Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Angela Patikis"'
Autor:
Stefan Senger, Máire A. Convery, Robert J. Young, Stephanie Irvine, Iain M. McLay, Robert I. West, David J. Belton, Savvas Kleanthous, Carl Adams, John R. Toomey, Anne M. Exall, Anthony J. Pateman, Theresa J. Roethke, Caroline M. Whittaker, Laiq Chaudry, David E. Davies, Angela Patikis, Cynthia L. Burns-Kurtis, Nigel S. Watson, Gary J. Stelman, David W. Brown, John D. Harling, Wendy R. Irving, Chuen Chan, Ping Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1588-1592
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dff85f937ce4e89e1a2bcffaac9ddca4
https://doi.org/10.1016/j.bmcl.2011.01.129
https://doi.org/10.1016/j.bmcl.2011.01.129
Autor:
Anthony J. Pateman, John R. Toomey, Paul F. Koster, Augustin Amour, Saul Needle, Laiq Chaudry, Melanie A Abboud, Champa Patel, Angela Patikis, Cynthia L. Burns-Kurtis, Robert J. Young, Richard E. Valocik, David Brown, Ping Zhou, Chuen Chan, Nigel S. Watson
Publikováno v:
Journal of Cardiovascular Pharmacology. 52:66-71
Background: Factor Xa (FXa) has been a target of considerable interest for drug development efforts aimed at suppressing thrombosis. In this report, a new orally active, small molecule, active-site directed FXa inhibitor, GW813893, has been profiled
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e4ecf88e87e341213f5fef72bbcb248
https://doi.org/10.1097/fjc.0b013e31817e9b9e
https://doi.org/10.1097/fjc.0b013e31817e9b9e
Autor:
Alan D. Borthwick, Marie Charbaut, Robert J. Young, Máire A. Convery, Ivan Leo Pinto, Andrew M. Mason, Weston Helen Elisabeth, Matthew Campbell, David W. Brown, Anthony J. Pateman, Henry Anderson Kelly, Derek Pollard, Shah Gita Punjabhai, John R. Toomey, N. Paul King, Stefan Senger, Eric Hortense, Ping Zhou, Hawa Diallo, Nigel S. Watson, Wendy R. Irving, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Chuen Chan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:28-33
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating basic biaryl P4 groups, producing highly potent inhibitors with significant anticoagulant activitie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03145f782eb525e093f927857c7919cd
https://doi.org/10.1016/j.bmcl.2007.11.019
https://doi.org/10.1016/j.bmcl.2007.11.019
Autor:
Robert J. Young, David W. Brown, Stefan Senger, Chuen Chan, Máire A. Convery, Anthony J. Pateman, Nigel S. Watson, John R. Toomey, Ping Zhou, Henry Anderson Kelly, Shah Gita Punjabhai, Julia A. Hubbard, Angela Patikis, Cynthia L. Burns-Kurtis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2927-2930
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhib
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::29c69eec9dfca70c859103d7b56e8c3a
https://doi.org/10.1016/j.bmcl.2007.03.080
https://doi.org/10.1016/j.bmcl.2007.03.080
Autor:
James Michael Woolven, Eugene T. Grygielko, Françoise Gellibert, Neil Mathews, Stéphane Huet, Nicholas J. Laping, Angela Patikis, Cécile Bertho-Ruault, Anne-Charlotte de Gouville, Van-Loc Nguyen
Publikováno v:
Journal of Medicinal Chemistry. 49:2210-2221
Inhibitors of transforming growth factor beta (TGF-beta) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::114d01271eafa1afb68f20a7a2c7cc1a
https://doi.org/10.1021/jm0509905
https://doi.org/10.1021/jm0509905
Autor:
and Martin J. Slater, J. Ed Robinson, Martin R. Johnson, Gail Mills, S. Lucy Hind, Tony J. Pateman, Tracy Jane Redfern, David M. Andrews, Paul Spencer Jones, Naimisha Trivedi, Angela Patikis, Michael C. Barnes, Mike D. Dowle
Publikováno v:
Organic Letters. 5:4631-4634
[reaction: see text] In this, the second of two Letters, the optimization of the pyrrolidine-5,5-trans-lactam template (exemplified by 1a) as a mechanism-based inhibitor of hepatitis C NS3/4A protease is described. "Right Box" analysis of cassette do
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38887863b133f85a34524a3302dbc5da
https://doi.org/10.1021/ol035827n
https://doi.org/10.1021/ol035827n
Autor:
Deborah L. Jackson, Graham J Hart, Angela Patikis, Gordon G. Weingarten, Nigel R. Parry, Alan D. Borthwick, James Michael Woolven, Terry M. Haley, Dave E. Davies, Anne M. Exall, Peter Franz Ertl, Naimisha Trivedi
Publikováno v:
Journal of Medicinal Chemistry. 46:4428-4449
A series of chiral, (S)-proline-alpha-methylpyrrolidine-5,5-trans-lactam serine protease inhibitors has been developed as antivirals of human cytomegalovirus (HCMV). The SAR of the functionality on the proline nitrogen has shown that derivatives of p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c2b6a73dae4a667f9c1ac9169b95e88
https://doi.org/10.1021/jm030810w
https://doi.org/10.1021/jm030810w
Autor:
Naimisha Trivedi, Martin R. Johnson, Angela Patikis, David M. Andrews, Paul Spencer Jones, S. Lucy Hind, Mike D. Dowle, Martin John Slater, J. Ed Robinson, Helene M. Chaignot, Coomber Ba, Tony J. Pateman, Gail Mills
Publikováno v:
European Journal of Medicinal Chemistry. 38:339-343
The pyrrolidine-5,5-trans-lactam template was used to design small, neutral, mechanism-based inhibitors of hepatitis C NS3/4A protease displaying potent activity in the replicon cell-based assay. The activity of this series is not dependent upon its
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d76fe97b2add8009252258f35d3b2874
https://doi.org/10.1016/s0223-5234(03)00050-3
https://doi.org/10.1016/s0223-5234(03)00050-3
Autor:
Máire A. Convery, Stephanie Irvine, Graham Foster, Mike Blows, Robert J. Young, Steve Jackson, Stefan Senger, Angela Patikis, Eric Hortense, Cynthia L. Burns-Kurtis, John R. Toomey, Carl Adams, Savvas Kleanthous, Gary J. Stelman, David W. Brown, John D. Harling, Nigel S. Watson, Ping Zhou, Robert I. West, Wendy R. Irving, Anne M. Exall, Theresa J. Roethka, David E. Davies, Anthony J. Pateman, Chuen Chan, Laiq Chaudry, Caroline M. Whittaker
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
The rational design, syntheses and evaluation of potent sulfonamidopyrrolidin-2-one-based factor Xa inhibitors incorporating aminoindane and phenylpyrrolidine P4 motifs are described. These series delivered highly potent anticoagulant compounds with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a38372eac43a80c90c25beb16d8fc57
https://pubmed.ncbi.nlm.nih.gov/21349710
https://pubmed.ncbi.nlm.nih.gov/21349710
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with biaryl P4 motifs
Autor:
N. Paul King, Stefan Senger, Matthew Campbell, Henry Anderson Kelly, Máire A. Convery, David W. Brown, Shah Gita Punjabhai, Angela Patikis, Cynthia L. Burns-Kurtis, Savvas Kleanthous, Marie Charbaut, Alan D. Borthwick, Ivan Leo Pinto, Weston Helen Elisabeth, John R. Toomey, Chuen Chan, Chun-wa Chung, Robert J. Young, Nigel S. Watson, Derek Pollard, Andrew M. Mason, Anthony J. Pateman
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(1)
Structure and property based drug design was exploited in the synthesis of sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups, producing highly potent inhibitors with encouraging oral pharmacokinetic profiles
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15050912d1dc4249e4e1cc6903a7abeb
https://pubmed.ncbi.nlm.nih.gov/18054228
https://pubmed.ncbi.nlm.nih.gov/18054228