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Use of 3-substituted oxindole derivatives as KCNQ potassium channel modulators

A technology of oxindole derivatives and uses, applied in the field of therapy

Inactive Publication Date: 2005-10-12
NEUROSEARCH AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

BK active compounds such as scorpion toxin did not show any effect on KCNQ channels, while potent KCNQ inhibitory compounds XE-991 and Linopiridine did not show any effect on BK channels

Method used

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  • Use of 3-substituted oxindole derivatives as KCNQ potassium channel modulators
  • Use of 3-substituted oxindole derivatives as KCNQ potassium channel modulators
  • Use of 3-substituted oxindole derivatives as KCNQ potassium channel modulators

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Embodiment Construction

[0013] KCNQ activating compounds

[0014] In its first aspect, the present invention relates to chemicals capable of activating KCNQ channels in the treatment or alleviation of pain, in particular neuropathic pain, chronic headache, central pain, diabetic neuropathy, post-herpetic neuralgia, or peripheral pain Use in the pain of nerve damage.

[0015] In the context of the present invention, a KCNQ-activating substance is one which, in the presence of micromolar or preferably sub-micromolar concentrations of said substance, is capable of enhancing KCNQ channel activity - ie through the channel, compared to KCNQ channel activity in the absence of said substance The current-substance in which the channel activity is measured under physiological conditions.

[0016] Enhanced activity can be specifically defined as an increase in current obtained under physiological conditions at any given membrane potential when the channel conducts current under physiological conditions, or a d...

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Abstract

The present invention relates to the use of substituted 3-phenyl oxindole derivatives as modulators of the potassium KCNQ channels, to pharmaceutical compositions comprising these compounds, and to methods of treatment herewith.

Description

technical field [0001] The present invention relates to the use of substituted 3-phenyloxindole derivatives as potassium KCNQ channel modulators, pharmaceutical compositions containing these compounds, and methods of treatment using them. Background of the Invention [0002] Potassium (K + ) channels are structurally and functionally diverse K + - A family of selective channel proteins, which are ubiquitous in cells, which means that they play a very important role in regulating a variety of key cellular functions. Although widely distributed as a class, K + Channels are differentially distributed as individual members of this class or as families. [0003] In general, K in cells + Activation of the channel results in hyperpolarization of the cell membrane, or repolarization in depolarized cells, thus acting as an endogenous membrane voltage clamp. This is particularly important in excitable cells such as neurons and muscle cells. K + Channels can r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/404A61P1/00A61P1/04A61P3/10A61P9/00A61P9/06A61P9/10A61P11/00A61P11/06A61P13/00A61P17/02A61P21/00A61P25/00A61P25/02A61P25/04A61P25/06A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P25/30A61P27/02A61P27/16A61P29/00A61P31/12A61P31/18A61P35/00A61P39/00A61P43/00
CPCA61K31/405A61K31/404A61P1/00A61P1/04A61P11/00A61P11/06A61P13/00A61P17/02A61P21/00A61P25/00A61P25/02A61P25/04A61P25/06A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P25/30A61P27/02A61P27/16A61P29/00A61P3/10A61P31/12A61P31/18A61P35/00A61P39/00A61P43/00A61P9/00A61P9/06A61P9/10
Inventor B·S·杰森R·L·斯库洛德D·斯托贝克S·P·奥勒森
Owner NEUROSEARCH AS