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

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Pages 1109-1127 | Published online: 19 May 2011

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Han-Yue Qiu, Peng-Fei Wang & Min Zhang. (2021) A patent review of mTOR inhibitors for cancer therapy (2011–2020). Expert Opinion on Therapeutic Patents 31:11, pages 965-975.
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Azam Roohi & Mohammad Hojjat-Farsangi. (2017) Recent advances in targeting mTOR signaling pathway using small molecule inhibitors. Journal of Drug Targeting 25:3, pages 189-201.
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Juan B. Rodriguez, Bruno N. Falcone & Sergio H. Szajnman. (2016) Detection and treatment of Trypanosoma cruzi: a patent review (2011-2015). Expert Opinion on Therapeutic Patents 26:9, pages 993-1015.
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Articles from other publishers (21)

Kewalin Posansee, Monrudee Liangruksa, Teerasit Termsaithong, Patchreenart Saparpakorn, Supa Hannongbua, Teeraphan Laomettachit & Thana Sutthibutpong. (2023) Combined Deep Learning and Molecular Modeling Techniques on the Virtual Screening of New mTOR Inhibitors from the Thai Mushroom Database. ACS Omega 8:41, pages 38373-38385.
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Edouard Duchamp, Rory Devin, Pedro M. Aguiar, Arthur Gaucherand & Stephen Hanessian. (2022) Polygonapholine: A Total Synthesis Questions the Identity for the Purported Structure of the Natural Product. The Journal of Organic Chemistry 87:22, pages 15713-15718.
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Pratibha Yadav & Kamal Shah. (2020) An overview on synthetic and pharmaceutical prospective of pyrido[2,3‐ d ]pyrimidines scaffold . Chemical Biology & Drug Design 97:3, pages 633-648.
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Chetna Kumari, Muhammad Abulaish & Naidu Subbarao. (2020) Using SMOTE to Deal with Class-Imbalance Problem in Bioactivity Data to Predict mTOR Inhibitors. SN Computer Science 1:3.
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Guobing Shen, Miaoqing Liu, Jianjun Lu & Tao Meng. (2019) Practical synthesis of Vistusertib (AZD2014), an ATP competitive mTOR inhibitor. Tetrahedron Letters 60:52, pages 151333.
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Gilles Ouvry, Laurence Clary, Loïc Tomas, Michèle Aurelly, Laetitia Bonnary, Emilie Borde, Claire Bouix-Peter, Laurent Chantalat, Claire Defoin-Platel, Sophie Deret, Mathieu Forissier, Craig S. Harris, Tatiana Isabet, Laurent Lamy, Anne-Pascale Luzy, Jonathan Pascau, Catherine Soulet, Alessandro Taddei, Nathalie Taquet, Etienne Thoreau, Emeric Varvier, Emmanuel Vial & Laurent F. Hennequin. (2019) Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors. ACS Medicinal Chemistry Letters 10:11, pages 1561-1567.
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Claudia Brandt, Petra Hillmann, Andreas Noack, Kerstin Römermann, Leon A. Öhler, Denise Rageot, Florent Beaufils, Anna Melone, Alexander M. Sele, Matthias P. Wymann, Doriano Fabbro & Wolfgang Löscher. (2018) 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. Neuropharmacology 140, pages 107-120.
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Shiva Krishna Reddy Guduru & Prabhat Arya. (2018) Synthesis and biological evaluation of rapamycin-derived, next generation small molecules. MedChemComm 9:1, pages 27-43.
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Chengbin Yang, Xi Zhang, Yi Wang, Yongtai Yang, Xiaofeng Liu, Mingli Deng, Yu Jia, Yun Ling, Ling-hua Meng & Yaming Zhou. (2017) Discovery of a Novel Series of 7-Azaindole Scaffold Derivatives as PI3K Inhibitors with Potent Activity. ACS Medicinal Chemistry Letters 8:8, pages 875-880.
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Ling Wang, Lei Chen, Miao Yu, Li-Hui Xu, Bao Cheng, Yong-Sheng Lin, Qiong Gu, Xian-Hui He & Jun Xu. (2016) Discovering new mTOR inhibitors for cancer treatment through virtual screening methods and in vitro assays. Scientific Reports 6:1.
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Charles J Malemud. (2015) The PI3K/Akt/PTEN/mTOR pathway: a fruitful target for inducing cell death in rheumatoid arthritis?. Future Medicinal Chemistry 7:9, pages 1137-1147.
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Asli Ozmen, Gozde Unek, Dijle Kipmen-Korgun, Busra Cetinkaya, Zeynep Avcil & Emin Türkay Korgun. (2015) Glucocorticoid exposure altered angiogenic factor expression via Akt/mTOR pathway in rat placenta. Annals of Anatomy - Anatomischer Anzeiger 198, pages 34-40.
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Ling Wang, Lei Chen, Zhihong Liu, Minghao Zheng, Qiong Gu & Jun Xu. (2014) Predicting mTOR Inhibitors with a Classifier Using Recursive Partitioning and Naïve Bayesian Approaches. PLoS ONE 9:5, pages e95221.
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Raffael Liegl, Susanna Koenig, Jakob Siedlecki, Christos Haritoglou, Anselm Kampik & Marcus Kernt. (2014) Temsirolimus Inhibits Proliferation and Migration in Retinal Pigment Epithelial and Endothelial Cells via mTOR Inhibition and Decreases VEGF and PDGF Expression. PLoS ONE 9:2, pages e88203.
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Wendy Lee, Daniel F. Ortwine, Philippe Bergeron, Kevin Lau, Lichuan Lin, Shiva Malek, Jim Nonomiya, Zhonghua Pei, Kirk D. Robarge, Stephen Schmidt, Steve Sideris & Joseph P. Lyssikatos. (2013) A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors. Bioorganic & Medicinal Chemistry Letters 23:18, pages 5097-5104.
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Jing Zhou, Shi-Hao Tan, Valérie Nicolas, Chantal Bauvy, Nai-Di Yang, Jianbin Zhang, Yuan Xue, Patrice Codogno & Han-Ming Shen. (2013) Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion. Cell Research 23:4, pages 508-523.
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Tommy Alain, Masahiro Morita, Bruno D. Fonseca, Akiko Yanagiya, Nadeem Siddiqui, Mamatha Bhat, Domenick Zammit, Victoria Marcus, Peter Metrakos, Lucie-Anne Voyer, Valentina Gandin, Yi Liu, Ivan Topisirovic & Nahum Sonenberg. (2012) eIF4E/4E-BP Ratio Predicts the Efficacy of mTOR Targeted Therapies. Cancer Research 72:24, pages 6468-6476.
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John G. Foster, Matthew D. Blunt, Edward Carter & Stephen G. Ward. (2012) Inhibition of PI3K Signaling Spurs New Therapeutic Opportunities in Inflammatory/Autoimmune Diseases and Hematological Malignancies. Pharmacological Reviews 64:4, pages 1027-1054.
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M. Raymond V. Finlay, David Buttar, Susan E. Critchlow, Allan P. Dishington, Shaun M. Fillery, Eric Fisher, Steve C. Glossop, Mark A. Graham, Trevor Johnson, Gillian M. Lamont, Simon Mutton, Paula Perkins, Kurt G. Pike & Anthony M. Slater.. (2012) Sulfonyl-morpholino-pyrimidines: SAR and development of a novel class of selective mTOR kinase inhibitor. Bioorganic & Medicinal Chemistry Letters 22:12, pages 4163-4168.
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Catherine Terret & Florence Solari. (2012) L’homéostasie métabolique au cœur du vieillissement. médecine/sciences 28:3, pages 311-315.
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Don Benjamin, Marco Colombi, Christoph Moroni & Michael N. Hall. (2011) Rapamycin passes the torch: a new generation of mTOR inhibitors. Nature Reviews Drug Discovery 10:11, pages 868-880.
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