Robert Gleave
GlaxoSmithKline
31 Papers
236 Citations
Robert Gleave is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Enantioselective synthesis & Catalysis. The author has an hindex of 14, co-authored 31 publications.
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Papers
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Muna H. Abdi,Paul John Beswick,Andy Billinton,Laura J. Chambers,Andrew Charlton,Sue D. Collins,Katharine Laura Collis,David Kenneth Dean,Elena Fonfria,Robert Gleave,Clarisse L. Lejeune,Livermore David,Stephen J. Medhurst,Anton D. Michel,Andrew P. Moses,Lee William Page,Sadhana Patel,Shilina Roman,Stefan Senger,Brian Peter Slingsby,Jon Graham Anthony Steadman,Alexander J. Stevens,Daryl S. Walter +22 more
TL;DR: Structural-activity relationships of a series of pyroglutamic acid amide analogues of 4 were investigated and compound 31 was identified as a potent P2X(7) antagonist with excellent in vivo activity in animal models of pain, and a profile suitable for progression to clinical studies.
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Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Laura J. Chambers,Alexander J. Stevens,Andrew P. Moses,Anton D. Michel,Daryl S. Walter,David John Davies,Livermore David,Elena Fonfria,Emmanuel Hubert Demont,Mythily Vimal,P. Theobald,Paul John Beswick,Robert Gleave,Shilina Roman,Stefan Senger +14 more
TL;DR: Structural-activity relationships of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X(7) antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties.
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Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Lee Abberley,Aude Bebius,Paul John Beswick,Andy Billinton,Katharine Laura Collis,David Kenneth Dean,Elena Fonfria,Robert Gleave,Stephen J. Medhurst,Anton D. Michel,Andrew P. Moses,Sadhana Patel,Shilina Roman,Tiziana Scoccitti,Beverley Smith,Jon Graham Anthony Steadman,Daryl S. Walter +16 more
TL;DR: A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule, and compound 18 was subsequently identified as a potent P2X(7) antagonist with very low in vivo clearance and high oral bioavailability.
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Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X7 antagonists
Robert Gleave,Daryl S. Walter,Paul John Beswick,Elena Fonfria,Anton D. Michel,Shilina Roman,Sac-Pham Tang +6 more
TL;DR: A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole, and structure-activity relationships (SAR) relationships were investigated both with respect to activity at the P2X(7) receptor and in vitro metabolic stability.
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Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Adrian Hall,Stephen John Atkinson,Susan H. Brown,Iain P. Chessell,Anita Chowdhury,Nicholas Maughan Clayton,Tanya Coleman,Gerard Martin Paul Giblin,Robert Gleave,Beverley Hammond,Mark Patrick Healy,Matthew R. Johnson,Anton D. Michel,Alan Naylor,Riccardo Novelli,David J. Spalding,Sac P. Tang +16 more
TL;DR: The preliminary SAR of a series of novel 1,5-biaryl pyrrole EP1 receptor antagonists derived from compound 1 is described and the most effective replacement was found to be the isobutyl group.
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