1,103
Views
47
CrossRef citations to date
0
Altmetric
Reviews

Selective PI3Kδ inhibitors, a review of the patent literature

Pages 1773-1790 | Published online: 22 Oct 2011

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (8)

Yifan Feng, Xiaochuan Cu & Minhang Xin. (2019) PI3Kδ inhibitors for the treatment of cancer: a patent review (2015-present). Expert Opinion on Therapeutic Patents 29:12, pages 925-941.
Read now
Minhang Xin, Weiming Duan, Yifan Feng, Yuan-Yuan Hei, Hao Zhang, Ying Shen, Hong-Yi Zhao, Shuai Mao & San-Qi Zhang. (2018) Introduction of pyrrolidineoxy or piperidineamino group at the 4-position of quinazoline leading to novel quinazoline-based phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry 33:1, pages 651-656.
Read now
Peter Norman. (2014) Evaluation of WO2014075392 and WO2014075393, Merck’s first PI3Kδ inhibitor filings. Expert Opinion on Therapeutic Patents 24:11, pages 1277-1282.
Read now
Peter Norman. (2014) Evaluation of WO2013116562A, an orally active PI3Kδ inhibitor for the treatment of asthma. Expert Opinion on Therapeutic Patents 24:5, pages 603-607.
Read now
Peter Norman. (2014) Evaluation of WO2013136076: two crystalline forms of the phosphatidylinositol 3-kinase-δ inhibitor RV-1729. Expert Opinion on Therapeutic Patents 24:4, pages 471-475.
Read now
William A Denny. (2013) Phosphoinositide 3-kinase α inhibitors: a patent review. Expert Opinion on Therapeutic Patents 23:7, pages 789-799.
Read now
Peter Norman. (2012) Evaluation of WO2012032067 and WO2012055846: two selective PI3Kδ inhibitors, which is GSK-2269557?. Expert Opinion on Therapeutic Patents 22:8, pages 965-970.
Read now

Articles from other publishers (39)

Yee Han Chan, Kong Yen Liew, Ji Wei Tan, Khozirah Shaari, Daud Ahmad Israf & Chau Ling Tham. (2021) Pharmacological Properties of 2,4,6-Trihydroxy-3-Geranyl Acetophenone and the Underlying Signaling Pathways: Progress and Prospects. Frontiers in Pharmacology 12.
Crossref
Jeong-Tae Yeon, Kwang-Jin Kim, Young-Jin Son, Sang-Joon Park & Seong Hwan Kim. (2019) Idelalisib inhibits osteoclast differentiation and pre-osteoclast migration by blocking the PI3Kδ-Akt-c-Fos/NFATc1 signaling cascade. Archives of Pharmacal Research 42:8, pages 712-721.
Crossref
Xiaodong Ma, Jun Wei, Chang Wang, Dongyan Gu, Yongzhou Hu & Rong Sheng. (2019) Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. European Journal of Medicinal Chemistry 170, pages 112-125.
Crossref
Xiaodong Ma, Fang Fang, Qiangqiang Tao, Li Shen, Guochen Zhong, Tao Qiao, Xiaoqing Lv & Jiaming Li. (2019) Conformationally restricted quinazolone derivatives as PI3Kδ-selective inhibitors: the design, synthesis and biological evaluation. MedChemComm 10:3, pages 413-420.
Crossref
Nick BartonMáire ConveryAnthony W. J. CooperKenneth Down, J. Nicole HamblinGraham InglisSimon PeaceJames RowedderPaul RowlandJonathan A. TaylorNatalie Wellaway. (2018) Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach. Journal of Medicinal Chemistry 61:24, pages 11061-11073.
Crossref
Chen-Chen Ma, Cheng-Mei Zhang, Long-Qian Tang & Zhao-Peng Liu. (2018) Discovery of novel quinazolinone derivatives as high potent and selective PI3Kδ and PI3Kδ/γ inhibitors. European Journal of Medicinal Chemistry 151, pages 9-17.
Crossref
Minhang Xin, Weiming Duan, Yifan Feng, Yuan-Yuan Hei, Hao Zhang, Ying Shen, Hong-Yi Zhao, Shuai Mao & San-Qi Zhang. (2018) Novel 6-aryl substituted 4-pyrrolidineaminoquinazoline derivatives as potent phosphoinositide 3-kinase delta (PI3Kδ) inhibitors. Bioorganic & Medicinal Chemistry 26:8, pages 2028-2040.
Crossref
Tadashi Katoh & Koichi Narita. (2018) Total Syntheses of Liphagal: A Potent and Selective Phosphoinositide 3-Kinase α (PI3Kα) Inhibitor from the Marine Sponge Aka coralliphaga. HETEROCYCLES 96:1, pages 3.
Crossref
Ji Wei Tan, Daud Ahmad Israf, Nur Fariesha Md Hashim, Yoke Kqueen Cheah, Hanis Hazeera Harith, Khozirah Shaari & Chau Ling Tham. (2017) LAT is essential for the mast cell stabilising effect of tHGA in IgE-mediated mast cell activation. Biochemical Pharmacology 144, pages 132-148.
Crossref
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.
Crossref
Qingjie Liu, Qing Shi, David Marcoux, Douglas G. Batt, Lyndon Cornelius, Lan-Ying Qin, Zheming Ruan, James Neels, Myra Beaudoin-Bertrand, Anurag S. Srivastava, Ling Li, Robert J. Cherney, Hua Gong, Scott H. Watterson, Carolyn Weigelt, Kathleen M. Gillooly, Kim W. McIntyre, Jenny H. Xie, Mary T. Obermeier, Aberra Fura, Bogdan Sleczka, Kevin Stefanski, R. M. Fancher, Shweta Padmanabhan, Thatipamula RP, Ipsit Kundu, Kallem Rajareddy, Rodney Smith, James K. Hennan, Dezhi Xing, Jingsong Fan, Paul C. Levesque, Qian Ruan, Sidney Pitt, Rosemary Zhang, Donna Pedicord, Jie Pan, Melissa Yarde, Hao Lu, Jonathan Lippy, Christine Goldstine, Stacey Skala, Richard A. Rampulla, Arvind Mathur, Anuradha Gupta, Pirama Nayagam Arunachalam, John S. Sack, Jodi K. Muckelbauer, Mary Ellen Cvijic, Luisa M. Salter-Cid, Rajeev S. Bhide, Michael A. Poss, John Hynes, Percy H. Carter, John E. Macor, Stefan Ruepp, Gary L. Schieven & Joseph A. Tino. (2017) Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders. Journal of Medicinal Chemistry 60:12, pages 5193-5208.
Crossref
Bernard Barlaam, Sabina Cosulich, Sébastien Degorce, Rebecca Ellston, Martina Fitzek, Stephen Green, Urs Hancox, Christine Lambert-van der Brempt, Jean-Jacques Lohmann, Mickaël Maudet, Rémy Morgentin, Patrick Plé, Lara Ward & Nicolas Warin. (2017) Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorganic & Medicinal Chemistry Letters 27:9, pages 1949-1954.
Crossref
Minhang Xin, Yuan-Yuan Hei, Hao Zhang, Ying Shen & San-Qi Zhang. (2017) Design and synthesis of novel 6-aryl substituted 4-anilinequinazoline derivatives as potential PI3Kδ inhibitors. Bioorganic & Medicinal Chemistry Letters 27:9, pages 1972-1977.
Crossref
Daniel C. Brookings. 2017. Comprehensive Medicinal Chemistry III. Comprehensive Medicinal Chemistry III 366 407 .
Klemens Hoegenauer, Nicolas Soldermann, Christina Hebach, Gregory J. Hollingworth, Ian Lewis, Anette von Matt, Alexander B. Smith, Romain M. Wolf, Rainer Wilcken, Dorothea Haasen, Christoph Burkhart & Frédéric Zécri. (2016) Discovery of novel pyrrolidineoxy-substituted heteroaromatics as potent and selective PI3K delta inhibitors with improved physicochemical properties. Bioorganic & Medicinal Chemistry Letters 26:23, pages 5657-5662.
Crossref
Takuya Kikuchi, Koichi Narita, Ken Saijo, Chikashi Ishioka & Tadashi Katoh. (2016) Enantioselective Total Synthesis of (-)-Siphonodictyal B and (+)-8- epi -Siphonodictyal B with Phosphatidylinositol 3-Kinase α (PI3Kα) Inhibitory Activity . European Journal of Organic Chemistry 2016:34, pages 5659-5666.
Crossref
Klemens Hoegenauer, Nicolas Soldermann, Frédéric Stauffer, Pascal Furet, Nadege Graveleau, Alexander B. Smith, Christina Hebach, Gregory J. Hollingworth, Ian Lewis, Sascha Gutmann, Gabriele Rummel, Mark Knapp, Romain M. Wolf, Joachim Blanz, Roland Feifel, Christoph Burkhart & Frédéric Zécri. (2016) Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors. ACS Medicinal Chemistry Letters 7:8, pages 762-767.
Crossref
Daniel Robinson, Thomas Bertrand, Jean-Christophe Carry, Frank Halley, Andreas Karlsson, Magali Mathieu, Hervé Minoux, Marc-Antoine Perrin, Benoit Robert, Laurent Schio & Woody Sherman. (2016) Differential Water Thermodynamics Determine PI3K-Beta/Delta Selectivity for Solvent-Exposed Ligand Modifications. Journal of Chemical Information and Modeling 56:5, pages 886-894.
Crossref
Bernard Barlaam, Sabina Cosulich, Sébastien Degorce, Martina Fitzek, Stephen Green, Urs Hancox, Christine Lambert-van der Brempt, Jean-Jacques Lohmann, Mickaël Maudet, Rémy Morgentin, Aurélien Péru, Patrick Plé, Twana Saleh, Lara Ward & Nicolas Warin. (2016) Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorganic & Medicinal Chemistry Letters 26:9, pages 2318-2323.
Crossref
Yvonne G Hewett, Dipesh Uprety & Binay K Shah. (2015) Idelalisib- a PI3K? targeting agent for B-cell malignancies. Journal of Oncology Pharmacy Practice 22:2, pages 284-288.
Crossref
Youngsook Shin, Julia Suchomel, Mario Cardozo, Jason Duquette, Xiao He, Kirk Henne, Yi-Ling Hu, Ron C. Kelly, John McCarter, Lawrence R. McGee, Julio C. Medina, Daniela Metz, Tisha San Miguel, Deanna Mohn, Thuy Tran, Christine Vissinga, Simon Wong, Sharon Wannberg, Douglas A. Whittington, John Whoriskey, Gang Yu, Leeanne Zalameda, Xuxia Zhang & Timothy D. Cushing. (2015) Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ Inhibitors. Journal of Medicinal Chemistry 59:1, pages 431-447.
Crossref
Bernard Barlaam, Sabina Cosulich, Bénédicte Delouvrié, Rebecca Ellston, Martina Fitzek, Hervé Germain, Stephen Green, Urs Hancox, Craig S. Harris, Kevin Hudson, Christine Lambert-van der Brempt, Honorine Lebraud, Françoise Magnien, Maryannick Lamorlette, Antoine Le Griffon, Rémy Morgentin, Gilles Ouvry, Ken Page, Georges Pasquet, Urszula Polanska, Linette Ruston, Twana Saleh, Michel Vautier & Lara Ward. (2015) Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Bioorganic & Medicinal Chemistry Letters 25:22, pages 5155-5162.
Crossref
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.
Crossref
Bernard Barlaam, Sabina Cosulich, Sébastien Degorce, Martina Fitzek, Stephen Green, Urs Hancox, Christine Lambert-van der Brempt, Jean-Jacques Lohmann, Mickaël Maudet, Rémy Morgentin, Marie-Jeanne Pasquet, Aurélien Péru, Patrick Plé, Twana Saleh, Michel Vautier, Mike Walker, Lara Ward & Nicolas Warin. (2015) Discovery of ( R )-8-(1-(3,5-Difluorophenylamino)ethyl)- N , N -dimethyl-2-morpholino-4-oxo-4 H -chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers . Journal of Medicinal Chemistry 58:2, pages 943-962.
Crossref
Ilkka T. Harvima, Francesca Levi-Schaffer, Petr Draber, Sheli Friedman, Iva Polakovicova, Bernhard F. Gibbs, Ulrich Blank, Gunnar Nilsson & Marcus Maurer. (2014) Molecular targets on mast cells and basophils for novel therapies. Journal of Allergy and Clinical Immunology 134:3, pages 530-544.
Crossref
Bernard Barlaam, Sabina Cosulich, Sébastien Degorce, Martina Fitzek, Fabrizio Giordanetto, Stephen Green, Tord Inghardt, Laurent Hennequin, Urs Hancox, Christine Lambert-van der Brempt, Rémy Morgentin, Sarah Pass, Patrick Plé, Twana Saleh & Lara Ward. (2014) Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours. Bioorganic & Medicinal Chemistry Letters 24:16, pages 3928-3935.
Crossref
Takaaki Kamishima, Takuya Kikuchi, Koichi Narita & Tadashi Katoh. (2014) Biogenetically Inspired Total Synthesis of (+)‐Liphagal: A Potent and Selective Phosphoinositide 3‐Kinase α (PI3Kα) Inhibitor from the Marine Sponge Aka coralliphaga . European Journal of Organic Chemistry 2014:16, pages 3443-3450.
Crossref
Susan Heavey, Kenneth J. O’Byrne & Kathy Gately. (2014) Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC. Cancer Treatment Reviews 40:3, pages 445-456.
Crossref
William A. Denny & Gordon W. Rewcastle. 2014. Cancer Drug Design and Discovery. Cancer Drug Design and Discovery 449 478 .
Giuseppe Giaccone & Jean-Charles SoriaSimona Wagner & Janet Dancey. 2013. Targeted Therapies in Oncology, Second Edition. Targeted Therapies in Oncology, Second Edition 81 114 .
Shu-Qiang Yin, Min Shi, Ting-Ting Kong, Cheng-Mei Zhang, Kunkun Han, Biyin Cao, Zubin Zhang, Xiaolin Du, Long-Qian Tang, Xinliang Mao & Zhao-Peng Liu. (2013) Preparation of S14161 and its analogues and the discovery of 6-bromo-8-ethoxy-3-nitro-2H-chromene as a more potent antitumor agent in vitro. Bioorganic & Medicinal Chemistry Letters 23:11, pages 3314-3319.
Crossref
Heping Xu, Xuanying Li, Dan Liu, Jianfu Li, Xu Zhang, Xin Chen, Shiyue Hou, Lixia Peng, Chenguang Xu, Wanli Liu, Lianfeng Zhang & Hai Qi. (2013) Follicular T-helper cell recruitment governed by bystander B cells and ICOS-driven motility. Nature 496:7446, pages 523-527.
Crossref
Shu-Qiang Yin, Can-Fei Zhang, Xinliang Mao & Zhao-Peng Liu. (2013) An efficient synthesis of (R)- and (S)-8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene. Tetrahedron: Asymmetry 24:5-6, pages 320-323.
Crossref
Hae-Rim Kim. (2013) Phosphoinositide 3-kinase (PI3K) as a New Therapeutic Target for Rheumatoid Arthritis. Journal of Rheumatic Diseases 20:2, pages 74.
Crossref
Arun Kannan, Weishan Huang, Fei Huang & Avery August. (2012) Signal transduction via the T cell antigen receptor in naïve and effector/memory T cells. The International Journal of Biochemistry & Cell Biology 44:12, pages 2129-2134.
Crossref
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.
Crossref
Kiran Mahajan & Nupam P. Mahajan. (2012) PI3K‐independent AKT activation in cancers: A treasure trove for novel therapeutics. Journal of Cellular Physiology 227:9, pages 3178-3184.
Crossref
Matthew D Blunt & Stephen G Ward. (2012) Targeting PI3K isoforms and SHIP in the immune system: new therapeutics for inflammation and leukemia. Current Opinion in Pharmacology 12:4, pages 444-451.
Crossref
Sonia Martínez González, Ana Isabel Hernández, Carmen Varela, Sonsoles Rodríguez-Arístegui, Rosa María Alvarez, Ana Belén García, Milagros Lorenzo, Virginia Rivero, Julen Oyarzabal, Obdulia Rabal, James R. Bischoff, Maribel Albarrán, Antonio Cebriá, Patricia Alfonso, Wolfgang Link, Jesús Fominaya & Joaquín Pastor. (2012) Imidazo[1,2-a]pyrazines as novel PI3K inhibitors. Bioorganic & Medicinal Chemistry Letters 22:5, pages 1874-1878.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.