1204669-69-1Relevant academic research and scientific papers
Preparation method of IDO1 inhibitor Epacadostat intermediate
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Paragraph 0007; 0015; 0033; 0060; 0061, (2018/06/26)
The invention relates to the drug synthesis field, specifically to a preparation method of an IDO1 (indoleamine-2, 3-dioxygenase 1) inhibitor Epacadostat intermediate 4-(3-bromo-4-fluorophenyl)-3-(4-((2-bromoethyl)amino)-1, 2, 5-oxadiazole-3-yl)-1, 2, 4-o
INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology
Yue, Eddy W.,Sparks, Richard,Polam, Padmaja,Modi, Dilip,Douty, Brent,Wayland, Brian,Glass, Brian,Takvorian, Amy,Glenn, Joseph,Zhu, Wenyu,Bower, Michael,Liu, Xiangdong,Leffet, Lynn,Wang, Qian,Bowman, Kevin J.,Hansbury, Michael J.,Wei, Min,Li, Yanlong,Wynn, Richard,Burn, Timothy C.,Koblish, Holly K.,Fridman, Jordan S.,Emm, Tom,Scherle, Peggy A.,Metcalf, Brian,Combs, Andrew P.
supporting information, p. 486 - 491 (2017/05/19)
A data-centric medicinal chemistry approach led to the invention of a potent and selective IDO1 inhibitor 4f, INCB24360 (epacadostat). The molecular structure of INCB24360 contains several previously unknown or underutilized functional groups in drug subs
1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
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Page/Page column 42; 43, (2016/05/24)
The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR
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Paragraph 0270; 0284; 0285; 0287, (2015/05/26)
The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful i
SYNERGISTIC COMBINATION OF IMMUNOLOGIC INHIBITORS FOR THE TREATMENT OF CANCER
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Paragraph 00196-00197; 00308, (2014/05/24)
In some embodiments, the methods involve the use of a combination of at least two of the following: an inhibitor of indoleamine-2,3-dioxygenase (IDO), an inhibitor of the PD-L1/PD-1 pathway, an inhibitor of CTLA-4, an inhibitor of CD25, or IL-7. The inven
1,2,5-OXADIAZOLES AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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, (2010/02/17)
The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.
