68559-60-4Relevant academic research and scientific papers
IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS
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Paragraph 0092; 00156, (2020/06/05)
The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH.
In-flow photooxygenation of aminothienopyridinones generates iminopyridinedione PTP4A3 phosphatase inhibitors
Tasker, Nikhil R.,Rastelli, Ettore J.,Blanco, Isabella K.,Burnett, James C.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
, p. 2448 - 2466 (2019/03/06)
A continuous flow photooxygenation of 7-aminothieno[3,2-c]pyridin-4(5H)-ones to produce 7-iminothieno[3,2-c]pyridine-4,6(5H,7H)-diones has been developed, utilizing ambient air as the sole reactant. N-H Imines are formed as the major products, and excellent functional group tolerance and conversion on gram-scale without the need for chromatographic purification allow for facile late-stage diversification of the aminothienopyridinone scaffold. Several analogs exhibit potent in vitro inhibition of the cancer-associated protein tyrosine phosphatase PTP4A3, and the SAR supports an exploratory docking model.
INHIBITORS OF PTP4A3 FOR THE TREATMENT OF CANCER
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Page/Page column 24, (2017/01/02)
The invention provides protein tyrosine phosphatase inhibitor compounds, Their pharmaceutical compositions, uses, and methods of use, such as in the treatment of various cancers, and process for making the compounds. Also disclosed is an improved synthesi
Photooxygenation of an amino-thienopyridone yields a more potent PTP4A3 inhibitor
Salamoun, Joseph M.,McQueeney, Kelley E.,Patil, Kalyani,Geib, Steven J.,Sharlow, Elizabeth R.,Lazo, John S.,Wipf, Peter
, p. 6398 - 6402 (2016/07/16)
The phosphatase PTP4A3 is an attractive anticancer target, but knowledge of its exact role in cells remains incomplete. A potent, structurally novel inhibitor of the PTP4A family was obtained by photooxygenation of a less active, electron-rich thienopyrid
17a-HYDROXYLASE/C17,20-LYASE INHIBITORS
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, (2014/03/21)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
Synthesis of new thienopyridine derivatives by a reaction of 4-(Methylsulfanyl)-6,7-dihydrothieno[3,2-c]pyridine with amino acids
Milen, Matyas,Abranyi-Balogh, Peter,Dancso, Andras,Drahos, Laszlo,Keglevich, Gyoergy
, p. 124 - 130 (2013/04/24)
New thienopyridine derivatives were synthesized by the reaction of 4-(methylsulfanyl)-6,7-dihydrothieno[3,2-c]pyridine (5) with amino acids. The use of β-amino acids led to thienopyridopyrimidone derivatives (9a-g). Using α-amino acids, such as glycine and racemic alanine under the same reaction conditions, compounds with two thienopyridine units were obtained. The structure of the novel compounds was confirmed by IR, 13C, and 1H NMR spectroscopy, as well as mass spectrometry, along with single crystal X-ray analysis. 2013 Wiley Periodicals, Inc. Heteroatom Chem 24:124-130, 2013; View this article online at wileyonlinelibrary.com. DOI 10.1002/hc.21073
17α-HYDROXYLASE/C17,20-LYASE INHIBITORS
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Page/Page column 47, (2012/04/04)
The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.
Thieno[2,3-c] and [3,2-c]pyridines, process for their preparation and therapeutic applications thereof
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, (2008/06/13)
This invention relates to compounds having the formulae STR1 in which: R1 represents hydrogen, a halogen atom or a lower alkyl radical, a lower alkoxy radical or a lower alkylthio radical; R2 represents hydrogen or a lower alkyl, ara
