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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

Journal of medicinal chemistry, 2017-09, Vol.60 (17), p.7524-7538

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

Journal of medicinal chemistry, 2013-12, Vol.56 (24), p.9874-9896

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

Antimicrobial Agents and Chemotherapy, 2001-03, Vol.45 (3), p.825-836

2001

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Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes

Organic & biomolecular chemistry, 2010-01, Vol.8 (4), p.758-760

2010

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Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

Synthesis (Stuttgart), 2023-02, Vol.55 (3), p.499-509

2023

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Abstract 293: Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitors suitable for the treatment of CNS disorders

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.293-293

2021

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New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine

Journal of medicinal chemistry, 2004-03, Vol.47 (6), p.1487-1513

2004

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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

Journal of medicinal chemistry, 2018-11, Vol.61 (22), p.10084-10105

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

Journal of medicinal chemistry, 2019-07, Vol.62 (13), p.6241-6261

2019

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A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

Journal of medicinal chemistry, 2019-09, Vol.62 (18), p.8609-8630

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

Journal of medicinal chemistry, 2020-11, Vol.63 (22), p.13595-13617

2020

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Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor

European journal of medicinal chemistry, 2023-02, Vol.248, p.115038-115038, Article 115038

2023

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

Organic process research & development, 2019-11, Vol.23 (11), p.2416-2424

2019

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Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex

Cancer research (Chicago, Ill.), 2020-08, Vol.80 (16_Supplement), p.665-665

2020

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

ACS medicinal chemistry letters, 2019-10, Vol.10 (10), p.1473-1479

2019

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Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability

RSC medicinal chemistry, 2021-04, Vol.12 (4), p.579-583

2021

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Molecular Structure and Crystal Packing of Monofluoromethoxyarenes

European journal of organic chemistry, 2018-08, Vol.2018 (27-28), p.3724-3734

2018

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Ring opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines

Tetrahedron letters, 2011-10, Vol.52 (41), p.5229-5233

2011

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A New DNA Gyrase Inhibitor Subclass of the Cyclothialidine Family Based on a Bicyclic Dilactam−Lactone Scaffold. Synthesis and Antibacterial Properties

Journal of medicinal chemistry, 2011-04, Vol.54 (7), p.2207-2224

2011

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Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.140-140

2017

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Abstract 153: Tricyclic fused pyrimidinopyrrolo-oxazines reveal conformational preferences of morpholine for PI3K hinge region binding

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.153-153

2017

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Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.1336-1336

2016

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Abstract 159: Pharmacological characterization of the selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor PQR530

Cancer research (Chicago, Ill.), 2017-07, Vol.77 (13_Supplement), p.159-159

2017

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Abstract 393A: Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620

Cancer research (Chicago, Ill.), 2016-07, Vol.76 (14_Supplement), p.393-393A

2016

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Abstract 4514: PQR309: A potent, brain-penetrant, dual pan-PI3K/mTOR inhibitor with excellent oral bioavailability and tolerability

Cancer research (Chicago, Ill.), 2015-08, Vol.75 (15_Supplement), p.4514-4514

2015

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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

6‑Alkoxy-5-aryl-3-pyridinecarboxamides, a New Series of Bioavailable Cannabinoid Receptor Type 1 (CB1) Antagonists Including Peripherally Selective Compounds

In Vitro and In Vivo Properties of Ro 63-9141, a Novel Broad-Spectrum Cephalosporin with Activity against Methicillin-Resistant Staphylococci

Enantioselective desymmetrizing palladium catalyzed carbonylation reactions: the catalytic asymmetric synthesis of quaternary carbon center containing 1,3-dienes

Stereospecific Synthesis of Substituted Sulfamidates as Privileged Morpholine Building Blocks

Abstract 293: Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitors suitable for the treatment of CNS disorders

New Antibacterial Agents Derived from the DNA Gyrase Inhibitor Cyclothialidine

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

(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

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

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

Investigation of morpholine isosters for the development of a potent, selective and metabolically stable mTOR kinase inhibitor

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

Abstract 665: Discovery and preclinical characterization of PQR626: A potent, orally available, and brain-penetrant mTOR inhibitor for the treatment of tuberous sclerosis complex

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

Second-generation tricyclic pyrimido-pyrrolo-oxazine mTOR inhibitor with predicted blood-brain barrier permeability

Molecular Structure and Crystal Packing of Monofluoromethoxyarenes

Ring opening of cyclic sulfamidates with bromophenyl metal reagents: complementarity of sulfamidates and aziridines

A New DNA Gyrase Inhibitor Subclass of the Cyclothialidine Family Based on a Bicyclic Dilactam−Lactone Scaffold. Synthesis and Antibacterial Properties

Abstract 140: Discovery and biological evaluation of PQR530, a highly potent dual pan-PI3K/mTORC1/2 inhibitor

Abstract 153: Tricyclic fused pyrimidinopyrrolo-oxazines reveal conformational preferences of morpholine for PI3K hinge region binding

Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor

Abstract 159: Pharmacological characterization of the selective, orally bioavailable, potent dual PI3K/mTORC1/2 inhibitor PQR530

Abstract 393A: Pharmacological characterization of the selective, orally bioavailable, potent mTORC1/2 inhibitor PQR620

Abstract 4514: PQR309: A potent, brain-penetrant, dual pan-PI3K/mTOR inhibitor with excellent oral bioavailability and tolerability

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