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A class of compounds and pharmaceutically acceptable salts thereof as antiepileptic drugs

A technology of antiepileptic drugs and compounds, applied in the field of preparation of antiepileptic drugs, capable of solving problems such as side effects and discomfort

Inactive Publication Date: 2016-03-30
全哲山 +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs all protect patients from various epileptic seizures to varying degrees, their side effects and discomfort prevent their use in long-term treatment

Method used

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  • A class of compounds and pharmaceutically acceptable salts thereof as antiepileptic drugs
  • A class of compounds and pharmaceutically acceptable salts thereof as antiepileptic drugs
  • A class of compounds and pharmaceutically acceptable salts thereof as antiepileptic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0013] Example A: Anticonvulsant Pharmacological Experiment and Neurotoxicity Experiment

[0014] All compounds provided herein were screened for their ability to prevent and treat electrically induced epilepsy in epilepsy. Maximal electroshock MES test, used to show the efficacy of antiepileptic drugs against generalized seizures. The compounds of the invention can be used to inhibit or prevent convulsions by oral (P.O) administration to mice.

[0015] A rotarod ataxia test was also performed on mice to evaluate the neurotoxicity of each of the claimed agents, measuring TD 50 And the protection index PI. Using mice, the biological activity and neurotoxicity of the test compounds in the maximum electroshock (MES) test seizure threshold test were tested. See Krall, R.J.; Penry, J.K.; White, B.G.; Kupferberg, H.J.; Swinyard, E.A. Epilepsia. 1978, 19, 409.

[0016] Table 1. Results of anticonvulsant pharmacological experiments and neurotoxicity experiments (mg / kg, p.o)

[001...

Embodiment B

[0018] Embodiment B: pharmaceutical composition

[0019] Formulation for 1000 tablets each containing 100 mg of active ingredient:

[0020] 4-(4-heptyloxy)phenyl-2H-1,2,4-triazol-3(4H)one-------------100g

[0021] Hydroxypropyl cellulose --------------------------------------- 2g

[0022] Wheat starch ------------------------------------------ 10g

[0023] Lactose ----------------------------------------- 100g

[0024] Magnesium stearate ------------------------------------------3g

[0025] Talc -------------------------------------------- 3g

[0026] The dosage used should be adapted to the nature and severity of the disease, the route of administration and the age and weight of the patient. The daily dose varies between 0.01mg-1g, and can be administered once or in fractions.

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PUM

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Abstract

The invention relates to a compound represented by a general formula I, an addition salt thereof with a pharmaceutically acceptable acid, and an application of a medicine composition in preparing antiepileptic medicines.

Description

technical field [0001] The present invention relates to the use of 4-alkoxyphenyl-1,2,4-triazol-1-one derivatives, their addition salts with pharmaceutically acceptable acids in the preparation of antiepileptic drugs and pharmaceutical combinations containing them thing. Background technique [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 application, such as phenobarbital, phenytoin, carbamazepine, and valproic acid. Although these drugs protect patients from various epileptic convulsions to varying degrees, their side effects and discomfort prevent their use in long-term treatment. In order to improve the therapeutic effect and eliminate or reduce side effects, new compounds with new structural features and new mechanisms of action are required. Contents of the invent...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4196A61P25/08
Inventor 全哲山宫国华魏成喜邓先清孙先宇
Owner 全哲山
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