1. Daryl Walter - Publications and Patents
(Papers and patents in-press are not included)
1) Cloning and pharmacological characterization of the dog P2X7 receptor. Roman, S.;
Cusdin, F. S.; Fonfria, E.; Goodwin, J. A.; Reeves, J.; Lappin, S. C.; Chambers, L.; Walter, D.
S.; Clay, W. C.; Michel, A. D.; British Journal of Pharmacology (2009), 158(6), 1513-1526.
2) A Lewis Acid Promoted Oxidative Cyclization. Donohoe, Timothy J.; Winship, Paul C. M.;
Walter, Daryl S.; Journal of Organic Chemistry (2009), 74(16), 6394-6397.
3) 5-Oxo-3-pyrrolidinecarboxamide derivatives as P2X7 modulators. Steadman, Jon
Graham Anthony; Walter, Daryl Simon. PCT Int. Appl. (2009), 39pp. WO 2009077559 A2
4) Isothiazolidine 1,1-dioxide and tetrahydro-2h-1,2-thiazine 1,1-dioxide derivatives as p2x7
modulators. Walter, Daryl Simon. PCT Int. Appl. (2009), 65pp. WO 2009077362 A1
5) Combinations of pyrazolyl or isoxazolyl p2x7 modulators with further therapeutic agents.
Michel, Anton Duval; Walter, Daryl Simon. PCT Int. Appl. (2009), 70pp. WO
2009074519 A1
6) Combinations of prolinamide p2x7 modulators with further therapeutic agents. Michel,
Anton Duval; Walter, Daryl Simon. PCT Int. Appl. (2009), 136pp. WO 2009074518 A1
7) Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine
transition state mimetics. Charrier, Nicolas; Clarke, Brian; Cutler, Leanne; Demont,
Emmanuel; Dingwall, Colin; Dunsdon, Rachel; Hawkins, Julie; Howes, Colin; Hubbard, Julia;
Hussain, Ishrut; Maile, Graham; Matico, Rosalie; Mosley, Julie; Naylor, Alan; O'Brien, Alistair;
Redshaw, Sally; Rowland, Paul; Soleil, Virginie; Smith, Kathrine J.; Sweitzer, Sharon;
Theobald, Pam; Vesey, David; Walter, Daryl S.; Wayne, Gareth. Bioorganic & Medicinal
Chemistry Letters (2009), 19(13), 3674-3678.
8) Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side
substituent. Charrier, Nicolas; Clarke, Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon,
Rachel; Hawkins, Julie; Hubbard, Julia; Hussain, Ishrut; Maile, Graham; Matico, Rosalie;
Mosley, Julie; Naylor, Alan; O'Brien, Alistair; Redshaw, Sally; Rowland, Paul; Soleil, Virginie;
Smith, Kathrine J.; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S.; Wayne,
Gareth. Bioorganic & Medicinal Chemistry Letters (2009), 19(13), 3669-3673.
9) Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Charrier, Nicolas; Clarke, Brian; Cutler, Leanne; Demont, Emmanuel; Dingwall, Colin;
Dunsdon, Rachel; Hawkins, Julie; Howes, Colin; Hubbard, Julia; Hussain, Ishrut; Maile,
Graham; Matico, Rosalie; Mosley, Julie; Naylor, Alan; O'Brien, Alistair; Redshaw, Sally;
Rowland, Paul; Soleil, Virginie; Smith, Kathrine J.; Sweitzer, Sharon; Theobald, Pam; Vesey,
David; Walter, Daryl S.; Wayne, Gareth. Bioorganic & Medicinal Chemistry Letters (2009),
19(13), 3664-3668.
10) Mechanism of action of species-selective P2X7 receptor antagonists. Michel, Anton D.;
Ng, Sin-Wei; Roman, Shilina; Clay, William C.; Dean, David K.; Walter, Daryl S. British
Journal of Pharmacology (2009), 156(8), 1312-1325.
11) 4-Benzoyl-1-substituted-piperazin-2-one derivatives as P2X7 modulators. Chambers,
Laura Jane; Collis, Katharine Laura; Dean, David Kenneth; Munoz-Muriedas, Jorge; Steadman,
Jon Graham Anthony; Walter, Daryl Simon. (Glaxo Group Limited, UK). PCT Int. Appl.
(2009), WO 2009053459 A1

2. 12) Preparation of pyrazole derivatives as modulators of P2X7 receptor. Beswick, Paul John;
Chambers, Laura Jane; Chessell, Iain Patrick; Davies, David John; Demont, Emmanuel Hubert;
Gleave, Robert James; Livermore, David George Hubert; Theobald, Pamela Joan; Vimal,
Mythily; Walter, Daryl Simon. PCT Int. Appl. (2008), WO 2008138876 A1
13) Pyrazole derivatives as p2x7 modulators. Beswick, Paul John; Dean, David Kenneth; Walter,
Daryl Simon. PCT Int. Appl. (2008), WO 2008125600 A2
14) Imidazolidine carboxamide derivatives as p2x7 modulators. Beswick, Paul John; Dean,
David Kenneth; Gleave, Robert James; Moses, Andrew Peter; Walter, Daryl Simon. (Glaxo
Group Limited, UK). PCT Int. Appl. (2008), WO 2008119825 A2
15) Preparation of morpholinecarboxamide derivatives and analogs as P2X7 modulators.
Beswick, Paul John; Walter, Daryl Simon. (Glaxo Group Limited, UK). PCT Int. Appl.
(2008), WO 2008119685 A2
16) Piperidinone carboxamide derivatives as p2x7 modulators. Beswick, Paul John; Gleave,
Robert James; Steadman, Jon Graham Anthony; Walter, Daryl Simon. PCT Int. Appl. (2008),
WO 2008116845 A1
17) Pyrrole and isoindole carboxamide derivatives as p2x7 modulators. Gleave, Robert James;
Livermore, David George Hubert; Walter, Daryl Simon. PCT Int. Appl. (2008), WO
2008116814 A1
18) Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral
bioavailability. Charrier, Nicolas; Clarke, Brian; Cutler, Leanne; Demont, Emmanuel;
Dingwall, Colin; Dunsdon, Rachel; East, Philip; Hawkins, Julie; Howes, Colin; Hussain, Ishrut;
Jeffrey, Phil; Maile, Graham; Matico, Rosalie; Mosley, Julie; Naylor, Alan; O'Brien, Alistair;
Redshaw, Sally; Rowland, Paul; Soleil, Virginie; Smith, Kathrine J.; Sweitzer, Sharon;
Theobald, Pam; Vesey, David; Walter, Daryl S.; Wayne, Gareth., J.Med.Chem. (2008), 51(11),
3313-3317.
19) Negative and positive allosteric modulators of the P2X7 receptor. Michel, A.D.; Chambers,
L.J.; Walter, D.S.; British Journal of Pharmacology (2008), 153(4), 737-750.
20) BACE-1 inhibitors Part 3: Identification of hydroxy ethylamines (HEAs) with nanomolar
potency in cells Beswick, Paul; Charrier, Nicolas; Clarke, Brian; Demont, Emmanuel;
Dingwall, Colin; Dunsdon, Rachel; Faller, Andrew; Gleave, Robert; Hawkins, Julie; Hussain,
Ishrut; Johnson, Christopher N.; MacPherson, David; Maile, Graham; Matico, Rosalie; Milner,
Peter; Mosley, Julie; Naylor, Alan; O'Brien, Alistair; Redshaw, Sally; Riddell, David; Rowland,
Paul; Skidmore, John; Soleil, Virginie; Smith, Kathrine J.; Stanway, Steven; Stemp, Geoffrey;
Stuart, Alistair; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S.; Ward, John;
Wayne, Gareth., Bioorg.Med.Chem.Lett., 18(3), 2008, 1022-1026.
21) BACE-1 inhibitors Part 2: Identification of novel hydroxy ethylamines (HEAs) with
reduced peptidic character Clarke, Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon,
Rachel; Faller, Andrew; Hawkins, Julie; Hussain, Ishrut; MacPherson, David; Maile, Graham;
Matico, Rosalie; Milner, Peter; Mosley, Julie; Naylor, Alan; O'Brien, Alistair; Redshaw, Sally;
Riddell, David; Rowland, Paul; Soleil, Virginie; Smith, Kathrine J.; Stanway, Steven; Stemp,
Geoffrey; Sweitzer, Sharon; Theobald, Pam; Vesey, David; Walter, Daryl S.; Ward, John;
Wayne, Gareth., Bioorg.Med.Chem.Lett., 18(3), 2008, 1017-1021.
22) BACE-1 inhibitors Part 1: Identification of novel hydroxy ethylamines (HEAs) Clarke,
Brian; Demont, Emmanuel; Dingwall, Colin; Dunsdon, Rachel; Faller, Andrew; Hawkins, Julie;

3. Hussain, Ishrut; MacPherson, David; Maile, Graham; Matico, Rosalie; Milner, Peter; Mosley,
Julie; Naylor, Alan; O'Brien, Alistair; Redshaw, Sally; Riddell, David; Rowland, Paul; Soleil,
Virginie; Smith, Kathrine J.; Stanway, Steven; Stemp, Geoffrey; Sweitzer, Sharon; Theobald,
Pam; Vesey, David; Walter, Daryl S.; Ward, John; Wayne, Gareth., Bioorg.Med.Chem.Lett.,
18(3), 2008, 1011-1016.
23) Preparation of N-(phenylmethyl)-5-oxoprolinamides derivatives as P2X7 antagonists for
the treatment of pain, inflammation and neurodegeneration. Chambers, Laura J.; Gleave,
Robert; Senger, Stefan; Walter, Daryl Simon. (Glaxo Group Limited, UK). PCT Int. Appl.
(2008), WO 2008003697 A1
24) Preparation of isoxazolylacetamides as P2X7 receptor antagonists. Beswick, Paul John;
Walter, Daryl Simon. (Glaxo Group Limited, UK). PCT Int. Appl. (2007), WO
2007141269 A1
25) Preparation of N-(phenylmethyl)-2-(1H-pyrazol-4-yl)acetamide derivatives as P2X7
antagonists for the treatment of pain, inflammation and neurodegeneration. Beswick,
Paul John; Chambers, Laura J.; Davies, David John; Dean, David Kenneth; Demont, Emmanuel
Hubert; Roomans, Susan; Walter, Daryl Simon. (Glaxo Group Limited, UK). PCT Int. Appl.
(2007), WO 2007141267 A1
26) Direct labeling of the human P2X7 receptor and identification of positive and negative
cooperativity of binding. Michel, A.D.; Chambers, L.J.; Clay, W.C.; Condreay, J.P.; Walter,
D.S.; Chessell, I.P.; British Journal of Pharmacology (2007), 151(1), 103-114.
27) A new route to highly functionalized heterocyclic rings. Parsons, Philip J.; Waters,
Alexander J.; Walter, Daryl S.; Board, Johnathan; J. Org. Chem., (2007), 72(4), 1395-1398.
28) Oral administration of a potent and selective non-peptidic BACE-1 inhibitor decreases b-
cleavage of amyloid precursor protein and amyloid-b production in-vivo. Hussain, Ishrut;
Hawkins, Julie; Harrison, David; Hille, Christopher; Wayne, Gareth; Cutler, Leanne; Buck,
Tania; Walter, Daryl; Demont, Emmanuel; Howes, Colin; Naylor, Alan; Jeffrey, Philip;
Gonzalez, Maria I.; Dingwall, Colin; Michel, Anton; Redshaw, Sally; Davis, John B.; Journal of
Neurochemistry (2007), 100(3), 802-809.
29) A novel cyclisation strategy for the synthesis of lactonamycin: A new route to highly
functionalized heterocyclic rings. Parsons, Philip J.; Board, Johnathan; Waters, Alexander J.;
Hitchcock, Peter B.; Wakenhut, Florian; Walter, Daryl S. Synlett (2006), (19), 3243-3246.
30) Synthesis of indoles: efficient functionalisation of the 7-position. Charrier, Nicolas; Demont
Emmanuel; Dunsdon, Rachel; Maile, Graham; Naylor, Alan; O’Brien, Alistair; Redshaw, Sally;
Theobald, Pam; Vesey, David; Walter, Daryl. Synthesis (2006), 20, 3467-3477.
31) Novel hydroxyethylamine and ketone compounds having asp2 inhibitory activity.
Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int. Appl. (2006),
WO2006103088 A1.
32) Tricyclic indole derivatives for use in the treatment of Alzheimer's disease.
Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int. Appl. (2006), WO
2006040148 A1.
33) Subsituted hydroxyethylamine compounds for treating Alzheimer's disease.
Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int. Appl. (2006), WO
2006040151 A1.

4. 34) Heterocyclic ketone compounds for treating Alzheimer’s disease.
Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int. Appl. (2006), WO
2006040149 A1.
35) Synthesis of 3,5,7-Substituted Indoles via Heck Cyclisation.
Nicolas Charrier, Emmanuel Demont, Rachel Dunsdon, Graham Maile, Alan Naylor, Alistair
O’Brien, Sally Redshaw, Pam Theobald, David Vesey, Daryl Walter, Synlett, 2005, No.20, pp
3071-3074.
36) N,N’-substituted-1,3-diamino-2-oxopropane derivatives, their pharmaceutical
compositions and use. Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon.
PCT Int. Appl. (2005), CODEN: PIXXD2 WO 2005113525 A1
37) Tricyclic indole hydroxyethylamine derivatives and their use in the treatment of
Alzheimer's disease. Redshaw, Sally; Demont, Emmanuel Hubert; Walter, Daryl Simon.
PCT Int. Appl. (2005), 29 pp. CODEN: PIXXD2 WO 2005058915 A1 20050630
38) 3-(1,1-dioxotetrahydro-1,2-thiazin-2-yl) or 3-(1,1-doxo-isothiazolidin-2yl) substituted
benzamide compounds as asp2 inhibitors. Demont, Emmanuel Hubert; Redshaw, Sally;
Walter, Daryl Simon. PCT Int. Appl. (2004), 29 pp. CODEN: PIXXD2 WO 2004111022
A1 20041223
39) Tricyclic indole derivatives and their use in the treatment of Alzheimer’s disease. Demont,
Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int.Appl. (2004),
WO2004094430 A1 20041104
40) Preparation of hydroxyethylamine derivatives for the treatment of Alzheimer’s disease.
Demont, Emmanuel Hubert; Redshaw, Sally; Walter, Daryl Simon. PCT Int. Appl. (2004),
CODEN: PIXXD2 WO 2004080376 A2 20040923
41) Hydroxyethylamine derivatives for the treatment of Alzheimer's disease. Demont,
Emmanuel H.; Faller, Andrew; MacPherson, David Timothy; Milner, Peter Henry; Naylor, Alan;
Redshaw, Sally; Stanway, Steven James; Vesey, David R.; Walter, Daryl S.. (Glaxo Group
Limited, UK). PCT Int. Appl. (2004), 201 pp WO 2004050619 A1 20040617
42) Galacto, Gluco, Manno, and Disaccharide-Based C-Glycosides of 2-Amino-2-deoxy Sugars.
Grant, Laura; Liu, Yan; Walsh, Kenneth E.; Walter, Daryl S.; Gallagher, Timothy. Organic
Letters (2002), 4(26), 4623-4625.
43) Preparation of imidazolylalkyl-aminopiperidines as HIV inhbitors. Edlin, Christopher
David; Redshaw, Sally; Smith, Ian Edward David; Walter, Daryl Simon. (F. Hoffmann-La
Roche A.-G., Switz.). PCT Int. Appl. (2002), WO 0279186 A2, 179 pp.
44) Partial reduction of 3-heteroatom substituted 2-furoic acids: the role of an ortho group in
viability and stereoselectivity. Donohoe, Timothy J.; Calabrese, Andrew A.; Guillermin, Jean-
Baptiste; Frampton, Christopher S.; Walter, Daryl. Journal of the Chemical Society, Perkin
Transactions 1 (2002), (15), 1748-1756.
45) Imidazolone derivatives for the treatment of viral diseases. Dymock, Brian W.; Jones,
Philip S.; Merrett, John H.; Parkes, Kevin E.B., Parratt, Martin J.; Walter, Daryl S. (F.
Hoffmann-La Roche A.-G., Switz.). PCT Int. Appl. (2000), WO 0242279 A1, 88 pp.
46) Preparation of (+)-nemorensic acid and approaches to nemorensine using the partial
reduction of electron deficient furans. Donohoe, Timothy J.; Guillermin, Jean-Baptiste;
Walter, Daryl S., Journal of the Chemical Society, Perkin Transactions 1 (2002), (11), 1369-

5. 1375.
47) Ro 32-7315, a selective and orally active inhibitor of tumour necrosis factor-α convertase.
Lad, N.; Beck, G.; Bottomley, G.; Bradshaw, D.; Brewster, M.; Broadhurst, M.; Devos, R.; Hill,
C.; Johnson, W.; Kim, H-J; Kirtland, S.; Kneer, J.; Mackenzie; R.; Martin, R.; Nixon, J.; Price,
G.; Rodwell, A.; Rose, F.; Tang, J-P.; Walter, D.S.; Wilson, K.; Worth, E. The Journal of
Pharmacology and Exp. Therapeutics. (2002), 302(1), 390-396.
48) Silyl-substituted furans in the stereoselective Birch reduction. Donohoe, Timothy J.;
Guillermin, Jean-Baptiste; Calabrese, Andrew A.; Walter, Daryl S., Tetrahedron Lett. (2001),
42(34), 5841-5844.
49) Radical-Mediated Synthesis of α-C-Glycosides Based on N-Acyl Galactosamine.
SanMartin, Raul; Tavassoli, Bahareh; Walsh, Kenneth E.; Walter, Daryl S.; Gallagher, Timothy.
Org. Lett. (2000), 2(25), 4051-4054.
50) Preparation of hydroxycarbamoylalkylcarboxylic acid azacyclic hydrazides as TNF-α
inhibitors. Broadhurst, Michael John; Johnson, William Henry; Walter, Daryl Simon. (F.
Hoffmann-La Roche Ag, Switz.). PCT Int. Appl. (2000), WO 0035885 A1, 128 pp.
51) Preparation of hydrazine derivatives as TNF-α inhibitors. Broadhurst, Michael John;
Johnson, William Henry; Walter, Daryl Simon. (F. Hoffmann-La Roche A.-G., Switz.). PCT
Int. Appl. (2000), WO 0032570 A1, 39 pp.
52) The synthesis of (+)-nemorensic acid. Donohoe, Timothy J.; Guillermin, Jean-Baptiste;
Frampton, Christopher; Walter, Daryl S., Chem. Commun. (Cambridge) (2000), (6), 465-466.
53) Preparation of hydroxycarbamoylalkylcarboxylic acid hydrazides as inhibitors of the
release of tumor necrosis factor. Broadhurst, Michael John; Johnson, William Henry;
Walter, Daryl Simon. (F. Hoffmann-La Roche A.-G., Switz.). PCT Int. Appl. (2000), WO
0000465 A1, 171 pp.
54) C-Glycosyl Tyrosines. Synthesis and Incorporation into C-Glycopeptides. Pearce, Alan J.;
Ramaya, Sharn; Thorn, Simon N.; Bloomberg, Graham B.; Walter, Daryl S.; Gallagher,
Timothy, J. Org. Chem. (1999), 64(15), 5453-5462.
55) Preparation of hydroxycarbamoylalkylcarboxylic acid hydrazides as inhibitors of tumor
necrosis factor and transforming growth factor release. Broadhurst, Michael John;
Johnson, William Henry; Walter, Daryl Simon. (F. Hoffmann-La Roche A.-G., Switz.). Ger.
Offen. (1999), DE 19829229 A1, 64 pp.
56) Matrix metalloproteinase inhibitors in arthritis. Bottomley, K. M.; Johnson, W. H.;
Walter, D. S., J. Enzyme Inhib. (1998), 13(2), 79-101.
57) Synthesis and reactivity of a novel group of hydroxylamine-containing 2π- and 4π -
components. Pearce, Alan J.; Walter, Daryl S.; Frampton, Christopher S.; Gallagher,
Timothy., J. Chem. Soc., Perkin Trans. 1 (1998), (5), 847-852.
58) Ketones bearing an α,β-aryl or -hetaryl substituent. Walter, Daryl S.. University
Nottingham, UK. Editor(s): Katrizky, Alan R.; Meth-Cohn, Otto; Rees, Charles Wayne.
Compr. Org. Funct. Group Transform. (1995), 3 277-312, 733-856. Publisher: Elsevier,
Oxford, UK. General Review written in English.
59) A cascade radical macrocyclization-transannulation approach towards the construction of

6. ring-fused tricycles and polycycles. Begley, Michael J.; Pattenden, Gerald; Smithies,
Allison; Tapolczay, David; Walter, Daryl S., J. Chem. Soc., Perkin Trans. 1 (1996), (1), 21-9.
60) Cascade radical mediated macrocyclization-transannulation reactions leading to ring-fused
bicycles. Pattenden, Gerald; Smithies, Allison J.; Tapolczay, David; Walter, Daryl S., J.
Chem. Soc., Perkin Trans. 1 (1996), (1), 7-19.
61) Regioselective allylation of enol silyl ethers with γ-heterosubstituted vinylthionium ions.
Hunter, Roger; Michael, Joseph P.; Walter, Daryl S., Tetrahedron Lett. (1994), 35(30), 5481-4.
62) Allylation with Substituted Vinylthionium Ions from SnCl4 Ionisation of 1,3- and 3,3-
Bis(alkyl/phenylthio)propenes. Hunter, Roger; Michael, Joseph P.; Walter, Daryl S.,
Tetrahedron (1994), 50(31), 9377-98.
63) Allylation with Pummerer-generated substituted vinylthionium ions. Hunter, Roger;
Michael, Joseph P.; Simon, Clive D.; Walter, Daryl S., Tetrahedron (1994), 50(31), 9365-76.
64) A cascade macrocyclization-transannulation approach to polycycle constructions.
Begley, Michael J.; Pattenden, Gerald; Smithies, Allison J.; Walter, Daryl S., Tetrahedron Lett.
(1994), 35(15), 2417-20.
65) Sequential radical macrocyclization-transannulation approach to ring-fused bicycles.
Pattenden, Gerald; Smithies, Allison J.; Walter Daryl S., Tetrahedron Lett. (1994), 35(15),
2413-16.
66) Alkylation of enol silyl ethers with vinylthionium ions generated from 1,1- and 1,3-
bis(phenylthio)propenes. Hunter, Roger; Michael, Joseph P.; Walter, Daryl S., Tetrahedron
Lett. (1992), 33(37), 5413-16.
67) Alkylation of enol silyl ethers by Pummerer-generated vinylthionium ions: a novel masked
Michael reaction. Hunter, Roger; Carlton, Laurence; Cirillo, Pier F.; Michael, Joseph P.;
Simon, Clive D.; Walter, Daryl S., J. Chem. Soc., Perkin Trans. 1 (1989), (9), 1631-7.