1204669-70-4

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 
• 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 
• 1189-71-5 isocyanate de chlorosulfonyle 
• 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 
• 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 
• 1204669-67-9 3‐{4‐[(2‐aminoethyl)amino]‐1,2,5‐oxadiazol‐3‐yl}‐4‐(3‐bromo‐4‐fluorophenyl)‐1,2,4‐oxadiazol‐5‐one hydrochloride 
• 1204669-68-0 tert‐butyl N‐[2‐({4‐[4‐(3‐bromo‐4‐fluorophenyl)‐5‐oxo‐1,2,4‐oxadiazol‐3‐yl]‐1,2,5‐oxadiazol‐3‐yl}amino)ethyl]carbamate 
• 1204669-66-8 3-(4-((2-azidoethyl)amino)-1,2,5-oxadiazole-3-yl)-4-(3-bromo-4-fluorophenyl)-1,2,4-oxadiazole-5(4H)-one 

Downstream Products

• 1204669-37-3 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N’-hydroxy-1,2,5-oxadiazole-3-carboximidamide 
• 1204669-37-3 (Z)-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

PROTAC compound for targeted degradation of IDO1, and preparation method and application thereof

The invention provides a PROTAC compound represented by formula I and used for targeted degradation of IDO1, and a pharmaceutically acceptable salt, a hydrate or a solvate thereof. In the formula I, Xrepresents -CH2 or -C = O, Y represents -CH2 or -C= O, and n is a natural number from 2 to 9. The PROTAC compound for targeted degradation of the IDO1 has efficient activity of targeted degradation of the IDO1 protein.

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

Singlet molecular oxygen regulates vascular tone and blood pressure in inflammation

Singlet molecular oxygen (1O2) has well-established roles in photosynthetic plants, bacteria and fungi1–3, but not in mammals. Chemically generated 1O2 oxidizes the amino acid tryptophan to precursors of a key metabolite called N-formylkynurenine4, whereas enzymatic oxidation of tryptophan to N-formylkynurenine is catalysed by a family of dioxygenases, including indoleamine 2,3-dioxygenase 15. Under inflammatory conditions, this haem-containing enzyme is expressed in arterial endothelial cells, where it contributes to the regulation of blood pressure6. However, whether indoleamine 2,3-dioxygenase 1 forms 1O2 and whether this contributes to blood pressure control have remained unknown. Here we show that arterial indoleamine 2,3-dioxygenase 1 regulates blood pressure via formation of 1O2. We observed that in the presence of hydrogen peroxide, the enzyme generates 1O2 and that this is associated with the stereoselective oxidation of l-tryptophan to a tricyclic hydroperoxide via a previously unrecognized oxidative activation of the dioxygenase activity. The tryptophan-derived hydroperoxide acts in vivo as a signalling molecule, inducing arterial relaxation and decreasing blood pressure; this activity is dependent on Cys42 of protein kinase G1α. Our findings demonstrate a pathophysiological role for 1O2 in mammals through formation of an amino?acid-derived hydroperoxide that regulates vascular tone and blood pressure under inflammatory conditions.

Preparation method of IDO1 inhibitor Epacadostat intermediate

The invention relates to the drug synthesis field, specifically to a preparation method of an IDO1 (indoleamine-2, 3-dioxygenase 1) inhibitor Epacadostat intermediate 4-(3-bromo-4-fluorophenyl)-3-(4-((2-bromoethyl)amino)-1, 2, 5-oxadiazole-3-yl)-1, 2, 4-o

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

Synthetic method of IDO inhibitor Aikaduosita

The invention discloses a synthetic method of an IDO inhibitor Aikaduosita, and relates to the technical field of organic synthesis. The method comprises the following steps: carrying out an addition rearrangement reaction on N-Boc-ethylene diamine used as a raw material to obtain an intermediate 1, carrying out an acid deprotection reaction on the intermediate 1 to obtain an intermediate 2, carrying out a condensation reaction on the intermediate 2 and a compound 1 to obtain an intermediate 3, and carrying out an alkaline ring opening reaction on the intermediate 3 to finally prepare the IDO inhibitor Aikaduosita. Compared with reported methods, the method disclosed in the invention has the advantages of short route, high yield, simplicity in post-treatment, avoiding of explosive reagents and ultralow temperature conditions, small pollution, and suitableness for industrial production.

METHOD FOR PREPARING IDO INHIBITOR EPACADOSTAT

Provided is a method for preparing IDO inhibitor epacadostat. The whole reaction route is simple, easy to control and has high yield.

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.

PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR

The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful i

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