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Ion channel modulating compounds and uses thereof

a technology of ion channel and modulating compounds, which is applied in the field of ion channel modulating compounds, can solve the problems of increasing mortality in patients with myocardial infarction, no satisfactory pharmacotherapy for the treatment and/or prevention of ventricular fibrillation during acute, and the use of antiarrhythmic compounds, so as to relieve or forestall the sensation of pain

Inactive Publication Date: 2005-09-01
CORREVIO INT SARL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The present invention provides compounds that can treat and prevent cardiac arrhythmias and other cardiac pathological conditions by selectively inhibiting certain ion currents in the heart. These compounds can be used alone or in combination with other compounds to achieve the desired effect. The compounds can also be used in the presence of an \"arrhythmogenic substrate\" in the heart, which is a condition that can lead to arrhythmias. The compounds can be administered orally or through other means such as injection or patch. The invention also provides specific compounds that can target specific ion currents and combinations of compounds that can inhibit multiple ion currents. Overall, the invention provides new ways to treat and prevent heart disease."

Problems solved by technology

At present, there is no satisfactory pharmacotherapy for the treatment and / or prevention of ventricular fibrillation during acute ischemia.
In fact, many Class I antiarrhythmic compounds may actually increase mortality in patients who have had a myocardial infarction.
However, drug therapy is often limited by adverse effects, including the possibility of increased mortality, and inadequate efficacy (Feld G.K., Circulation.
Conversion rates for these drugs range between 30-50% for recent onset AF (Capucci A., Aschieri D., Villani G.Q., Drugs & Aging13(1):51-70, 1998), but they are also associated with a risk of inducing the ventricular tachyarrhythmias known as torsades de pointes.
Such events are particularly tragic in the case of AF as this arrhythmia is rarely a fatal in and of itself.

Method used

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  • Ion channel modulating compounds and uses thereof
  • Ion channel modulating compounds and uses thereof
  • Ion channel modulating compounds and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

example 2

(±)-Trans-[2-(4-Morpholinyl)-1-(1-Naphthenethoxy)]Cyclohexane Monohydrochloride

(Compound #2)

[0170] (i) The starting trans-aminocyclohexanol is prepared according to example 1.

[0171] (ii) To a chilled (0ºC) solution of (±)-trans-[2-(4-morpholinyl)]cyclohexanol (6.0 g, 32 mmol) and triethylamine (6.8 mL, 48 mmol) in dichloromethane (100 mL) was added via cannula a solution of methanesulfonyl chloride (3.10 mL, 40 mmol) in dichloromethane (50 mL). The addition was completed in 10 min., the reaction mixture was stirred for another hour at 0ºC and then at room temperature for 4 hours. The dichloromethane mixture was washed with water (2 x 50 mL) and the combined aqueous washings back extracted with dichloromethane (50 mL). The combined organic layers were dried over sodium sulfate and concentrated in vacuo to provide 9.0 g of the crude mesylate.

[0172] (iii) To sodium hydride, 80% oil dispersion, previously washed with hexanes (3 x 20 mL) (1.30 g, 51.6 mmol), in dry dimethylformamide (...

example 3

(±)-Trans-[2-(4-Morpholinyl)-1-(4-Bromophenethoxy)]Cyclohexane Monohydrochloride

(Compound #3)

[0173] (i) The starting trans-aminocyclohexanol is prepared according to example 1.

[0174] (ii) To a chilled (0ºC) solution of (±)-trans-[2-morpholinyl)]cyclohexanol (3.0 g, 16.2 mmol) and triethylamine (3.4 mL, 24 mmol) in dichloromethane (25 mL) was added via cannula a solution of methanesulfonyl chloride (1.55 mL, 20.0 mmol) in dichloromethane (25 mL). The addition was completed in 5 min., the reaction mixture was stirred for another hour at 0ºC and then at room temperature for 2 hours. The reaction mixture was diluted with dichloromethane (50 mL) and washed with water (2 x 50 mL) and the combined aqueous washings back extracted with dichloromethane (25 mL). The combined organic layers were dried over sodium sulfate and concentrated in vacuo to provide 4.7 g of the crude mesylate.

[0175] (iii) To sodium hydride, 80% oil dispersion, previously washed with hexanes (3 x 10 mL), (0.62 g, 25....

example 4

(±)-Trans-[2-(4-Morpholinyl)-1-[2-(2-Naphthoxy)Ethoxy)]Cyclohexane Monohydrochloride

(Compound #4)

[0176] (i) The starting trans-aminocyclohexanol is prepared according to example 1.

[0177] (ii) To a chilled (0ºC) solution of (()-trans-[2-(4-morpholinyl)]cyclohexanol (3.0 g, 16.2 mmol) and triethylamine (3.4 mL, 24 mmol) in dichloromethane (50 mL) was added via cannula a solution of methanesulfonyl chloride (1.55 mL, 20.0 mmol) in dichloromethane (50 mL). The addition was completed in 10 min., the reaction mixture was stirred for another hour at 0ºC and then at room temperature for 4 hours. The dichloromethane mixture was washed with water (2 x 50 mL) and the combined aqueous washings back extracted with dichloromethane (50 mL). The combined organic layers were dried over sodium sulfate and concentrated in vacuo to provide 4.3 g (100% yield) of the crude mesylate.

[0178] (iii) To sodium hydride, 80% oil dispersion, previously washed with hexanes (3 x 10 mL), (0.7 g, 29 mmol) in dry d...

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Abstract

Abstract of the DisclosureIon channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.

Description

Detailed Description of the InventionTECHNICAL FIELD[0001] The present invention is generally directed toward ion channel modulating compounds, pharmaceutical compositions and kits containing the ion channel modulating compounds, and therapeutic uses thereof.BACKGROUND OF THE INVENTION[0002] Cardiac ion channels are proteins that reside in the cell membrane and control the electrical activity of cardiac tissue. In response to external stimuli, such as changes in potential across the cell membrane, ion channels can form a pore through the cell membrane, and allow movement of specific ions into or out of the cell. The integrated behavior of thousands of ion channels in a single cell results in an ion current, and the integrated behavior of many ion currents makes up the characteristic cardiac action potential.[0003] Arrhythmia is a variation from the normal rhythm of the heart beat and generally represents the end product of abnormal ion-channel structure, number or function. Both ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61KC07D295/08A61K31/13A61K31/133A61K31/135A61K31/40A61K31/4015A61K31/407A61K31/41A61K31/4162A61K31/426A61K31/495A61K31/535A61K31/5375A61K31/5377A61P3/10A61P9/00A61P9/02A61P9/04A61P9/06A61P9/10A61P9/12A61P15/00A61P15/10A61P17/14A61P21/00A61P21/04A61P23/00A61P25/00A61P25/06A61P25/28A61P27/02A61P29/00A61P37/06C07CC07C217/52C07DC07D207/04C07D207/12C07D207/24C07D207/26C07D207/27C07D277/04C07D295/096C07D295/15C07D295/18C07D295/185C07D333/54C07D333/56C07D491/10C07D491/113
CPCC07C217/52C07C2101/14C07D207/12C07D207/27C07D277/04C07D295/08C07D491/10C07D295/14C07D295/15C07D295/185C07D333/54C07D333/56C07D295/096C07C2601/14A61P1/00A61P1/04A61P11/00A61P11/06A61P11/14A61P13/00A61P13/10A61P15/00A61P15/10A61P17/00A61P17/14A61P19/02A61P21/00A61P21/04A61P23/00A61P25/00A61P25/04A61P25/06A61P25/08A61P25/16A61P25/22A61P25/24A61P25/28A61P27/02A61P29/00A61P3/00A61P3/10A61P37/00A61P37/06A61P37/08A61P5/00A61P9/00A61P9/02A61P9/04A61P9/06A61P9/10A61P9/12
Inventor BAIN, ALLEN I.BEATCH, GREGORY N.LONGLEY, CINDY J.PLOUVIER, BERTRAND M. C.SHENG, TAOWALKER, MICHAEL J. A.WALL, RICHARD A.YONG, SANDRO L.ZHU, JEFF JIQUNZOLOTOY, ALEXANDER B.
Owner CORREVIO INT SARL
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