722486-66-0

Upstream product

• 95-92-1 oxalic acid diethyl ester 
• 765-30-0 Cyclopropylamine 
• 4755-77-5 Ethyl oxalyl chloride 

Downstream Products

• 1622208-11-0 N-cyclopropyl-3-(3-fluoro-4-methylphenyl)-3H-imidazo[4,5-b]pyridine-2-carboxamide 
• 1622208-35-8 N-cyclopropyl-3-(3,4-dichlorophenyl)-3H-imidazo[4,5-b]pyridine-2-carboxamide 
• 1622209-06-6 N-cyclopropyl-N'-{2-[(3-fluoro-4-methylphenyl)amino]pyridin-3-yl}ethanediamide 
• 1464139-80-7 5-(6-benzyloxy-3-ethyl-1H-indazol-5-yl)-4-(4-morpholin-4-yl-phenyl)-4H-[1,2,4]triazole carboxylic acid cyclopropylamide 
• 35265-06-6 2-(cyclopropylamino)ethan-1-ol 
• 945255-55-0 C₃₇H₆₀N₆O₇ 
• 183235-79-2 (cyclopropylamino)(oxo)acetic acid 

Relevant academic research and scientific papers

Direct C?H Carbamoylation of Nitrogen-Containing Heterocycles

Nucleophilic radical additions at innately electrophilic C(sp2) centers are perfectly suited for the direct functionalization of heterocycles. Using bench stable and commercially available alkyl oxamate and oxamic acid derivatives in combination with photoredox catalysis, a direct carbamoylation of heterocycles yielding amide functionalized pharmacophores in a single step is reported. The reaction conditions reported are compatible with structurally complex heterocyclic substrates of pharmaceutical interest. Notably, derivatives containing functional groups incompatible with standard amidation reactions, such as carboxylic acids and unprotected amines, were found to be amenable to this reaction paradigm.

SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE

The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.

Substituted heteroaryl compounds and compositions and uses thereof (by machine translation)

The invention discloses substituted heteroaryl compounds and compositions thereof and their use. The compounds of formula (I) compound or type shown in (I) a compound represented by stereo isomers, tautomers, nitrogen oxide, solvate, metabolite, pharmaceutically acceptable salt or its prodrug. The invention also provides a pharmaceutical composition, the compounds and pharmaceutical compositions can be regulated protein kinase, particularly Aurora kinase and JAK kinase activity, for the prevention, treatment, treatment and reduce protein kinase, in particular JAK kinase activity mediated diseases or disorders. (by machine translation)

Discovery of Cytochrome P450 4F11 Activated Inhibitors of Stearoyl Coenzyme A Desaturase

Stearoyl-CoA desaturase (SCD) catalyzes the first step in the conversion of saturated fatty acids to unsaturated fatty acids. Unsaturated fatty acids are required for membrane integrity and for cell proliferation. For these reasons, inhibitors of SCD represent potential treatments for cancer. However, systemically active SCD inhibitors result in skin toxicity, which presents an obstacle to their development. We recently described a series of oxalic acid diamides that are converted into active SCD inhibitors within a subset of cancers by CYP4F11-mediated metabolism. Herein, we describe the optimization of the oxalic acid diamides and related N-acyl ureas and an analysis of the structure-activity relationships related to metabolic activation and SCD inhibition.

Azabenzimidazole Compounds

The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.

Inhibitors of hepatitis C virus NS3·4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics

Reversible tetrapeptide-based compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease. Inhibition of viral replicon RNA production in Huh-7 cells has also been demonstrated. We show herein that the inclusion of hydrogen bond donors on the P4 capping group of tetrapeptide-based inhibitors result in increased binding potency to the NS3·4A protease. The capping groups also impart significant effects on the pharmacokinetic profile of these inhibitors.

Hydrogen bond patterns in solid state carboxylic acids. Vibrational behaviour of the catamer pattern as exhibited by the N-alkyloxamic acids

The vibrational study presented in this publication shows that the N-alkyloxamic acids are hydrogen bonded through a catamer hydrogen bond pattern in the solid state. Two different hydrogen bond patterns are possible for these products, and these patterns can be very clearly distinguished by their vibrational behaviour. Deuteration and low temperature spectra make the assignment and characterisation more obvious.