1211592-38-9

Basic information

• Product Name: 5-Bromo-N-methoxy-N-methylpicolinamide
• Synonyms: 5-Bromo-N-methoxy-N-methylpicolinamide;5-bromo-N-methoxy-N-methyl-2-Pyridinecarboxamide;(3S,4S)-1-tert-butyl 3-ethyl 4-(cyanomethyl)pyrrolidine-1,3-dicarboxylate;(3S,4S)-1-tert-butyl 3-ethyl 4-(cyanomethyl)pyrrolidine-1,3-dicarboxylate(WXC05384)
• CAS NO: 1211592-38-9
• Molecular Formula: C₈H₉BrN₂O₂
• Molecular Weight: 245.07326
• Mol File: 1211592-38-9.mol
• Article Data: 7

Chemical Properties

• Boiling Point: 365.8±27.0 °C(Predicted)
• Appearance: /
• Density: 1.526±0.06 g/cm3(Predicted)
• Storage Temp.: 2-8°C
• PKA: -0.54±0.10(Predicted)
• CAS DataBase Reference: 5-Bromo-N-methoxy-N-methylpicolinamide(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Bromo-N-methoxy-N-methylpicolinamide(1211592-38-9)
• EPA Substance Registry System: 5-Bromo-N-methoxy-N-methylpicolinamide(1211592-38-9)

Safety Data

• Hazardous Substances Data: 1211592-38-9(Hazardous Substances Data)

Upstream product

• 30766-11-1 5-bromoisonicotinic acid 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 137178-88-2 5-bromopyridine-2-carbonyl chloride 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 1088496-42-7 [6-(1-hydroxy-1-methylethyl)pyridin-3-yl]boronic acid 
• 214701-49-2 1-(5-bromopyridin-2-yl)ethanone 

Relevant articles and documents

Investigation of cardiovascular effects of tetrahydro-β-carboline sstr3 antagonists

Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first preclinical candidate, MK-4256, was discontinued due to a dose-dependent QTc (QT interval corrected for heart rate) prolongation observed in a conscious cardiovascular (CV) dog model. As the fate of the entire program rested on resolving this issue, it was imperative to determine whether the observed QTc prolongation was associated with hERG channel (the protein encoded by the human Ether-à-go-go-Related Gene) binding or was mechanism-based as a result of antagonizing sstr3. We investigated a structural series containing carboxylic acids to reduce the putative hERG off-target activity. A key tool compound, 3A, was identified from this SAR effort. As a potent sstr3 antagonist, 3A was shown to reduce glucose excursion in a mouse oGTT assay. Consistent with its minimal hERG activity from in vitro assays, 3A elicited little to no effect in an anesthetized, vagus-intact CV dog model at high plasma drug levels. These results afforded the critical conclusion that sstr3 antagonism is not responsible for the QTc effects and therefore cleared a path for the program to progress.

FACTOR XIa INHIBITORS

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma Kallikrein.

USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS

The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: or pharmaceutically acceptable salts thereof.