64464-22-8

Usage

InChI:InChI=1/C10H9N3O4/c1-10(8(14)11-9(15)12-10)6-2-4-7(5-3-6)13(16)17/h2-5H,1H3,(H2,11,12,14,15)/t10-/m1/s1

Upstream product

• 151-50-8 potassium cyanide 
• 100-19-6 (4-nitrophenyl)ethanone 
• 143-33-9 sodium cyanide 
• 506-87-6 ammonium carbonate 
• 98-95-3 nitrobenzene 
• 773837-37-9 sodium cyanide 

Downstream Products

• 169808-25-7 (R,S)-[4-methyl-4-(4-nitro-phenyl)-2,5-dioxo-imidazolidin-1-yl]acetic acid methyl ester 
• 868635-08-9 2-(4-nitrophenyl)-2-methylglycine 
• 169808-26-8 [4-(R,S)-(4-amino-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]acetic acid methyl ester 
• 169808-27-9 [4-(R,S)-(4-benzyloxycarbonylguanidino-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]acetic acid methyl ester 
• 169808-28-0 [4-(R,S)-(4-benzyloxycarbonylguanidino-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]acetic acid 
• 169808-24-6 {2-[4-(R,S)-(4-benzyloxycarbonyl-guanidino-phenyl)-4-methyl-2,5-dioxo-imidazolidin-1-yl]acetyl}-Asp(O-t-Bu)-(S)-phenylglycine-O-t-Bu 
• 1186118-17-1 5-methyl-5-(4-nitrophenyl)-3-(4-(2-oxo-6,8-di-n-propyl-4-(trifluoromethyl)-2H-chromen-7-yloxy)butyl)imidazolidine-2,4-dione 
• 1031393-79-9 3-(4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-2-n-propylphenoxy)butyl)-5-methyl-5-(4-nitrophenyl)imidazolidine-2,4-dione 
• 103273-09-2 5-(4-amino-phenyl)-5-methyl-imidazolidine-2,4-dione 

Relevant academic research and scientific papers

Design, synthesis and pharmacology of 1,1-bistrifluoromethylcarbinol derivatives as liver X receptor β-selective agonists

A novel series of 1,3-bistrifluoromethylcarbinol derivatives that act as liver X receptor (LXR) β-selective agonists was discovered. Structure-activity relationship studies led to the identification of molecule 62, which was more effective (Emax) and selective toward LXRβ than T0901317 and GW3965. Furthermore, 62 decreased LDL-C without elevating the plasma TG level and significantly suppressed the lipid-accumulation area in the aortic arch in a Bio F1B hamster fed a diet high in fat and cholesterol. We demonstrated that our LXRβ agonist would be potentially useful as a hypolipidemic and anti-atherosclerotic agent. In this manuscript, we report the design, synthesis and pharmacology of 1,3-bistrifluoromethylcarbinol derivatives.

TYK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Hydrophobic and electronic factors in the design of dialkylglycine decarboxylase mimics

The first functional catalytic mimic of the enzyme dialkylglycine decarboxylase is described. This system utilizes a hydrophobically modified polyethylenimine polymer, a pyridoxamine cofactor, and a 2-aryl-2-alkylglycine sacrificial amine source to convert α-keto acids to α-amino acids at biologically relevant temperatures with multiple turnovers of the pyridoxamine catalyst. The effects of hydrophobic and electronic factors in the 2,2-disubstituted sacrificial amine source and the pyridoxamine catalyst on turnover frequency and turnover number are explored.

Novel heterocycles as inhibitors of leucocyte adhesion and as VLA-4 antagonists

The present invention relates to compounds of the formula I which are inhibitors of the adhesion and migration of leucocytes and/or antagonists of the adhesion receptor VLA-4 which belongs to the group of integrins. The invention also relates to processes

Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold

Antagonists of the platelet fibrinogen receptor (GP IIb/IIIa receptor) are expected to be a promising new class of antithrombotic agents. The binding of fibrinogen to the fibrinogen receptor depends on an Arg-Gly-Asp-Ser (RGDS) tetrapeptide recognition motif. Structural modifications of the RGDS lead have led to the discovery of a non-peptide RGD mimetic GP IIb/IIIa antagonist 44 (S 1197). Compound 44 inhibited, in a dose dependent and reversible manner, human and dog platelet aggregation as well as 125I-fibrinogen binding to ADP-activated human gel filtered platelets and isolated GP IIb/IIIa with Ki values of 9 nM and 0.17 nM, respectively. A pharmacophore mapping procedure with QXP and a 3D-QSAR analysis applying the GRID/GOLPE methodology yielded a stable, rather predictive model and revealed structural features which are important for binding. Hydrophobic substitutions both at the hydantoin nucleus and at the C-terminus increase the affinity toward the fibrinogen receptor. The crystalline ethyl ester prodrug 48 (HMR 1794) is an orally active antithrombotic agent which is a promising drug candidate for the treatment of thrombotic diseases in humans.

Substituted 5-membered ring heterocycles, their preparation and their use

The present invention pertains to 5-ring heterocycles of general formula (I), wherein W, Y, Z, B, D, E and R as well as b, c, d, e, f, g, and h are as indicated in the description; to methods for preparing them, and to their use as inhibitors of platelet aggregation, metastasizing of carcinomatous cells and the attachment of osteoclasts to the bone surface. STR1