Publications by authors named "Reiner Aichholz"

18Publications

Optimization of the Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood.

Authors:
Jean Quancard Oliver Simic Carole Pissot Soldermann Reiner Aichholz Markus Blatter Martin Renatus Paulus Erbel Samu Melkko Ralf Endres Mickael Sorge Laurence Kieffer Trixie Wagner Karen Beltz Paul Mcsheehy Markus Wartmann Catherine H Régnier Thomas Calzascia Thomas Radimerski Marc Bigaud Andreas Weiss Frédéric Bornancin Achim Schlapbach

J Med Chem 2020 12 20;63(23):14594-14608. Epub 2020 Nov 20.

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

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December 2020

Discovery of the First Potent, Selective, and Orally Bioavailable Signal Peptide Peptidase-Like 2a (SPPL2a) Inhibitor Displaying Pronounced Immunomodulatory Effects In Vivo.

Authors:
Juraj Velcicky Ursula Bodendorf Pascal Rigollier Robert Epple Daniel R Beisner Danilo Guerini Philip Smith Bo Liu Roland Feifel Peter Wipfli Reiner Aichholz Philippe Couttet Ina Dix Toni Widmer Ben Wen Trixi Brandl

J Med Chem 2018 02 23;61(3):865-880. Epub 2018 Jan 23.

The Genomics Institute of the Novartis Research Foundation , 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.

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February 2018

ADAM17 is the main sheddase for the generation of human triggering receptor expressed in myeloid cells (hTREM2) ectodomain and cleaves TREM2 after Histidine 157.

Authors:
Dominik Feuerbach Patrick Schindler Carmen Barske Stefanie Joller Edwige Beng-Louka Katie A Worringer Sravya Kommineni Ajamete Kaykas Daniel J Ho Chaoyang Ye Karl Welzenbach Gaelle Elain Laurent Klein Irena Brzak Anis K Mir Christopher J Farady Reiner Aichholz Simone Popp Nathalie George Ulf Neumann

Neurosci Lett 2017 Nov 18;660:109-114. Epub 2017 Sep 18.

Neuroscience Research, Novartis Institutes for Biomedical Research, Basel, Switzerland.

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November 2017

Evaluation of relative MS response factors of drug metabolites for semi-quantitative assessment of chemical liabilities in drug discovery.

Authors:
Joachim Blanz Gareth Williams Jerôme Dayer Thierry Délémonté Werner Gertsch Philippe Ramstein Reiner Aichholz Markus Trunzer David Pearson

J Mass Spectrom 2017 04;52(4):210-217

DMPK, Novartis Institutes for Biomedical Research, Postfach, Basel, CH-4002, Switzerland.

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April 2017

Increasing metabolic stability via the deuterium kinetic isotope effect: An example from a proline-amide-urea aminothiazole series of phosphatidylinositol-3 kinase alpha inhibitors.

Authors:
Robin A Fairhurst Giorgio Caravatti Vito Guagnano Reiner Aichholz Joachim Blanz Francesca Blasco Peter Wipfli Christine Fritsch Sauveur-Michel Maira Christian Schnell Frank H Seiler

Bioorg Med Chem Lett 2016 10 17;26(19):4729-4734. Epub 2016 Aug 17.

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

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October 2016

Micropreparative isolation and NMR structure elucidation of metabolites of the drug candidate 1-isopropyl-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy) quinazolin-2(1H)-one from rat bile and urine.

Authors:
Joachim Blanz Thierry Délémonté David Pearson Alexandre Luneau Michael Ritzau Werner Gertsch Philippe Ramstein Jérôme Dayer Sandrine Desrayaud Elisabeth Braun Reiner Aichholz

J Chromatogr B Analyt Technol Biomed Life Sci 2015 May 10;989:1-10. Epub 2015 Mar 10.

Analytical Sciences & Imaging, Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland.

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May 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

Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.

Authors:
Pascal Furet Vito Guagnano Robin A Fairhurst Patricia Imbach-Weese Ian Bruce Mark Knapp Christine Fritsch Francesca Blasco Joachim Blanz Reiner Aichholz Jacques Hamon Doriano Fabbro Giorgio Caravatti

Bioorg Med Chem Lett 2013 Jul 14;23(13):3741-8. Epub 2013 May 14.

Novartis Institutes for BioMedical Research, WKL-136.4.12, CH-4002 Basel, Switzerland.

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July 2013

The kinetic deuterium isotope effect as applied to metabolic deactivation of imatinib to the des-methyl metabolite, CGP74588.

Authors:
Paul W Manley Francesca Blasco Jürgen Mestan Reiner Aichholz

Bioorg Med Chem 2013 Jun 1;21(11):3231-9. Epub 2013 Apr 1.

Disease Area Oncology, Novartis Institutes for Biomedical Research, CH-4002 Basel, Switzerland.

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June 2013

Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589).

Authors:
Andreas Fredenhagen Matthias Kittelmann Lukas Oberer Anton Kuhn Jürgen Kühnöl Thierry Délémonté Reiner Aichholz Ping Wang Peter Atadja Michael D Shultz

Drug Metab Dispos 2012 May 16;40(5):1041-50. Epub 2012 Feb 16.

Global Ciscovery Chemistry, Novartis Institutes for BioMedical Research, WKL-122.P.37, CH-4002 Basel, Switzerland.

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May 2012

Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.

Authors:
Samuel Hintermann Konstanze Hurth Joachim Nozulak Marina Tintelnot-Blomley Reiner Aichholz Joachim Blanz Klemens Kaupmann Johannes Mosbacher

Bioorg Med Chem Lett 2011 Mar 28;21(5):1523-6. Epub 2010 Dec 28.

Novartis Institutes for BioMedical Research, Neuroscience Research, Basel, Switzerland.

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March 2011

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.

Authors:
Laszlo Revesz Achim Schlapbach Reiner Aichholz Roland Feifel Stuart Hawtin Richard Heng Peter Hiestand Wolfgang Jahnke Guido Koch Markus Kroemer Henrik Möbitz Clemens Scheufler Juraj Velcicky Christine Huppertz

Bioorg Med Chem Lett 2010 Aug 13;20(15):4715-8. Epub 2010 Apr 13.

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

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August 2010

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.

Authors:
Laszlo Revesz Achim Schlapbach Reiner Aichholz Janet Dawson Roland Feifel Stuart Hawtin Amanda Littlewood-Evans Guido Koch Markus Kroemer Henrik Möbitz Clemens Scheufler Juraj Velcicky Christine Huppertz

Bioorg Med Chem Lett 2010 Aug 11;20(15):4719-23. Epub 2010 Apr 11.

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

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August 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

2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.

Authors:
Eva Altmann Reiner Aichholz Claudia Betschart Thomas Buhl Jonathan Green Osamu Irie Naoki Teno René Lattmann Marina Tintelnot-Blomley Martin Missbach

J Med Chem 2007 Feb 27;50(4):591-4. Epub 2007 Jan 27.

Novartis Institutes of BioMedical Research, CH-4002 Basel, Switzerland.

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February 2007

Dipeptide nitrile inhibitors of cathepsin K.

Authors:
Eva Altmann Reiner Aichholz Claudia Betschart Thomas Buhl Jonathan Green René Lattmann Martin Missbach

Bioorg Med Chem Lett 2006 May 9;16(9):2549-54. Epub 2006 Feb 9.

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

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May 2006

Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach.

Authors:
Francis Bitsch Reiner Aichholz Joerg Kallen Sabine Geisse Brigitte Fournier Jean Marc Schlaeppi

Anal Biochem 2003 Dec;323(1):139-49

Central Technologies, Novartis Institutes for Biomedical Research, Lichtstrasse 35, CH-4002 Basel, Switzerland.

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December 2003

Complementary use of ion trap/time-of-flight mass spectrometry in combination with capillary high-pressure liquid chromatography: early characterization of in vivo metabolites of the cathepsin K inhibitor NVP-AAV490 in rat.

Authors:
Wolfgang Blum Thomas Buhl Eva Altmann Jürgen Kühnöl Philippe Ramstein Reiner Aichholz

J Chromatogr B Analyt Technol Biomed Life Sci 2003 Apr;787(2):255-70

Novartis Pharma AG, Research Department, Building WKL-121.200, CH-4002 Basel, Switzerland.

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April 2003