Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Emilio F. Stuart"'
Autor:
Emilio F. Stuart, Nick Clarke, Paul Alan Glossop, Neil Feeder, Strang Ross Sinclair, J. W. Watson, Jane L. Burrows, Amy S. Kenyon, Matthew D. Selby, Michael A. Trevethick, Sheena Patel, Rhys M. Jones, Kim James, Karen N. Wright, Dannielle Frances Roberts, Lyn H. Jones
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5121-5126
A 1,2,4-triazole motif was employed as a bioisostere for the ester commonly used in muscarinic antagonists, and subsequent integrative conjugation to a β2 agonist quinolinone furnished a new class of bifunctional MABAs for the treatment of COPD. Med
Autor:
Emilio F. Stuart, Stuart Rozze, Fiona Macintyre, D. K. Walker, Michael A. Trevethick, Sandra Marina Monaghan, Michael Yeadon, Maw Graham Nigel, Patricia Wright, Simon John Mantell, Matthew D. Selby, Helene Chavaroche, Peter T. Stephenson, Arnaud Lemaitre, David V. Batchelor, Karen N. Wright, Lynsey Whitlock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4471-4475
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be th
Autor:
Adrian Barnard, Michael Yeadon, Simon John Mantell, Karen N. Wright, Mike Trevethick, Emilio F. Stuart
Publikováno v:
British Journal of Pharmacology. 155:463-474
Adenosine A2A receptor agonists may be important regulators of inflammation. Such conclusions have come from studies demonstrating that, (i) adenosine A2A agonists exhibit anti-inflammatory properties in vitro and in vivo, (ii) selective A2A antagoni
Autor:
D. K. Walker, Emilio F. Stuart, Arnaud Lemaitre, David V. Batchelor, Peter G. Dodd, Maw Graham Nigel, Helene Chavaroche, Sandra Marina Monaghan, Ruth F. Keir, Matthew D. Selby, Simon John Mantell, Tim J. Hobson, Michael A. Trevethick, Peter T. Stephenson, Stuart Rozze, Rhys M. Jones, Karen N. Wright, Michael Yeadon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1284-1287
COPD is a major cause of mortality in the western world. A(2A) agonists are postulated to reduce the lung inflammation that causes COPD. The cardiovascular effects of A(2A) agonists dictate that a compound needs to be delivered by inhalation to be th
Autor:
Paul A, Glossop, Christine A L, Watson, David A, Price, Mark E, Bunnage, Donald S, Middleton, Anthony, Wood, Kim, James, Dannielle, Roberts, Ross S, Strang, Michael, Yeadon, Christelle, Perros-Huguet, Nicholas P, Clarke, Michael A, Trevethick, Ian, Machin, Emilio F, Stuart, Steven M, Evans, Anthony C, Harrison, David A, Fairman, Balaji, Agoram, Jane L, Burrows, Neil, Feeder, Craig K, Fulton, Barry R, Dillon, David A, Entwistle, Fiona J, Spence
Publikováno v:
Journal of medicinal chemistry. 54(19)
A novel tertiary amine series of potent muscarinic M(3) receptor antagonists are described that exhibit potential as inhaled long-acting bronchodilators for the treatment of chronic obstructive pulmonary disease. Geminal dimethyl functionality presen
Autor:
Emilio F. Stuart, Nick Clarke, Maria Stanley, Michele Coghlan, Matthew Strawbridge, Susan Summerhill, Mike Yeadon, Sheena Patel, Christelle Perros-Huguet, Mike Trevethick, Stuart Marshall
Publikováno v:
A45. BRONCHODILATORS FOR COPD: OLD FAITHFULS AND NOVEL COMPOUNDS.
Autor:
Craig K. Fulton, David Price, Kim James, Mark E. Bunnage, Sandra D. Newman, Sheena Patel, Jane L. Burrows, Emilio F. Stuart, Rachel Osborne, Stuart Marshall, Nick Clarke, Matthew D. Selby, Neil Feeder, David A. Entwistle, Helen Baldock, Rhys M. Jones, Michele Coghlan, Laura Hilton, Michael A. Trevethick, Karen N. Wright, David Fairman, Lyn H. Jones, Amy S. Kenyon
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(9)
This paper describes the successful design and development of dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder using the principles of 'inhalation by design'. A key feature of this work is th
Optimized glucuronidation of dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD
Autor:
Rachel Osborne, David A. Entwistle, Michael Yeadon, Graham Lunn, Karen N. Wright, Jane L. Burrows, Emilio F. Stuart, Lyn H. Jones, Sandra D. Newman, Kim James, Amy S. Kenyon, Fiona J. Spence, Susan Summerhill, Matthew D. Selby, Nick Clarke, David Price, Stuart Marshall, Laura Hilton, Helen Baldock, Rhys M. Jones, Neil Feeder, Michael A. Trevethick, Sheena Patel, Nadia Laouar, Michele Coghlan, Mark E. Bunnage, David Fairman
Publikováno v:
MedChemComm. 2:870
‘Inhalation by design’ concepts were developed to create novel dual pharmacology β-2 agonists-M3 antagonists, for the treatment of chronic obstructive pulmonary disorder. A key feature of this work is the combination of balanced potency and phar