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
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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

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  • 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
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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...

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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

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Application Information

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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
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