Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Han Min, Tong"'
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Thomas M. Bridges, Claire Mackie, María Luz Martín-Martín, Miguel-Angel Pena, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Han Min Tong, Hilde Lavreysen, J. Scott Daniels, Sergio A. Alonso de Diego, Jesús Alcázar, P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:429-434
As part of our efforts to identify a suitable back-up compound to our recently disclosed mGlu5 positive allosteric modulator (PAM) clinical candidate VU0490551/JNJ-46778212, this letter details the investigation and challenges of a novel series of 6,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0c3b86aa42123689c0f8547589986f3f
https://doi.org/10.1016/j.bmcl.2015.11.098
https://doi.org/10.1016/j.bmcl.2015.11.098
Autor:
Carlos M. Martínez-Viturro, Colleen M. Niswender, Han Min Tong, Meredith J. Noetzel, Gregor James Macdonald, Susana Conde-Ceide, Carrie K. Jones, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, P. Jeffrey Conn, Shaun R. Stauffer, Craig W. Lindsley, María Luz Martín-Martín, Thomas M. Bridges, J. Scott Daniels, Hilde Lavreysen, Silvia López, Sergio A. Alonso de Diego
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1310-1317
We report the discovery and SAR of two novel series of imidazopyrimidinones and dihydroimidazopyrimidinones as metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs). Exploration of several structural features in the western
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e4a364a4c4741589a3db21524a2a658a
https://doi.org/10.1016/j.bmcl.2015.01.038
https://doi.org/10.1016/j.bmcl.2015.01.038
Autor:
Shaun R. Stauffer, Thomas M. Bridges, J. Scott Daniels, Meredith J. Noetzel, Hilde Lavreysen, Colleen M. Niswender, Craig W. Lindsley, P. Jeffrey Conn, Han Min Tong, Susana Conde-Ceide, José Manuel Bartolomé-Nebreda, Thomas Steckler, Carrie K. Jones, Paige N. Vinson, Gregor James Macdonald, Claire Mackie, Mark Turlington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3641-3646
We report the optimization of a series of novel metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs) from a 5,6-bicyclic class of dihydropyrazolo[1,5-a]pyridin-4(5H)-ones containing a phenoxymethyl linker. Studies focused o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::570caf0830a9486752156fe572e3bde1
https://doi.org/10.1016/j.bmcl.2014.04.087
https://doi.org/10.1016/j.bmcl.2014.04.087
Autor:
Jason Manka, Hilde Lavreysen, Colleen M. Niswender, Jon Jacobs, M. Luz Martín-Martín, P. Jeffrey Conn, Meredith J. Noetzel, Han Min Tong, Elizabeth J. Herman, C. David Weaver, Chrysa Malosh, J. Scott Daniels, Susana Conde-Ceide, Paige N. Vinson, Shaun R. Stauffer, Gregor James Macdonald, Claire Mackie, José Manuel Bartolomé-Nebreda, Thomas Steckler, Silvia López, Craig W. Lindsley, Carrie K. Jones, Satyawan Jadhav, Mark Turlington
Publikováno v:
Journal of Medicinal Chemistry. 57:5620-5637
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ec9e09891e97fb3e6b29c5a56f045fdf
https://doi.org/10.1021/jm500259z
https://doi.org/10.1021/jm500259z
Autor:
José Manuel Bartolomé-Nebreda, Marijke Somers, Laura Iturrino, Greet Vanhoof, Joaquín Pastor, Susana Conde-Ceide, María Luz Martín-Martín, Xavier Langlois, Gregor James Macdonald, Anton Megens, Francisca Delgado, Wendy Sanderson, Carlos M. Martínez-Viturro, Han Min Tong
Publikováno v:
Journal of Medicinal Chemistry. 57:4196-4212
We report the discovery of a series of imidazo[1,2-a]pyrazine derivatives as novel inhibitors of phosphodiesterase 10A (PDE10A). In a high-throughput screening campaign we identified the imidazopyrazine derivative 1, a PDE10A inhibitor with limited s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12ac9ae359ff0523ce350342854294aa
https://doi.org/10.1021/jm500073h
https://doi.org/10.1021/jm500073h
Autor:
Michiel Van Gool, Francisca Delgado, Oscar Delgado, Carlos M. Martínez-Viturro, Miguel Ángel Pena, Sergio A. Alonso de Diego, Greet Vanhoof, Marta Artola, Gregor James Macdonald, José Manuel Bartolomé-Nebreda, María Luz Martín-Martín, Xavier Langlois, José Manuel Alonso, Han Min Tong, Susana Conde-Ceide, Anton Megens, Marijke Somers, Alberto Fontana
We report the continuation of a focused medicinal chemistry program aimed to further optimize a series of imidazo[1,2-a]pyrazines as a novel class of potent and selective phosphodiesterase 10A (PDE10A) inhibitors. In vitro and in vivo pharmacokinetic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::752a138a2d02674e482528380d513b5e
https://hdl.handle.net/1887/3203217
https://hdl.handle.net/1887/3203217
Autor:
Mark, Turlington, Chrysa, Malosh, Jon, Jacobs, Jason T, Manka, Meredith J, Noetzel, Paige N, Vinson, Satyawan, Jadhav, Elizabeth J, Herman, Hilde, Lavreysen, Claire, Mackie, José M, Bartolomé-Nebreda, Susana, Conde-Ceide, M Luz, Martín-Martín, Han Min, Tong, Silvia, López, Gregor J, MacDonald, Thomas, Steckler, J Scott, Daniels, C David, Weaver, Colleen M, Niswender, Carrie K, Jones, P Jeffrey, Conn, Craig W, Lindsley, Shaun R, Stauffer
Publikováno v:
Journal of Medicinal Chemistry
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicycli
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::4df281b61dd2aa143b71583ecf87d1c8
https://pubmed.ncbi.nlm.nih.gov/24914612
https://pubmed.ncbi.nlm.nih.gov/24914612
Publikováno v:
Tetrahedron Letters. 46:6015-6017
A stereoselective total synthesis of the core unit of pseudodistomin D, starting from l -serine, is described. The key step is a stereoselective intramolecular Michael reaction in which the piperidine ring is formed with the obtention of 1 .
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d638a638eb1c8e056a3889bf0c02da9
https://doi.org/10.1016/j.tetlet.2005.07.014
https://doi.org/10.1016/j.tetlet.2005.07.014
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Publikováno v:
Organic letters. 7(12)
[reaction: see text] A short synthesis of intermediates possessing the tricyclic core of natural madangamines, bioactive alkaloids found in marine sponges, is described. The key reaction entails the condensation of the sodium salt of diethylacetonedi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee456f98375e65a5299b043068023dea
https://pubmed.ncbi.nlm.nih.gov/15932217
https://pubmed.ncbi.nlm.nih.gov/15932217