2019140-71-5

Upstream product

• 656-64-4 3-bromo-4-fluoroaniline 
• 914471-43-5 3‐(4‐amino‐1,2,5‐oxadiazol‐3‐yl)‐4‐(3‐bromo‐4‐fluorophenyl)‐1,2,4‐oxadiazol‐5‐one 

Relevant academic research and scientific papers

Discovery of novel hydroxyamidine derivatives as indoleamine 2,3-dioxygenase 1 inhibitors with in vivo anti-tumor efficacy

Indoleamine 2,3-dioxygenase 1 (IDO1) is closely associated with immune escape in many tumor tissues, and is considered to be a valuable therapeutic target in cancer immunotherapy. In this study, the modification of amino sidechain was performed with the hydroxyamidine core kept intact to optimize lead compound Epacadostat. 19 new compounds with hydrazide, thietane or sulfonamide moiety as polar capping group in sidechain were prepared and their IDO1 inhibitory activities were evaluated. Sulfonamide 3a showed potent IDO1 inhibition in both enzymatic and cellular assays with the IC50 value of 71 nM and EC50 value of 11 nM, respectively. Furthermore, in vivo Lewis lung cancer (LLC) allograft studies of 3a indicated that it handicapped the tumor growth with similar efficacy to Epacadostat. Molecular docking demonstrated that the change of polar capping group affords influence on the orientation of amino ethylene side chain and forms new hydrogen bonding.

Design, synthesis, and biological evaluation of 1,2,5-oxadiazole-3-carboximidamide derivatives as novel indoleamine-2,3-dioxygenase 1 inhibitors

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

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.

2,3-dioxygenase inhibitor containing thio four-membered ring structure as well as preparation method and application of 2, 3-dioxygenase inhibitor

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

2, 3-dioxygenase inhibitor containing substituted amidino structure as well as preparation method and application thereof

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

DEUTERATED INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR AND APPLICATION THEREOF

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

SULFONYL AMIDINE AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR, AND PREPARATION METHOD THEREFOR AND USE THEREOF

Provided in the present application are a sulfonyl amidine as represented by formula (I) as an indoleamine-2,3-dioxygenase inhibitor, and a preparation method therefor and the use thereof. The compound of formula (I) in the present application can be used as an indoleamine-2,3-dioxygenase inhibitor in the preparation of a drug for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.

Indoleamine-2,3-dioxygenase inhibitor containing sulfonamide structure as well as preparation method and application thereof

The invention discloses an indoleamine-2,3-dioxygenase inhibitor containing a sulfonamide structure as well as a preparation method and application thereof, belongs to the field of drug synthesis, andparticularly relates to 1,2,5-oxadiazole compounds containing a sulfonamide structure as shown in a general formula (I) and pharmaceutically acceptable salts thereof, as well as a preparation methodand medical application thereof. The compounds, stereoisomers or pharmaceutically acceptable salts or pharmaceutical combinations thereof are used in combination with an anti-CTLA-4 antibody, an anti-PD-1 antibody, an anti-PD-L1 antibody, an antiviral agent, a chemotherapeutic agent, an immunosuppressive agent, radiation, an antitumor vaccine, an antiviral vaccine, a cytokine therapy or a tyrosinekinase inhibitor to regulate the activity of indoleamine-2,3-dioxygenase, and can be used for treating or preventing cancers or tumors, virus infection, depression, neurodegenerative diseases, wounds, age-related cataract, organ transplant rejection or autoimmune diseases. The general formula (I) is shown in the specification.

IMINO-UREA DERIVATIVES

The present invention relates to the field of medicines, and in particular to an imino-urea derivative containing a furan structure and a composition thereof. The derivative and the composition thereof can be used in the manufacture of a medicament for treating a disease pathologically characterized by indoleamine 2,3-dioxygenase-mediated tryptophan metabolic pathway. The present invention also relates to a method for preparing the derivative and an intermediate thereof.

A kind of IDO inhibitor and use thereof

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