Publications by authors named "Claudia Betschart"

19Publications

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

Discovery of potent, orally bioavailable in vivo efficacious antagonists of the TLR7/8 pathway.

Authors:
Phil B Alper Jonathan Deane Claudia Betschart David Buffet Géraldine Collignon Zipfel Perry Gordon Janice Hampton Stuart Hawtin Maureen Ibanez Tao Jiang Tobias Junt Thomas Knoepfel Bo Liu Jillian Maginnis Una McKeever Pierre-Yves Michellys Daniel Mutnick Bishnu Nayak Satoru Niwa Wendy Richmond James S Rush Peter Syka Yi Zhang Xuefeng Zhu

Bioorg Med Chem Lett 2020 09 24;30(17):127366. Epub 2020 Jun 24.

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

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September 2020

Structure-Based and Property-Driven Optimization of -Aryl Imidazoles toward Potent and Selective Oral RORγt Inhibitors.

Authors:
Klemens Hoegenauer Joerg Kallen Eloísa Jiménez-Núñez Ross Strang Peter Ertl Nigel G Cooke Samuel Hintermann Markus Voegtle Claudia Betschart Daniel J J McKay Juergen Wagner Johannes Ottl Christian Beerli Andreas Billich Janet Dawson Klemens Kaupmann Markus Streiff Nathalie Gobeau Stephanie Harlfinger Rowan Stringer Christine Guntermann

J Med Chem 2019 12 3;62(23):10816-10832. Epub 2019 Dec 3.

Global Discovery Chemistry , 181 Massachusetts Avenue , 02139 Cambridge , Massachusetts , United States.

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December 2019

Discovery of 1H-pyrazolo[3,4-b]pyridines as potent dual orexin receptor antagonists (DORAs).

Authors:
Dirk Behnke Simona Cotesta Samuel Hintermann Markus Fendt Christine E Gee Laura H Jacobson Grit Laue Arndt Meyer Trixie Wagner Sangamesh Badiger Vinod Chaudhari Murali Chebrolu Chetan Pandit Daniel Hoyer Claudia Betschart

Bioorg Med Chem Lett 2015 Dec 19;25(23):5555-60. Epub 2015 Oct 19.

Global Discovery Chemistry, Novartis Institutes for BioMedical Research, WKL-136.3.26, CH-4002 Basel, Switzerland.

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December 2015

Kinetic properties of "dual" orexin receptor antagonists at OX1R and OX2R orexin receptors.

Authors:
Gabrielle E Callander Morenike Olorunda Dominique Monna Edi Schuepbach Daniel Langenegger Claudia Betschart Samuel Hintermann Dirk Behnke Simona Cotesta Markus Fendt Grit Laue Silvio Ofner Emmanuelle Briard Christine E Gee Laura H Jacobson Daniel Hoyer

Front Neurosci 2013 3;7:230. Epub 2013 Dec 3.

Department of Pharmacology and Therapeutics, Faculty of Medicine, Dentistry and Health Sciences, School of Medicine, The University of Melbourne Parkville, VIC, Australia ; The Florey Institute of Neuroscience and Mental Health, The University of Melbourne Parkville, VIC, Australia ; Department of Neuroscience, Novartis Institutes for Biomedical Research Basel, Switzerland.

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December 2013

Distinct effects of IPSU and suvorexant on mouse sleep architecture.

Authors:
Daniel Hoyer Thomas Dürst Markus Fendt Laura H Jacobson Claudia Betschart Samuel Hintermann Dirk Behnke Simona Cotesta Grit Laue Silvio Ofner Eric Legangneux Christine E Gee

Front Neurosci 2013 10;7:235. Epub 2013 Dec 10.

Neuroscience, Novartis Institutes for BioMedical Research Basel, Switzerland ; Center for Molecular Neuroscience Hamburg, Institute for Synaptic Physiology Hamburg, Germany.

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December 2013

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia.

Authors:
Claudia Betschart Samuel Hintermann Dirk Behnke Simona Cotesta Markus Fendt Christine E Gee Laura H Jacobson Grit Laue Silvio Ofner Vinod Chaudhari Sangamesh Badiger Chetan Pandit Juergen Wagner Daniel Hoyer

J Med Chem 2013 Oct 18;56(19):7590-607. Epub 2013 Sep 18.

Global Discovery Chemistry, ‡Neuroscience, and §Metabolism and Pharmacokinetics, Novartis Institutes for BioMedical Research , CH-4002 Basel, Switzerland.

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October 2013

Huntingtin cleavage product A forms in neurons and is reduced by gamma-secretase inhibitors.

Authors:
Kimberly B Kegel Ellen Sapp Jonathan Alexander Patrick Reeves Dorothee Bleckmann Linsday Sobin Nicholas Masso Antonio Valencia Hyunkyung Jeong Dimitri Krainc James Palacino Daniel Curtis Rainer Kuhn Claudia Betschart Miguel Sena-Esteves Neil Aronin Paolo Paganetti Marian Difiglia

Mol Neurodegener 2010 Dec 14;5:58. Epub 2010 Dec 14.

Department of Neurology, Massachusetts General Hospital, Charlestown, MA 02129, USA.

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December 2010

The mTOR kinase inhibitor Everolimus decreases S6 kinase phosphorylation but fails to reduce mutant huntingtin levels in brain and is not neuroprotective in the R6/2 mouse model of Huntington's disease.

Authors:
Jonathan H Fox Teal Connor Vanita Chopra Kate Dorsey Jibrin A Kama Dorothee Bleckmann Claudia Betschart Daniel Hoyer Stefan Frentzel Marian Difiglia Paolo Paganetti Steven M Hersch

Mol Neurodegener 2010 Jun 22;5:26. Epub 2010 Jun 22.

MassGeneral Institute for Neurodegenerative Disease and Harvard Medical School, Charlestown, MA, USA.

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June 2010

Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.

Authors:
Stephen Hanessian Zhihui Shao Claudia Betschart Jean-Michel Rondeau Ulf Neumann Marina Tintelnot-Blomley

Bioorg Med Chem Lett 2010 Mar 2;20(6):1924-7. Epub 2010 Feb 2.

Department of Chemistry, Université de Montréal, Montréal, Canada.

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March 2010

Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.

Authors:
Andreas Lerchner Rainer Machauer Claudia Betschart Siem Veenstra Heinrich Rueeger Clive McCarthy Marina Tintelnot-Blomley Anne-Lise Jaton Sabine Rabe Sandrine Desrayaud Albert Enz Matthias Staufenbiel Paolo Paganetti Jean-Michel Rondeau Ulf Neumann

Bioorg Med Chem Lett 2010 Jan 22;20(2):603-7. Epub 2009 Nov 22.

Novartis Institutes for BioMedicalResearch, Novartis Pharma AG, PO Box, CH 4002, Basel, Switzerland.

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January 2010

Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.

Authors:
Rainer Machauer Kurt Laumen Siem Veenstra Jean-Michel Rondeau Marina Tintelnot-Blomley Claudia Betschart Anne-Lise Jaton Sandrine Desrayaud Matthias Staufenbiel Sabine Rabe Paolo Paganetti Ulf Neumann

Bioorg Med Chem Lett 2009 Mar 22;19(5):1366-70. Epub 2009 Jan 22.

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

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March 2009

Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.

Authors:
Rainer Machauer Siem Veenstra Jean-Michel Rondeau Marina Tintelnot-Blomley Claudia Betschart Ulf Neumann Paolo Paganetti

Bioorg Med Chem Lett 2009 Mar 19;19(5):1361-5. Epub 2009 Jan 19.

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

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March 2009

New chemotypes for cathepsin K inhibitors.

Authors:
Naoki Teno Osamu Irie Takahiro Miyake Keigo Gohda Miyuki Horiuchi Sachiyo Tada Kazuhiko Nonomura Motohiko Kometani Genji Iwasaki Claudia Betschart

Bioorg Med Chem Lett 2008 Apr 16;18(8):2599-603. Epub 2008 Mar 16.

Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki 300-2611, Japan.

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April 2008

Novel scaffold for cathepsin K inhibitors.

Authors:
Naoki Teno Takahiro Miyake Takeru Ehara Osamu Irie Junichi Sakaki Osamu Ohmori Hiroki Gunji Naoko Matsuura Keiichi Masuya Yuko Hitomi Kazuhiko Nonomura Miyuki Horiuchi Keigo Gohda Atsuko Iwasaki Ichiro Umemura Sachiyo Tada Motohiko Kometani Genji Iwasaki Sandra W Cowan-Jacob Martin Missbach René Lattmann Claudia Betschart

Bioorg Med Chem Lett 2007 Nov 15;17(22):6096-100. Epub 2007 Sep 15.

Novartis Institutes for BioMedical Research, Ohkubo 8, Tsukuba, Ibaraki, Japan.

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November 2007

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

Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).

Authors:
Stephen Hanessian Gaoqiang Yang Jean-Michel Rondeau Ulf Neumann Claudia Betschart Marina Tintelnot-Blomley

J Med Chem 2006 Jul;49(15):4544-67

Department of Chemistry, Université de Montréal, C. P. 6128, Station Centre-ville, Montréal, Quebec H3C 3J7, Canada.

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July 2006

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

Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.

Authors:
Stephen Hanessian Hongying Yun Yihua Hou Gaoqiang Yang Malken Bayrakdarian Eric Therrien Nicolas Moitessier Silvio Roggo Siem Veenstra Marina Tintelnot-Blomley Jean-Michel Rondeau Christian Ostermeier André Strauss Paul Ramage Paolo Paganetti Ulf Neumann Claudia Betschart

J Med Chem 2005 Aug;48(16):5175-90

Department of Chemistry, Université de Montréal, C. P. 6128, Succursale Centre-Ville, Montréal, Province Quebec, Canada H3C 3J7.

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August 2005