Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Lubos Remen"'
Autor:
Melanie Kessler, Eric A. Ertel, John Gatfield, Rick D Gaston, Corinna Grisostomi, Thomas Pfeifer, Lubos Remen, Lloyd Simons, Olivier Bezencon, Johannes Mosbacher, Catherine Roch, Richard Moon, Dennis Michael Downing, Markus Rey
Publikováno v:
Journal of Medicinal Chemistry. 59:8398-8411
A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij ra
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f1d15b224e97575ffd39760a63e490e
https://doi.org/10.1021/acs.jmedchem.6b00756
https://doi.org/10.1021/acs.jmedchem.6b00756
Autor:
Corinna Grisostomi, Beat Steiner, Walter Fischli, Patrick Hess, Sylvia Richard-Bildstein, Olivier Corminboeuf, Panja Strickner, Lars Prade, Olivier Bezencon, Lubos Remen, Alexander Treiber, Daniel Bur
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6286-6290
The discovery of a new series of piperidine-based renin inhibitors is described herein. SAR optimization upon the P3 renin sub-pocket is described, leading to the discovery of 9 and 41, two bioavailable renin inhibitors orally active at low doses in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::790d8e7561f139716c99db343d0e8c9e
https://doi.org/10.1016/j.bmcl.2010.08.086
https://doi.org/10.1016/j.bmcl.2010.08.086
Autor:
Volker Jager, Tibor Gracza, Eric Dubois, Thomas Hasenohrl, Walter Hummer, Ulrich Kautz, Bettina Kirschbaum, Albrecht Lieberknecht, Lubos Remen, Duncan Shaw, et al. et al.
Publikováno v:
ChemInform. 30
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::10a5b3e4e4e6b8670f2e899b998d608a
https://doi.org/10.1002/chin.199915337
https://doi.org/10.1002/chin.199915337
Autor:
Christoph Binkert, Panja Strickner, Thierry Sifferlen, Walter Fischli, Stephane Delahaye, Sylvia Richard-Bildstein, Olivier Corminboeuf, Olivier Bezencon, Daniel Bur, Lubos Remen, Alexander Treiber, Corinna Grisostomi, Thomas Weller, Christoph Boss, Beat Steiner, Lars Prade, Patrick Hess
Publikováno v:
Journal of medicinal chemistry. 52(12)
Starting from known piperidine renin inhibitors, a new series of 3,9-diazabicyclo[3.3.1]nonene derivatives was rationally designed and prepared. Optimization of the positions 3, 6, and 7 of the diazabicyclonene template led to potent renin inhibitors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72d2a84c795e1462c8f281d555be392e
https://pubmed.ncbi.nlm.nih.gov/19358611
https://pubmed.ncbi.nlm.nih.gov/19358611
Autor:
Volker Jäger, Tibor Gracza, Eric Dubois, Thomas Hasenöhrl, Walter Hümmer, Ulrich Kautz, Bettina Kirschbaum, Albrecht Lieberknecht, Lubos Remen, Duncan Shaw, Ulrich Stahl, Oliver Stephan
Publikováno v:
Organic Synthesis via Organometallics OSM 5 ISBN: 9783642493508
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::328439628f21b0e253636a8bc12e0c2c
https://doi.org/10.1007/978-3-642-49348-5_21
https://doi.org/10.1007/978-3-642-49348-5_21
Autor:
Lubos Remen, Andrea Vasella
Publikováno v:
Helvetica Chimica Acta. 85:1118
The enol ether 7 was prepared by cleavage of the N−O bond of the known isoxazolidine 3, followed by N-alkylation to 4, silylation and oxidation to the N-oxide 6, and Cope elimination. Cu-Catalysed cyclopropanation of 7 led to the diastereoisomeric
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ca7368d5e558cb0caf3e4581af28c928
https://doi.org/10.1002/1522-2675(200204)85:4<1118::aid-hlca1118>3.0.co
https://doi.org/10.1002/1522-2675(200204)85:4<1118::aid-hlca1118>3.0.co
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