1. Invited Presentations and Publications:
Phosphodiesterase Type 4 Inhibitors For The Treatment Of Asthma presented at:
Asthma Therapeutics, London, 20-21 March 2002
East Of England Medicinal Chemistry Meeting, Hatfield, April, 2002
28th National Medicinal Chemistry Symposium, San Diego, CA, USA, 8-12 June 2002
The BSI/BSACI Joint Congress 2002, Harrogate 3-6 December 2002
University of Sheffield, March 2003
Phosphodiesterases In Disease, Princeton, NJ, USA, 13-14 November 2003
RSC Medicinal Chemistry School, Nottingham, 2004
Several patent applications in preparation
Fused tricyclic imidazole derivativesas modulators of TNF activity and their preparation
Alexander, Rikki Peter; Brown, Julien Alistair; Deligny, Michael; Heer, Jag Paul; Jackson, Victoria
Elizabeth; Jadot, Sophie; Kroeplien, Boris; Mac Coss, Malcolm; Sabnis, Yogesh Anil; Swinnen,
Dominique Louis Leon; et al WO 2015086527
Imidazothiazole derivativesas modulators of TNF activity and their preparation
Alexander, Rikki Peter; Ali, Mezher Hussein; Brown, Julien Alistair; Jackson, Victoria Elizabeth
WO 2015086504
Fused tricyclic imidazole derivativesas modulators of TNF activity and their preparation
Alexander, Rikki Peter; Brace, Gareth Neil; Brown, Julien Alistair; Calmiano, Mark Daniel; Chovatia,
Praful Tulshi; Deligny, Michael; Gallimore, Ellen Olivia; Heer, Jag Paul; Jackson, Victoria Elizabeth;
Kroeplien, Boris; et al WO 2015086526
Fused bicyclic heteroaromatic derivatives as modulators of TNF activity and their preparation
Alexander, Rikki Peter; Foulkes, Gregory; Hutchings, Martin Clive; Jackson, Victoria Elizabeth;
Kroeplien, Boris; Reuberson, James Thomas; Rook, Sarah Margaret; Zhu, Zhaoning
WO 2015086523
Fused imidazole and pyrazole derivativesas modulators of TNF activity and their preparation
Alexander, Rikki Peter; Bentley, Jonathan Mark; Brace, Gareth Neil; Brookings, Daniel Christopher;
Chovatia, Praful Tulshi; Deboves, Herve Jean Claude; Johnstone, Craig; Jones, Elizabeth Pearl;
Kroeplien, Boris; Lecomte, Fabien Claude; et al WO 201508650
Fused tricyclic imidazole derivativesas modulators of TNF activity and their preparation
Alexander, Rikki Peter; Calmiano, Mark Daniel; Defays, Sabine; Durieu, Veronique; Deligny, Michael;
Heer, Jag Paul; Jackson, Victoria Elizabeth; Keyaerts, Jean; Kroeplien, Boris; Mac Coss, Malcolm; et
al WO 2015086525
Small Molecule Inhibitors of Bromodomain−Acetyl-lysine Interactions
Michael Brand, Angelina M. Measures, Brian G. Wilson, Wilian A. Cortopassi, Rikki Alexander,
Matthias Höss, David S. Hewings, Timothy P. C. Rooney, Robert S. Paton, and Stuart J. Conway
ACS Chem. Biol. (2015), 10, 22−39
Morpholine-thiophene derivatives as PI3 kinase inhibitors and their preparation,
pharmaceutical compositions and use in the treatment of diseases
Alexander, Rikki Peter; Bailey, Stuart; Brookings, Daniel Christopher; Brown, Julien Alistair;
Callaghan, Sacha; Pollard, Faye Charlotte WO 2010001126
Preparation of fused tricyclic thiazole and thiophene derivatives as PI3-kinase inhibitors
Alexander, Rikki Peter; Aujla, Pavandeep Singh; Brown, Julien Alistair; De Candole, Benjamin
Charles; Trevitt, Graham Peter WO 2009071890
4-(1,3-Thiazol-2-yl)morpholine derivatives as inhibitors of phosphoinositide 3-kinase
Alexander, Rikki; Balasundaram, Ahrani; Batchelor, Mark; Brookings, Daniel; Crepy, Karen; Crabbe,

2. Tom; Deltent, Marie-France; Driessens, Frank; Gill, Andrew; Harris, Sue; et al
Bioorganic & Medicinal Chemistry Letters (2008), 18(15), 4316-4320
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-
benzo[1,4]oxazines
Perry Benjamin; Alexander Rikki; Bennett Gavin; Buckley George; Ceska Tom; Crabbe Tom; Dale
Verity; Gowers Lewis; Horsley Helen; James Lynwen; et al
Bioorganic & medicinal chemistry letters (2008), 18(16), 4700-4
Fused thiazole derivatives as PI3 kinase inhibitors and their preparation, pharmaceutical
compositions and use in the treatment of diseases
Alexander, Rikki Peter; Aujla, Pavandeep Singh; Crepy, Karen Viviane Lucile; Foley, Anne Marie;
Franklin, Richard Jeremy; Haughan, Alan Findlay; Horsley, Helen Tracey; Jones, William Mark;
Lallemand, Benedicte Irma Leonce Frederique; Mack, Stephen Robert; et al WO 2008001076
Thiazole derivativesas PI3 kinase inhibitors and their preparation, pharmaceutical
compositions and use in the treatment of diseases
Alexander, Rikki Peter; Brown, Julien Alistair; Crepy, Karen Viviane Lucile; Mack, Stephen Robert
WO 2008047109 A1
Fused thiophene derivatives as kinase inhibitors and their preparation, pharmaceutical
compositions and use in the treatment of diseases
Alexander, Rikki Peter; Bailey, Stuart; Brand, Stephen; Brookings, Daniel Christopher; Brown, Julien
Alistair; Haughan, Alan Findlay; Kinsella, Natasha; Lowe, Christopher; Mack, Stephen Robert; Pitt,
William Ross; et al WO 2007141504
Preparation of morpholinobenzothiazoles and related compounds as phosphoinositide 3
kinase (PI3K) inhibitors. Alexander, Rikki Peter; Aujla, Pavandeep; Batchelor, Mark James;
Brookings, Daniel Christopher; Buckley, George Martin; Crepy, Karen Viviane Lucile; Kulisa, Claire
Louise; Turner, James Petrie. WO 2006114606
Preparation of thieno[2,3-b]pyridinone derivatives as kinase, especially p38 MAP kinase,
inhibitors useful in the treatment of and/or prevention of immune or inflammatory disorders.
Alexander, Rikki Peter; Davis, Jeremy Martin; Hutchings, Martin Clive; Laing, Victoria Elizabeth;
Trevitt, Graham Peter. WO 2005042540
Structure of an Allosteric Inhibitor of LFA-1 Bound to the I-Domain Studied by Crystallography,
NMR, and Calorimetry. Crump, Matthew P.; Ceska, Thomas A.; Spyracopoulos, Leo; Henry,
Alistair; Archibald, Sarah C.; Alexander, Rikki; Taylor, Richard J.; Findlow, Stuart C.; O'Connell,
James; Robinson, Martyn K.; Shock, Anthony. Biochemistry (2004), 43(9), 2394-2404.
The use of enantiomerically pure ketene dithioacetal bis(sulfoxides) in highly
diastereoselective intramolecular nitrone cycloadditions. Application in the total synthesis of
the  -amino acid (-)-cispentacin and the first asymmetric synthesis of cis-(3R,4R)-4-
aminopyrrolidine-3-carboxylic acid. Aggarwal, Varinder K.; Roseblade, Stephen; Alexander,
Rikki. Organic & Biomolecular Chemistry (2003), 1(4), 684-691.
CDP840. A prototype of a novel class of orally active anti-inflammatory phosphodiesterase 4
inhibitors. Alexander, R. P.; Warrellow, G. J.; Eaton, M. A. W.; Boyd, E. C.; Head, J. C.; Porter, J.
R.; Brown, J. A.; Reuberson, J. T.; Hutchinson, B.; Turner, P.; Boyce, B.; Barnes, D.; Mason, B.;
Cannell, A.; Taylor, R. J.; Zomaya, A.; Millican, A.; Leonard, J.; Morphy, R.; Wales, M.; Perry, M.;
Allen, R. A.; Gozzard, N.; Hughes, B.; Higgs, G. Bioorganic & Medicinal Chemistry Letters (2002),
12(11), 1451-1456.
Squaric acid derivatives as VLA-4 integrin antagonists. Porter, John R.; Archibald, Sarah C.;
Childs, Kirstie; Critchley, David; Head, John C.; Linsley, Janeen M.; Parton, Ted A. H.; Robinson,
Martyn K.; Shock, Anthony; Taylor, Richard J.; Warrellow, Graham J.; Alexander, Rikki P.; Langham,
Barry. Bioorganic & Medicinal Chemistry Letters (2002), 12(7), 1051-1054.
Highly Diastereoselective Nitrone Cycloaddition onto a Chiral Ketene Equivalent: Asymmetric

3. Synthesis of Cispentacin. Aggarwal, Varinder K.; Roseblade, Stephen J.; Barrell, Juliet K.;
Alexander, Rikki. Organic Letters (2002), 4(7), 1227-1229.
Preparation of squaric acid derivatives containing a bicyclic heteroaromatic ring as integrin
antagonists. Langham, Barry John; Alexander, Rikki Peter; Head, John Clifford; Linsley, Janeen
Marsha; Porter, John Robert; Archibald, Sarah Catherine; Warrellow, Graham John. WO
2002004426
Preparation of naphthyridine squaric acid derivatives as integrin inhibitors. Langham, Barry
John; Alexander, Rikki Peter; Head, John Clifford; Linsley, Janeen Marsha; Porter, John Robert;
Archibald, Sarah Catherine; Warrellow, Graham John. WO 2001092256
Investigation of the in vitro metabolism profile of a phosphodiesterase -IV inhibitor, CDP-840:
leading to structural optimization. Li C; Chauret N; Trimble L A; Nicoll-Griffith D A; Silva J M;
MacDonald D; Perrier H; Yergey J A; Parton T; Alexander R P; Warrellow G J. Drug metabolism and
disposition: the biological fate of chemicals (2001), 29(3), 232-41.
Preparation of squaric acid isoquinoline derivatives as integrin binding inhibitors. Langham,
Barry John; Alexander, Rikki Peter; Head, John Clifford; Linsley, Janeen Marsha; Porter, John Robert;
Archibald, Sarah Catherine; Warrelow, Graham John. WO2001092233
Preparation of enaminesfor inhibiting the binding of integrins to their ligands. Norman,
Timothy John; Porter, John Robert; Hutchinson, Brian Woodside; Ratcliffe, Andrew James; Head,
John Clifford; Alexander, Rikki Peter; Langham, Barry John; Warrellow, Graham John; Archibald,
Sarah Catherine; Linsley, Janeen Marsha. WO 2001079173
Preparation of squaric acid derivatives as integrin antagonists. Langham, Barry John;
Alexander, Rikki Peter; Head, John Clifford; Linsley, Janeen Marsha; Porter, John Robert; Archibald,
Sarah Catherine; Warrellow, Graham John. WO 2001047867
Preparation of pyridinylpropanoic acid derivatives as v3 and v5 integrin inhibitors.
Alexander, Rikki Peter; Langham, Barry John; Reuberson, James Thomas; Trown, Emma Louise;
Warrellow, Graham John. WO 2001044194
Preparation of squaric acid derivatives as cell adhesion molecules. Langham, Barry John;
Alexander, Rikki Peter; Head, John Clifford; Linsley, Janeen Marsha; Porter, John Robert; Archibald,
Sarah Catherine; Warrelow, Graham John. WO 2000073260
Diastereomerically pure spirocyclic bis-sulfinyl oxiranes and their application to the
asymmetric synthesis of  -amino amides. Aggarwal, Varinder K.; Barrell, Juliet K.; Worrall,
Julia M.; Alexander, Rikki. Phosphorus, Sulfur and Silicon and the Related Elements (1999), 153-
154 337-338
Preparation of propanoic acid derivatives as integrin inhibitors. Alexander, Rikki Peter;
Langham, Barry John; Reuberson, James Thomas; Trown, Emma Louise; Warrellow, Graham John.
WO 2000031067
Substituted oxime derivatives useful as PDE IV inhibitors. Head, John Clifford; Warrellow,
Graham John; Alexander, Rikki Peter. WO 9600215
Highly Diastereoselective Epoxidation of Ketene Dithioacetal Dioxides: A New Approach to the
Asymmetric Synthesis of  -Amino Amides. Aggarwal, Varinder K.; Barrell, Juliet K.; Worrall,
Julia M.; Alexander, Rikki. Journal of Organic Chemistry (1998), 63(21), 7128-7129.
Stereoselective epoxidation of bis-sulfinyl alkenesand application to the asymmetric
synthesis of  -substituted carboxylic acids. Aggarwal, Varinder K.; Worrall, Julia M.;
Alexander, Rikki. Phosphorus, Sulfur and Silicon and the Related Elements (1997), 120 & 121
351-352
Preparation of substituted arenesand heteroarenesas inhibitors of phosphodiesterase IV.

4. Warrellow, Graham J.; Boyd, Ewan C.; Alexander, Rikki P.; Head, John C. US 5622977
Direct measurement of the anomeric effect in sulfoxides: conformational analysis and X-ray
crystal structures of 2-bromo- and 2-chloro-1,3-dithiane trans-1,3-dioxides. Aggarwal,
Varinder K.; Worrall, Julia M.; Adams, Harry; Alexander, Rikki; Taylor, Brian F. Journal of the
Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1997), (1), 21-24
2-Halo-1,3-dithiane 1,3-dioxide: a diastereoselective carbonyl anion equivalent in reactions
with aldehydes. Aggarwal, Varinder K.; Boccardo, Giorgio; Worrall, Julia M.; Adam, Harry;
Alexander, Rikki. Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic
Chemistry (1997), (1), 11-19
A N-nitrosochloroethyl-cephalosporin carbamate prodrug for antibody-directed enzyme
prodrug therapy (ADEPT). Alexander, Rikki P.; Bates, Robert W.; Pratt, Andrew J.; Kraunsoe,
James A. E. Tetrahedron (1996), 52(16), 5983-8
The inhibition of antigen-induced eosinophilia and bronchoconstriction by CDP840, a novel
stereo-selective inhibitor of phosphodiesterase type 4. Hughes B; Howat D; Lisle H; Holbrook
M; James T; Gozzard N; Blease K; Hughes P; Kingaby R; Warrellow G; Alexander R; Head J; Boyd E;
Eaton M; Perry M; Wales M; Smith B; Owens R; Catterall C; Lumb S; Russell A; Allen R; Merriman M;
Bloxham D; Higgs G British journal of pharmacology (1996), 118(5), 1183-91.
Preparation of 4-(2-phenylethyl)pyridine derivatives as phosphodiesterase IV inhibitors.
Warrellow, Graham John; Boyd, Ewan Campbell; Alexander, Rikki Peter. WO 9535283
Preparation of 4-(2-phenylethyl)pyridine derivatives as phosphodiesterase IV inhibitors.
Head, John Clifford; Warrellow, Graham John; Alexander, Rikki Peter. WO 9535284
Tri-substituted phenyl and pyridine derivatives useful as PDE IV inhibitors. Warrellow,
Graham John; Alexander, Rikki Peter. WO 9535281
(R)-4-[2-(3-Cyclopentyloxy-4-methoxyphenyl)-2-phenylethyl]pyridine hydrogen sulfate salt as
PDE type IV inhibitor. Head, John Clifford; Warrellow, Graham John; Alexander, Rikki Peter;
Boyd, Ewan Campbell. WO 9535282
Tetra-substituted phenyl and pyridine derivatives useful as PDE IV inhibitors. Alexander,
Rikki Peter; Warrellow, Graham John. WO 9535285
An enantioselective process for the preparation of chiral triaryl derivatives and chiral
intermediatesfor use therein. Alexander, Rikki Peter; Warrellow, Graham John; Head, John
Clifford; Boyd, Ewan Campbell; Porter, John Robert. WO 9517386
Preparation of phenethylheterocycles as phosphodiesterase type IV inhibitors. Warrellow,
Graham John; Boyd, Ewan Campbell; Alexander, Rikki Peter; Eaton, Michael Anthony William. WO
9517392
Trisubstituted phenyl derivatives, processes for their preparation, and their use as
phosphodiesterase (type IV) inhibitors. Warrellow, Graham John; Boyd, Ewan Campbell;
Alexander, Rikki Peter. WO 9517399
Styryl-derivative inhibitors of PDE IV. Warrellow, Graham John; Boyd, Ewan Campbell;
Alexander, Rikki Peter. WO 9414800
Trisubstituted phenyl derivatives as phosphodiesterase inhibitors. Warrellow, Graham John;
Boyd, Ewan Campbell; Alexander, Rikki Peter. WO 9414742
Trisubstituted phenyl derivatives as phosphodiesterase inhibitors and processes for their
preparation. Warrellow, Graham John; Cole, Valerie Anne; Alexander, Rikki Peter. WO 9420446
Preparation of styryl derivatives as PDE-IV inhibitors. Warrellow, Graham John; Cole, Valerie

5. Anne; Alexander, Rikki Peter. WO 9420455
Stereoselective addition reactions of lithiated 2-chloro-1,3-dithiane-1,3-dioxide to aldehydes.
Aggarwal, Varinder K.; Worrall, Julia M.; Adams, Harry; Alexander, Rikki. Tetrahedron Letters
(1994), 35(33), 6167-70.
The synthesis of novel bifunctional linker molecules. Billington, Susan; Mann, John; Quazi,
Paula; Alexander, Rikki; Eaton, Michael A. W.; Millar, Kenneth; Millican, Andrew. Tetrahedron
(1991), 47(28), 5231-6.
Cephalosporin nitrogen mustard carbamate prodrugs for ADEPT. Alexander, Rikki P.; Beeley,
Nigel R. A.; O'Driscoll, Maraid; O'Neill, Faye P.; Millican, T. Andrew; Pratt, Andrew J.; Willenbrock,
Frances W. Tetrahedron Letters (1991), 32(27), 3269-72.
Towards tumor targeting with copper-radiolabeled macrocycle-antibody conjugates:
synthesis, antibody linkage, and complexation behavior. Morphy, J. Richard; Parker, David;
Kataky, Ritu; Eaton, Michael A. W.; Millican, Andrew T.; Alexander, Rikki; Harrison, Alice; Walker,
Carol. Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-
1999) (1990), (4), 573-85.
Immunoconjugates and prodrugs and their use in association for drug delivery. Eaton,
Michael Anthony William; Pratt, Andrew John; Alexander, Rikki Peter. EP 392745
Transition-metal mediated asymmetric synthesis. Part 6. Organometallic approaches to the
enantiomer synthesis of tridachione: a role for planar chirality in synthesis design.
Alexander, Rikki P.; Morley, Christopher; Stephenson, G. Richard. Journal of the Chemical Society,
Perkin Transactions 1: Organic and Bio-Organic Chemistry (1972-1999) (1988), (8), 2069-74.
 -Complexes with planar chirality: control centers for stereoselective synthesis.
Stephenson, G. R.; Alexander, R. P.; Morley, C.; Howard, P. W. Philosophical Transactions of the
Royal Society of London, Series A: Mathematical, Physical and Engineering Sciences (1988),
326(1592), 545-56.
Vinylpyridine derivatives as thiol-reactive cross-linking reagents and their preparation.
Alexander, Rikki Peter; Eaton, Michael Anthony William; Millican, Thomas Andrew; Titmas, Richard
Charles Dominic. WO 8805433
Antibody labeling with functionalized cyclam macrocycles. Morphy, J. Richard; Parker, David;
Alexander, Rikki; Bains, Amarjit; Carne, Alex F.; Eaton, Michael A. W.; Harrison, Alice; Millican,
Andrew; Phipps, Alison; et al. Journal of the Chemical Society, Chemical Communications (1988),
(3), 156-8
Alkylation of tricarbonyliron complexesby trimethylsilyl cyanide: synthetic and kinetic
studies. Alexander, Rikki P.; James, Tony D.; Stephenson, G. Richard. Journal of the Chemical
Society, Dalton Transactions: Inorganic Chemistry (1972-1999) (1987), (8), 2013-16.
Transition-metal mediated asymmetric synthesis. Part 5. Alternative methods for the
formation of tricarbonyl( 5-cyclohexadienyl)iron(1+) salts. Alexander, Rikki P.; Stephenson,
G. Richard. Journal of the Chemical Society, Dalton Transactions: Inorganic Chemistry (1972-1999)
(1987), (4), 885-8.
Reversal of regiocontrol in the alkylation of an arene  -complex. Alexander, Rikki P.;
Stephenson, G. Richard. Journal of Organometallic Chemistry (1986), 314(3), C73-C75.
A superior method for the addition of cyanide to substituted tricarbonyl( 5-
cyclohexadienyl)iron(1+) salts. Alexander, Rikki P.; Stephenson, G. Richard. Journal of
Organometallic Chemistry (1986), 299(1), C1-C3.
Asymmetric alkylation and sulfenylation of chiral O-silylated imide enolates. Alexander, Rikki
P.; Paterson, Ian. Tetrahedron Letters (1985), 26(43), 5339-40.

6. Alkene carbosulfenylation and carboselenylation: the use of allyltrimethylsilane and O-
silylated enolates. Alexander, Rikki P.; Paterson, Ian. Tetrahedron Letters (1983), 24(52),
5911-14.