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Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain

A heteroaryl, aryl technology, applied in the field of heteroaryl aminosulfonyl phenyl derivatives used as sodium or calcium channel blockers in the treatment of pain, can solve sodium channel blockers and calcium channels Blocker side effects, etc.

Inactive Publication Date: 2010-02-10
VERTEX PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0026] However, 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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  • Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
  • Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain
  • Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain

Examples

Experimental program
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Effect test

Embodiment Construction

[0628] 4-(2,4-Dichloro-phenoxy)-butyric acid ethyl ester

[0629]

[0630] At 80°C, to 2,4-dichlorophenol (32.6g, 0.2mol), NaI (3g) and K 2 CO 3 (69 g, 0.5 mol) in DMF (500 mL) was added dropwise with ethyl 4-bromobutyrate (39 g, 0.2 mol). The reaction mixture was stirred at 80 °C for 2 hours until the reaction mixture became colorless. The cooled mixture was filtered and the filtrate was diluted with EtOAc (1000 mL), washed with water (3 x 500 mL), dried and concentrated to give crude butyrate (57 g) as a colorless oil.

[0631] 1 H-NMR (CDCl 3 ): δ7.34(d, 1H, J=8.8Hz), 7.16(dd, 1H, J 1 =8.8Hz,J 2 =2.4Hz), 6.84(d, 1H, J=8.8Hz), 4.15(q, 2H, J=7.2Hz), 4.06(t, 2H, J=7.2Hz), 2.54(t, 2H, J=7.2 Hz), 2.17(p.2H, 6.4), 1.25(t, 3H, J=7.2Hz).

[0632] 4-(2,4-Dichloro-phenoxy)-butanoic acid

[0633]

[0634] Add LiOH.H 2 O (12.6 g, 0.3 mol), the reaction mixture was stirred at room temperature (RT) for 5 hours. The mixture was washed with Et 2 O washed (3 x 200 mL), aci...

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Abstract

The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. 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

[0001] This application is a divisional application of the Chinese patent application whose application number is 2004800293492 (PCT / US2004 / 025827), the application date is August 9, 2004, and the title of the invention is the same as above. technical field [0002] 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 [0003] 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) "...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D285/135C07C311/46C07D277/52C07D239/52C07D239/42C07D417/12C07D413/12C07D401/12C07D209/92C07D409/12C07D405/12C07D261/16A61K31/635A61K31/403A61P43/00A61P25/04A61P29/00A61P19/02A61P25/06A61P25/00A61P9/06A61P1/00
Inventor J·E·冈萨雷斯三世A·P·特门E·马丁波罗N·齐默曼
Owner VERTEX PHARMA INC
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