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 
• 773837-37-9 sodium cyanide 
• 98-95-3 nitrobenzene 

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 
• 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 
• 103273-09-2 5-(4-amino-phenyl)-5-methyl-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 
• 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 

Relevant academic research and scientific papers

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.

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.

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