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Treatment methods using triaryl methane compounds

A technology of compounds, substituents, applied in the field of therapy using triarylmethane compounds, which can solve the problems of exacerbation, low bioavailability, low efficacy, etc.

Inactive Publication Date: 2009-05-20
ICAGEN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

While having demonstrable efficacy, the imidazolyl-based Kv1.3 and / or IK1 channel inhibitors studied to date have been limited by several drawbacks including a well-documented potential for hepatotoxicity
This toxicity is exacerbated by the inhibitor's low potency, nonspecific interaction with calcium-activated potassium channels rather than Kv1.3 and / or IK1 channels, and low bioavailability, each of which contributes to inhibition higher doses and more frequent dosing of

Method used

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  • Treatment methods using triaryl methane compounds
  • Treatment methods using triaryl methane compounds
  • Treatment methods using triaryl methane compounds

Examples

Experimental program
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Embodiment 1

[0140] Example 1 illustrates the methods used to synthesize and characterize compounds of the invention. Using the methods detailed in this example, the compounds of the invention were isolated in substantially pure form and in good yields. Other synthetic methods are disclosed in US Patent 6,288,122 and US Patent 6,028,103.

Embodiment 2

[0141] Example 2 describes the biological assay used to measure the inhibition of potassium channels by compounds of the invention.

[0142] Example 1

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PUM

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Abstract

The use of novel inhibitors of potassium flux is disclosed for the treatment of inflammatory processes, such as multiple sclerosis, insulin-dependent (type I) diabetes mellitus, rheumatoid arthritis, peripheral neuritis and pulmonary hypertension. The compounds are also of use in treating and preventing stroke. These inhibitors have a high specificity for the IK1 channel and greater stability relative to non-fluorine substituted homologues.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application 60 / 752,935, filed December 20, 2005, the disclosure of which is incorporated herein in its entirety for all purposes. Background of the invention [0003] One aspect of the invention relates to methods of treating or preventing inflammatory processes, including in particular multiple sclerosis and pulmonary hypertension. [0004] Multiple sclerosis (MS) is a chronic inflammatory disease of the central nervous system. Individuals with MS experience deficits in neurological function, including vision loss, motor deterioration, sensory impairment, incontinence, and other events related to central nervous system deficits; however, MS does not impair cognitive function. MS disease progression has a highly variable course, with patients experiencing acute symptoms, followed by periods of remission of symptoms, and later progression to chronic and degenerative cond...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N55/00A61K31/695A61K31/65
CPCA61K31/165A61P1/04A61P11/00A61P11/06A61P13/12A61P17/00A61P17/02A61P17/12A61P19/02A61P21/00A61P21/04A61P25/00A61P25/02A61P29/00A61P31/14A61P31/20A61P31/22A61P35/00A61P3/06A61P37/06A61P37/08A61P43/00A61P9/00A61P9/10A61P9/12A61P3/10
Inventor N·A·卡斯特尔G·C·里戈登D·S·克拉弗特
Owner ICAGEN INC
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