Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Bruno, Capeleto"'
Autor:
Olivier Bezençon, Thomas Pfeifer, Johannes Mosbacher, Isabelle Reymond, Eric A. Ertel, Ruben de Kanter, Bruno Capeleto, Elvire Fournier, Markus Rey, Luca Moccia, Michael Toeroek-Schafroth, René Roscher, Richard Moon, John Gatfield, Melanie Kessler, Romain Siegrist, Bibia Heidmann, Davide Pozzi, Simon Stamm, Luboš Remeň, Sylvia Richard, Lloyd Simons, Rick Gaston, Dennis Downing, Corinna Grisostomi, Catherine Roch, Benno Schindelholz
Publikováno v:
CHIMIA, Vol 71, Iss 10 (2017)
We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemic
Externí odkaz:
https://doaj.org/article/77760779eafd425e854518b6109e1f36
Autor:
Eric A. Ertel, Bruno Capeleto, Sylvia Richard, Olivier Bezencon, Jacques Mawet, Melanie Kessler, Thomas Pfeifer, Catherine Roch, Luboš Remeň, Richard Moon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:5322-5325
We identified and characterized a series of pyrazole amides as potent, selective Ca v 3.1-blockers. This series culminated with the identification of pyrazole amides 5a and 12d , with excellent potencies and/or selectivities toward the Ca v 3.2- and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::239da9b43525ccbdc87df59151643997
https://doi.org/10.1016/j.bmcl.2017.09.063
https://doi.org/10.1016/j.bmcl.2017.09.063
Autor:
Olivier, Bezençon, Luboš, Remeň, Sylvia, Richard, Catherine, Roch, Melanie, Kessler, Eric A, Ertel, Richard, Moon, Jacques, Mawet, Thomas, Pfeifer, Bruno, Capeleto
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(23)
We identified and characterized a series of pyrazole amides as potent, selective Ca
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::d9b2a0a0237f0f2b76d7bcd37b74d58f
https://pubmed.ncbi.nlm.nih.gov/29066309
https://pubmed.ncbi.nlm.nih.gov/29066309
Autor:
Bruno Capeleto, Keith Morrison, Thomas Weller, Marc Iglarz, Changbin Qiu, Christoph Boss, Alexander Treiber, Walter Fischli, Martin Bolli, Christoph Binkert, Patrick Hess, Stephan Buchmann, John Gatfield, Martine Clozel
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 327:736-745
Macitentan, also called Actelion-1 or ACT-064992 [N-[5-(4-bromophenyl)-6-(2-(5-bromopyrimidin-2-yloxy)ethoxy)-pyrimidin-4-yl]-N'-propylaminosulfonamide], is a new dual ET(A)/ET(B) endothelin (ET) receptor antagonist designed for tissue targeting. Sel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::743d04b2a091c2fdebfdd7df5b3dc3b4
https://doi.org/10.1124/jpet.108.142976
https://doi.org/10.1124/jpet.108.142976
Autor:
Davide Pozzi, Olivier Corminboeuf, Eric A. Ertel, Thomas Pfeifer, Catherine Roch, Bibia Heidmann, Ruben de Kanter, Melanie Kessler, Bruno Capeleto, Michael Toeroek-Schafroth, Jacques Mawet, Isabelle Reymond, Simon Stamm, Romain Siegrist, Olivier Bezencon, Richard Moon, Sylvia Richard, Elvire Fournier, Markus Rey, Luca G. Moccia
Publikováno v:
Journal of Medicinal Chemistry. 60:9769
We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15030607383f062e48b3e587859864b3
https://doi.org/10.1021/acs.jmedchem.7b01236
https://doi.org/10.1021/acs.jmedchem.7b01236