Denise Rageot

发表

PQR309 Is a Novel Dual PI3K/mTOR Inhibitor with Preclinical Antitumor Activity in Lymphomas as a Single Agent and in Combination Therapy

D. Fabbro, L. Cascione, D. Rossi, 2017, Clinical Cancer Research.

Scalable, Economical, and Practical Synthesis of 4-(Difluoromethyl)pyridin-2-amine, a Key Intermediate for Lipid Kinase Inhibitors

M. Neuburger, M. Wymann, F. Beaufils, 2019, Organic Process Research & Development.

The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax

D. Fabbro, L. Cascione, A. Stathis, 2019, Cancers.

The novel, catalytic mTORC1/2 inhibitor PQR620 and the PI3K/mTORC1/2 inhibitor PQR530 effectively cross the blood-brain barrier and increase seizure threshold in a mouse model of chronic epilepsy

D. Fabbro, W. Löscher, M. Wymann, 2018, Neuropharmacology.

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

D. Fabbro, M. Zvelebil, Roger L. Williams, 2017, Nature Communications.

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.

J. Mestan, D. Fabbro, M. Zvelebil, 2017, Journal of medicinal chemistry.

Chiral Proline‐Based P,O and P,N Ligands for Iridium‐Catalyzed Asymmetric Hydrogenation

A. Pfaltz, Denise Rageot, 2012 .

Proline-based P,O ligand/iridium complexes as highly selective catalysts: asymmetric hydrogenation of trisubstituted alkenes.

B. Pugin, A. Pfaltz, Denise Rageot, 2011, Angewandte Chemie.

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-Pyrrolo-Oxazine mTOR Inhibitor.

D. Fabbro, M. Wymann, F. Beaufils, 2019, Journal of medicinal chemistry.

Preclinical Development of PQR514, a Highly Potent PI3K Inhibitor Bearing a Difluoromethyl–Pyrimidine Moiety

Ivan V. Buslov, D. Fabbro, M. Wymann, 2019, ACS medicinal chemistry letters.

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.

D. Fabbro, W. Löscher, M. Wymann, 2020, Journal of medicinal chemistry.

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.

D. Fabbro, M. Zvelebil, W. Löscher, 2018, Journal of medicinal chemistry.

Brain-penetrant PQR620 mTOR and PQR530 PI3K/mTOR inhibitor reduce huntingtin levels in cell models of HD

D. Fabbro, O. Riess, M. Wymann, 2020, Neuropharmacology.

( 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.

D. Fabbro, J. Burke, M. Wymann, 2019, Journal of medicinal chemistry.

The Novel TORC1/2 Kinase Inhibitor PQR620 Has Anti-Tumor Activity in Lymphomas as a Single Agent and in Combination with Venetoclax

D. Fabbro, L. Cascione, A. Stathis, 2019, Cancers.

Abstract 671: BKM120-mediated G2 arrest: Structural and functional segregation of off-target action and PI3K inhibition

D. Fabbro, M. Zvelebil, Roger L. Williams, 2015 .