Publications by authors named "Frederic Cumin"

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Discovery of 4-((2,4)-4-Ethoxy-1-((5-methoxy-7-methyl-1-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Nello Mainolfi, Takeru Ehara, Rajeshri G Karki, Karen Anderson, Aengus Mac Sweeney, Frederic Cumin

J Med Chem· June 2020

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Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors.
Toshio Kawanami, Rajeshri G Karki, Emma Cody, Qian Liu, Guiqing Liang, Frederic Cumin

ACS Med Chem Lett· February 2020

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Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Rajeshri G Karki, James Powers, Nello Mainolfi, Karen Anderson, David B Belanger, Frederic Cumin

J Med Chem· May 2019

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Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Anna Schubart, Karen Anderson, Nello Mainolfi, Holger Sellner, Takeru Ehara, Frederic Cumin

Proc Natl Acad Sci U S A· April 2019

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Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D.
Anna Vulpetti, Nils Ostermann, Stefan Randl, Taeyoung Yoon, Aengus Mac Sweeney, Frederic Cumin

ACS Med Chem Lett· May 2018

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Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Edwige Lorthiois, Karen Anderson, Anna Vulpetti, Olivier Rogel, Frederic Cumin

J Med Chem· July 2017

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The effect of angiotensin receptor neprilysin inhibitor, sacubitril/valsartan, on central nervous system amyloid-β concentrations and clearance in the cynomolgus monkey.
Heidi A Schoenfeld, Tim West, Philip B Verghese, Mary Holubasch, Neeta Shenoy, Frederic Cumin

Toxicol Appl Pharmacol· May 2017

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Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
Anna Vulpetti, Stefan Randl, Simon Rüdisser, Nils Ostermann, Paul Erbel, Frederic Cumin

J Med Chem· March 2017

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Small-molecule factor D inhibitors targeting the alternative complement pathway.
Jürgen Maibaum, Sha-Mei Liao, Anna Vulpetti, Nils Ostermann, Stefan Randl, Frederic Cumin

Nat Chem Biol· December 2016

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Structure of neprilysin in complex with the active metabolite of sacubitril.
Nikolaus Schiering, Allan D'Arcy, Frederic Villard, Paul Ramage, Claude Logel, Frederic Cumin

Sci Rep· June 2016

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Plasma contact system activation drives anaphylaxis in severe mast cell-mediated allergic reactions.
Anna Sala-Cunill, Jenny Björkqvist, Riccardo Senter, Mar Guilarte, Victoria Cardona, Frederic Cumin

J Allergy Clin Immunol· April 2015

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trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Holger Sellner, Sylvain Cottens, Frédéric Cumin, Claus Ehrhardt, Takatoshi Kosaka

Bioorg Med Chem Lett· April 2015

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trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Edwige Lorthiois, Frederic Cumin, Claus Ehrhardt, Takatoshi Kosaka, Holger Sellner

Bioorg Med Chem Lett· April 2015

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Fluorescence Lifetime-Based Competitive Binding Assays for Measuring the Binding Potency of Protease Inhibitors In Vitro.
Andreas Boettcher, Nathalie Gradoux, Edwige Lorthiois, Trixi Brandl, David Orain, Frederic Cumin

J Biomol Screen· July 2014

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Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Takeru Ehara, Osamu Irie, Takatoshi Kosaka, Takanori Kanazawa, Werner Breitenstein, Frederic Cumin

ACS Med Chem Lett· July 2014

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A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Nils Ostermann, Simon Ruedisser, Claus Ehrhardt, Werner Breitenstein, Andreas Marzinzik, Frederic Cumin

J Med Chem· March 2013

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The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Edwige Lorthiois, Werner Breitenstein, Frederic Cumin, Claus Ehrhardt, Eric Francotte

J Med Chem· March 2013

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The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.
Yasuchika Yamaguchi, Keith Menear, Nissim-Claude Cohen, Robert Mah, Frédéric Cumin

Bioorg Med Chem Lett· August 2009

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Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.
Richard Göschke, Stefan Stutz, Vittorio Rasetti, Nissim-Claude Cohen, Joseph Rahuel, Frédéric Cumin

J Med Chem· October 2007

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Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.
Jürgen Maibaum, Stefan Stutz, Richard Göschke, Pascal Rigollier, Yasuchika Yamaguchi, Frédéric Cumin

J Med Chem· October 2007

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Aspartic proteases in drug discovery.
Jörg Eder, Ulrich Hommel, Frederic Cumin, Bruno Martoglio, Bernd Gerhartz

Curr Pharm Des· March 2007

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Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats.
Jeanette M Wood, Christian R Schnell, Frederic Cumin, Joël Menard, Randy L Webb

J Hypertens· February 2005

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Structure-based design of aliskiren, a novel orally effective renin inhibitor.
Jeanette M Wood, Jürgen Maibaum, Joseph Rahuel, Markus G Grütter, Nissim-Claude Cohen, Frederic Cumin

Biochem Biophys Res Commun· September 2003

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Uncoupling of protein-3 induces an uncontrolled uncoupling of mitochondria after expression in muscle derived L6 cells.
Danilo Guerini, Elisabetta Prati, Urvi Desai, Hans Peter Nick, Rolf Flammer, Frederic Cumin

Eur J Biochem· March 2002

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