Zobrazeno 1 - 10
of 31
pro vyhledávání: '"J. Richard Morphy"'
Autor:
Jack Pick, Mark Craighead, Heather A. Zanetakos, Jeffrey J. Letourneau, Rachel Milne, Hema Desai, Leigh Campbell-Wan, Jeremy Presland, Michael Ohlmeyer, James R. Baker, Nasrin Ansari, Ray Jui-Hsiang Chan, Cliona P MacSweeney, Douglas S. Auld, Maria L. Webb, Jiuqiao Zhao, Chris Riviello, J. Richard Morphy, Stuart A. Best, Irina Neagu, Susan Elizabeth Napier, Koc-Kan Ho
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3813-3817
Synthesis and structure–activity relationships (SAR) of a novel series of vasopressin V1b antagonists are described. 2-(6-Aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide have been identified with low nanomolar affinity for the V1b recept
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::644306305bb4a232c2c9422c904af22d
https://doi.org/10.1016/j.bmcl.2011.04.022
https://doi.org/10.1016/j.bmcl.2011.04.022
Autor:
Richard Goodwin, Fiona Thomson, John W. Clark, Brad Sherborne, Lynn Watson, Angus R. Brown, Morag Grassie, Jack Pick, Angela Cowley, Olaf Nimz, J. Richard Morphy, Lorraine McIntosh, Niall M. Hamilton, Littlewood Peter Thomas Albert, Alasdair Smith, Koc-Kan Ho, Michael Speake, Alison Hillier, Ashvin Mistry, Michael Bosies, Simon James Anthony Grove, Mark Craighead, Theresa McIntyre, Michael Kiczun, Grant Emma Jane, Moira A. Elmore, Hannah Hampson, Mark Weston, Susan MacDonald, Susan Goutcher, Scott J. Lusher, Gayle Spinks, Zoran Rankovic, Michael Ohlmeyer, Helen Cameron, Alistair Firth, Steven G. Kultgen, Celia Kingsbury
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:137-140
High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d62da153327bd28fcc24657573e661d2
https://doi.org/10.1016/j.bmcl.2010.11.054
https://doi.org/10.1016/j.bmcl.2010.11.054
Autor:
Andrew G. Cole, Douglas S. Auld, Riviello Christopher, Hema Desai, Hong Li, Heather A. Zanetakos, Fiona Thomson, J. Richard Morphy, Jiuqiao Zhao, Susan Elizabeth Napier, Michael Ohlmeyer, Katharine A. Goan, Koc-Kan Ho, Maria L. Webb, Jeffrey J. Letourneau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5394-5397
The discovery, synthesis, and preliminary structure–activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse, three million-member compo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::af9cd65c56eed38d36dbec9326862276
https://doi.org/10.1016/j.bmcl.2010.07.118
https://doi.org/10.1016/j.bmcl.2010.07.118
Autor:
J. Richard Morphy
Publikováno v:
Attrition in the Pharmaceutical Industry: Reasons, Implications, and Pathways Forward
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d673b5f15dde3aa9129e2c466c3d42c
https://doi.org/10.1002/9781118819586.ch8
https://doi.org/10.1002/9781118819586.ch8
Autor:
Zoran Rankovic, Hardy Sundaram, Guizhen Dong, Maria L. Webb, Edward Mcdonald, Adolph Bohnstedt, Tao Guo, Koc-Kan Ho, Steven G. Kultgen, Christopher M. Masterson, Khondaker R. Islam, Robert A. Horlick, J. Richard Morphy, Baldwin John J, Kirk Mcmillan, Kenneth C. Appell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:545-548
Structure-activity studies on benzamide 1 obtained from library screening led to the discovery of a novel series of potent and selective glycine transporter type-2 inhibitors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::384842067b150363b62c90e14d82e7aa
https://doi.org/10.1016/j.bmcl.2003.09.080
https://doi.org/10.1016/j.bmcl.2003.09.080
Publikováno v:
Tetrahedron. 59:2137-2145
The use of reagent concentration has resulted in increased rates for all stages of the REM resin synthesis of tertiary amines. These increases in rate translate into faster reaction times, higher yields and lower reagent consumption. Of the methods e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::45eda34931c8aeac6d30e53a324c10bf
https://doi.org/10.1016/s0040-4020(03)00176-5
https://doi.org/10.1016/s0040-4020(03)00176-5
Publikováno v:
Journal of Combinatorial Chemistry. 4:199-203
A study into the effect of reaction variables on the quaternization of REM resin-bound tertiary amines was undertaken. The influence of resin matrix, solvent, reaction time, temperature, and amount of quaternization agent on the outcome of reaction w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0e148177a0a8f9da1e494795561b38a
https://doi.org/10.1021/cc010059h
https://doi.org/10.1021/cc010059h
Autor:
J. Richard Morphy, C John Harris
Multi-target drug discovery (MTDD) is an emerging area of increasing interest to the drug discovery community. Drugs that modulate several targets have the potential for an improved balance of efficacy and safety compared to single targets agents. Al
Publikováno v:
Journal of the American Chemical Society. 119:3288-3295
A range of tertiary amines was constructed using a “traceless” linker on a polystyrene resin (REM resin), starting from secondary amines, primary amines, and resin-bound “ammonia”. The methodology is characterized by three essential steps con
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::487c8184efc0d0d7388e09a4bedb05f2
https://doi.org/10.1021/ja963829f
https://doi.org/10.1021/ja963829f