Zobrazeno 1 - 10
of 59
pro vyhledávání: '"Louis Grenier"'
Autor:
Christian M. Martin, Jennifer Proctor, Patrick O'Hearn, Janid A. Ali, Andre Lescarbeau, Jennifer Hoyt, Jonathan P. DiNitto, Ann M. Rowley, Thomas T. Tibbitts, Catherine A. Evans, Martin R. Tremblay, Tao Liu, Vito J. Palombella, John Soglia, Johan A. Pradeilles, Somarajan J. Nair, Melissa Pink, David G. Winkler, Stanley Goldstein, Quentin Glenadel, Erin L. O’Hearn, Culver Cheung, Erin Brophy, Alfredo C. Castro, Louis Grenier
Publikováno v:
ACS Medicinal Chemistry Letters. 7:862-867
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust
Autor:
Michael Foley, Andre Lescarbeau, Martin R. Tremblay, Lombardy Richard John, Grogan Michael John, Andrew B. Hague, Kristopher M. Depew, Jimin Xiong, Joseph Helble, Priscilla L. White, Julian Adams, Brian C. Austad, Caroline D. Lory, Somarajan J. Nair, Stéphane Peluso, Lin-Chen Yu, Alfredo C. Castro, André B. Charette, Benjamin S. Lane, Jeanne Shaffer, Louis Grenier, James R. Porter, Matthew Campbell, Koney Nii O, Mark L. Behnke
Publikováno v:
Organic Process Research & Development. 20:786-798
The formation of the d-homocyclopamine ring system in IPI-926 is the key step in its semisynthesis and proceeds via a chemoselective cyclopropanation followed by a stereoselective acid-catalyzed carbocation rearrangement. In order to perform large-sc
Autor:
Martin Trudeau, Louis Grenier, Kristopher M. Depew, Daniel G. Genov, Alexandre Côté, Brian C. Austad, Lin-Chen Yu, Andre Lescarbeau, Theodore A. Martinot, Priscilla L. White, Joseph Helble, Somarajan J. Nair
Publikováno v:
Organic Process Research & Development. 19:1693-1702
A design of experiments (DoE) approach was taken to optimize purity and reaction yield of the final debenzylation and hydrochloride salt formation of IPI-926. The study involved a careful dissection of the different process steps to enable an indepen
Autor:
John Lee, Roger H. Pak, Louis Grenier, Vince Ammoscato, Michael Curtis, Kaiming Li, John Henderson, Matthew Campbell, Denise Mayes, Jason Kropp, Natalie Goltz, Bennett Carter, Johan Sebastian Basuki, Bradley Maurer, Gary Baker, James R. Wright, David Rusch, Rebecca Ahn, Brian C. Austad, Kris Depew, Joseph Helble, Jie Ge, Jason J. Piotrowski, Marlene R. Booth, Julian Adams, Mark Douglas, Steven G. Wong, Laila Kott, James R. Porter, Geoff E. Sylvester, Dumitru Ionescu, Jennifer R. Porter, Brendan Arsenault
Publikováno v:
Drug Development Research. 71:429-438
IPI-504 (retaspimycin hydrochloride) is an Hsp90 inhibitor that is the subject of multiple clinical trials for the treatment of cancer. IPI-504 is an aqueous soluble (>200 mg/ml) hydroquinone hydrochloride salt of 17-(allylamino)-17-demethoxygeldanam
Autor:
Matthew Campbell, Caroline N. Woodward, Jens Sydor, Alfredo C. Castro, James R. Porter, Margaret A. Read, Kerrie Faia, Kerry White, Martin R. Tremblay, Jill Cushing, Julian Adams, Lin-Chen Yu, Mark L. Behnke, Jennifer Hoyt, Vito J. Palombella, Karen McGovern, Somarajan J. Nair, Jeffrey K. Tong, Margit Hagel, Marta Nevalainen, Louis Grenier, Michael Foley
Publikováno v:
Journal of Medicinal Chemistry. 51:6646-6649
Herein is reported the synthesis of a novel class of hedgehog antagonists derived from cyclopamine. The acid sensitive D-ring of cyclopamine was homologated utilizing a sequence of chemoselective cyclopropanation and stereoselective acid-catalyzed re
Autor:
Roger H. Pak, Louis Grenier, Julian Adams, Jeffrey K. Tong, James D. Wright, Janid A. Ali, Courtney Penders, Emmanuel Normant, Jens R. Sydor, Jon S. Patterson, Melissa Pink, Jie Ge, Jebecka Hudak, Marlene Dembski, Yilong Zhang, Jim Sang, Christine S. Pien, Caroline N. Woodward, James R. Porter, Margaret Read, John A. Barrett, David Grayzel, Vito J. Palombella
Publikováno v:
Proceedings of the National Academy of Sciences. 103:17408-17413
Heat shock protein 90 (Hsp90) is an emerging therapeutic target of interest for the treatment of cancer. Its role in protein homeostasis and the selective chaperoning of key signaling proteins in cancer survival and proliferation pathways has made it
Autor:
Marie Simard, Pierrette Gourde, Denis Beauchamp, Louise Thibault, Louis Grenier, Isabelle Plante, Michel LeBrun, Gaston Labrecque, Marianne Pons
Publikováno v:
Journal of Renal Nutrition. 13:84-92
The objective of the present study was to look at the effect of a protein-rich diet on cyclosporine A (CsA)-induced acute nephrotoxicity in rodents using markers of tubular damage.Female Sprague-Dawley rats were conditioned to either a standard or a
Autor:
Louis Grenier, Marc Ouellette, François J. Picard, Michel G. Bergeron, Paul H. Roy, Francis Martineau
Publikováno v:
Journal of Antimicrobial Chemotherapy. 46:527-534
Multiresistant staphylococci (82 Staphylococcus aureus and 114 coagulase-negative staphylococci) were characterized by testing with rapid multiplex polymerase chain reaction (PCR) assays for species identification and detection of associated antibiot
Autor:
Julian Adams, Teresa A. McCormack, Francois Soucy, Louis Grenier, Mark L. Behnke, Louis Plamondon, Antonia T. Destree
Publikováno v:
Journal of the American Chemical Society. 121:9967-9976
Herein, we describe a new convergent synthesis of a more potent analogue of clasto-lactacystin β-lactone (2), PS-519 compound 4, which is currently in preclinical development for the treatment of i...
Autor:
Louis Plamondon, Shaowu Chen, Janice M. Klunder, Amy A. Cruickshank, Julian Adams, Yu-Ting Ma, Lawrence R. Dick, Mark L. Behnke, Louis Grenier, Ross L. Stein
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:333-338
Potent and selective dipeptidyl boronic acid proteasome inhibitors are described. As compared to peptidyl aldehyde compounds, boronic acids in this series display dramatically enhanced potency. Compounds such as 15 are promising new therapeutics for