Enhancing and Facilitating Drug Discovery

Dr. Stephen A Smith CSci CChem FRSC

Publications

Publications:

K.Biggadike, M.Ahmed, D.I.Ball, D.M.Coe, D.A.D.Wilk, C. D.Edwards, B.H.Gibbon, C.J.Hardy, S. A.Hermitage, J.O.Hessey, A.E.Hillegas, S.C.Hughes, L.Lazarides, X.Q.Lewell, A.Lucas, D.N.Mallett, M.A.Price, F.M.Priest, D.J.Quint, P.Shah, A.Sitaram, S.A.Smith, R.Stocker, N.A.Trivedi, D.C.Tsitoura, V.Weller. Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma. J. Med. Chem. 2016, 59, 1711-1726.

K.Biggadike, A.C.Champigny, D.M.Coe, D.T.Tape, S.A.Smith. Pyrrolo[3,2]pyrimidine derivatives as inducers of human interferon. PCT Int. Appl. WO 2015124591, published (27/08/15).

D.M.Coe, S.A.Smith. Novel Compounds. PCT Int. Appl. WO2014081645, published (30/05/14).

D.M.Coe, S.A.Smith. Novel Compounds. PCT Int. Appl. WO2014081644, published (30/05/14).

D.M.Coe, S.A.Smith. Novel Compounds. PCT Int. Appl. WO2014081643, published (30/05/14).

B. Ellinger, J.Silber, A.Prashari, J.Landskron, J.Weber, S.Rehermann, F.-J.Müller, S.Smith, S.Wrigley, K.Taskén, P.Gribbon, A.Labes,J.F.Imhoff. A Phenotypic Screening Approach to Identify Anticancer Compounds Derived from Marine Fungi. ASSAY and Drug Development Technologies. 2014, 12(3): 162-175. doi:10.1089/adt.2013.564.

D.M.Coe, S.A.Smith. Novel Compounds. PCT Int. Appl. WO2014031815, published (27/02/14).

S.C.Rosenkranz, M.Geissen, K.Härter, B.Szalay, I.Ferrer, J.Vogel, S.Smith, M.Glatzel (2013). Amyloid-Precursor-Protein-Lowering Small Molecules for Disease Modifying Therapy of Alzheimer's Disease: PLoS ONE 8(12): e82255. doi:10.1371/journal.pone.0082255.

H.Bazin-Lee, D.M.Coe, L.Lazarides, C.J.Mitchell, S.A.Smith, N.Trivedi. Novel Adenine Derivatives. PCT Int. Appl. WO2010018134, published (18/02/10).

K.Biggadike, D.M.Coe, X.Q.Lewell, C.J.Mitchell, S.A.Smith, N.Trivedi. Purine Derivatives for use in the treatment of Allergic, Inflammatory and Infectious Diseases. PCT Int. Appl. WO2010018133, published (18/02/10).

S.A.Campos, D.M.Coe, S.A.Smith, N.Trivedi. Compounds. PCT Int. Appl. WO2010018132, published (18/02/10).

L.Lazarides, S.A.Smith, R.Stocker, C.J.Theobald. Purine derivatives as Immunomodulators. PCT Int. Appl. WO2008101867, published (28/08/08).

L.C.Pattenden, H.Adams, S.A.Smith, J.P.A.Harrity. Development of a [3+3] approach to tetrahydropyridines and its application in indolizidine alkaloid synthesis. Tetrahedron 2008, 64, 2951-2961.

D.Haigh, E.Amphlett, G.S. Bravi, H.Bright, V.Chung, C.L.Chambers, A.G.Cheasty, M.A.Convery, M.R.Ellis, R.Fenwick, D.F.Gray, C.D.Hartley, P.D.Howes, R.L.Jarvest, K.J.Medhurst, A.Mehbob, D.Mesogiti, F.Mirzai, F.Nerozzi, N.R.Parry, N.Roughley, T.Skarzynski, M.J.Slater, S.A.Smith, R.Stocker, C.J.Theobald, P.J.Thomas, P.A.Thommes, J.H.Thorpe, C.S.Wilkinson, E.Williams. Structure-based design of GSK625433: A novel clinical candidate for treatment of HCV. Oral presentation to Virus Molecular Interactions: Therapeutic Targets, Oxford, 17-19th September 2007.

P.A.Thommes, E.A.Amphlett, G.S.Bravi, H.Bright, V.Chung, L.Chambers, A.G.Cheasty, M.A.Convery, M.R.Ellis, R.H.Fenwick, D.F.Gray, D.Haigh, D.C.Hartley, P.D.Howes, R.L.Jarvest, D.M.Mesogiti, F.Mirzai, F.Nerozzi, N.R.Parry, M.J.Slater, S.Smith, R.V.Stocker, C.J.Theobald, C.S.Wilkinson, E.Williams. GSK625433: a Novel and Highly Potent Inhibitor of the HCV NS5B RNA polymerase. Oral presentation to the 14th International Symposium on Hepatitis C Virus and Related Viruses, Glasgow, 9-13th September 2007.

F.Nerozzi, G.Bravi, C.L.Chambers, M.A.Convery, M.C.Crowe, D.Haigh, C.D.Hartley, P.D.Howes, R.L.Jarvest, L.Lazarides, K.J.Medhurst, S.A.Smith, T.Skarzynski, R.Stocker, C.J.Theobald, N.R.Parry, P.A.Thommes. Acyl Pyrrolidines: A Series of Genotypes 1a and 1b NS5b Polymerase Inhibitors. Poster presentation to the International Symposium on Advances in Synthetic and Medicinal Chemistry, St Petersburg, Russia, 27-31st August, 2007.

S.A.Smith. Clinical Candidate SB-480848, Identification of a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation at RSC Med Chem School, University of Nottingham, 25-29th June 2007.

D.Haigh, C.D.Hartley, P.D.Howes, L.Lazarides, F.Nerozzi, S.A.Smith. C(2)-Heteroarylmethyl-C(4)-pyrazinyl-2-yl acyl pyrrolidine compounds and their use for treating viral infections, especially Hepatitis C Virus. PCT Int. Appl. WO2007039145, published (12/04/07).

D.Haigh, C.D.Hartley, P.D.Howes, R.L.Jarvest, L.Lazarides, F.Nerozzi, S.A.Smith. Pyrrolidine derivatives for treating viral infections. PCT Int. Appl. WO2007039144, published (12/04/07).

D.Haigh, C.D.Hartley, P.D.Howes, L.Lazarides, F.Nerozzi, S.A.Smith. C(2)-Heteroarylmethyl-C(4)-pyrazin-2-yl acyl pyrrolidine compounds and their use for treating viral infections, especially Hepatitis C (HCV). PCT Int. Appl. WO2007039143, published (12/04/07).

D.Haigh, C.D.Hartley, P.D.Howes, R.L.Jarvest, L.Lazarides, F.Nerozzi, S.A.Smith. C(2)-Heteroarylmethyl-C(4)-methoxymethyl acyl pyrrolidine compounds and their use for treating viral infections, especially Hepatitis C Virus. PCT Int. Appl. WO2007039142, published (12/04/07).

F.Gray, L.Amphlett, H.Bright, L.Chambers, A.Cheasty, R.Fenwick, D.Haigh, D.Hartley, P.Howes, R.Jarvest, F.Mirzai, F.Nerozzi, N.Parry, M.Slater, S.Smith, P.Thommes, C.Wilkinson, E.Williams. GSK625433: A Novel and Highly Potent Inhibitor of the HCV NS5B Polymerase. Journal of Hepatology, 2007, 46, S225.

D.Haigh, E.Amphlett, G.S. Bravi, H.Bright, V.Chung, C.L.Chambers, A.G.Cheasty, M.A.Convery, M.R.Ellis, R.Fenwick, D.F.Gray, C.D.Hartley, P.D.Howes, R.L.Jarvest, K.J.Medhurst, A.Mehbob, D.Mesogiti, F.Mirzai, F.Nerozzi, N.R.Parry, N.Roughley, T.Skarzynski, M.J.Slater, S.A.Smith, R.Stocker, C.J.Theobald, P.J.Thomas, P.A.Thommes, J.H.Thorpe, C.S.Wilkinson, E.Williams. Identification of GSK625433: A novel clinical candidate for the treatment of hepatitis C. Abstracts of Papers, 233rd ACS National Meeting, Chicago, IL, United States, 25-29th March 2007.

L.C.Pattenden, J.P.A.Harrity, S.A.Smith. Investigation of New [3+3] Annelation Reactions. Poster presentation to Pfizer poster competition, London, 5th December 2006.

S.A.Smith. Clinical Candidate SB-480848, Identification of a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation at University of Hull, 25th October 2006.

D.Haigh, C.Wilkinson, H.Bright, V.Chung, D.Mesogiti, M.Ellis, E.Williams, T.Zurcher, N.Parry, F.Gray, S.Bains, T.Skarzynski, G.Bravi, O.Singh, P.Thomas, P.Howes, S.Smith, P.Thommes. Genotype Profiles of the Acylpyrrolidine Series of Potent HCV Polymerase Inhibitors. Poster presentation to 13th International Meeting on Hepatitis C Virus and Related Viruses, Cairns, Australia, 27-31 August 2006.

F.Nerozzi, C.L.Chambers, M.C.Crowe, D.Haigh, C.D.Hartley, P.D.Howes, R.L.Jarvest, S.A.Smith, R.Stocker, C.J.Theobald, N.R.Parry, P.A.Thommes. Conformationally Constrained Acyl Pyrrolidines as Sub-Micromolar HCV NS5B Polymerase inhibitors. Poster presentation to Medicinal Chemistry Gordon Conference, New London, USA, 6-11th August 2006.

L.C.Pattenden, R.A.J.Wybrow, S.A.Smith, J.P.A.Harrity. A [3+3] annulation approach to tetrahydropyridines. Org. Lett. 2006, 8, 3089-3091.

R.Guidetti, D.Haigh, C.D.Hartley, P.D.Howes, F. Nerozzi, S.A.Smith. Preparation of 4-(methoxycarbonyl)pyrrolidine-2-carboxylic acid derivatives as hepatitis C virus inhibitors. Pat. Appl. WO2006/045613, published (04/05/06).

R.Guidetti, D.Haigh, C.D.Hartley, P.D.Howes, F. Nerozzi, S.A.Smith. Preparation of 4-(pyrazin-2-yl)pyrrolidine-2-carboxylic acid derivatives as hepatitis C virus inhibitors. Pat. Appl. WO2006/045615, published (04/05/06).

S.A.Smith. Identification of Clinical Candidate SB-480848, a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation at University of Sheffield, 1st November 2005.

S.A.Smith. Identification of Clinical Candidate SB-480848, a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation at University College London, 15th December 2004.

A.E.Fenwick, D.M.B.Hickey, R.J.Ife, C.A.Leach, I.L.Pinto, S.A.Smith Pyrimidinone compounds. EP Div. Pat. Appl. 04077397.0, published as EP1479671 (24/11/04).

A.D.Borthwick, C.Chan, H.A.Kelly, S.Peace, S.Senger, G.P.Shah, S.A.Smith, S.Smith, N.S.Watson, R.I.West, R.J.Young. Pyrrolydin-2-one derivatives as inhibitors of Thrombin and Factor Xa. Pat. Appl. WO 2004052851, published (24/06/04).

G.L.Young, S.A.Smith, R.J.K.Taylor. 4-Bromomethyl-2-chlorooxazole - a versatile oxazole cross-coupling unit for the synthesis of 2,4-disubstituted oxazoles. Tetrahedron Lett. 2004, 45, 3797-3801.

G.L.Young, R.J.K.Taylor, S.A.Smith. Development of a Versatile Oxazole Cross Coupling Fragment for the Synthesis of 2,4-Disubstituted Oxazoles - Towards the Synthesis of Ajudazol A. Poster presentation to the Pfizer Poster Competition, London, 11th December 2003.

S.A.Smith. Identification of Clinical Candidate SB-480848, a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation at Kingston University, 26th November 2003.

C.A.Leach, S.A.Smith. Novel compounds. Pat. Appl. WO 2003087088, published (23/10/03).

C.A.Leach, S.A.Smith. N-Substituted pyridinone and pyrimidinone derivatives for use as Lp-PLA2 inhibitors in the treatment of artherosclerosis. Pat. Appl. WO 2003086400, published (23/10/03).

G.L.Young, S.A.Smith, R.J.K.Taylor. Stille Coupling Approaches towards Ajudazol A. Poster presentation to the Komppa Centenary Symposium, Espoo, Finland, 6-10th July 2003.

S.A.Smith. The Important Role of Developability Criteria in the Identification of SB-480848: A Potent, Orally Active Inhibitor of Lipoprotein-Associated Phospholipase A2. Oral presentation to Intelligent Drug Discovery and Development 2003 (organised by Cambridge Healthtech Institute), Philadelphia, USA, 28-30 May 2003.

C.A.Leach, I.L.Pinto, S.A.Smith, S.J.Stanway. Novel compounds. Pat. Appl. WO 0342218,published (22/05/03).

C.A.Leach, S.A.Smith. Pyridinone and pyrimidinone compounds. Pat. Appl. WO 0342206, published (22/05/03).

R.L.Elliott, D.M.B.Hickey, R.J.Ife, C.A.Leach, J.Liddle, I.L.Pinto, S.J.Stanway, S.A.Smith. Heterocyclic derivatives of glycinamide and their medical use. Pat. Appl. WO 0342179, published (22/05/03).

S.C.M.Fell, D.M.B.Hickey, C.A.Leach, J.Liddle, I.L.Pinto, S.A.Smith. Pyridone, pyridazone and triazone derivatives as Lp-PLA2 inhibitors. Pat. Appl. WO 0341712, published (22/05/03).

S.A.Smith. The Discovery of SB-480848, a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis. Oral presentation to XIVth Symposium on Medicinal Chemistry in Eastern England, Hatfield, 10th April 2003.

J.A.Blackie, J.C.Bloomer, M.J.B.Brown, H-Y.Cheng, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, S.A.Smith, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald. The Identification of Clinical Candidate SB-480848: A Potent Inhibitor of Lipoprotein-Associated Phospholipase A2. Bioorg. Med. Chem. Lett. 2003, 13, 1067-1070.

R.L.Elliott, C.A.Leach, S.A.Smith. 2,5-Substituted 1-(aminocarbonylalkyl)-pyrimidin-4-one derivatives with Lp-PLA2 inhibitory activity for the treatment of atherosclerosis. Pat. Appl. WO 0315786, published (27/02/03).

A.Lewis, I.Stefanuti, S.A.Swain, S.A.Smith, R.J.K.Taylor A formal total synthesis of (+)-apicularen A: base-induced conversion of apicularen-derived intermediates into salicylihalamide-like products. Org. Biomol. Chem. 2003, 1, 104-116.

S.A.Smith. Identification of Clinical Candidate SB-435495, a Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for the Treatment of Atherosclerosis: Rationale, Leads, Chemistry and Optimisation. Oral presentation at the University of York 5th December 2002.

J.A.Blackie, J.C.Bloomer, M.J.B.Brown, H-Y.Cheng, R.L.Elliott, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, S.A.Smith, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker. The Discovery of SB-435495: A Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for Evaluation in Man. Bioorg. Med. Chem. Lett. 2002, 12, 2603-2606.

S.A.Smith, J.A.Blackie, J.C.Bloomer, M.J.B.Brown, H-Y.Cheng, R.L.Elliott, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker. Importance of Developability Criteria in the Discovery of Clinical Candidate SB-435495: A Potent, Orally Active Inhibitor of Lipoprotein-Associated Phospholipase A2. Poster presentation to Division of Medicinal Chemistry, 224th ACS National Meeting, Boston, USA, 18-22nd August 2002.

S.A.Smith, J.A.Blackie, J.C.Bloomer, M.J.B.Brown, H-Y.Cheng, R.L.Elliott, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker. Importance of Developability Criteria in the Discovery of Clinical Candidate SB-435495: A Potent, Orally Active Inhibitor of Lipoprotein-Associated Phospholipase A2. Poster presentation to Sci-Mix session, 224th ACS National Meeting, Boston, USA, 18-22nd August 2002.

S.A.Smith. Key Role of Developability Criteria in the Discovery of SB-435495: A Potent Inhibitor of Lipoprotein-Associated Phospholipase A2 for Evaluation in Man. Oral presentation to Division of Medicinal Chemistry, 224th ACS National Meeting, Boston, USA, 18-22nd August 2002.

G.A.Young, R.J.K.Taylor, S.A.Smith Transition-Metal Catalysed Approaches towards The Lobatamides - Novel Marine Cytotoxic Macrolides. Poster presentation to the 3rd International Meeting on Drugs from Natural Products, Dublin, 14-16th July 2002.

S.A.Smith. Inhibition of Lipoprotein-Associated Phospholipase A2: A New Target for the Treatment of Atherosclerosis. Oral presentation at the XXIIth Advanced Course in Medicinal Chemistry, Urbino Italy, 1-5th July 2002.

R.L.Elliott, D.M.B.Hickey, R.J.Ife, C.A.Leach, I.L.Pinto, S.A.Smith Pyrimidinone derivatives and their use in the treatment of atherosclerosis. Pat. Appl. WO 0230911, published (18/04/02).

D.M.B.Hickey, R.J.Ife, C.A.Leach, J.Liddle, I.L.Pinto, S.A.Smith, S.J.Stanway Pyridinone derivatives for the treatment of atherosclerosis. Pat. Appl. WO 0230904, published (18/04/02).

S.A.Smith, J.A.Blackie, J.C.Bloomer, M.J.B.Brown, H-Y.Cheng, R.L.Elliott, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker. The Importance of Developability Criteria in the Discovery of SB-435495: A Potent, Orally Active Inhibitor of Lipoprotein-Associated Phospholipase A2 for Evaluation in Man. Poster presentation to XIIIth Symposium on Medicinal Chemistry in Eastern England, Hatfield, 18th April 2002.

H.F.Boyd, S.C.M.Fell, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, I.L.Pinto, D.A.Rawlings, S.A.Smith, I.G.Stansfield, S.J.Stanway, C.J.Theobald, C.M.Whittaker. Potent, orally active inhibitors of lipoprotein-associated phospholipase A2: 1-(Biphenylmethylamidoalkyl)-pyrimidones. Bioorg. Med. Chem. Lett. 2002, 12, 51-55.

S.A.Smith, J.C.Bloomer, H.F.Boyd, R.L.Elliott, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, I.L.Pinto, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker. 1-(Pyridyl- and pyrimidyl-methylacetamido)-pyrimidones: potent inhibitors of lipoprotein-associated phospholipase A2. Poster presentation to 11th RSC-SCI Medicinal Chemistry Symposium, Cambridge, 9-12th September 2001.

S.A.Smith. Inhibition of lipoprotein-associated phospholipase A2 - a novel approach for the treatment of atherosclerosis. Oral presentation to 11th RSC-SCI Medicinal Chemistry Symposium, Cambridge, 9-12th September 2001.

D.M.B.Hickey, R.J.Ife, C.A.Leach, I.L.Pinto, S.A.Smith, S.J.Stanway Pyrimidine-4-one derivatives as LDL-PLA2 inhibitors. Pat. Appl. WO 0160805, published (23/08/01).

A.Lewis, I.Stefanuti, S.A.Swain, S.A.Smith, R.J.K.Taylor Carbohydrate-based routes to salicylate natural products: formal total synthesis of (+)-apicularen A from D-glucal. Tetrahedron Lett. 2001, 42, 5549-5552.

J.C.Bloomer, H.F.Boyd, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, I.L.Pinto, D.A.Rawlings, S.A.Smith, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker 1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A2. Bioorg. Med. Chem. Lett. 2001, 11, 1925-1929.

S.A.Smith, J.C.Bloomer, H.F.Boyd, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, I.L.Pinto, D.A.Rawlings, I.G.Stansfield, S.J.Stanway, M.A.Taylor, C.J.Theobald, C.M.Whittaker 1-(Arylpiperazinylamidoalkyl)-pyrimidones: Orally Active Inhibitors of Lipoprotein-Associated Phospholipase A2. Poster presentation to XIIth Symposium on Medicinal Chemistry in Eastern England, Hatfield, 26th April 2001.

S.A.Smith, H.F.Boyd, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, I.G.Stansfield, C.J.Theobald Lipoprotein-Associated Phospholipase A2: The Discovery of a Potent, Water Soluble Inhibitor. Poster presentation to XIIth Symposium on Medicinal Chemistry in Eastern England, Hatfield, 26th April 2001.

C.A.Leach, D.M.B.Hickey, R.J.Ife, C.H.Macphee, S.A.Smith, D.G.Tew Lipoprotein-Associated PLA2 inhibition - a novel, non-lipid lowering strategy for atherosclerosis therapy. Il Farmaco 2001, 56, 45-50.

H.F.Boyd, B.Hammond, D.M.B.Hickey, R.J.Ife, C.A.Leach, V.A.Lewis, C.H.Macphee, K.J.Milliner, I.L.Pinto, S.A.Smith, I.G.Stansfield, C.J.Theobald, C.M.Whittaker The Identification of a Potent, Water Soluble Inhibitor of Lipoprotein-Associated Phospholipase A2. Bioorg. Med. Chem. Lett. 2001, 11, 701-704.

I.Stefanuti, A.Lewis, R.J.K.Taylor, S.A.Smith Synthesis of Enamide Containing Natural Products; Towards a Total Synthesis of Apicularen A. Poster presentation to 1st Binational RSC/SACI International Conference of Organic Chemistry, Cape Town, South Africa, 7-11th January 2001.

H.F.Boyd, S.C.M.Fell, S.T.Flynn, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, R.A.Porter, D.A.Rawlings, S.A.Smith, I.G.Stansfield, D.G.Tew, C.J.Theobald, C.M.Whittaker N-1 Substituted Pyrimidin-4-ones: Novel, Orally Active Inhibitors of Lipoprotein-Associated Phospholipase A2. Bioorg. Med. Chem. Lett. 2000, 10, 2557-2561.

A.E.Fenwick, D.M.B.Hickey, R.J.Ife, C.A.Leach, S.A.Smith Pyrimidinone derivatives for the treatment of atherosclerosis. Pat. Appl. WO 0068208, published(16/11/00).

A.E.Fenwick, D.M.B.Hickey, R.J.Ife, C.A.Leach, I.L.Pinto, S.A.Smith Pyrimidinone compounds. Pat. Appl. WO 0066567, published (09/11/00).

D.M.B.Hickey, R.J.Ife, C.A.Leach, S.A.Smith Pyrimidine compounds. Pat. Appl. WO 0066566, published (09/11/00).

S.A.Smith, H.F.Boyd, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, I.G.Stansfield, C.J.Theobald The Identification of a Potent, Water Soluble Inhibitor of Lipoprotein-Associated Phospholipase A2. Poster presentation to XVIth International Symposium on Medicinal Chemistry, Bologna, Italy, 18th - 22nd September 2000.

S.A.Smith, H.F.Boyd, S.C.M.Fell, S.T.Flynn, D.M.B.Hickey, R.J.Ife, C.A.Leach, C.H.Macphee, K.J.Milliner, K.E.Moores, I.L.Pinto, R.A.Porter, D.A.Rawlings, I.G.Stansfield, D.G.Tew, C.J.Theobald, C.M.Whittaker N-1 Substituted Pyrimidin-4-ones: Novel, Orally Active Inhibitors of Lipoprotein-Associated Phospholipase A2. Poster presentation to XVIth International Symposium on Medicinal Chemistry, Bologna, Italy, 18th - 22nd September 2000.

I.Stefanuti, S.A..Smith, R.J.K.Taylor Unsaturated enamides via organometallic addition to isocyanates: the synthesis of Lansamide-I, Lansiumamides A-C and SB-204900. Tetrahedron Lett. 2000, 41, 3735-3738.

S.A.Smith, C.A.Leach Pyrimidone derivatives for the treatment of atherosclerosis. Pat. Appl. WO 0010980, published (02/03/00).

H.F.Boyd, S.T.Flynn, D.M.B.Hickey, R.J.Ife, M.Jones, C.A.Leach, C.H.Macphee, K.J.Milliner, D.A.Rawlings, B.P.Slingsby, S.A.Smith, I.G.Stansfield, D.G.Tew, C.J.Theobald 2-(Alkylthio)pyrimidin-4-ones as Novel, Reversible Inhibitors of Lipoprotein-Associated Phospholipase A2. Bioorg. Med. Chem. Lett. 2000, 10, 395-398.

C.A.Leach, S.A.Smith, H.F.Boyd, S.T.Flynn, D.M.B.Hickey, R.J.Ife, M.Jones, C.H.Macphee, K.J.Milliner, D.A.Rawlings, B.P.Slingsby, I.G.Stansfield, D.G.Tew, C.J.Theobald 2-(Alkylthio)pyrimidin-4-ones as Novel, Reversible Inhibitors of Lipoprotein-Associated Phospholipase A2. Poster presentation to the 10th RSC/SCI Medicinal Chemistry Symposium Cambridge, 5-8th September 1999.

D.M.B.Hickey, R.J.Ife, C.A.Leach, R.A.Porter, S.A.Smith New pyrimidone derivatives are Lp-PLA2 inhibitors. Pat. Appl. WO9924420, published (20/05/99).

N.E.Austin, K.Y.Avenell, I.Boyfield, C.L.Branch, M.C.Coldwell, M.S.Hadley, P.Jeffrey, A.Johns, C.N.Johnson, D.J.Nash, G.J.Riley, S.A.Smith, R.Stacey, G.Stemp, K.M. Thewlis, A.K.K.Vong Novel 1,2,3,4-Tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 Receptor. Bioorg. Med. Chem. Lett. 1999, 9, 179-184.

K.Avenell, I.Boyfield, M.C.Coldwell, M.S.Hadley, M.A.M.Healy, P.Jeffrey, C.N.Johnson, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, R.Stacey, G.Stemp, K.M. Thewlis Fused Aminotetralins: Novel Antagonists with high selectivity for the Dopamine D3 Receptor. Bioorg. Med. Chem. Lett. 1998, 8, 2859-2864.

G.Stemp, N.E.Austin, K.Avenell, I.Boyfield, C.L.Branch, M.C.Coldwell, M.S.Hadley, P.Jeffrey, A.Johns, C.N.Johnson, D.J.Nash, G.J.Riley, S.A.Smith, K.M. Thewlis, Antonio K.K.Vong Novel 1,2,3,4-Tetrahydroisoquinolines with high affinity and selectivity for the Dopamine D3 receptor. Poster presentation to XVth International Symposium on Medicinal Chemistry, Edinburgh, Scotland 6th - 10th September 1998.

K.Avenell, I.Boyfield, M.C.Coldwell, M.S.Hadley, M.A.M.Healy, P.Jeffrey, C.N.Johnson, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, R.Stacey, G.Stemp, K.M. Thewlis Fused Aminotetralins: Novel Antagonists with high selectivity for the Dopamine D3 Receptor. Poster presentation to XVth International Symposium on Medicinal Chemistry, Edinburgh, Scotland 6th - 10th September 1998.

G.Stemp, C.N.Johnson, S.A.Smith, P.Jeffrey New tricyclic amine derivatives are Dopamine D3 modulators. Pat. Appl. WO9747602, published (18/12/97).

D.Bolton, I.Boyfield, M.C.Coldwell, M.S.Hadley, A.Johns, C.N.Johnson, R.E.Markwell, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, G.Stemp, H.J.Wadsworth, E.A.Watts 2-[(Substituted)phenyl] -[1-(2-phenylazacycloheptyl)methyl]-1H-Pyrroles with High Affinity and Selectivity for the Dopamine D3 receptor. Bioorg. Med. Chem. Lett. 1997, 7(4), 485-488.

I.Boyfield, M.C.Coldwell, M.S.Hadley, M.A.M.Healy, C.N.Johnson, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, G.Stemp Novel 2,5-disubstituted-1H-pyrroles with High Activity for the Dopamine D3 receptor: N-Benzyl modifications. Bioorg. Med. Chem. Lett. 1997, 7(3), 327-330.

I.Boyfield, M.C.Coldwell, M.S.Hadley, M.A.M.Healy, A.Johns, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, G.Stemp, K.Wilson N- (Substituted-Phenyl)Piperazines: Antagonists with High Binding and Functional Selectivity for Dopamine D4 Receptors. Bioorg. Med. Chem. Lett. 1996, 6(11), 1227-1232.

I.Boyfield, T.H.Brown, M.C.Coldwell, D.C.Cooper, M.S.Hadley, M.A.Healy, A.Johns, R.J.King, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, G.Stemp Methoxynaphthalene Derivatives: Antagonists with High Selectivity for the Dopamine D4 receptor. Poster presentation to XIVth International Symposium on Medicinal Chemistry, Maastricht The Netherlands 8th - 12th September 1996.

G.-J.Boons, R.Eveson, S.Smith A Critical Evaluation of Cationic C-Glycosylations with 4-Acetoxy-1,3-Dioxanes. Poster presentation to Organic Synthesis (ICOS-11) Meeting, Amsterdam The Netherlands, 30th June - 4th July 1996.

G.-J.Boons, R.Eveson, S.Smith, T.Stauch A Critical Evaluation of the Cationic Coupling of 4-Acetoxy-1,3-Dioxanes. Synlett. 1996, 536-538.

I.Boyfield, T.H.Brown, M.C.Coldwell, D.C.Cooper, M.S.Hadley, J.J.Hagan, M.A.Healy, A.Johns, R.J.King, D.N.Middlemiss, D.J.Nash, G.J.Riley, E.E.Scott, S.A.Smith, G.Stemp Design and Synthesis of 2-Naphthoate Esters as Selective Dopamine D4 Antagonists. J. Med. Chem. 1996, 39(10), 1946-1948.

M.A.M.Healy, S.A.Smith, G.Stemp A Convenient Preparation of 3-Aza-2-Phenyl Bicyclo[3.2.2] Nonane and Related 2-Substituted Cyclic Amines. Syn. Commun. 1995, 25(23), 3789-3797.

S.A.Smith, B.Beszant, J.Bird, G.P.Harper, I.Hughes, E.H.Karran, R.E.Markwell, A.J.Miles-Williams, C.O.Ugwuegbulam Novel Low Molecular Weight Inhibitors of Human Collagenase: b-Mercapto-Carbonyl and Thiophenol Derivatives. Poster presentation to the 8th RSC/SCI Medicinal Chemistry Symposium Cambridge, 10-13th September 1995.

B.Beszant, J.Bird, L.M.Gaster, G.P.Harper, I.Hughes, E.H.Karran, A. Miles-Williams, R.E.Markwell, S.A.Smith Novel Modified Dipeptide Inhibitors of Human Collagenase: b-Mercapto-Carbonyl and Thiophenol Derivatives. Poster presentation to meeting on Biological Challenges for Organic Chemistry, St Andrews, 10-13th July 1995.

D.J.Hunter, R.E.Markwell, S.A.Smith, P.A.Wyman The Reaction of 1-Aryl and 1-Pyridyl- 1,2,3,4-tetrahydroisoquinol-3-ones with Dimethylcarbamoyl Chloride: The Preparation of Amidines, Isoquinolines and N-carbamoylated Products. J. Chem. Soc., Perkin Trans 1 1994, 2585-2590.

S.A.Smith, K.A.Al-Barazanji, R.E.Buckingham, F.Cassidy, M.C.Coldwell, F.J.L.Finney, M.S.Hadley, P.Ham, S.A.Lawrence, D.J.Nash, E.J.R.Tingley, J.M.Watson The Identification of a Novel Renin Inhibitor of Equivalent Efficacy following Oral or Intravenous Administration. Bioorg. Med. Chem. Lett. 1994, 4(11), 1291-1296.

B.Beszant, J.Bird, L.M.Gaster, G.P.Harper, I.Hughes, E.H.Karran, R.E.Markwell, A.J.Miles-Williams, S.A.Smith Synthesis of Novel Modified Dipeptide Inhibitors of Human Collagenase: b-Mercapto Carboxylic Acid Derivatives. J. Med. Chem. 1993, 36, 4030-4039.

J.Bermudez, I.Hughes, F.R.Mangan, R.E.Markwell, S.A.Smith, M.J.Thomson, P.A.Wyman Synthesis and Anti-Arthritic Activity of a series of 1-Aryl-3-Dimethylamino-1,4-Dihydro-isoquinolines. Bioorg. Med. Chem. Lett. 1993, 3, 2571-2576.

S.A.Smith, K.A.Al -Barazanji, R.E.Buckingham, F.Cassidy, M.C.Coldwell, F.J.L.Cunningham, M.S.Hadley, P.Ham, S.A.Lawrence, D.J.Nash, E.J.R.Tingley, J.M.Watson The Identification of a Novel, Efficacious Renin Inhibitor with High apparent Oral Bioavailability. Poster presentation to the 7th RSC/SCI Medicinal Chemistry Symposium Cambridge, September 1993.

F.Cassidy, S.A.Smith, P.Ham, D.J.Nash Preparation of peptides as antihypertensives. GB Pat. Appl. 89/27872, published (9/6/91).

S.A.Smith, D.J.Nash, P.Ham Preparation of heterocyclyl phenylalanyl leucine - containing peptides as renin inhibitors. Eur. Pat. Appl. 416740, published (13/3/91).

S.A.Smith, P.Ham Preparation of renin-inhibiting heterocyclyl-containing peptides. Eur. Pat. Appl. 411751, published (6/2/91).

S.A.Smith, P.Ham Preparation of N-(heterocyclylacyl) peptides, containing 4(S)-amino-5-cyclohexyl-3(S)-hydroxypentanoic acid (ACHPA) amides as renin inhibitors. Eur. Pat. Appl. 375451, published (27/6/90).

S.A.Smith, P.Ham, D.J.Nash Renin inhibitory peptides containing 4(S)-amino-5-cyclohexyl-3(S)-hydroxypentanoic acid Eur. Pat. Appl. 350163, published (10/1/90).

R.E.Markwell, S.A.Smith, L.M.Gaster Preparation of N-(2-alkyl-3-mercapto-1,5-dioxoalkyl) glycinamides as collagenase inhibitors Eur. Pat. Appl. 322184, published (28/6/89).

R.E.Markwell, S.A.Smith, I.Hughes N-(2-Alkyl-3-mercaptoglutaryl) a-amino acid derivatives, processes for their preparation, and their use as collagenase inhibitors Eur. Pat. Appl. 273689, published (6/7/88).

D.R.Buckle, K.A.Foster, J.F.Taylor, J.M.Tedder, V.E.Thody, R.A.B.Webster, J.Bermudez, R.E.Markwell, S.A.Smith Novel 1H-benzimidazol-4-ols with Potent 5-lipoxygenase Inhibitory Activity. J. Med. Chem. 1987, 30(12), 2216-2221.

R.E.Markwell, S.A.Smith 2-(Fluoroalkyl)-benzimidazoles as inhibitors of 5-lipoxygenase. US pat 4,755,525, granted (5/7/88).

R.E.Markwell, S.A.Smith Dihydroisoquinoline derivatives. Pat. Appl. WO 86/06068, published (23/10/86).

D.J.Hunter, S.A.Smith, R.E.Markwell Dihydroisoquinoline derivatives. Eur. Pat. Appl. 183369, published (4/6/86).

R.E.Markwell, S.A.Smith Benzimidazoles. Eur. Pat. Appl. 178413, published (23/4/86).

E.A.Boyle, F.R.Mangan, R.E.Markwell, S.A.Smith, M.J.Thompson, R.W.Ward, P.A.Wyman 7-Aroyl-2,3-dihydrobenzo(b)furan-3-carboxylic acids and 7-benzoyl-2,3-dihydrobenzo(b)thiophene-3-carboxylic acids as Analgesic Agents. J. Med. Chem. 1986, 29(6), 894-898.

R.E.Markwell, S.A.Smith Dihydroisoquinoline derivatives. Eur. Pat. Appl. 139296, published (2/5/85).

R.W.Ward, S.A.Smith and R.E.Markwell Benzofuran- and benzothiophenecarboxylic acid derivatives. Eur. Pat. Appl. 117675, published (5/9/84).

A.F.Barnes, J.Bermudez, N.E.Bowring, F.Cassidy, S.A.Smith, M.Thompson. The effect of a-chain Terminal Modification on the Bronchodilator Activity of 8,10,12 -Triazaprostaglandin Analogues. Poster publication to the 1st RSC/SCI Medicinal Chemistry Symposium Cambridge September 1981.

G.W.Wootton, S.A.Smith. Imidazole derivatives and their pharmaceutical compositions. Eur. Pat. Appl. 20039, published (10/12/80).

R.C.Cookson, S.A.Smith. Synthesis of 2-hydroxy-3-methylcyclopent-2-enone from Methyl Acrylate. J. Chem. Soc. Perkin Trans 1 1979, 2447-2448.

R.C.Cookson, S.A.Smith Control of stereochemistry of cyclisation by orbital overlap: conversion of g,d-Unsaturated Aldehydes into Cyclopentanones. J. Chem. Soc., Chem Commun, 1979, 145-146.