1204669-68-0

Upstream product

• 1204669-59-9 4-amino-N‘-hydroxy-N-(2-methoxyethyl)-1,2,5-oxadiazole-3-carboximidamide 
• 1204669-60-2 N¹-hydroxy-4-((2-methoxyethyl)amino)-1,2,5-oxadiazole-3-carboximidamide 
• 1204669-61-3 N-hydroxy-4-[(2-methoxyethyl)amino]-1,2,5-oxadiazole-3-carboximidoyl chloride 
• 1204669-62-4 N-(3-bromo-4-fluorophenyl)-N‘-hydroxy-4-((2-methoxyethyl)amino)-1,2,5-oxadiazole-3-carboximidamide 
• 1204669-63-5 4-(3-bromo-4-fluorophenyl)-3-{4-[(2-methoxyethyl)amino]-1,2,5-oxadiazol-3-yl}-1,2,4-oxadiazol-5(4H)-one 
• 1204669-64-6 4-(3-bromo-4-fluorophenyl)-3-{4-[(2-hydroxyethyl)amino]-1,2,5-oxadiazol-3-yl}-1,2,4-oxadiazol-5(4H)-one 
• 1204669-65-7 2-({4-[4-(3-bromo-4-fluorophenyl)-5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl]-1,2,5-oxadiazol-3-yl}amino)ethyl methanesulfonate 
• 914471-43-5 3‐(4‐amino‐1,2,5‐oxadiazol‐3‐yl)‐4‐(3‐bromo‐4‐fluorophenyl)‐1,2,4‐oxadiazol‐5‐one 
• 89711-08-0 N-(t-butoxycarbonyl)glycinal 
• 24424-99-5 di-tert-butyl dicarbonate 
• 656-64-4 3-bromo-4-fluoroaniline 
• 57260-73-8 N-BOC-1,2-diaminoethane 
• 2019140-71-5 4‐(3‐bromo‐4‐fluorophenyl)‐3‐(4‐nitro‐1,2,5‐oxadiazol‐3‐yl)‐4,5‐dihydro‐1,2,4‐oxadiazol‐5‐one 

Downstream Products

• 1204669-67-9 3‐{4‐[(2‐aminoethyl)amino]‐1,2,5‐oxadiazol‐3‐yl}‐4‐(3‐bromo‐4‐fluorophenyl)‐1,2,4‐oxadiazol‐5‐one hydrochloride 
• 1204669-37-3 (Z)-4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide 
• 1204669-70-4 N-[2-({4-[4-(3-bromo-4-fluorophenyl)-5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl]-1,2,5-oxadiazol-3-yl}amino)ethyl]sulfamide 
• 1204669-69-1 (Ν-(2-((4-(4-(3-bromo-4-fluorophenyl)-5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-1,2,5-oxadiazol-3-yl)amino)ethyl)tert-butylsulfamoyl)carbamate 
• 1204669-37-3 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide 

Relevant academic research and scientific papers

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

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

1,2,5-oxadiazole derivative and purpose thereof

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

1,2,5-oxadiazole derivative used as indoleamine 2,3-dioxygenase inhibitor

The invention belongs to the technical field of 1,2,5-oxadiazole derivatives, and particularly relates to a 1,2,5-oxadiazole derivative or a pharmaceutically acceptable salt thereof which is used as an indoleamine 2,3-dioxygenase inhibitor. The structure of the 1,2,5-oxadiazole derivative or the pharmaceutically acceptable salt thereof used as the IDO inhibitor is shown in the following formula I.The invention provides a general formula compound I with a novel structure. Experimental results show that some compounds have excellent IDO inhibitory activity and permeation performance at the sametime. The compound is expected to be marketed as a tumor molecular immunotherapeutic drug for cancer treatment.

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.

IDO1 inhibitor (I) containing substituted phosphonamide ester derivative, preparation method and application of inhibitor

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

Preparation method of key intermediate of Epacadostat

The invention relates to the field of medicine synthesis, and concretely relates to a preparation method of a key intermediate 3-(4-((2-aminoethyl)amino)-1,2,5-oxadiazol-3-yl)-4-(3-bromo-4-fluorophenyl)-1,2,4-oxadiazole-5(4H)-one hydrochloride (II) of an

INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE

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

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

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.