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Design and synthesis of potent, isoxazole-containing renin inhibitors. 2012
Pierre-André Fournier, and
Mélissa Arbour, and
Elizabeth Cauchon, and
Austin Chen, and
Amandine Chefson, and
Yves Ducharme, and
Jean-Pierre Falgueyret, and
Sébastien Gagné, and
Erich Grimm, and
Yongxin Han, and
Robert Houle, and
Patrick Lacombe, and
Jean-François Lévesque, and
Dwight MacDonald, and
Bruce Mackay, and
Dan McKay, and
M David Percival, and
Yeeman Ramtohul, and
René St-Jacques, and
Sylvie Toulmond
Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada. pierre-andre_fournier@merck.com
The design and optimization of a novel isoxazole S(1) linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin inhibitor even in the presence of human plasma. When compound 18 was found to inhibit CYP3A4 in a time dependent manner, two strategies were pursued that successfully delivered equipotent compounds with minimal TDI potential.
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Elizabeth Cauchon, and
Austin Chen, and
Amandine Chefson, and
Yves Ducharme, and
Jean-Pierre Falgueyret, and
Sébastien Gagné, and
Erich Grimm, and
Yongxin Han, and
Robert Houle, and
Patrick Lacombe, and
Jean-François Lévesque, and
Dwight MacDonald, and
Bruce Mackay, and
Dan McKay, and
M David Percival, and
Yeeman Ramtohul, and
René St-Jacques, and
Sylvie Toulmond
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