1192569-99-5

Basic information

• Product Name: beta-(4,4-Difluoro-1-piperidinyl)-2-(trifluoromethyl)-5-pyrimidineethanamine
• Synonyms: beta-(4,4-Difluoro-1-piperidinyl)-2-(trifluoromethyl)-5-pyrimidineethanamine
• CAS NO: 1192569-99-5
• Molecular Formula: C12H15F5N4
• Molecular Weight: 310.266316
• Mol File: 1192569-99-5.mol
• Article Data: 3

Chemical Properties

• Appearance: /
• Density: 1.37±0.1 g/cm3 (20 ºC 760 Torr)
• CAS DataBase Reference: beta-(4,4-Difluoro-1-piperidinyl)-2-(trifluoromethyl)-5-pyrimidineethanamine(CAS DataBase Reference)
• NIST Chemistry Reference: beta-(4,4-Difluoro-1-piperidinyl)-2-(trifluoromethyl)-5-pyrimidineethanamine(1192569-99-5)
• EPA Substance Registry System: beta-(4,4-Difluoro-1-piperidinyl)-2-(trifluoromethyl)-5-pyrimidineethanamine(1192569-99-5)

Safety Data

• Hazardous Substances Data: 1192569-99-5(Hazardous Substances Data)

Upstream product

• 304693-66-1 2-trifluoromethyl-5-pyrimidinecarboxaldehyde 

Relevant articles and documents

The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists

The synthesis, SAR and preclinical characterization of a series of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists is described herein. The lead compounds are potent inhibitors in Ca2+flux and whole blood IL-1β P2X7 release assays at both human and mouse isoforms. Compound 1e showed a robust reduction of IL-1β release in a mouse ex vivo model with a 50?mg/kg oral dose. Evaluation of compound 1e in the mouse SNI tactile allodynia, carrageenan-induced paw edema or CIA models resulted in no analgesic or anti-inflammatory effects.

QUINOLINE OR ISOQUINOLINE SUBSTITUTED P2X7 ANTAGONISTS

The present invention is related to novel compounds of formula (I) having P2X7 antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans. (I)