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Purine ribosides as antiarrhythmics

A technology for arrhythmia and purine nucleosides, which can be used in drug combinations, pharmaceutical formulations, cardiovascular system diseases, etc., and can solve problems such as side effects

Inactive Publication Date: 2004-03-17
CV THERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Adenosine A 1 Receptor subtype highly specific, but like all therapeutic compounds, potential side effects

Method used

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  • Purine ribosides as antiarrhythmics
  • Purine ribosides as antiarrhythmics
  • Purine ribosides as antiarrhythmics

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 a. Preparation of (3-(S)-aminotetrahydrofuranyl)purine nucleoside step 1. Resolution of 3-(S)-aminotetrahydrofuran

[0053] A mixture of 3-aminotetrahydrofuran hydrochloride (0.5 g, 4 mmol) and (S)-(+)-10-camphorsulfonyl chloride (1.1 g, 4.4 mmol) in pyridine (10 ml) was stirred at room temperature for 4 hours, then concentrate. The residue was dissolved in EtOAc and washed with 0.5N HCl, sodium bicarbonate and brine. The organic layer was dried over magnesium sulfate, filtered and concentrated to give 1.17 g of a brown oil (97%) which was chromatographed on silica gel (25% to 70% EtOAc / Hex). The obtained white solid was repeatedly recrystallized in acetone until 1 HNMR showed that the purity increased to over 90%, and (S)-camphorsulfonate of 3-(S)-aminotetrahydrofuran was obtained. Step 2. Preparation of 3-(S)-aminotetrahydrofuran hydrochloride

[0054] The (S)-camphorsulfonate salt of 3-(S)-aminotetrahydrofuran (170 mg, 0.56 mmol) was dissolved ...

Embodiment 2

[0059] The effect of CVT-510 on prolongation of the AH interval, which is the adenosine A of CVT-510, and on heart rate (sinus rhythm) in patients with PSVT was tested in patients undergoing clinically indicated electrophysiological studies 1 Measure of the effect mediated. In the first study, a single bolus of CVT-510 was administered to patient volunteers. In the second study, patients were induced with PSVT prior to administration of CVT-510.

[0060] All antiarrhythmic drugs, including digoxin, beta-blockers and calcium channel blockers, were discontinued five half-lives prior to the study.

[0061] The following patients were excluded from the study: if the RR interval was >200 ms or if the resting heart rate was 100 / min. Other exclusion criteria included evidence of ventricular preexcitation, class II-IV congestive heart failure, or asthma. Patients were required to have a normal baseline of electrophysiological parameters, including a Winkbach paced cycle length of 5...

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PUM

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Abstract

A method for treating arrhythmias is provided comprising administering a low dose of an adenosine receptor agonist, in particular CVT-510, to a mammal in need of such treatment.

Description

technical field [0001] The present invention relates to a method of treating atrial arrhythmias with minimal adverse side effects comprising administering adenosine A at low doses 1 receptor agonist. Background technique [0002] Atrial arrhythmias such as primary atrial fibrillation, atrial flutter, and paroxysmal atrial tachycardia (PSVT) are abnormal heart rhythms due to various causes. Arrhythmias can range from occasional, asymptomatic clinical manifestations to life-threatening abnormalities. Cardiac arrhythmias account for a considerable percentage of human deaths. There is therefore a need to develop methods of mitigating the effects of cardiac arrhythmias. [0003] A variety of antiarrhythmic drug treatments are currently available. But these compounds have obvious limitations. For example, digoxin has a slow onset of action (approximately 30 minutes) and its peak effect is not observed until 3-4 hours after administration. Other examples are beta-blockers and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/167A61K31/70A61K31/7076A61P9/06
CPCA61K31/7076A61K31/70A61P9/06
Inventor 安德鲁·A·沃尔夫
Owner CV THERAPEUTICS INC
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