1204669-80-6

Upstream product

• 914471-09-3 4-amino-N-(3-chloro-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide 
• 530-62-1 1,1'-carbonyldiimidazole 
• 367-21-5 3-chloro-4-fluorophenylamine 
• 914471-09-3 4-amino-N-(3-chloro-4-fluorophenyl)-N‘-hydroxy-1,2,5-oxadiazole-3-carboximidamide 

Downstream Products

• 1204669-81-7 N-{4-[4-(3-chloro-4-fluorophenyl)-5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl]-1,2,5-oxadiazol-3-yl}-2,2,2-trifluoroacetamide 
• 1204669-86-2 3-{4-[(3-aminopropyl)amino]-1,2,5-oxadiazol-3-yl}-4-(3-chloro-4-fluorophenyl)-1,2,4-oxadiazol-5(4H)-one trifluoroacetate 
• 1204669-83-9 3-{4-[(2-aminoethyl)amino]-1,2,5-oxadiazol-3-yl}-4-(3-chloro-4-fluorophenyl)-1,2,4-oxadiazol-5(4H)-one hydrochloride 

Relevant academic research and scientific papers

Design, synthesis and antitumor study of a series of N-Cyclic sulfamoylaminoethyl substituted 1,2,5-oxadiazol-3-amines as new indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitors

Indoleamine 2, 3-dioxygenase 1 (IDO1) plays a key role in tryptophan catabolism which is an important mechanism in immune tolerance. The small molecule epacadostat is the most advanced IDO1 inhibitor, but its phase III trials as a single agent or in combi

Discovery of phosphonamidate IDO1 inhibitors for the treatment of non-small cell lung cancer

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.

SULFOXIMINE, SULFONIMIDAMIDE, SULFONDIIMINE AND DIIMIDOSULFONAMIDE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2, 3-DIOXYGENASE

Provided are certain IDO inhibitors, pharmaceutical compositions thereof, and methods of use thereof.

SUBSTITUTED N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3- DIOXYGENASE

The invention provides modulators of indoleamine 2,3-dioxygenase (IDO1) and their use in the prophylaxis and/or treatment of IDO1-mediated diseases. Specifically, the present invention provides compounds according to Formula (I) an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof.

Indoleamine 2,3-dioxygenase inhibitor, and preparation method and application of same

The invention provides a novel indoleamine 2,3-dioxygenase inhibitor, and a preparation method and a medicine composition of same, wherein the n, Y, Z, R1, R2, R3 and R4 are defined as the specification. The invention also provides an application of the c

INCB24360 (Epacadostat), a Highly Potent and Selective Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitor for Immuno-oncology

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

Ureido-containing IDO1 (indoleamine-2,3-dioxygenase-1) and IDO2 (indoleamine-2,3-dioxygenase-2) double inhibitor and preparation method and pharmaceutical application thereof

The invention relates to the field of pharmaceutical chemistry, in particular to ureido-containing IDO1 (indoleamine-2,3-dioxygenase-1) and IDO2 (indoleamine-2,3-dioxygenase-2) double inhibitor (I) and a preparation method thereof; pharmacodynamic tests s

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

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

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

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.