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Markus Voegtle

Novartis

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Publication

Featured researches published by Markus Voegtle.

Bioorganic & Medicinal Chemistry Letters | 2018

Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.

Siem Jakob Veenstra; Heinrich Rueeger; Markus Voegtle; Rainer Martin Lueoend; Philipp Holzer; Konstanze Hurth; Marina Tintelnot-Blomley; Mathias Frederiksen; Jean-Michel Rondeau; Laura H. Jacobson; Matthias Staufenbiel; Ulf Neumann; Rainer Machauer

New amino-1,4-oxazine derived BACE-1 inhibitors were explored and various synthetic routes developed. The binding mode of the inhibitors was elucidated by co-crystallization of 4 with BACE-1 and X-ray analysis. Subsequent optimization led to inhibitors with low double digit nanomolar activity in a biochemical and single digit nanomolar potency in a cellular assays. To assess the inhibitors for their permeation properties and potential to cross the blood-brain-barrier a MDR1-MDCK cell model was successfully applied. Compound 8a confirmed the in vitro results by dose-dependently reducing Aβ levels in mice in an acute treatment regimen.

Archive | 2010

Oxazine derivatives and their use as bace inhibitors for the treatment of neurological disorders

Sangamesh Badiger; Murali Chebrolu; Mathias Frederiksen; Philipp Holzer; Konstanze Hurth; Rainer Martin Lueoend; Rainer Machauer; Henrik Moebitz; Ulf Neumann; Rita Ramos; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

Archive | 2012

NOVEL HETEROCYCLIC DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Sangamesh Badiger; Murali Chebrolu; Konstanze Hurth; Sébastien Jacquier; Rainer Martin Lueoend; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

Archive | 2012

Oxazine derivatives and their use in the treatment of disease

Konstanze Hurth; Sébastien Jacquier; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

Archive | 2013

Heterocyclic derivatives and their use in the treatment of neurological disorders

Sangamesh Badiger; Murali Chebrolu; Konstanze Hurth; Sébastien Jacquier; Rainer Martin Lueoend; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

Archive | 2017

derivados de oxazina e uso dos mesmos no tratamento de doença

Heinrich Rueeger; Konstanze Hurth; Marina Tintelnot-Blomley; Markus Voegtle; Rainer Machauer; Siem Jacob Veenstra; Sébastien Jacquier

Archive | 2016

derivados de oxazina e seu uso no tratamento de distúrbios neurológicos

Heinrich Rueeger; Henrik Moebitz; Hui Liu; Konstanze Hurth; Lei Li; Marina Tintelnot-Blomley; Markus Voegtle; Mathias Frederiksen; Michael Schaefer; Murali Chebrolu; Philipp Holzer; Rainer Machauer; Rainer Martin Lueoend; Rita Ramos; Sangamesh Badiger; Siem Jacob Veenstra; Ulf Neumann; Xin Xiong

Archive | 2014

Compuestos derivados heterociclicos nitrogenados, inhibidores de la bace-1 o de la bace-2; composicion farmaceutica que los comprende; combinacion farmaceutica; su uso en el tratamiento o prevencion de la enfermedad de alzheimer o un deterioro cognitivo leve.

Sangamesh Badiger; Murali Chebrolu; Konstanze Hurth; Rainer Martin Lueoend; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle; Sébastien Jacquier

Archive | 2013

Compuestos derivados de heterociclos, como inhibidores de bace 1 o 2; composicion farmaceutica que los comprende; combinacion farmaceutica; y su uso para el tratamiento o prevencion de la enfermedad de alzheimer o deterioro cognitivo leve, resistencia a la insulina, diabetes tipo 2, entre otras.

Sangamesh Badiger; Murali Chebrolu; Konstanze Hurth; Sébastien Jacquier; Rainer Martin Lueoend; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

Archive | 2012

Nouveaux dérivés hétérocycliques et leur utilisation dans le traitement de troubles neurologiques

Sangamesh Badiger; Murali Chebrolu; Konstanze Hurth; Sébastien Jacquier; Rainer Martin Lueoend; Rainer Machauer; Heinrich Rueeger; Marina Tintelnot-Blomley; Siem Jacob Veenstra; Markus Voegtle

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Collaboration

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Heinrich Rueeger

Novartis

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Konstanze Hurth

Novartis

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Marina Tintelnot-Blomley

Novartis

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Rainer Machauer

Novartis

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Siem Jacob Veenstra

Novartis

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Rainer Martin Lueoend

Novartis

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Murali Chebrolu

Novartis

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Sangamesh Badiger

Novartis

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Sébastien Jacquier

Novartis

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Mathias Frederiksen

Novartis

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