914471-43-5Relevant articles and documents
2, 3-dioxygenase inhibitor containing substituted amidino structure as well as preparation method and application thereof
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Paragraph 0019; 0025; 0032-0033, (2020/10/06)
The invention belongs to the field of drug synthesis, and relates to a 1,2,5-oxadiazole compound csubstituted amidino group as shown in a general formula (I) and pharmaceutically acceptable salts thereof, and a preparation method and medical application o
2,3-dioxygenase inhibitor containing thio four-membered ring structure as well as preparation method and application of 2, 3-dioxygenase inhibitor
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Paragraph 0020; 0027-0028, (2020/10/04)
The invention belongs to the field of drug synthesis, and relates to a 1,2,5-oxadiazole compound containing a thio four-membered ring shown in a general formula (I) and pharmaceutically acceptable salts thereof, and a preparation method and medical applic
Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors
Song, Xiaohan,Sun, Pu,Wang, Jiang,Guo, Wei,Wang, Yi,Meng, Ling-hua,Liu, Hong
, (2020/01/23)
Indoleamine 2,3-dioxygenase 1 (IDO1) is the enzyme catalyzing the oxidative metabolism of tryptophan, which accounts for cancer immunosuppression in tumor microenvironment. Several compounds targeting IDO1 have been reported and epacadostat shows strong i
Oxadiazole derivative, preparation method and applications thereof
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Paragraph 0069; 0070; 0075; 0076, (2020/05/30)
The invention relates to an oxadiazole derivative, a preparation method and applications thereof, wherein the oxadiazole derivative has a structure represented by a formula (I), and R1, X and R2 are defined in the specification.
DEUTERATED INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR AND APPLICATION THEREOF
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Paragraph 0167-0169, (2020/12/05)
The present invention belongs to the technical field of medicine, and particularly relates to a compound represented by Formula I, a pharmaceutically acceptable salt thereof, and a stereoisomer thereof, R4, R4′, R5, R
A kind of IDO inhibitor and use thereof
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Paragraph 0300; 0304-0306, (2019/07/11)
The embodiment of the invention provides general formula (I) compound or its pharmaceutically acceptable salts, stereoisomers, a tautomeric form each other, polymorphs, solvate, prodrug, metabolite or isotope derivatives, wherein the substituents R1
IDO1 inhibitor (I) containing substituted phosphonamide ester derivative, preparation method and application of inhibitor
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Paragraph 0068; 0069; 0076; 0077, (2019/04/02)
The invention relates to the field of pharmaceutical chemistry, in particular to an IDO1 inhibitor (I) containing a substituted phosphonamide ester derivative and a preparation method of the inhibitor. Pharmacodynamic and pharmacokinetic experiments prove
1,2,5-oxadiazole derivative and purpose thereof
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Paragraph 0036; 0037; 0047; 0048; 0049, (2019/04/17)
The invention discloses a compound having the following general formula (I), wherein K is selected from a cycloalkane group shown in the following formula. The invention also discloses an indoleamine-2,3-dioxygenase inhibitor comprising the compound and a
IDO1 INHIBITOR AND PREPARATION METHOD AND APPLICATION THEREOF
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Paragraph 0078; 0079; 0086; 0087, (2019/06/14)
A compound as an indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, and an application thereof in the field of IDO1-related diseases, and in particular a compound as shown in formula (I) and a pharmaceutically acceptable salts thereof.
Discovery of phosphonamidate IDO1 inhibitors for the treatment of non-small cell lung cancer
Du, Qianming,Feng, Xi,Wang, Yinuo,Xu, Xi,Zhang, Yan,Qu, Xinliang,Li, Zhiyu,Bian, Jinlei
, (2019/08/26)
Targeting indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as an attractive approach for the development of cancer immunotherapy. In this study, a series of phosphonamidate ester containing compounds were designed, synthesized and evaluated for their inhibitory activities against IDO1. Among them, compounds 16, 17, and 26 with good IDO1 inhibitory (HeLa IDO1 IC50 = 10–21 nM, hIDO1 IC50 = 78–121 nM) activities were selected for further investigation and showed good physicochemical properties. Furthermore, based on comparable PK profile and excellent IDO2/TDO inhibitory potency, representative compound 16 was selected for further bio-evaluation and characterized with good efficacy in suppressing lung metastasis (77% inhibition rate) of Lewis cells in vivo. Thus, compound 16 could be a potential and efficacious agent for further evaluation.