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Remedy or preventive for integration dysfunction syndrome

A disorder and drug technology, applied in the direction of drug combinations, pharmaceutical formulas, medical preparations containing active ingredients, etc., can solve the problem that the treatment effect of comprehensive disorders has not been disclosed, and achieve a significant therapeutic effect

Inactive Publication Date: 2012-02-29
TORAY IND INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, Patent Document 8 discloses the use of treating "mental and neurological diseases", but specifically only discloses the effect on restless legs syndrome (RLS), which belongs to neurological diseases, and does not have any effect on the therapeutic effect of the syndrome syndrome of the present invention. public

Method used

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  • Remedy or preventive for integration dysfunction syndrome
  • Remedy or preventive for integration dysfunction syndrome
  • Remedy or preventive for integration dysfunction syndrome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] (-)-17-(cyclopropylmethyl)-3,14β-dihydroxy-4,5α-epoxy-6β-[N-methyl-trans-3-(3-furyl)acrylamide ]Effect of morphinan hydrochloride (compound 1) on PCP-induced hyperkinesia in mice

[0079] In the experiment, 12 to 14 ddy male mice aged 7 to 8 weeks were used in each group. The mouse was placed in a measuring cage (22 cm×38 cm×20 cm: W×L×H) installed under the infrared counter, and allowed to acclimatize for 2 hours until the start of the measurement. Next, phencyclidine (PCP, 10 mg / kg) was subcutaneously administered to the mouse, and immediately returned to the measurement cage, and the spontaneous movement of the mouse was measured every 5 minutes thereafter by Supermex (Muromachi Machinery). The measurement time was 90 minutes. In addition, in the treatment of the test substance, the substance dissolved in the solvent was subcutaneously administered 1 minute before administration of PCP.

[0080] The structure of compound 1 is shown in the following formula (II). ...

reference example 1

[0085] As in Example 1, nalmefene and U-50,488H were evaluated. The result is as figure 1 shown. At 10 mg / kg, nalmefene had no effect on exercise capacity. U-50,488H showed a significant inhibitory effect, but had to be treated at a high dose of 1 mg / kg (p<0.05 and p<0.001, respectively, relative to the vehicle-administered group). As mentioned above, it can be confirmed that the effect of compound 1 is more remarkable than that of nalmefene and U-50,488H.

Embodiment 2

[0087] Effect of compound 1 on startle response in rat prepulse inhibition (PPI) model

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PUM

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Abstract

It is intended to provide a preventive or remedy for integration dysfunction syndrome by which integration dysfunction syndrome, in particular, positive symptoms thereof, can be treated without inducing information-processing disorder relating to cognition disorder, i.e., one of the syndromes of integration dysfunction syndrome. Thus, a preventive or remedy for integration dysfunction syndrome, which comprises as the active ingredient a compound having a specific morphinane skeleton typified by the following compound 1 or a pharmacologically acceptable acid addition salt thereof, is provided.

Description

technical field [0001] The present invention relates to a drug for treating or preventing syndromes comprising a morphinan derivative or a pharmacologically acceptable acid addition salt thereof as an active ingredient. Background technique [0002] Syndrome disorder (Schizophrenia, schizophrenia) mostly occurs in adolescence to young adulthood, and its lifetime incidence rate is equivalent to about 1% of the population, which is a kind of mental illness. Its symptoms are classified into positive symptoms such as psychomotor excitement, hallucinations, and delusions, negative symptoms such as lack of spontaneity, blunted affect, and communication impairment, and cognitive impairment (Non-Patent Document 1). [0003] Some people advocate the theory of excessive dopamine in the brain as the pathogenesis of the syndrome. Therefore, stereotyped and non-stereotype antipsychotic drugs that directly block dopamine receptors as the main way are currently used as drugs for the treatm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/485A61P25/00A61P25/18C07D489/08
CPCC07D489/08A61P25/00A61P25/18A61K31/485
Inventor 吉川悟望月英典
Owner TORAY IND INC