Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Pyrimidines useful as modulators of voltage-gated ion channels

A heteroatom, nitrogen atom technology, applied in the field of pyrimidines that can be used as voltage-gated ion channel regulators, can solve problems such as side effect limitation

Inactive Publication Date: 2006-10-11
VERTEX PHARMA INC
View PDF3 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] Unfortunately, as mentioned above, the efficacy of sodium channel blockers and calcium channel blockers currently used in the above disease states is largely limited by a large number of side effects

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Pyrimidines useful as modulators of voltage-gated ion channels
  • Pyrimidines useful as modulators of voltage-gated ion channels
  • Pyrimidines useful as modulators of voltage-gated ion channels

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0519]

[0520] In a 250 mL three-necked round bottom flask equipped with a magnetic stirrer and reflux condenser, N , N-Dimethylaniline (2.10 mL, 16.3 mmol). The suspension was heated at reflux for 30 minutes, slowly forming a clear solution. The solution was concentrated under reduced pressure and the residue was poured on ice (100 g). The solution was basified to pH = 9.0 with concentrated aqueous sodium bicarbonate. Make the mixture in CH 2 Cl 2 with H 2 O distribution. The organic solution was dried (MgSO 4 ), evaporated to dryness under reduced pressure. The residue was dissolved in anhydrous THF (30 mL), cooled to 0°C. Dimethylaniline (16.3 mL, 32.6 mmol, 2.0 M in THF) was added dropwise over 10 minutes with stirring. The solution was then stirred at 0 °C for 1 hour. The solution was concentrated under reduced pressure and the residue was purified by silica gel chromatography eluting with 90% hexane / 10% ethyl acetate to afford 2 (1.70 g, 7.34 mmol, 45% yiel...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention relates to compounds of formula (I) useful as inhibitors of voltage-gated ion channels for the treatment of pain. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.

Description

technical field [0001] The present invention relates to compounds useful as inhibitors of voltage-gated sodium and calcium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using these compositions to treat various disorders. Background technique [0002] Na channels are central to the generation of action potentials in all excitable cells, such as neurons and muscle cells. They play key roles in excitable tissues, including the brain, gastrointestinal smooth muscle, skeletal muscle, peripheral nervous system, spinal cord, and airways. As such, they play key roles in various disease states such as epilepsy ( see , Moulard, B. and D. Bertrand (2002) "Epilepsy and sodium channel blockers" Expert Opin. Ther. Patents 12(1):85-91)), Pain ( see , Waxman, S.G., S.Dib-Hajj, et al. (1999) "Sodium channels and pain" Proc Natl Acad Sci U S A 96(14):7635-9 and Waxman, S.G., T.R. Cummins, et...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12C07D403/12C07D239/42C07D403/04C07D239/48C07D405/04C07D401/04C07D409/04C07D405/12C07D413/04A61K31/506A61P29/00
Inventor D·M·威尔逊E·马丁伯拉夫T·D·纽伯特A·P·泰尔民J·E·冈萨雷斯三世N·齐默尔曼
Owner VERTEX PHARMA INC
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com