation searching .2. Similar compounds"
Goodman, J. M.; Leach, A. G. J. Chem. Soc., Perkin Trans. 2 1997, 1205-1208.

5) Anomalous Products from Intramolecular Insertion Reactions of Rhodium Carbenoids into the a -C-H Bonds of Ethers.      Clark, J. Stephen; Dossetter, Alexander G.; Russell, C. Adam; Whittingham, William G.    Department of Chemistry,  University of Nottingham,  Nottingham,  UK.    Journal of Organic Chemistry  (1997),  62(15),  4910-4911.  

4. Synthesis of the bifunctional chelating agent 6-(4-aminobenzyl)-1,4,8,11-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid (H2NBn-TETA)
Moreau, P.; Tinkl, M.; Tsukazaki, M.; Bury, P. S.; Griffen, E. J.; Snieckus, V.; Maharajh, R. B.; Kwok, C. S.; Somayaji, V. V.; Peng, Z.; Synthesis (1997), (9), 1010-1012. DOI: 10.1055/s-1997-1314

3) Stereoselective synthesis of the bicyclic core structure of the highly oxidized sesquiterpene neoliacinic acid.      Clark, J. Stephen; Dossetter, Alexander G.; Whittingham, William G.    Department of Chemistry,  University of Nottingham,  Nottingham,  UK.    Tetrahedron Lett.  (1996),  37(31),  5605-5608.

2. 7-Methoxyphthalide [1(3H)-isobenzofuranone, 7-methoxy-]
Wang, X.; de Silva, S. O.; Reed, J. N.; Billadeau, R.; Griffen, E. J.; Chan, A.; Snieckus, V.  Organic Syntheses (1995), 72, 163-72.

1. Benzenoid Ring Functionalization of Indoles and Tryptophols via Combined Directed Ortho Metalation-Cross Coupling Methodology
Griffen, Edward J.; Roe, David G.; Snieckus, Victor Journal of Organic Chemistry (1995), 60(6), 1484-5. DOI: 10.1021/jo00111a003

PATENTS

37. Cyanocyclopropylcarboxamides as cathepsin inhibitors and their preparation and use in the treatment of diseases. Dossetter, Alexander Graham; Heron, Nicola Murdoch PCT Int. Appl. (2008), WO 2009001129.

36. 1,2-Cyclohexanedicarboxamides as cathepsin inhibitors and their preparation and use in the treatment of diseases. Dossetter, Alexander Graham; Heron, Nicola Murdoch. PCT Int. Appl. (2008), WO 2009001128.

35. Cyanocyclopropylcarboxamides as cathepsin inhibitors and their preparation and use in the treatment of diseases. Crawford, James John; Dossetter, Alexander Graham; Finlayson, Jonathan Erle; Heron, Nicola Murdoch. PCT Int. Appl. (2008), WO 2009001127.

34. Preparation of amide-indoles as antagonists of gonadotropin releasing hormone (GnRH).      Wardleworth, James Michael; Dossetter, Alexander Graham; Halsall, Christopher Thomas.  (Astrazeneca AB, Swed.; Astrazeneca UK Limited).    PCT Int. Appl. (2002), 61 pp.  WO 2002092565  

33. Preparation of 6H-thieno[2,3-b]pyrrole derivatives as antagonists of gonadotropin-releasing hormone (GnRh) for treating sex hormone related conditions.      Foote, Kevin Michael; Matusiak, Zbigniew; Dossetter, Alexander Graham; Arnould, Jean Claude; Lamorlette, Maryannick Andree; Delouvrie, Benedicte; Hamon, Annie.  (AstraZeneca AB, Swed.; AstraZeneca UK Limited).    PCT Int. Appl.  (2004),     215 pp.   WO2004018480  A1 

32. Amine derivatives of imidazo[1,2-a]pyridine useful as antagonists of gonadotropin releasing hormone.      Dossetter, Alexander Graham; Kenny, Peter; McKerrecher, Darren; Wardleworth, Michael.  (Astrazeneca AB, Swed.; Astrazeneca UK Limited).    PCT Int. Appl. (2002), WO2002066478

31. Preparation of substituted imidazopyridines for antagonizing gonadotropin releasing hormone activity.      Dossetter, Alexander Graham; Kenny, Peter; McKerrecher, Darren; Wardleworth, Michael.  (Astrazeneca AB, Swed.; Astrazeneca UK Limited).    PCT Int. Appl. (2002), 98 pp. WO2002066477A2  

30. Preparation of cyanoguanidinoethylindoles GnRH antagonists.      Wardleworth, Michael; Dossetter, Alexander Graham; Halsall, Chris T.  (Astrazeneca AB, Swed.; Astrazeneca UK Limited).    PCT Int.Appl. (2002), 65 pp. WO2002066459  

29. Catalytic asymmetric cycloaddition reactions of dienes and aldehydes.      Jacobsen, Eric N.; Schaus, Scott E.; Dossetter, Alexander G.; Jamison, Timothy F.  (Harvard University, USA).    U.S.  (2001), 39 pp., US 6,130,340. 

28. Asymmetric cycloaddition reactions using transition metal chiral Schiff base complexes.      Jacobsen, Eric N.; Schaus, Scott E.; Dossetter, Alexander G.; Jamison, Timothy F.  WO 2000050365A1  

27. 4-Amino-7,8-Dihydropyrimido[5,4-F][1,4]Oxazepin-5(6h)-One Based Dgat1 Inhibitors Birch, A. M.; Goldberg, F. W.; Leach, A. WO 2011121350.

26. Adamantyl Iminocarbonyl-Substituted Pyrimidines As Inhibitors Of 11-Beta-HSD1  Bennett, S. N. L.; Goldberg, F. W.; Leach, A.; Whittamore, P. R. O.; Sörme, P. US20110092526.

25. Pyrazine Carboxamides As Inhibitors Of DGAT1 Birch, A. M.; Butlin, R. J.; Campbell, L.; Green, C.; Leach, A.; Murray, P. M.; Ryberg, P. O.; Waring, M. J. WO/2010/146395.

24. Substituted Pyrimidin-5-Carboxamides Gill, A. L.; Leach, A.; Packer, M.; Scott, J. S.; Sörme, P.; Swales, J. G.; Whittamore, P. R. O. WO/2009/130496.

23. Carbamoyl compounds as DGAT1 inhibitors. Bauer, U. A.; Birch, A. M.; Butlin, R. B.; Green, C.; Barlind, J. G.; Hovland, R.; Johannesson, P.; Leach, A.; Noeske, A. T.; Petersson, A. U. WO/2009/081195

22. Pyrrolo [2, 3 -d] pyrimidin derivatives as protein kinase B inhibitors. Johnson, P. D.; Leach, A; Luke, R. W. A.; Matusiak,  Z. S.; Morris, J. J. WO/2009/047/563.

21. Substituted piperidines having protein kinase inhibiting activity Woodhead, S. J.; Frederickson, M.; Hamlett, C.; Woodhead, A. J.; Verdonk, M. L.; Sore, H. F.; Walker, D. W.; Blurton, P.; Collins, I.; Cheung, K. M.; Caldwell, J.; Da Fonseca Mchardy, T. F.; Luke, R. W. A.; Matusiak, Z. S.; Leach, A.; Morris, J. J. WO/2008/075109.

20. Piperidine derivatives for the treatment of obesity Butlin, R. J.; Caulkett, P. W. R.; Leach, A.; Newcombe, N. J.; O’Donnell, C. J.; Wood, J. M. WO/2008/075077.

19. Piperidine derivatives for the treatment of obesity Butlin, R. J.; Caulkett, P. W. R.; Leach, A.; Newcombe, N. J.; O’Donnell, C. J.; Wood, J. M. WO/2008/075064.

18. Sulfonamide derivatives for therapeutic use as fatty acid synthase inhibitors Butlin, R. J.; Caulkett, P. W. R.; Johanesson, P.; Knerr, L. D.; Leach, A.; Newcombe, N. J.; O’Donnell, C. J.; Pointon, H.; Wood, J. M. WO/2008/075070.

17. Pyrimidine derivatives as EphB4 inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. Kettle, J. G.; Read, J.; Leach, A.; Barlaam, B. C.; Ducray, R.; Lambert-Van der Brampt, C. M. P. WO/2007/085833.

16. Preparation of acylamino dibenzothiophenes as DNA-PK inhibitors
Frigerio, Mark; Hummersone, Marc Geoffrey; Menear, Keith Allan; Finlay, Maurice Raymond Verschoyle; Griffen, Edward Jolyon; Ruston, Linette Lys; Morris, Jeffrey James; Ting, Attila Kuan Tsuei; Golding, Bernard Thomas; Griffin, Roger John; et al WO 2010136778 A1.

15. Preparation of 2-benzimidazolyl-6-morpholino-4-(piperidin-4-yl)pyrimidine derivatives as PI3K and mTOR inhibitors for treatment of proliferative disease
Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032072 A1.

14. Preparation of 2-benzimidazolyl-6-morpholino-4-heterocyclylpyrimidine derivatives as PI3K and mTOR inhibitors for treatment of proliferative disease
Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032028 A1.

13. Preparation of 2-benzimidazolyl-6-morpholino-4-phenylpyrimidine derivatives as PI3K and mTOR inhibitors for treatment of proliferative disease Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032086 A1.

12. Preparation of 4-benzimidazolyl-2-morpholino-6-piperazinyl-pyrimidine derivatives as PI3K and mTOR kinase inhibitors for the treatment of proliferative disorder Butterworth, Sam; Griffen, Edward Jolyon; Hill, George Beresford; Pass, Martin WO 2008032033 A1.

11. Preparation of 4-benzimidazolyl-2-morpholino-6-piperidinyl-4-pyrimidine derivatives as PI3K and mTOR kinase inhibitors for the treatment of proliferative disorder Butterworth, Sam; Griffen, Edward Jolyon; Hill, George Beresford; Pass, Martin WO 2008032089 A1.

10. Preparation of 4-benzimidazolyl-6-morpholino-2-piperazinyl-pyrimidine derivatives as PI3K and mTOR kinase inhibitors for the treatment of proliferative disorder Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin  WO 2008032060 A1.

9. Preparation of 4-benzimidazolyl-6-morpholino-2-piperidinyl-4-pyrimidine derivatives as PI3K and mTOR kinase inhibitors for the treatment of proliferative disorder Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032091 A1.

8. Preparation of 6-benzimidazolyl-2-morpholino-4-(azetidine, pyrrolidine, piperidine, or azepine) pyrimidine derivatives as PI3K and mTOR kinase inhibitors for the treatment of proliferative disorders Butterworth, Sam; Griffen, Edward Jolyon; Hill, George Beresford; Pass, Martin WO 2008032036 A1.

7. Preparation of pyrimidine derivatives for treating proliferative disorders sensitive to inhibition of PI3K and/or mTOR kinase. Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032077 A1.

6. Preparation of pyrimidine derivatives having inhibitory activity against PI3K enzymes Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin  WO 2008032064 A1.

5. Preparation of pyrimidine derivatives having inhibitory activity against PI3K enzymes Butterworth, Sam; Griffen, Edward Jolyon; Pass, Martin WO 2008032041 A1.

4. Pyrimidine derivatives as antiproliferative agents and their preparation, pharmaceutical compositions and use in the treatment of diseases  Butterworth, Sam; Griffen, Edward Jolyon; Hill, George Beresford; Pass, Martin WO 2008032027 A1.

3. Indole derivatives, processes for preparing them, pharmaceutical compositions containing them, and their use as inhibitors of PI3K and /or mTOR kinase  Foote, Kevin Michael; Griffen, Edward Jolyon WO 2007135398 A1.

2. Preparation of thiazole derivatives as antitumor agents Arnould, Jean-Claude; Foote, Kevin Michael; Griffen, Edward Jolyon WO 2007129044 A1.

1. Preparation of 5-heteroaryl thiazoles and their use as phosphoinositide 3-kinase (PI3K) inhibitors Bengtsson, Malena; Larsson, Joakim; Nikitidis, Grigorios; Storm, Peter; Bailey, John, Peter; Griffen, Edward, Jolyon; Arnould, Jean-Claude; Bird, Thomas, Geoffrey, Colerick WO 2006051270 A1.