Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Christophe Mellon"'
Autor:
Danielle Denis, François G. Gervais, Rino Stocco, Stephen Lau, Birgit Kosjek, Michel Gallant, Vouy Linh Truong, Helmi Zaghdane, Dan Sørensen, Deborah Slipetz, Christophe Mellon, Gary P. O'Neill, Ernest E. Lee, Robert Houle, Yves Leblanc, Carl Berthelette, Daniel Guay, Carmela Molinaro, Jean-François Lévesque, Elizabeth Wong, Jin Wu, Yves Ducharme, Michael A. Crackower, John Colucci, Connie M. Krawczyk, Richard Friesen, Paul D. O’Shea, Nicole Sawyer, Susan Sillaots, Zhaoyin Wang, Christian Beaulieu, Daniel Simard, Chad Dalton, Wayne Mullet, Martine Hamel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:288-293
In this manuscript we wish to report the discovery of MK-7246 (4), a potent and selective CRTH2 (DP2) antagonist. SAR studies leading to MK-7246 along with two synthetic sequences enabling the preparation of this novel class of CRTH2 antagonist are r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62517a8c6d9944543c6229358efce07b
https://doi.org/10.1016/j.bmcl.2010.11.015
https://doi.org/10.1016/j.bmcl.2010.11.015
Autor:
Christophe Mellon, Nathalie Méthot, Deborah A. Nicoll-Griffith, Momar Ndao, Frédéric Massé, Christian Beaulieu, Angélique Fortier, Hyeram Park, W. Cameron Black, Elise Isabel, Doris Lee
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7444-7449
Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease is described. The identified inhibitors bearing an amino nitrile warhead in P1 exhibit low nanomolar in vitro potency against cruzipain. Further SAR in P
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6582e07a38a94405e3fdc8c323756d1
https://doi.org/10.1016/j.bmcl.2010.10.015
https://doi.org/10.1016/j.bmcl.2010.10.015
Autor:
W. Cameron Black, Jean-François Lévesque, Denis Riendeau, Jean-Pierre Falgueyret, Kevin P. Bateman, M. David Percival, Elise Isabel, Tammy LeRiche, Vouy Linh Truong, Jacques Yves Gauthier, Michel Therien, Robert Zamboni, Sevgi B. Rodan, Sylvie Desmarais, Christophe Mellon, Deborah A. Nicoll-Griffith, Renata Oballa, Gregg Wesolowski, Sonia Lamontagne, Carmai Seto, Nathalie Chauret, Chun Sing Li, Robert N. Young, Frédéric Massé, Wanda Cromlish, Daniel J. McKay, Le T. Duong, Cheuk K. Lau, Serge Leger, Joel Robichaud, Gideon A. Rodan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:887-892
MK-0674 is a potent and selective cathepsin K inhibitor from the same structural class as odanacatib with a comparable inhibitory potency profile against Cat K. It is orally bioavailable and exhibits long half-life in pre-clinical species. In vivo st
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::04ce075aa9949065722c92768a34c9f4
https://doi.org/10.1016/j.bmcl.2009.12.083
https://doi.org/10.1016/j.bmcl.2009.12.083
Autor:
Anne Marie Alarco, Dan Sørensen, Arjun H. Banskota, Emmanuel Zazopoulos, Mahmood Piraee, Christophe Mellon, Chris M. Farnet, Henriette Gourdeau, Ashraf S. Ibrahim, Mustapha Aouidate, James B. McAlpine, Pierre Falardeau
Publikováno v:
The Journal of Antibiotics. 62:565-570
The deposited strain of the hazimicin producer, Micromonospora echinospora ssp. challisensis NRRL 12255 has considerable biosynthetic capabilities as revealed by genome scanning. Among these is a locus containing both type I and type II PKS genes. Th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f79a0d9e16cc2bed0225f57ac9043aaf
https://doi.org/10.1038/ja.2009.77
https://doi.org/10.1038/ja.2009.77
Autor:
Andre Giroux, Dita M. Rasper, Steven Xanthoudakis, Johanne Renaud, Rejean Fortin, Christophe Mellon, Erich L. Grimm, John P. Vaillancourt, John Tam, Renee Aspiotis, Yongxin Han, Sophie Roy, W. Cameron Black, John Colucci, Paul Tawa, Robert Zamboni, Elise Isabel, Donald W. Nicholson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1671-1674
Caspase-3 is a cysteinyl protease that mediates apoptotic cell death. Its inhibition may have an important impact on the treatment of several degenerative diseases. Here we report the synthesis of reversible inhibitors via a solid-support palladium-c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce3ef3107740aa2248fa1a467ca00e24
https://doi.org/10.1016/j.bmcl.2006.12.110
https://doi.org/10.1016/j.bmcl.2006.12.110
Autor:
Paul Tawa, M. David Percival, Wanda Cromlish, Kathryn E. Bass, Sylvie Desmarais, Shankar Venkatraman, Sonia Lamontagne, W. Cameron Black, Gregg Wesolowski, Jean-Pierre Falgueyret, Sevgi B. Rodan, Denis Riendeau, Christophe Mellon
Publikováno v:
Analytical Biochemistry. 335:218-227
We describe a novel diazomethylketone-containing irreversible inhibitor (BIL-DMK) which is specific for a subset of pharmaceutically important cysteine cathepsin proteases. BIL-DMK rapidly inactivates cathepsins B, F, K, L, S, and V in isolated enzym
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a84040a1008f6fba5cc76af2791ce2db
https://doi.org/10.1016/j.ab.2004.09.005
https://doi.org/10.1016/j.ab.2004.09.005
Autor:
Mélissa Arbour, Gavin Chit Tsui, Jean-Pierre Falgueyret, Pierre-André Fournier, Yongxin Han, Michel Gallant, Patrick Lacombe, Daniel Dube, Daniel Simard, Elizabeth Cauchon, Austin Chen, Renee Aspiotis, Suzanna Liu, René St-Jacques, Christophe Mellon, Erich L. Grimm, Yeeman K. Ramtohul, Helene Juteau
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(5)
The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC(50), had a clean CYP 3A4 profile and displayed micromo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::72bbcef3547c253b1c7b45e16084feb3
https://pubmed.ncbi.nlm.nih.gov/22325946
https://pubmed.ncbi.nlm.nih.gov/22325946
Autor:
Elise Isabel, Christophe Mellon, Michael J. Boyd, Nathalie Chauret, Denis Deschênes, Sylvie Desmarais, Jean-Pierre Falgueyret, Jacques Yves Gauthier, Karine Khougaz, Cheuk K. Lau, Serge Léger, Dorothy A. Levorse, Chun Sing Li, Frédéric Massé, M. David Percival, Bruno Roy, John Scheigetz, Michel Thérien, Vouy Linh Truong, Gregg Wesolowski, Robert N. Young, Robert Zamboni, W. Cameron Black
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(3)
The trifluoroethylamine group found in cathepsin K inhibitors like odanacatib can be replaced by a difluoroethylamine group. This change increased the basicity of the nitrogen which positively impacted the log D. This translated into an improved oral
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f7ac2065bec9654d54655621ebfc7a4
https://pubmed.ncbi.nlm.nih.gov/21232956
https://pubmed.ncbi.nlm.nih.gov/21232956
Autor:
M. David Percival, Alain Veilleux, W. Cameron Black, Jean-Pierre Falgueyret, Paul Tawa, Jacques Yves Gauthier, Christophe Mellon
Publikováno v:
Analytical biochemistry. 411(1)
Using the cell-permeable, radioiodinated, irreversible inhibitor BIL-DMK, we probed active cysteine cathepsins in blood. Incubation of the probe in human whole blood followed by separation of white blood cells by dextran sedimentation led to the labe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dd6919f67d5fc42e6190d5270955dd2
https://pubmed.ncbi.nlm.nih.gov/21094118
https://pubmed.ncbi.nlm.nih.gov/21094118
Autor:
Erika Vigneault, Rino Stocco, Julie Farand, Daigen Xu, Marc Blouin, Steve Rowland, Marie-Claude Mathieu, Mireille Gaudreault, Jean-François Lévesque, Yongxin Han, Alex G. Therien, Jason Burch, R. W. Friesen, Danielle Denis, Yves Ducharme, Mark Wrona, Patsy Clark, Christophe Mellon, Gary P. O'Neill
Publikováno v:
Journal of medicinal chemistry. 53(5)
The discovery of highly potent and selective second generation EP(4) antagonist MK-2894 (34d) is discussed. This compound exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9aae4dd330bf132835f31b8767df9cc2
https://pubmed.ncbi.nlm.nih.gov/20163116
https://pubmed.ncbi.nlm.nih.gov/20163116