874298-19-8

Basic information

• Product Name: 4-(3-pyridyl)ureido-phenylboronic acid pinacol ester
• Synonyms: 4-(3-pyridyl)ureido-phenylboronic acid pinacol ester
• CAS NO: 874298-19-8
• Molecular Weight: 339.202
• Mol File: 874298-19-8.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: 4-(3-pyridyl)ureido-phenylboronic acid pinacol ester(CAS DataBase Reference)
• NIST Chemistry Reference: 4-(3-pyridyl)ureido-phenylboronic acid pinacol ester(874298-19-8)
• EPA Substance Registry System: 4-(3-pyridyl)ureido-phenylboronic acid pinacol ester(874298-19-8)

Safety Data

• Hazardous Substances Data: 874298-19-8(Hazardous Substances Data)

Upstream product

• 462-08-8 pyridin-3-ylamine 
• 2493-02-9 4-bromophenyl isocyanate 

Downstream Products

• 1250868-50-8 1-(4-(4-(3-oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-((dimethylamino)methyl)pyrimidin-2-yl)phenyl)-3-(pyridin-3-yl)urea monotrifluoroacetate 
• 1251838-41-1 4-morpholin-4-yl-2-[4-(3-pyridin-3-yl-ureido)-phenyl]-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester 
• 1251857-47-2 4-(3-oxa-8-aza-bicyclo[3.2.1]oct-8-yl)-2-[4-(3-pyridin-3-yl-ureido)phenyl]-5,8-dihydro-6H-pyrido[3,4-d]pyrimidine-7-carboxylic acid tert-butyl ester 

Relevant articles and documents

ADENOSINE COMPOUND, PHARMACEUTICALLY ACCEPTABLE SALT OR STEREOISOMERIDE THEREOF, AND USE

The present invention relates to a compound represented by Formula I, its pharmaceutically acceptable salt, its stereoisomer, its pharmaceutically acceptable hydrate or solvate, or its pharmaceutically acceptable ester, wherein R is selected from heteroaryl, substituted heteroaryl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, alkyl, and substituted alkyl, wherein the substituted heteroaryl, the substituted aryl, the substituted cycloalkyl and the substituted alkyl are each independently substituted with one or more hydroxyalkylene groups. The compound or its pharmaceutically acceptable salt, its stereoisomer, its pharmaceutically acceptable hydrate or solvate, its pharmaceutically acceptable ester of the present invention has agonistic activity on A2A adenosine receptor and can improve the permeability of blood-brain barrier to promote the delivery of drug across blood-brain barrier, and can also prevent or treat a disease associated with A2A adenosine receptor agonistic activity.

5,6,7,8-TETRAHYDROPYRIDO[3,4-D]PYRIMIDINE COMPOUNDS, THEIR USE AS MTOR KINASE AND PI3 KINASE INHIBITORS, AND THEIR SYNTHESES

A compound of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): Optimization of the 6-aryl substituent

Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d] pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of the 6-aryl substituent led to the discovery of inhibitors carrying 6-ureidophenyl groups, the first reported active site inhibitors of mTOR with subnanomolar inhibitory concentrations. The data presented in this paper show that 6-arylureidophenyl substituents led to potent mixed inhibitors of mTOR and phosphatidylinositol 3-kinase α (PI3K-α), whereas 6-alkylureidophenyl appendages gave highly selective mTOR inhibitors. Combination of 6-alkylureidophenyl groups with 1-carbamoylpiperidine substitution resulted in compounds with subnanomolar IC50 against mTOR and greater than 1000-fold selectivity over PI3K-α. In addition, structure based drug design resulted in the preparation of several 6-arylureidophenyl-1H-pyrazolo[3,4-d]pyrimidines, substituted in the 4-position of the arylureido moiety with water solubilizing groups. These compounds combined potent mTOR inhibition (IC50501 nM). 2009 American Chemical Society.