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Non-sedating barbituric acid derivatives

A sedative and barbiturate technology, applied in the direction of drug combinations, organic active ingredients, nervous system diseases, etc., can solve the problems of not teaching non-sedating barbiturates, not teaching sedative barbiturates, etc.

Inactive Publication Date: 2005-06-08
TARO PHARMA INDS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the prior art does not teach the use of sedative barbiturates for neuroprotection due to their toxicity, nor does the prior art teach the use of non-sedating barbiturates as neuroprotective agents due to their lack of sedative or anesthetic properties

Method used

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Examples

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Effect test

Embodiment 1

[0123] The anticonvulsant activity of the barbituric acid derivatives of the invention can be demonstrated or tested by evaluating the prevention of maximal electroshock seizures (MES) in treated mice. The MES test is widely used to evaluate the anticonvulsant properties of compounds, mainly because of the good correlation between test results and clinical findings of effects in patients with epilepsy. In a typical MES test in which corneal electrodes are used, a current of about 150 mA and a stimulus of 60 Hz are applied for about 200 milliseconds to evaluate the anticonvulsant properties of the barbituric acid derivatives of the present invention. Mice were tested prior to dosing in order to exclude from the study any animal that did not respond to complete tonic convulsions including tonic extension of the hind limbs (THE), which served as a basis for evaluating the efficacy of the active substances used. Animals protected by THE are considered protected in the MES test.

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Embodiment 2

[0126] The non-toxicity of the barbituric acid derivatives of the present invention can be tested by repeated high-dose administration, as follows:

[0127] The test compound is suspended in warmed polyethylene glycol 400 or other suitable solvent and administered to eg Sprague-Dawley rats via gastric tube at an initial dose of about 1500 mg / kg. A similar dose was given to the same mice 24 hours later, and a similar dose was given to the same mice again 48 hours after the first dose. Animals were checked several hours after dosing, again before the next dose, and 3 days after the last dose. Administration is monitored for toxic effects as well as behavioral effects such as locomotion, avoidance behavior, feeding or any other observable effects.

Embodiment 3

[0129] The sedative and muscle relaxant properties of the barbituric acid derivatives of the invention can be demonstrated by monitoring the behavior and locomotor effects of the treated mice.

[0130] For example, a test composition may be administered intraperitoneally, eg, in Swiss Webster rat alkalized saline. The time required for animals to receive various doses to exhibit specific motor and behavioral effects is recorded. Surveillance effects may include, for example, muscle hypotonia, locomotor activity, tranquility, and avoidance behavior. Toxic effects were also recorded.

[0131] The efficacy of the composition can be evaluated against known drugs that are primarily used as skeletal muscle relaxants and / or sedatives. The combination of sedation and not impairing the animal's ability to respond to its environment is highly desirable in an agent used to treat anxiety. The compositions of the present invention preferably do not exhibit central nervous system hypnoti...

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Abstract

The present invention relates to novel non-sedating barbituric acid derivatives, pharmaceutical compositions containing them and methods of neuroprotection in cases of cerebral ischemia, head trauma and other acute neurologic injuries, and prevention of resulting neuronal damage. The invention also relates to the use of non-sedating barbituric acid derivatives given in a manner and dosage effective to produce blood levels and brain levels of these drugs and / or their active metabolites sufficient to provide a therapeutic effect.

Description

Background of the invention [0001] The present invention relates to novel non-sedating barbituric acid derivatives, pharmaceutical compositions containing them, and methods of neuroprotection in conditions of cerebral ischemia, head trauma, and other acute neurological injuries, and the prevention of the resulting neuroprotective meta damage. The present invention also relates to the use of non-sedating barbituric acid derivatives administered in effective doses in such a manner as to produce sufficient concentrations of these drugs and / or their active metabolites in the blood and brain to provide a therapeutic effect. [0002] Barbituric acid and its derivatives have been known to have pharmacological properties since the late 19th and early 20th centuries, and some of them are used as active ingredients in many pharmaceuticals. Barbituric acid derivatives are known to be mainly used as sedatives, hypnotics and anesthetics. Certain derivatives also have anticonvulsant effec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/62A61K31/515A61K31/675A61P25/00C07D239/64C07D409/10
CPCA61K31/515A61K31/675A61P25/00C07D239/64
Inventor 戴尼尔·A·莫罗斯丹尼拉·吉特曼
Owner TARO PHARMA INDS
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