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Use of isovaleric acid derivatives CNS inhibitors in preparing medicine for curing headache

A technology of isovaleric acid and pharmaceutical preparations, applied in the direction of drug combination, anhydride/acid/halide active ingredients, plant/algae/fungus/moss ingredients, etc., which can solve problems such as application restrictions and muscle relaxation

Inactive Publication Date: 2004-09-29
NPS PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Of the other two drugs, 2-propylvalerate is hepatotoxic and baclofen causes excessive muscle relaxation and sedation
This limits their use in therapeutic

Method used

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  • Use of isovaleric acid derivatives CNS inhibitors in preparing medicine for curing headache
  • Use of isovaleric acid derivatives CNS inhibitors in preparing medicine for curing headache
  • Use of isovaleric acid derivatives CNS inhibitors in preparing medicine for curing headache

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0087] Use of valerian preparations to alleviate and multiple

[0088] sclerosis-associated ankylosis

[0089] A human female subject, 42 years of age, with one or more symptoms of multiple sclerosis, was experiencing considerable stress and had difficulty falling asleep at night and delayed sleep onset, often suffering from catatonic dreaming and often Disturbance of awakening. The subject also experienced frequent nocturnal painful lower extremity extensor cramps, which also frequently aroused her from sleep. The next day, these painful extensor spasms cause deep muscle pain (bruising) with muscle / joint stiffness.

[0090] The subjects decided to use a preparation of valerian root known for its sleep aiding properties. This valerian product, "Baldriparan Stark N," is a tablet made in Germany that contains valerian root, hop and melissa extracts. Each tablet of this coated compressed tablet contains 95 mg of dried 70% (v / v) ethanol extract ...

example 2

[0092] Spinal Cord Relief with Valerian Preparations

[0093] Trauma-Related Tonic Symptoms

[0094] A human male subject, 38 years old, had tonic symptoms (hyperreflexia, tendon reflexes, and extensor spasms.) developed with early spinal cord trauma. All of these symptoms interrupt the sleep of the patient and reduce the quality of his sleep. When taking the same valerian preparation produced in Germany as in Example 1, the subjects noticed a significant improvement in sleep quality in addition to a significant reduction in nocturnal extensor spasms. The subject continued to take the preparation as necessary (prn) to relieve the above symptoms.

example 3

[0096] Isovaleramide antitonic test

[0097] (1) Evaluation of ankylosis in rats with chronic spinal cord transection

[0098] In these studies, male albino rats of Holtzman origin (Harlan Sprague-Dawley Laboratories) weighing between 270-530 grams were used as subjects. The animals were housed individually and given continuous access to food and water throughout the experimental period. All experimental procedures were reviewed and approved by the Animal Care and Use Committee. Anesthetize the animal with a mixture of isoflurane and oxygen at a flow rate of 4 L / min, then place the rat in a stereotaxy frame and maintain anesthesia, make a contractile incision around the spinal column and between T6-T9 Laminectomy was performed to remove a piece of spinal cord tissue with a size of about 1-2mm by suction, and filled with gel foam to reduce bleeding, and then the incision was sutured layer by layer.

[0099] After transection is complete, to maintain the rat'...

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PUM

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Abstract

Preparations and extracts of valerian, as well as isovaleramide, isovaleric acid, and its pharmaceutically acceptable salts, esters, and substituted amides, exhibit clinically significant pharmacological properties which implicate a treatment for a variety of pathological conditions, including spasticity and convulsions, which are ameliorated by effecting a mild depression of CNS activity. The compositions in question generally are non-cytotoxic and do not elicit weakness or sedative activity at doses that are effective for the symptomatic treatment of such pathological conditions.

Description

[0001] This application is a divisional application filed on August 29, 1997, the application number is 97199257.6, and the invention name is isovaleric acid derivative CNS inhibitors for the treatment of rigidity and convulsions. Background of the invention [0002] The present invention is relevant to the treatment of disease states, such as rigidity and convulsions, which can be alleviated by mild depression of central nervous system (CNS) function without causing excessive sedation or muscle tension in animal subjects, including humans. Excessive slack. More specifically, the invention relates to the therapeutic use of isovaleramide, isovaleric acid, and related compounds in patients with these disease states. [0003] Many drugs currently used to treat disease states such as tonicity and convulsions exhibit annoying side effects. This limits their long-term clinical use. One such example is benzodiazepines, which can cause cognitive impairment. Of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/18A61K31/00A61K31/16A61K31/164A61K31/19A61K31/215A61K36/84A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P43/00
CPCA61K31/19A61K36/84A61K31/16A61P23/00A61P25/00A61P25/04A61P25/06A61P25/08A61P25/14A61P25/20A61P43/00
Inventor L·D·阿特曼M·F·巴兰德林
Owner NPS PHARM INC