Use of Glutaric Acid Derivatives or the Pharmaceutically Acceptable Salts Thereof as Anti-Arrhythmic Agents

a technology of glutaric acid and derivatives, which is applied in the direction of biocide, plant growth regulators, animal husbandry, etc., can solve the problems of low anti-arrhythmic activity upon parenteral administration, low therapeutic diapason, and insufficient effectiveness

Inactive Publication Date: 2011-09-15
OBSCHESTVO S OGRANICHENNOI OTVETABTVENNOSTIYU PHARMENTERPRISES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Their main defects are insufficient effectiveness and low therapeutic diapason, which is manifested by the high frequency of cardial and extracardial side effects.
A defect of the known compound is the low anti-arrhythmic activity upon parenteral administration, and also insufficient diapason of therapeutic action.

Method used

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  • Use of Glutaric Acid Derivatives or the Pharmaceutically Acceptable Salts Thereof as Anti-Arrhythmic Agents
  • Use of Glutaric Acid Derivatives or the Pharmaceutically Acceptable Salts Thereof as Anti-Arrhythmic Agents
  • Use of Glutaric Acid Derivatives or the Pharmaceutically Acceptable Salts Thereof as Anti-Arrhythmic Agents

Examples

Experimental program
Comparison scheme
Effect test

example 1

Anti-Arrhythmic Activity of Compounds of General Formula (I) and N-succinyl-D,L-tryptophane Dipotasassium Salt and Also the Effect Thereof on Mortality Upon Adrenal Arrhythmia in Mice

[0034]Adrenal disorders of cardiac rhythm were reproduced on pedigreeless white laboratory mice of either sex having a weight of 18-22 g. Experimental arrhythmia in the animals was caused in accordance with the method described in the source Moore E. N., Spear J. F. Acute animal models for the study of antiarrhythmic drugs for the prevention of sudden coronary death. / / Clin. Pharmacol. Antiarhythmic Therapy. New-York. 1984. pp. 31-46.

[0035]The results of comparative testing of the claimed compounds and N-succinyl-D,L-tryptophane dipotasassium salt are presented in Table 2.

TABLE 2Effectiveness of compounds of general formula (I) and N-succinyl-D,L-tryptophane dipotasassium salt upon adrenal intoxication in miceNumber of animals in groupswithTrial conditions, doseventricularwith AVLifetimeNo.(mg / kg)in tri...

example 2

Activity of Compound III (Nα-glutaryl-L-histidine) and of N-succinyl-D,L-tryptophane Dipotassium Salt on Models of Aconitic Arrhythmia in Mice

[0039]Arrhythmia was reproduced according to the method of Ju. I. Vikhlyayev and N. V. Kaverina (1958) [Kaverina N. V., Berdyaev S. Ju., Kuschuk E. P., Paskhina O. E. Methodical indications in respect to a study of the anti-arrhythmic activity of new pharmacological substances. Manual on experimental (pre-clinical) study of new pharmacological substances. Edited by V. P. Fisenko.—Moscow. 2000. Page 210]. Aconitine nitrate was administered to the animals in a dose of 50 μg / kg intravenously.

[0040]This model makes it possible to assess the scope of the therapeutic action of the presented compounds and the N-succinyl-D,L-tryptophane dipotassium salt. Assessment of the scope of the therapeutic action was carried out in accordance with the value of the anti-arrhythmic index (AAI), determined as the ratio LD50 upon the oral method of administering to...

example 3

A Study of the Effect of Compound III (Nα-glutaryl-L-histidine) and of N-succinyl-D,L-tryptophane Dipotassium Salt on the Course of Early Occlusive Arrhythmia in Cats

[0042]At present, in order to assess the effectiveness of therapy under conditions of transistor ischemic arrhythmogenesis, a method is used that is described by Storozhuk V G. [Antifibrilic activity of some anti-arrhythmic agents upon maximum coronary artery ligation and the reperfusion thereof in cats. Pharmacology and Toxicology. 1985. No. 3, pp. 47-49].

[0043]The results of a study of compound III (Nα-glutaryl-L-histidine), N-succinyl-D,L-tryptophane dipotassium salt and classical anti-arrhythmics are presented in Table 4.

TABLE 4Anti-arrhythmic activity of compound III (Nα-glutaryl-L-histidine),comparative preparations and N-succinyl-D,L-tryptophane dipotassiumsalt on models of occlusive arrhythmia in catsStudiedNumber ofTime ofsubstance oranimals withoccurrence ofAnimalspreparation,ventriculararrhythmia,died inNo.do...

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Abstract

The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.

Description

[0001]The instant invention relates to medicine and to the use of glutaric acid derivatives, in particular N-acyl amino acid derivatives and pharmaceutically acceptable salts thereof as anti-arrhythmic agents for correction of disorders in the rhythm of cardiac activity.BACKGROUND ART[0002]It is well-known that at the present time propranolol (anaprilin, obzidan) and amiodaron (cordaron) are anti-arrhythmic agents that are widely used in clinical practice.[0003]Their main defects are insufficient effectiveness and low therapeutic diapason, which is manifested by the high frequency of cardial and extracardial side effects. [Mashkovsky M. D. Medicaments. Manual for doctors. Publication 15. Publishing House Novaya Volna. 2005. pages 390-392, 264-266].[0004]The analog of the claimed compounds that is closest in respect to action is the N-succinyl-D,L-tryptophane dipotassium salt exhibiting anti-ischemic, cardiotonic and anti-arrhythmic action upon research [Bulletin of experimental biol...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/5375C07D209/20A61K31/405A61P9/06C07D233/64A61K31/4172A61K31/4409C07D213/56C07D295/15C07D207/09A61K31/40C07D211/26A61K31/4453C07D333/20A61K31/381
CPCA61K31/405A61K31/4172C07D207/09C07D333/20C07D213/40C07D233/64C07D295/13C07D209/20A61P9/06
Inventor NEBOLSIN, VLADIMIR EVGENIEVICHBLINOV, DMITRY SERGEEVICHBALASHOV, VLADIMIR PAVLOVICHKROMOVA, TATYANA ALEXANDROVNAZHELTUKHINA, GALINA ALEXANDROVNA
Owner OBSCHESTVO S OGRANICHENNOI OTVETABTVENNOSTIYU PHARMENTERPRISES
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