129852-39-7

Basic information

• Product Name: 4-Amino-3-(3,4-dimethoxyphenyl)pyrazolo<3,4-d>pyrimidine
• Synonyms: 4-Amino-3-(3,4-dimethoxyphenyl)pyrazolo<3,4-d>pyrimidine
• CAS NO: 129852-39-7
• Molecular Weight: 271.279
• Mol File: 129852-39-7.mol

Chemical Properties

• CAS DataBase Reference: 4-Amino-3-(3,4-dimethoxyphenyl)pyrazolo<3,4-d>pyrimidine(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Amino-3-(3,4-dimethoxyphenyl)pyrazolo<3,4-d>pyrimidine(129852-39-7)
• EPA Substance Registry System: 4-Amino-3-(3,4-dimethoxyphenyl)pyrazolo<3,4-d>pyrimidine(129852-39-7)

Safety Data

• Hazardous Substances Data: 129852-39-7(Hazardous Substances Data)

Upstream product

• 122775-35-3 3,4-Dimethoxyphenylboronic acid 
• 151266-23-8 4-amino-3-iodo-1H-pyrazolo[3,4-d]pyrimidine 
• 111509-95-6 2-Cyano-3-(3,4-dimethoxyphenyl)-3-morpholinoacrylonitrile 
• 87428-43-1 (3,4-dimethoxyphenyl)(morpholino)methanethione 
• 111510-06-6 5-Amino-3-(3,4-dimethoxyphenyl)-1H-pyrazole-4-carbonitrile 
• 77287-34-4 formamide 

Downstream Products

• 1300584-94-4 2-(1-(4-amino-3-(3,4-dihydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H-chromen-4-one 
• 1300584-93-3 2-(1-(4-amino-3-(3,4-dimethoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-3-(3-fluorophenyl)-4H-chromen-4-one 

Relevant articles and documents

Discovery of (S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1 H-pyrazolo[3,4- d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3 H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3KδInhibitor for the Treatment of Chronic Obstructive Pulmonary Disease

Accumulated pieces of evidence have shown that PI3Kδplays a critical role in chronic obstructive pulmonary disease (COPD). Using a fragment-hybrid approach, we discovered a potent and selective PI3Kδinhibitor (S)-18. In the biochemical assay, (S)-18 inhibits PI3Kδ(IC50 = 14 nM) with high selectivity over other class I PI3Ks (56～83 fold). (S)-18 also achieves good selectivity over other protein kinases in the kinome (S-score (35) = 0.015). In the cell, (S)-18 selectively and potently inhibits the PI3Kδ-mediated phosphorylation of AKT T308 but not other class I PI3K-mediated signaling. Additionally, (S)-18 exhibits no apparent inhibitory effect on CYP isoforms except for a moderate effect on CYP2C9. Furthermore, it shows no apparent inhibitory activity against hERG (IC50 > 10 μM). In vivo, (S)-18 displays favorable PK properties for inhaled delivery and improves lung function in a rodent model of pulmonary inflammation. These results suggest that (S)-18 might be a new potential therapeutic candidate for COPD.

NOVEL KINASE MODULATORS

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Polarized Ethylenes. IV. Synthesis of Polarized Ethylenes Using Thioamides and Methyl Dithiocarboxylates and their Application to Syntheses of Pyrazoles, Pyrimidines, Pyrazolopyrimidines, and 5-Azacyclazines

Polarized ethylenes having both electron-donating (an amino or a methylthio group) and electron-accepting (cyano, carbamoyl, methyl ester) groups on the adjacent two olefinic carbon atoms were prepared by the condensation of S-alkylthioamidinium salts or