Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Helen Oakman"'
Autor:
Saskia M. Brachmann, Simona Cotesta, Anna F. Farago, Frederic Zecri, Kun Xu, Rainer Wilcken, Toni Widmer, Peter Wessels, Hans Voshol, Andrea Vaupel, Rowan Stringer, Toshio Shimizu, Richard Sedrani, Christian Schnell, Danielle Roman, Pascal Rigollier, Johannes Ottl, Nils Ostermann, Helen Oakman, Jason Murphy, Sauveur-Michel Maira, Catherine Leblanc, Jeffrey D. Kearns, Eloísa Jiménez Núñez, Ashley Jaeger, Victoria Head, Daniel Alexander Guthy, Marc Gerspacher, Carmine Fedele, Lekshmi Dharmarajan, Ruben de Kanter, Xiaoming Cui, Xueying Chen, Heather Burks, Claudio Bomio-Confaglia, Kim S. Beyer, Louise Barys, Edwige Lorthiois, Andreas Weiss
Supplementary Data from Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1d58af020ff3289026b12e3df1b9a0f4
https://doi.org/10.1158/2159-8290.22541471.v1
https://doi.org/10.1158/2159-8290.22541471.v1
Autor:
Saskia M. Brachmann, Simona Cotesta, Anna F. Farago, Frederic Zecri, Kun Xu, Rainer Wilcken, Toni Widmer, Peter Wessels, Hans Voshol, Andrea Vaupel, Rowan Stringer, Toshio Shimizu, Richard Sedrani, Christian Schnell, Danielle Roman, Pascal Rigollier, Johannes Ottl, Nils Ostermann, Helen Oakman, Jason Murphy, Sauveur-Michel Maira, Catherine Leblanc, Jeffrey D. Kearns, Eloísa Jiménez Núñez, Ashley Jaeger, Victoria Head, Daniel Alexander Guthy, Marc Gerspacher, Carmine Fedele, Lekshmi Dharmarajan, Ruben de Kanter, Xiaoming Cui, Xueying Chen, Heather Burks, Claudio Bomio-Confaglia, Kim S. Beyer, Louise Barys, Edwige Lorthiois, Andreas Weiss
Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional strategies are needed to improve outcomes. JDQ443 is a structurally unique covalent inhibitor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::090908cffff39039ae33828ed26022f4
https://doi.org/10.1158/2159-8290.c.6549647
https://doi.org/10.1158/2159-8290.c.6549647
Autor:
Andreas Weiss, Edwige Lorthiois, Louise Barys, Kim S. Beyer, Claudio Bomio-Confaglia, Heather Burks, Xueying Chen, Xiaoming Cui, Ruben de Kanter, Lekshmi Dharmarajan, Carmine Fedele, Marc Gerspacher, Daniel Alexander Guthy, Victoria Head, Ashley Jaeger, Eloísa Jiménez Núñez, Jeffrey D. Kearns, Catherine Leblanc, Sauveur-Michel Maira, Jason Murphy, Helen Oakman, Nils Ostermann, Johannes Ottl, Pascal Rigollier, Danielle Roman, Christian Schnell, Richard Sedrani, Toshio Shimizu, Rowan Stringer, Andrea Vaupel, Hans Voshol, Peter Wessels, Toni Widmer, Rainer Wilcken, Kun Xu, Frederic Zecri, Anna F. Farago, Simona Cotesta, Saskia M. Brachmann
Publikováno v:
Cancer Discovery. 12:1500-1517
Covalent inhibitors of KRASG12C have shown antitumor activity against advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and additional strategies are needed to improve outcomes. JDQ443 is a structurally unique covalent inhibitor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a2edd83624df412b8b1d836bfe665fa6
https://doi.org/10.1158/2159-8290.cd-22-0158
https://doi.org/10.1158/2159-8290.cd-22-0158
Autor:
Nicola Arnold, Julie Christie, Sandra Haberthuer, Roger J. Taylor, Alastair Denholm, Mark Keenan, Julia Hatto, Mark Mercer, Lyndon Nigel Brown, Clive Mccarthy, Neil John Press, Helen Oakman, Andrew R. Tuffnell, Morris Tweed, Alexandre Trifilieff, Robert Cheung, Joseph D. Fullerton, Thomas H. Keller, David Beer, Helene Sahri, Pamela Tranter
Publikováno v:
Journal of Medicinal Chemistry. 58:6747-6752
Herein we describe the optimization of a series of PDE4 inhibitors, with special focus on solubility and pharamcokinetics, to clinical compound 2, 4-(8-(3-fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic acid. Although compound 2 produc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f1713cba513710940b786b9defedf19
https://doi.org/10.1021/acs.jmedchem.5b00902
https://doi.org/10.1021/acs.jmedchem.5b00902
Autor:
John R. Fozard, Martin Gosling, David Farr, Lynne Jordan, David A. Sykes, Darryl Brynley Jones, David Beattie, Joe Fullerton, Lyndon Nigel Brown, Julia Hatto, Rachel Profit, Mark Mercer, Diana Janus, Christine Lewis, Helen Oakman, Robin Alec Fairhurst, Friedrich Schuerch, Michelle Bradley, Nicola Arnold, Roger J. Taylor, Janet Maas, Steven J. Charlton, Andrew Brearley, Andrew R. Tuffnell, Alexandre Trifilieff, Clive Mccarthy, Neil John Press
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4341-4347
The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-phenethyl amino-substituents, as inhaled long-acting bronchodilators is described. Analogues were selected for syn
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6783b59db6f184a0eb19d182e169bc4
https://doi.org/10.1016/j.bmcl.2014.06.014
https://doi.org/10.1016/j.bmcl.2014.06.014
Autor:
David Beattie, Christine Lewis, Clive Mccarthy, Darryl Brynley Jones, Andrew R. Tuffnell, Bernard Cuenoud, Robin Alec Fairhurst, Andrew Brearley, Martin Gosling, Helen Oakman, Rowan Stringer, Steven J. Charlton, Roger J. Taylor, Diana Janus, Michelle Bradley, Peter Gedeck
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5302-5307
The chiral synthesis of a 4-hydroxybenzothiazolone based series of β2-adrenoceptor agonists is described. Using this methodology a library of N-substituted analogues were prepared for the rapid identification of leads with the potential to be fast o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a07dbf2769e10012f92d88393c10afb
https://doi.org/10.1016/j.bmcl.2010.06.136
https://doi.org/10.1016/j.bmcl.2010.06.136
Autor:
Robin Alec Fairhurst, James Neef, Brian Cox, Koremu Meja, Robert J. Turner, Paul Kirkham, David Beattie, Ryan West, Steven J. Charlton, Gillian Spooner, Helen Oakman, Zarin Brown, Lana Nanson, Roger J. Taylor, Hannah Woodward, John R. Fozard, Peter Gedeck, Andrew Brearley
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1219-1224
The synthesis of two series of 4'-aza-carbocyclic nucleosides are described in which the 4'-substituent is either a reversed amide, relative to the carboxamide of NECA, or an N-bonded heterocycle. Using established purine substitution patterns, poten
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::de070cc31c79e2dda4cfa38c65e5ab93
https://doi.org/10.1016/j.bmcl.2009.11.131
https://doi.org/10.1016/j.bmcl.2009.11.131
Autor:
Sandra Haberthuer, Trixie Wagner, Lyndon Nigel Brown, Julia Hatto, Nicola Arnold, Clive Mccarthy, Julie Christie, John R. Fozard, Helene Sahri, Helen Oakman, Thomas H. Keller, Roger J. Taylor, Robert Cheung, Mark Keenan, Neil John Press, Joseph D. Fullerton, Andrew R. Tuffnell, Alexandre Trifilieff, John W. Tyler, David Beer, Alastair Denholm, Morris Tweed, Mark Mercer, Pamela Tranter
Publikováno v:
Journal of medicinal chemistry. 55(17)
The solubility-driven optimization of a series of 1,7-napthyridine phosphodiesterase-4 inhibitors is described. Directed structural changes resulted in increased aqueous solubility, enabling superior pharmacokinetic properties with retention of PDE4
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::817ed3d0e78a77ec4c0cc42ee5087e6b
https://pubmed.ncbi.nlm.nih.gov/22889281
https://pubmed.ncbi.nlm.nih.gov/22889281