Search Results - "VERHEIJEN, Jeroen" :: K.UTB vyhledávací portál | TBU Library Retrieval Portal

Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β‑Lactamases

Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β‑Lactamases

by Durand-Réville, Thomas F, Comita-Prevoir, Janelle, Zhang, Jing, Wu, Xiaoyun, May-Dracka, Tricia L, Romero, Jan Antoinette C, Wu, Frank, Chen, April, Shapiro, Adam B, Carter, Nicole M, McLeod, Sarah M, Giacobbe, Robert A, Verheijen, Jeroen C, Lahiri, Sushmita D, Sacco, Michael D, Chen, Yu, O’Donnell, John P, Miller, Alita A, Mueller, John P, Tommasi, Rubén A
Published in Journal of medicinal chemistry (12.11.2020)

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Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

Biochemical, Cellular, and In vivo Activity of Novel ATP-Competitive and Selective Inhibitors of the Mammalian Target of Rapamycin

by KER YU, TORAL-BARZA, Lourdes, COLE, Derek C, ELLINGBOE, John, AYRAL-KALOUSTIAN, Semiramis, MANSOUR, Tarek S, GIBBONS, James J, ABRAHAM, Robert T, NOWAK, Pawel, ZASK, Arie, SHI, Celine, ZHANG, Wei-Guo, LUCAS, Judy, SHOR, Boris, KIM, Jamie, VERHEIJEN, Jeroen, CURRAN, Kevin, MALWITZ, David J
Published in Cancer research (Chicago, Ill.) (01.08.2009)

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Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2

Beyond Rapalog Therapy: Preclinical Pharmacology and Antitumor Activity of WYE-125132, an ATP-Competitive and Specific Inhibitor of mTORC1 and mTORC2

by KER YU, SHI, Celine, SUNG KYOO KIM, CONANT, Roger, CURRAN, Kevin, KAPLAN, Joshua, VERHEIJEN, Jeroen, AYRAL-KALOUSTIAN, Semiramis, MANSOUR, Tarek S, ABRAHAM, Robert T, ZASK, Arie, GIBBONS, James J, TORAL-BARZA, Lourdes, LUCAS, Judy, SHOR, Boris, JAE EUN KIM, ZHANG, Wei-Guo, MAHONEY, Robert, GAYDOS, Christine, TARDIO, Luanna
Published in Cancer research (Chicago, Ill.) (15.01.2010)

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Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors

Morpholine Derivatives Greatly Enhance the Selectivity of Mammalian Target of Rapamycin (mTOR) Inhibitors

by Zask, Arie, Kaplan, Joshua, Verheijen, Jeroen C, Richard, David J, Curran, Kevin, Brooijmans, Natasja, Bennett, Eric M, Toral-Barza, Lourdes, Hollander, Irwin, Ayral-Kaloustian, Semiramis, Yu, Ker
Published in Journal of medicinal chemistry (24.12.2009)

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Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabicyclo[3.2.1 ]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K

Discovery of 2-arylthieno[3,2-d]pyrimidines containing 8-oxa-3-azabicyclo[3.2.1 ]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K

by VERHEIJEN, Jeroen C, YU, Ker, TORAL-BARZA, Lourdes, HOLLANDER, Irwin, ZASK, Arie
Published in Bioorganic & medicinal chemistry letters (2010)

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ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines

ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines

by Zask, Arie, Verheijen, Jeroen C, Curran, Kevin, Kaplan, Joshua, Richard, David J, Nowak, Pawel, Malwitz, David J, Brooijmans, Natasja, Bard, Joel, Svenson, Kristine, Lucas, Judy, Toral-Barza, Lourdes, Zhang, Wei-Guo, Hollander, Irwin, Gibbons, James J, Abraham, Robert T, Ayral-Kaloustian, Semiramis, Mansour, Tarek S, Yu, Ker
Published in Journal of medicinal chemistry (27.08.2009)

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Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

Discovery of 3,6-dihydro-2H-pyran as a morpholine replacement in 6-aryl-1H-pyrazolo[3,4-d]pyrimidines and 2-arylthieno[3,2-d]pyrimidines: ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR)

by KAPLAN, Joshua, VERHEIJEN, Jeroen C, BROOIJMANS, Natasja, TORAL-BARZA, Lourdes, HOLLANDER, Irwin, YU, Ker, ZASK, Arie
Published in Bioorganic & medicinal chemistry letters (15.01.2010)

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Discovery of 2-arylthieno[3,2- d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K

Discovery of 2-arylthieno[3,2- d]pyrimidines containing 8-oxa-3-azabi-cyclo[3.2.1]octane in the 4-position as potent inhibitors of mTOR with selectivity over PI3K

by Verheijen, Jeroen C., Yu, Ker, Toral-Barza, Lourdes, Hollander, Irwin, Zask, Arie
Published in Bioorganic & medicinal chemistry letters (2010)

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Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent

Pyrazolopyrimidines as highly potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 1-substituent

by Curran, Kevin J., Verheijen, Jeroen C., Kaplan, Joshua, Richard, David J., Toral-Barza, Lourdes, Hollander, Irwin, Lucas, Judy, Ayral-Kaloustian, Semiramis, Yu, Ker, Zask, Arie
Published in Bioorganic & medicinal chemistry letters (15.02.2010)

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Triazines incorporating ( R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα

Triazines incorporating ( R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kα

by Richard, David J., Verheijen, Jeroen C., Yu, Ker, Zask, Arie
Published in Bioorganic & medicinal chemistry letters (15.04.2010)

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Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review

Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review

by Zask, Arie, Verheijen, Jeroen C, Richard, David J
Published in Expert opinion on therapeutic patents (01.07.2011)

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Discovery of 4-Morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as Highly Potent and Selective ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin (mTOR): Optimization of the 6-Aryl Substituent

Discovery of 4-Morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as Highly Potent and Selective ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin (mTOR): Optimization of the 6-Aryl Substituent

by Verheijen, Jeroen C, Richard, David J, Curran, Kevin, Kaplan, Joshua, Lefever, Mark, Nowak, Pawel, Malwitz, David J, Brooijmans, Natasja, Toral-Barza, Lourdes, Zhang, Wei-Guo, Lucas, Judy, Hollander, Irwin, Ayral-Kaloustian, Semiramis, Mansour, Tarek S, Yu, Ker, Zask, Arie
Published in Journal of medicinal chemistry (24.12.2009)

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Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors

Discovery of 2-ureidophenyltriazines bearing bridged morpholines as potent and selective ATP-competitive mTOR inhibitors

by Zask, Arie, Verheijen, Jeroen C., Richard, David J., Kaplan, Joshua, Curran, Kevin, Toral-Barza, Lourdes, Lucas, Judy, Hollander, Irwin, Yu, Ker
Published in Bioorganic & medicinal chemistry letters (15.04.2010)

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2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability

2-Arylureidophenyl-4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)triazines as highly potent and selective ATP competitive mTOR inhibitors: Optimization of human microsomal stability

by Verheijen, Jeroen C., Richard, David J., Curran, Kevin, Kaplan, Joshua, Yu, Ker, Zask, Arie
Published in Bioorganic & medicinal chemistry letters (15.04.2010)

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Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase

Discovery of Potent and Selective Inhibitors of the Mammalian Target of Rapamycin (mTOR) Kinase

by Nowak, Pawel, Cole, Derek C, Brooijmans, Natasja, Bursavich, Matthew G, Curran, Kevin J, Ellingboe, John W, Gibbons, James J, Hollander, Irwin, Hu, YongBo, Kaplan, Joshua, Malwitz, David J, Toral-Barza, Lourdes, Verheijen, Jeroen C, Zask, Arie, Zhang, Wei-Guo, Yu, Ker
Published in Journal of medicinal chemistry (26.11.2009)

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New antibacterial agents: patent applications published in 2011

New antibacterial agents: patent applications published in 2011

by Keating, Thomas A, Lister, Troy, Verheijen, Jeroen C
Published in Pharmaceutical patent analyst (01.01.2014)

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4,5-Disubstituted 6‑Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β‑Lactamase Inhibitors

4,5-Disubstituted 6‑Aryloxy-1,3-dihydrobenzo[c][1,2]oxaboroles Are Broad-Spectrum Serine β‑Lactamase Inhibitors

by McKinney, David C, Zhou, Fei, Eyermann, Charles J, Ferguson, Andrew D, Prince, D. Bryan, Breen, John, Giacobbe, Robert A, Lahiri, Sushmita, Verheijen, Jeroen C
Published in ACS infectious diseases (10.07.2015)

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Alkylidene Oxapenem β‑Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges

Alkylidene Oxapenem β‑Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges

by Miller, Matthew D, Kale, Manoj, Reddy, Kishore, Tentarelli, Sharon, Zambrowski, Mark, Zhang, Minli, Palmer, Tiffany, Breen, John, Lahiri, Sushmita, Shirude, Pravin S, Verheijen, Jeroen C
Published in ACS medicinal chemistry letters (14.08.2014)

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New antibacterial agents: patent applications published in 2010

New antibacterial agents: patent applications published in 2010

by Stokes, Suzanne S, Morningstar, Marshall, Kocis, Helena, Verheijen, Jeroen C
Published in Pharmaceutical patent analyst (01.11.2012)

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Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition

Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition

by Verheijen, Jeroen C., Wiig, Kjesten A., Du, Shoucheng, Connors, Stacie L., Martin, Ashley N., Ferreira, Jennifer P., Slepnev, Vladimir I., Kochendörfer, Ulrike
Published in Bioorganic & medicinal chemistry letters (15.06.2009)

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