Carol Bachand
Bristol-Myers Squibb
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Publication
Featured researches published by Carol Bachand.
Journal of Medicinal Chemistry | 2014
Makonen Belema; Van N. Nguyen; Carol Bachand; Dan H. Deon; Jason Goodrich; Clint A. James; Rico Lavoie; Omar D. Lopez; Alain Martel; Jeffrey L. Romine; Edward H. Ruediger; Lawrence B. Snyder; Denis R. St. Laurent; Fukang Yang; Juliang Zhu; Henry S. Wong; David R. Langley; Stephen P. Adams; Glenn H. Cantor; Anjaneya Chimalakonda; Aberra Fura; Benjamin M. Johnson; Jay O. Knipe; Dawn D. Parker; Kenneth S. Santone; Robert A. Fridell; Julie A. Lemm; Donald R. O’Boyle; Richard J. Colonno; Min Gao
The biphenyl derivatives 2 and 3 are prototypes of a novel class of NS5A replication complex inhibitors that demonstrate high inhibitory potency toward a panel of clinically relevant HCV strains encompassing genotypes 1-6. However, these compounds exhibit poor systemic exposure in rat pharmacokinetic studies after oral dosing. The structure-activity relationship investigations that improved the exposure properties of the parent bis-phenylimidazole chemotype, culminating in the identification of the highly potent NS5A replication complex inhibitor daclatasvir (33) are described. An element critical to success was the realization that the arylglycine cap of 2 could be replaced with an alkylglycine derivative and still maintain the high inhibitory potency of the series if accompanied with a stereoinversion, a finding that enabled a rapid optimization of exposure properties. Compound 33 had EC50 values of 50 and 9 pM toward genotype-1a and -1b replicons, respectively, and oral bioavailabilities of 38-108% in preclinical species. Compound 33 provided clinical proof-of-concept for the NS5A replication complex inhibitor class, and regulatory approval to market it with the NS3/4A protease inhibitor asunaprevir for the treatment of HCV genotype-1b infection has recently been sought in Japan.
Bioorganic & Medicinal Chemistry | 2001
Anne Marinier; Alain Martel; Carol Bachand; Serge Plamondon; Brigitte Turmel; Jean-Paul Daris; Jacques Banville; Philippe Lapointe; Carl Ouellet; Pierre Dextraze; Marcel Menard; John J Wright; Julie Alford; Debbie Lee; Paul L. Stanley; Xina Nair; Gordon Todderud; Kenneth M. Tramposch
A series of potent inhibitors of P-selectin as potential anti-inflammatory agents is reported. These compounds are derivatives of galactocerebrosides bearing a malonate side chain in positions 2 and 3 of the galactose moiety. Based on the binding mode of sialyl Lewis X, the two acidic groups of the malonate are designed to form ionic interactions with two important lysines in the active site of P-selectin, Lys113 and Lys111. On the other hand, the 4- and 6-hydroxy groups on the galactose ring are arranged to chelate the calcium ion in the P-selectin active site. The synthesis and the biological activity of this series of compounds are described. Lead compounds having a greater potency than sialyl Lewis X are identified.
Tetrahedron | 1995
Philippe Remuzon; Daniel Bouzard; Pierre Dicesare; Munir Essiz; Jean-Pierre Jacquet; Andrei Nicolau; Alain Martel; Marcel Menard; Carol Bachand
Abstract An efficient and stereocontrolled preparation of the key a/etidinone-acid 5a is described.
Archive | 2003
Tao Wang; John F. Kadow; Nicholas A. Meanwell; Kap-Sun Yeung; Zhongxing Zhang; Zhiwei Yin; Zhilei Qiu; Daniel H. Deon; Clint A. James; Edward H. Ruediger; Carol Bachand
Archive | 2009
Carol Bachand; Makonen Belema; Daniel H. Deon; Andrew C. Good; Jason Goodrich; Clint A. James; Rico Lavoie; Omar D. Lopez; Alain Martel; Nicholas A. Meanwell; Van N. Nguyen; Jeffrey L. Romine; Edward H. Ruediger; Lawrence B. Snyder; R Laurent Denis; Fukang Yang; David R. Langley; Gan Wang; Lawrence G. Hamann
Journal of Medicinal Chemistry | 2005
Mark G. Saulnier; Balu Balasubramanian; Byron H. Long; David B. Frennesson; Edward H. Ruediger; Kurt Zimmermann; Jeffrey Eummer; Denis R. St. Laurent; Karen Stoffan; B. Narasimhulu Naidu; Mikael Mahler; Francis Beaulieu; Carol Bachand; Frank Y. Lee; Craig R. Fairchild; Linda K. Stadnick; William C. Rose; Carola Solomon; Henry Wong; Alain Martel; John J. Wright; Robert Kramer; David R. Langley; Dolatrai M. Vyas
Journal of Medicinal Chemistry | 2004
Balu Balasubramanian; Denis R. St. Laurent; Mark G. Saulnier; Byron H. Long; Carol Bachand; Francis Beaulieu; Wendy Clarke; Milind Deshpande; Jeffrey Eummer; Craig R. Fairchild; David B. Frennesson; Robert Kramer; Frank Y. Lee; Mikael Mahler; Alain Martel; B. Narasimhulu Naidu; William C. Rose; John W. Russell; Edward H. Ruediger; Carola Solomon; Karen Stoffan; Henry Wong; Kurt Zimmermann; Dolatrai M. Vyas
Archive | 2008
Carol Bachand; Makonen Belema; Daniel H. Deon; Andrew C. Good; Jason Goodrich; Clint A. James; Rico Lavoie; Omar D. Lopez; Alain Martel; Nicholas A. Meanwell; Van N. Nguyen; Jeffrey L. Romine; Edward H. Ruediger; Lawrence B. Snyder; R Laurent Denis; Fukang Yang; David R. Langley; Gan Wang; Lawrence G. Hamann
Journal of Pharmacology and Experimental Therapeutics | 1997
Gordon Todderud; Xina Nair; Debbie Lee; Julie Alford; Lynda B. Davern; Paul L. Stanley; Carol Bachand; Philippe Lapointe; Anne Marinier; Alain Martel; Marcel Menard; John J. Wright; Jürgen Bajorath; Diane Hollenbaugh; Alejandro Aruffo; Kenneth M. Tramposch
Journal of Medicinal Chemistry | 1997
Anne Marinier; Alain Martel; Jacques Banville; Carol Bachand; R. Remillard; Philippe Lapointe; Brigitte Turmel; Marcel Menard; W. E. Harte; John J Wright; Gordon Todderud; Kenneth M. Tramposch; J. Bajorath; Diane Hollenbaugh; Alejandro Aruffo