1204669-63-5Relevant academic research and scientific papers
INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATION
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Paragraph 0112, (2019/02/19)
The present invention relates to an indoleamine 2,3-dioxygenase inhibitor having the structure of formula (I), a preparation method therefor, and an application. The IDO inhibitor is an N′-hydroxyl-N-phenylformamidine derivative, which has a high inhibito
INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, ITS PREPARATION METHOD AND THE USE THEREOF
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Paragraph 31; 32; 35, (2018/11/22)
The present invention relates to Indoleamine 2,3-dioxygenase inhibitor represented by formula (I), its preparation method and the use thereof. The inhibitor of Indoleamine 2,3-dioxygenase (IDO for short) is the derivative of (Z)-N'-hydroxy-N-phenylformami
Improving the Potency of Cancer Immunotherapy by Dual Targeting of IDO1 and DNA
Fang, Kun,Dong, Guoqiang,Wang, Hongyu,He, Shipeng,Wu, Shanchao,Wang, Wei,Sheng, Chunquan
supporting information, p. 30 - 36 (2017/12/26)
Herein we report the first exploration of a dual-targeting drug design strategy to improve the efficacy of small-molecule cancer immunotherapy. New hybrids of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors and DNA alkylating nitrogen mustards that respectively target IDO1 and DNA were rationally designed. As the first-in-class examples of such molecules, they were found to exhibit significantly enhanced anticancer activity in vitro and in vivo with low toxicity. This proof-of-concept study has established a critical step toward the development of a novel and effective immunotherapy for the treatment of cancers.
Discovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors
Fang, Kun,Dong, Guoqiang,Li, Yu,He, Shipeng,Wu, Ying,Wu, Shanchao,Wang, Wei,Sheng, Chunquan
supporting information, p. 312 - 317 (2018/04/20)
In order to take advantage of both immunotherapeutic and epigenetic antitumor agents, the first generation of dual indoleamine 2,3-dioxygenase 1 (IDO1) and histone deacetylase (HDAC) inhibitors were designed. The highly active dual inhibitor 10 showed exc
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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Page/Page column 19; 22; 23, (2017/01/23)
Provided are compounds of formula (I) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the prog
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 39; 40, (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.
SYNERGISTIC COMBINATION OF IMMUNOLOGIC INHIBITORS FOR THE TREATMENT OF CANCER
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Paragraph 00190; 00296, (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.
