5‑(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology
Beaufils, Florent, Cmiljanovic, Natasa, Cmiljanovic, Vladimir, Bohnacker, Thomas, Melone, Anna, Marone, Romina, Jackson, Eileen, Zhang, Xuxiao, Sele, Alexander, Borsari, Chiara, Mestan, Jürgen, Hebeisen, Paul, Hillmann, Petra, Giese, Bernd, Zvelebil, Marketa, Fabbro, Doriano, Williams, Roger L, Rageot, Denise, Wymann, Matthias P
Published in Journal of medicinal chemistry (14.09.2017)
Published in Journal of medicinal chemistry (14.09.2017)
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6‑Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds
Röver, Stephan, Andjelkovic, Mirjana, Bénardeau, Agnès, Chaput, Evelyne, Guba, Wolfgang, Hebeisen, Paul, Mohr, Susanne, Nettekoven, Matthias, Obst, Ulrike, Richter, Wolfgang F, Ullmer, Christoph, Waldmeier, Pius, Wright, Matthew B
Published in Journal of medicinal chemistry (27.12.2013)
Published in Journal of medicinal chemistry (27.12.2013)
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In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci
HEBEISEN, Paul, HEINZE-KRAUSS, Ingrid, ANGEHRN, Peter, HOHL, Peter, PAGE, Malcolm G. P, THEN, Rudolf L
Published in Antimicrobial Agents and Chemotherapy (01.03.2001)
Published in Antimicrobial Agents and Chemotherapy (01.03.2001)
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Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes
Byrne, Simon J., Fletcher, Anthony J., Hebeisen, Paul, Willis, Michael C.
Published in Organic & biomolecular chemistry (01.01.2010)
Published in Organic & biomolecular chemistry (01.01.2010)
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Journal Article
New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine
Angehrn, Peter, Buchmann, Stefan, Funk, Christoph, Goetschi, Erwin, Gmuender, Hans, Hebeisen, Paul, Kostrewa, Dirk, Link, Helmut, Luebbers, Thomas, Masciadri, Raffaello, Nielsen, Joergen, Reindl, Peter, Ricklin, Fabienne, Schmitt-Hoffmann, Anne, Theil, Frank-Peter
Published in Journal of medicinal chemistry (11.03.2004)
Published in Journal of medicinal chemistry (11.03.2004)
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Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-y1})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders
Rageot, Denise, Bohnacker, Thomas, Melone, Anna, Langlois, Jean-Baptiste, Borsari, Chiara, Hillmann, Petra, Sele, Alexander M., Beaufils, Florent, Zvelebil, Marketa, Hebeisen, Paul, Loescher, Wolfgang, Burke, John, Fabbro, Doriano, Wymann, Matthias P.
Published in Journal of medicinal chemistry (22.11.2018)
Published in Journal of medicinal chemistry (22.11.2018)
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Abstract 293: Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitors suitable for the treatment of CNS disorders
Borsari, Chiara, Keles, Erhan, Treyer, Andrea, De Pascale, Martina, Hebeisen, Paul, Hamburger, Matthias, Wymann, Matthias P.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
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Discovery and Preclinical Characterization of 5‑[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders
Rageot, Denise, Bohnacker, Thomas, Melone, Anna, Langlois, Jean-Baptiste, Borsari, Chiara, Hillmann, Petra, Sele, Alexander M, Beaufils, Florent, Zvelebil, Marketa, Hebeisen, Paul, Löscher, Wolfgang, Burke, John, Fabbro, Doriano, Wymann, Matthias P
Published in Journal of medicinal chemistry (21.11.2018)
Published in Journal of medicinal chemistry (21.11.2018)
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(S)‑4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase
Rageot, Denise, Bohnacker, Thomas, Keles, Erhan, McPhail, Jacob A, Hoffmann, Reece M, Melone, Anna, Borsari, Chiara, Sriramaratnam, Rohitha, Sele, Alexander M, Beaufils, Florent, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Burke, John E, Wymann, Matthias P
Published in Journal of medicinal chemistry (11.07.2019)
Published in Journal of medicinal chemistry (11.07.2019)
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A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor
Borsari, Chiara, Rageot, Denise, Dall’Asen, Alix, Bohnacker, Thomas, Melone, Anna, Sele, Alexander M, Jackson, Eileen, Langlois, Jean-Baptiste, Beaufils, Florent, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in Journal of medicinal chemistry (26.09.2019)
Published in Journal of medicinal chemistry (26.09.2019)
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4‑(Difluoromethyl)-5-(4-((3R,5S)‑3,5-dimethylmorpholino)-6-((R)‑3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders
Borsari, Chiara, Keles, Erhan, Rageot, Denise, Treyer, Andrea, Bohnacker, Thomas, Bissegger, Lukas, De Pascale, Martina, Melone, Anna, Sriramaratnam, Rohitha, Beaufils, Florent, Hamburger, Matthias, Hebeisen, Paul, Löscher, Wolfgang, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor
De Pascale, Martina, Bissegger, Lukas, Tarantelli, Chiara, Beaufils, Florent, Prescimone, Alessandro, Mohamed Seid Hedad, Hayget, Kayali, Omar, Orbegozo, Clara, Raguž, Luka, Schaefer, Thorsten, Hebeisen, Paul, Bertoni, Francesco, Wymann, Matthias P., Borsari, Chiara
Published in European journal of medicinal chemistry (15.02.2023)
Published in European journal of medicinal chemistry (15.02.2023)
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Journal Article
Scalable, Economical, and Practical Synthesis of 4‑(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors
Rageot, Denise, Beaufils, Florent, Borsari, Chiara, Dall’Asen, Alix, Neuburger, Markus, Hebeisen, Paul, Wymann, Matthias P
Published in Organic process research & development (15.11.2019)
Published in Organic process research & development (15.11.2019)
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Journal Article
Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex
Borsari, Chiara, Keles, Erhan, Rageot, Denise, Melone, Anna, Bohnacker, Thomas, Batchelor, Lucinda Kate, De Pascale, Martina, Hebeisen, Paul, Hillmann, Petra, Fabbro, Doriano, Wymann, Matthias
Published in Cancer research (Chicago, Ill.) (15.08.2020)
Published in Cancer research (Chicago, Ill.) (15.08.2020)
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5-HT2C receptor agonists for the treatment of obesity. Biological and chemical adventures
Adams, D, Benardeau, A, Bickerdike, MJ, Bentley, JM, Bissantz, C, Bourson, A, Cliffe, IA, Hebeisen, P, Kennett, GA, Knight, AR, Malcolm, CS, Mizrahi, J, Plancher, JM, Richter, H, Rover, S, Taylor, S, Vickers, SP
Published in Chimia (01.09.2004)
Published in Chimia (01.09.2004)
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Journal Article
Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability
Borsari, Chiara, Keles, Erhan, Treyer, Andrea, De Pascale, Martina, Hebeisen, Paul, Hamburger, Matthias, Wymann, Matthias P
Published in MedChemComm (28.04.2021)
Published in MedChemComm (28.04.2021)
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Journal Article
Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety
Borsari, Chiara, Rageot, Denise, Beaufils, Florent, Bohnacker, Thomas, Keles, Erhan, Buslov, Ivan, Melone, Anna, Sele, Alexander M, Hebeisen, Paul, Fabbro, Doriano, Hillmann, Petra, Wymann, Matthias P
Published in ACS medicinal chemistry letters (10.10.2019)
Published in ACS medicinal chemistry letters (10.10.2019)
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Molecular Structure and Crystal Packing of Monofluoromethoxyarenes
Hebeisen, Paul, Weiss, Urs, Alker, André, Kuhn, Bernd, Müller, Klaus, Wang, Fang, Surya Prakash, G. K.
Published in European journal of organic chemistry (01.08.2018)
Published in European journal of organic chemistry (01.08.2018)
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