Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Lesa Watson"'
Autor:
Robin Marshall, Catherine Smyth, J. Alf Davis, Alasdair Garnett, Julian Scott Northen, John S. Carey, Stephen J. Byard, Urvish Pandya, Stephen John Martin, Antonio Codina, Gary Patrick Reid, John Mykytiuk, Sophie L. Berrell, Katherine Filer, Lesa Watson
Publikováno v:
Organic Process Research & Development. 23:762-770
This paper describes the process development conducted toward the multi-kilogram synthesis of a hemiadipic acid pro-drug of buprenorphine. The major challenges were to control the levels of the dibuprenorphine monoadipate impurity and to improve the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::878ee5f6f614c4c5a97ffeffdec68649
https://doi.org/10.1021/acs.oprd.9b00025
https://doi.org/10.1021/acs.oprd.9b00025
Autor:
Kathy F. K. Cheung, Jean-Yves Chiva, Satish Dayal, Darren Stead, Carly L. Nichols, Rob Webster, Lee R. Roberts, David Stonehouse, Felice Daverio, Iain Gardner, Andrew Pike, Michael Paradowski, David C. Blakemore, Gilles H. Goetz, Lesa Watson, Chris Pickford, Jared B.J. Milbank, Ye Che, Robert Wybrow, Florian Wakenhut, Keith Statham, Caroline Smith-Burchnell, Samuel Crook, Fiona M. Adam, David C. Pryde, David Leese, Mike Westby, Duncan Hay, Stephen M. Shaw, Tram T. Tran
Publikováno v:
ChemMedChem. 9:1378-1386
Nonstructural protein 5A (NS5A) represents a novel target for the treatment of hepatitis C virus (HCV). Daclatasvir, recently reported by Bristol-Myers-Squibb, is a potent NS5A inhibitor currently under investigation in phase 3 clinical trials. While
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2f34d031ac0ffb04451e59d88ca8e2e5
https://doi.org/10.1002/cmdc.201400045
https://doi.org/10.1002/cmdc.201400045
Autor:
Charlotte Alice Louise Lane, David Ellis, Rachel Russel, Mathias John Paul, Lesa Watson, James R. Gosset, David James Rawson, Maw Graham Nigel, Street Stephen Derek Albert, Martin Corless, Mark E. Bunnage, Stephen Martin Denton, Kevin Beaumont, Laura Foster, Susan Cole, Stephen Ballard, Marion Floc’h, Jenny Price, William A. Million, Barber Christopher Gordon, Cedric Poinsard, David Leahy, Laura Barker, Frances Holmwood
Publikováno v:
Bioorganic & Medicinal Chemistry. 20:498-509
This paper describes our recent efforts to design and synthesise potent and selective PDE5 inhibitors and the use of in vitro predictors of clearance, absorption and permeability to maximise the potential for dose-proportional pharmacokinetics and go
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d2e73870f13e700ef6c38371fd0684c
https://doi.org/10.1016/j.bmc.2011.10.022
https://doi.org/10.1016/j.bmc.2011.10.022
Autor:
Alan Daniel Brown, Christopher Ronald Smith, Lesa Watson, Dave Ellis, Lindsay Brown, Olga Wallace, Nicholas Puhalo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4278-4281
A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e7274339bfdb8e3e7366e346f4c77841
https://doi.org/10.1016/j.bmcl.2008.06.098
https://doi.org/10.1016/j.bmcl.2008.06.098
Autor:
Florian Wakenhut, Thien Duc Tran, Chris Pickford, Stephen Shaw, Mike Westby, Caroline Smith-Burchnell, Lesa Watson, Michael Paradowski, Jared Milbank, David Stonehouse, Kathy Cheung, Robert Wybrow, Felice Daverio, Samuel Crook, Keith Statham, David Leese, Darren Stead, Fiona Adam, Duncan Hay, Lee R. Roberts, Jean-Yves Chiva, Carly Nichols, David C. Blakemore, Gilles H. Goetz, Ye Che, Iain Gardner, Satish Dayal, Andrew Pike, Rob Webster, David C. Pryde
Publikováno v:
ChemMedChem. 9(7)
In ongoing studies towards novel hepatitis C virus (HCV) therapeutics, inhibitors of nonstructural protein 5A (NS5A) were evaluated. Specifically, starting from previously reported lead compounds, peripheral substitution patterns of a series of biary
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6853494795d71988e823e2d45de7ec55
https://pubmed.ncbi.nlm.nih.gov/24729518
https://pubmed.ncbi.nlm.nih.gov/24729518
Autor:
Christopher Ronald Smith, Nicholas Puhalo, Andrew A. Calabrese, Lindsay Brown, Olga Wallace, Dave Ellis, T. Bruce Brown, Alan Daniel Brown, Lesa Watson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5242-5244
Several potent aryl ether/triazole oxytocin antagonists are described. The lead compound in this series had significantly improved aqueous solubility over related systems containing a biaryl substituent.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c0e7473c8b1c8a93b6fb8cb54a202a15
https://doi.org/10.1016/j.bmcl.2008.08.066
https://doi.org/10.1016/j.bmcl.2008.08.066
Autor:
David C. Pryde, Michelle Y. Platts, Sebastien Galan, Satish Dayal, Lesa Watson, Donald Stuart Middleton, Rob Webster, Helen Bright, Iain Gardner, Tanya Parkinson, Edward J. Murray, Tram T. Tran, Stupple Paul Anthony, Liam Alsop
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(3)
Several non-benzimidazole containing inhibitors of respiratory syncytial virus are described. Core template modification, analysis of antiviral activity, physicochemistry and optimisation of properties led to the thiazole-imidazole 13, that showed a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::652cc900d0f9657bd39f769c96e13871
https://pubmed.ncbi.nlm.nih.gov/23265891
https://pubmed.ncbi.nlm.nih.gov/23265891
Autor:
Andrew A. Calabrese, Dave Ellis, Michael J. Ralph, Alan Daniel Brown, Lesa Watson, Nicholas Puhalo, T. Bruce Brown
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(2)
A series of aryloxyazetidines, aryloxypyrrolidines and aryloxypiperidines were designed based on structural overlap with previously reported arylpyrazine Oxytocin antagonists. Similarly high levels of Oxytocin antagonism were achievable in these new
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bea95352ec099a4104bd9b85a1567819
https://pubmed.ncbi.nlm.nih.gov/19963374
https://pubmed.ncbi.nlm.nih.gov/19963374
Autor:
Martin P. Green, Vivienne Sanderson, Gordon McMurray, Lesa Watson, Edel Evrard, Kevin K.-C. Liu, Michael J. Ralph, Charlotte Moira Norfor Allerton, Robin Ward, David Ellis, Andrews Mark David, Julian Blagg
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(19)
The SAR of a series of pyridazinone derived 5-HT 2C agonists has been explored and resulted in identification of a compound with excellent levels of 5-HT 2C functional agonism and selectivity over 5-HT 2A and 5-HT 2B . This compound displayed good in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f2064b35c0d38ca034a9006643d1e0f
https://pubmed.ncbi.nlm.nih.gov/19716297
https://pubmed.ncbi.nlm.nih.gov/19716297
Autor:
Martin P. Green, Julian Blagg, Lesa Watson, David W. Gordon, Andrews Mark David, Charlotte Moira Norfor Allerton, Gordon McMurray, David V. Batchelor, Alan Daniel Brown, Daniel J. Millns, Carly L. Nichols
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(18)
This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT(2C) agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT(2A) and 5-HT(2B) re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03e0d29dd39906a85b6d7ad4e886b5f6
https://pubmed.ncbi.nlm.nih.gov/19692241
https://pubmed.ncbi.nlm.nih.gov/19692241