Publications by authors named "Eric Vangrevelinghe"

22Publications

Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.

Authors:
Thomas Knoepfel Pierre Nimsgern Sébastien Jacquier Marjorie Bourrel Eric Vangrevelinghe Ralf Glatthar Dirk Behnke Phil B Alper Pierre-Yves Michellys Jonathan Deane Tobias Junt Géraldine Zipfel Sarah Limonta Stuart Hawtin Cedric Andre Thomas Boulay Pius Loetscher Michael Faller Jutta Blank Roland Feifel Claudia Betschart

J Med Chem 2020 08 30;63(15):8276-8295. Epub 2020 Jul 30.

Genomics Institute of the Novartis Research Foundation, San Diego, California 92121, United States.

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August 2020

Identification and characterization of a phenyl-thiazolyl-benzoic acid derivative as a novel RAR/RXR agonist.

Authors:
Chie Koshiishi Takanori Kanazawa Eric Vangrevelinghe Toshiyuki Honda Shinji Hatakeyama

Heliyon 2019 Nov 19;5(11):e02849. Epub 2019 Nov 19.

Novartis Institutes for BioMedical Research, Novartis Pharma AG, Basel, Switzerland.

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November 2019

Discovery and Structural Characterization of ATP-Site Ligands for the Wild-Type and V617F Mutant JAK2 Pseudokinase Domain.

Authors:
Randall McNally Qing Li Kunhua Li Carien Dekker Eric Vangrevelinghe Matthew Jones Patrick Chène Rainer Machauer Thomas Radimerski Michael J Eck

ACS Chem Biol 2019 04 11;14(4):587-593. Epub 2019 Mar 11.

Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School and Department of Cancer Biology , Dana-Farber Cancer Institute , Boston , Massachusetts 02115 , United States.

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April 2019

Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model.

Authors:
David A Carcache Anna Vulpetti Joerg Kallen Henri Mattes David Orain Rowan Stringer Eric Vangrevelinghe Romain M Wolf Klemens Kaupmann Johannes Ottl Janet Dawson Nigel G Cooke Klemens Hoegenauer Andreas Billich Juergen Wagner Christine Guntermann Samuel Hintermann

J Med Chem 2018 08 24;61(15):6724-6735. Epub 2018 Jul 24.

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August 2018

An Activating Janus Kinase-3 Mutation Is Associated with Cytotoxic T Lymphocyte Antigen-4-Dependent Immune Dysregulation Syndrome.

Authors:
Heiko Sic Matthaios Speletas Vanessa Cornacchione Maximillian Seidl Martin Beibel Bolan Linghu Fan Yang Eirini Sevdali Anastasios E Germenis Edward J Oakeley Eric Vangrevelinghe Andreas W Sailer Elisabetta Traggiai Hermann Gram Hermann Eibel

Front Immunol 2017 15;8:1824. Epub 2017 Dec 15.

Center for Chronic Immunodeficiency, University Medical Center Freiburg, Freiburg, Germany.

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December 2017

Indolyl-naphthyl-maleimides as potent and selective inhibitors of protein kinase C-α/β.

Authors:
Maurice J van Eis JeanPierre Evenou Walter Schuler Gerhard Zenke Eric Vangrevelinghe Juergen Wagner Peter von Matt

Bioorg Med Chem Lett 2017 02 16;27(4):781-786. Epub 2017 Jan 16.

Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland.

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February 2017

Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.

Authors:
Gebhard Thoma Siem Veenstra Ross Strang Joachim Blanz Eric Vangrevelinghe Jörg Berghausen Christian C Lee Hans-Günter Zerwes

Bioorg Med Chem Lett 2015 Oct 18;25(20):4642-7. Epub 2015 Aug 18.

Autoimmunity, Transplantation and Inflammation Research, Novartis Institutes for Biomedical Research, 4056 Basel, Switzerland.

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October 2015

Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

Authors:
Shuo-Chieh Wu Loretta S Li Nadja Kopp Joan Montero Bjoern Chapuy Akinori Yoda Amanda L Christie Huiyun Liu Alexandra Christodoulou Diederik van Bodegom Jordy van der Zwet Jacob V Layer Trevor Tivey Andrew A Lane Jeremy A Ryan Samuel Y Ng Daniel J DeAngelo Richard M Stone David Steensma Martha Wadleigh Marian Harris Emeline Mandon Nicolas Ebel Rita Andraos Vincent Romanet Arno Dölemeyer Dario Sterker Michael Zender Scott J Rodig Masato Murakami Francesco Hofmann Frank Kuo Michael J Eck Lewis B Silverman Stephen E Sallan Anthony Letai Fabienne Baffert Eric Vangrevelinghe Thomas Radimerski Christoph Gaul David M Weinstock

Cancer Cell 2015 Jul;28(1):29-41

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Broad Institute, Cambridge, MA 02142, USA. Electronic address:

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July 2015

Discovery and profiling of a selective and efficacious Syk inhibitor.

Authors:
Gebhard Thoma Alexander B Smith Maurice J van Eis Eric Vangrevelinghe Joachim Blanz Reiner Aichholz Amanda Littlewood-Evans Christian C Lee Hong Liu Hans-Günter Zerwes

J Med Chem 2015 Feb 9;58(4):1950-63. Epub 2015 Feb 9.

Global Discovery Chemistry, ‡Analytical Sciences & Imaging, §Autoimmunity, Transplantation and Inflammation Research, Novartis Institutes for Biomedical Research , 4056 Basel, Switzerland.

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February 2015

Novel ROCK inhibitors for the treatment of pulmonary arterial hypertension.

Authors:
Duncan Shaw Greg Hollingworth Nicolas Soldermann Elizabeth Sprague Walter Schuler Eric Vangrevelinghe Nicholas Duggan Matthew Thomas Takatoshi Kosaka Nigel Waters Maurice J van Eis

Bioorg Med Chem Lett 2014 Oct 6;24(20):4812-7. Epub 2014 Sep 6.

Novartis Institutes for Biomedical Research, Forum 1 Novartis Campus, 4056 Basel, Switzerland. Electronic address:

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October 2014

Syk inhibitors with high potency in presence of blood.

Authors:
Gebhard Thoma Joachim Blanz Peter Bühlmayer Peter Drückes Matthias Kittelmann Alexander B Smith Maurice van Eis Eric Vangrevelinghe Hans-Günter Zerwes Jianwei John Che Xiaohui He Yunho Jin Christian C Lee Pierre-Yves Michellys Tetsuo Uno Hong Liu

Bioorg Med Chem Lett 2014 May 3;24(10):2278-82. Epub 2014 Apr 3.

Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, CA 92121, USA.

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May 2014

A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.

Authors:
Nils Ostermann Simon Ruedisser Claus Ehrhardt Werner Breitenstein Andreas Marzinzik Edgar Jacoby Eric Vangrevelinghe Johannes Ottl Martin Klumpp J Constanze D Hartwieg Frederic Cumin Ulrich Hassiepen Jörg Trappe Richard Sedrani Sabine Geisse Bernd Gerhartz Paul Richert Eric Francotte Trixie Wagner Markus Krömer Takatoshi Kosaka Randy L Webb Dean F Rigel Jürgen Maibaum Daniel K Baeschlin

J Med Chem 2013 Mar 15;56(6):2196-206. Epub 2013 Mar 15.

Novartis Pharma AG, Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland.

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March 2013

Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.

Authors:
Rita Andraos Zhiyan Qian Débora Bonenfant Joëlle Rubert Eric Vangrevelinghe Clemens Scheufler Fanny Marque Catherine H Régnier Alain De Pover Hugues Ryckelynck Neha Bhagwat Priya Koppikar Aviva Goel Lorenza Wyder Gisele Tavares Fabienne Baffert Carole Pissot-Soldermann Paul W Manley Christoph Gaul Hans Voshol Ross L Levine William R Sellers Francesco Hofmann Thomas Radimerski

Cancer Discov 2012 Jun 3;2(6):512-523. Epub 2012 May 3.

Disease Area Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland.

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June 2012

Genetic resistance to JAK2 enzymatic inhibitors is overcome by HSP90 inhibition.

Authors:
Oliver Weigert Andrew A Lane Liat Bird Nadja Kopp Bjoern Chapuy Diederik van Bodegom Angela V Toms Sachie Marubayashi Amanda L Christie Michael McKeown Ronald M Paranal James E Bradner Akinori Yoda Christoph Gaul Eric Vangrevelinghe Vincent Romanet Masato Murakami Ralph Tiedt Nicolas Ebel Emeline Evrot Alain De Pover Catherine H Régnier Dirk Erdmann Francesco Hofmann Michael J Eck Stephen E Sallan Ross L Levine Andrew L Kung Fabienne Baffert Thomas Radimerski David M Weinstock

J Exp Med 2012 Feb 23;209(2):259-73. Epub 2012 Jan 23.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02115, USA.

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February 2012

2,6-Naphthyridines as potent and selective inhibitors of the novel protein kinase C isozymes.

Authors:
Maurice J van Eis Jean-Pierre Evenou Philipp Floersheim Christoph Gaul Sandra W Cowan-Jacob Lauren Monovich Gabriele Rummel Walter Schuler Wilhelm Stark Andre Strauss Anette von Matt Eric Vangrevelinghe Juergen Wagner Nicolas Soldermann

Bioorg Med Chem Lett 2011 Dec 21;21(24):7367-72. Epub 2011 Oct 21.

Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, CH-4056 Basel, Switzerland.

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December 2011

Identification of a potent Janus kinase 3 inhibitor with high selectivity within the Janus kinase family.

Authors:
Gebhard Thoma Francois Nuninger Rocco Falchetto Erwin Hermes Gisele A Tavares Eric Vangrevelinghe Hans-Günter Zerwes

J Med Chem 2011 Jan 14;54(1):284-8. Epub 2010 Dec 14.

Novartis Institutes for BioMedical Research, Forum 1, Novartis Campus, Basel, Switzerland.

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January 2011

Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.

Authors:
Fabienne Baffert Catherine H Régnier Alain De Pover Carole Pissot-Soldermann Gisele A Tavares Francesca Blasco Josef Brueggen Patrick Chène Peter Drueckes Dirk Erdmann Pascal Furet Marc Gerspacher Marc Lang David Ledieu Lynda Nolan Stephan Ruetz Joerg Trappe Eric Vangrevelinghe Markus Wartmann Lorenza Wyder Francesco Hofmann Thomas Radimerski

Mol Cancer Ther 2010 Jul 29;9(7):1945-55. Epub 2010 Jun 29.

Disease Area Oncology, Novartis Institutes for BioMedical Research, 4057 Basel, Switzerland.

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July 2010

Discovery and SAR of potent, orally available 2,8-diaryl-quinoxalines as a new class of JAK2 inhibitors.

Authors:
Carole Pissot-Soldermann Marc Gerspacher Pascal Furet Christoph Gaul Philipp Holzer Clive McCarthy Thomas Radimerski Catherine H Regnier Fabienne Baffert Peter Drueckes Gisele A Tavares Eric Vangrevelinghe Francesca Blasco Giorgio Ottaviani Flavio Ossola Julien Scesa Janitha Reetz

Bioorg Med Chem Lett 2010 Apr 19;20(8):2609-13. Epub 2010 Feb 19.

Novartis Institutes for Biomedical Research, Novartis Pharma AG, WKL-136.4.96, CH-4002 Basel, Switzerland.

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April 2010

2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.

Authors:
Marc Gerspacher Pascal Furet Carole Pissot-Soldermann Christoph Gaul Philipp Holzer Eric Vangrevelinghe Marc Lang Dirk Erdmann Thomas Radimerski Catherine H Regnier Patrick Chene Alain De Pover Francesco Hofmann Fabienne Baffert Thomas Buhl Reiner Aichholz Francesca Blasco Ralf Endres Jörg Trappe Peter Drueckes

Bioorg Med Chem Lett 2010 Mar 21;20(5):1724-7. Epub 2010 Jan 21.

Novartis Institutes for BioMedical Research, Novartis Pharma AG, CH-4002 Basel, Switzerland.

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March 2010

A small-molecule dengue virus entry inhibitor.

Authors:
Qing-Yin Wang Sejal J Patel Eric Vangrevelinghe Hao Ying Xu Ranga Rao Deana Jaber Wouter Schul Feng Gu Olivier Heudi Ngai Ling Ma Mee Kian Poh Wai Yee Phong Thomas H Keller Edgar Jacoby Subhash G Vasudevan

Antimicrob Agents Chemother 2009 May 17;53(5):1823-31. Epub 2009 Feb 17.

Novartis Institute for Tropical Diseases, 10 Biopolis Rd., Chromos Building, Singapore 138670, Singapore.

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May 2009

Discovery of a potent and selective protein kinase CK2 inhibitor by high-throughput docking.

Authors:
Eric Vangrevelinghe Kaspar Zimmermann Joseph Schoepfer Robert Portmann Doriano Fabbro Pascal Furet

J Med Chem 2003 Jun;46(13):2656-62

Oncology Research, Novartis Pharma AG, 4002 Basle, Switzerland.

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June 2003

Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.

Authors:
Joseph Schoepfer Heinz Fretz Bhabatosh Chaudhuri Lionel Muller Egge Seeber Laurent Meijer Olivier Lozach Eric Vangrevelinghe Pascal Furet

J Med Chem 2002 Apr;45(9):1741-7

Oncology Research, NOVARTIS Pharma AG, 4002 Basle, Switzerland.

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April 2002