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5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt thereof

A compound, 3-a technology, applied in the field of 5-substituted phenoxy-1,2,4-triazolo[4,3-a]pyridine compounds and their pharmaceutically acceptable salts used as antiepileptic drugs , which can solve the problems of limited long-term use, side effects and discomfort

Inactive Publication Date: 2012-08-15
ZHEJIANG OCEAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A variety of antiepileptic drugs are available in clinical practice, such as phenytoin, phenobarbital, valproic acid, carbamazepine, lamotrigine, etc., although these drugs can be used to treat or relieve Suffering from various epilepsy patients, but their side effects and discomfort limit their long-term use

Method used

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  • 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt thereof
  • 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt thereof
  • 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt thereof

Examples

Experimental program
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Effect test

Embodiment A

[0030] Example A: Anticonvulsant Pharmacological Experiment and Neurotoxicity Experiment

[0031] All compounds provided herein were screened for their ability to prevent and treat electrically and chemically induced epilepsy in epilepsy. Maximal electroshock MES test, used to show the efficacy of antiepileptic drugs against generalized seizures. Convulsions are inhibited or prevented by administering the compounds of the invention intraperitoneally to mice.

[0032] The rotarod ataxia test was also performed on mice to evaluate the neurotoxicity of each drug, and the TD50 and protection index PI values ​​were measured. The biological activity or neurotoxicity of the test compound in the maximal electroshock (MES) test seizure threshold test is used as a decimal. See R.J. Krall, J.K. Penry, B.G. White, H.J. Kupferberg, Epilepsia. 19 (1978) 409-428.

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Abstract

The invention relates to a 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound used for antiepileptic medicament, and medical salt of the compound. The invention provides the new 5-substituted phenoxy-1, 2, 4-triazole [4, 3-a] pyridine compound which has comparatively low toxic and side effects and shows the valuable pharmacological properties as anticonvulsant, and addition salt of pharmaceutically acceptable acid of the compound. The formula I shows the compound and the addition salt of the pharmaceutically acceptable acid of the compound, wherein R is selected from all bromoalkanes. The compound is high in anticonvulsion activity, comparatively low in toxic and side effects and high in safety index, thus laying the foundation for the research and application of the antiepileptic medicament.

Description

(1) Technical field [0001] The present invention relates to 5-substituted phenoxy-1,2,4-triazol[4,3-a]pyridine compounds and their pharmaceutically acceptable acid addition salts, their preparation methods and their use in the preparation of antiepileptic drugs Uses and pharmaceutical compositions containing them. (2) Background technology [0002] Epilepsy is a collective term used to describe a group of chronic convulsive disorders that are characterized by transient seizures accompanied by loss or disturbance of consciousness. A variety of antiepileptic drugs are available in clinical practice, such as phenytoin, phenobarbital, valproic acid, carbamazepine, lamotrigine, etc., although these drugs can be used to treat or relieve Various epilepsy patients suffer, but their side effects and discomfort limit their long-term use. In order to eliminate or reduce toxic side effects and improve therapeutic effect, new compounds with new structural features and new mechanisms of...

Claims

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Application Information

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IPC IPC(8): C07D471/04A61K31/437A61P25/08
Inventor 关丽萍赵东海徐银峰张瑞鹏常月
Owner ZHEJIANG OCEAN UNIV
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