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Therapeutic agent for motor disorders

a technology for motor disorders and therapeutic agents, applied in the direction of biocide, muscular disorders, drug compositions, etc., can solve the problems of motor fluctuations and dyskinesias, poor facial expression of parkinson patients, and increased disability with disease progression, so as to achieve treatment and/or prophylaxis of parkinson, and the effect of a movement disorder

Inactive Publication Date: 2012-04-26
KYOWA HAKKO KIRIN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0027]The present invention provides an agent for the treatment and / or prophylaxis of a movement disorder, comprising a thiazole derivative or a pharmaceutically acceptable salt thereof as an active ingredient; a pharmaceutical composition comprising (a) a thiazole derivative or a pharmaceutically acceptable salt thereof and (b) L-DOPA and / or a dopamine agonist; an agent for the treatment and / or prophylaxis of Parkinson's disease comprising (a) a thiazole derivative or a pharmaceutically acceptable salt thereof and (b) L-DOPA and / or a dopamine agonist in combination; a kit comprising (a) a first component comprising a thiazole derivative or a pharmaceutically acceptable salt thereof and (b) a second component comprising L-DOPA and / or a dopamine agonist; a thiazole derivative or a pharmaceutically acceptable salt thereof, which has a selective adenosine A2A antagonistic activity and is useful for the treatment of a movement disorder, and the like.

Problems solved by technology

Patients with Parkinson's disease are poor in facial expression, and tend to speak in a soft voice.
Early stage patients of Parkinson's disease mostly respond well to a symptomatic therapy by a dopamine replacement therapy; however, the disability increases with progression of the disease.
Although currently available medications for Parkinson's disease generally provide adequate symptomatic control for several years, however, many patients develop motor fluctuations and dyskinesias that compromise clinical response (The New England Journal of Medicine (N. Eng. J. Med.
As the disease progresses, however, L-DOPA tends to become less helpful.
This is not due to the loss of efficacy of L-DOPA, but rather, for example, to development of motor complications such as end-of-dose deterioration or adverse fluctuation in motor response including “wearing-off phenomenon”, “on-off fluctuations”, and dyskinesias.
However, even if such symptoms are expressed, the treatment effect may recover all of a sudden.

Method used

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  • Therapeutic agent for motor disorders
  • Therapeutic agent for motor disorders
  • Therapeutic agent for motor disorders

Examples

Experimental program
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Effect test

example 1

[0117]Tablets having the following formulations are prepared according to the conventional manner. Compound (IA) (40 g), lactose (286.8 g), and potato starch (60 g) are mixed, and then a 10% aqueous solution of hydroxypropylcellulose (120 g) is added thereto. The resulting mixture is kneaded according to the conventional manner, granulated, and dried to form granules for tableting. After adding thereto 1.2 g of magnesium stearate followed by mixing, the mixture is punched with a tableting machine having a punch measuring 8 mm in diameter (Model RT-15; Kikusui) to obtain tablets (containing 20 mg of an active ingredient per tablet).

TABLE 5FormulationCompound (IA)20mglactose143.4mgpotato starch30mghydroxypropylcellulose6mgmagnesium stearate0.6mg200mg

example 2

[0118]Tablets having the following formulation are prepared in the same manner as in Example 1.

TABLE 6FormulationCompound (IB)20mglactose143.4mgpotato starch30mghydroxypropylcellulose6mgmagnesium stearate0.6mg200mg

example 3

[0119]Tablets having the following formulation are prepared in the same manner as in Example 1.

TABLE 7FormulationCompound (IC)20mglactose143.4mgpotato starch30mghydroxypropylcellulose6mgmagnesium stearate0.6mg200mg

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Abstract

Provided are an agent for the treatment and / or prophylaxis of a movement disorder, the agent for the treatment and / or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and / or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and / or prophylaxis wherein the movement disorder is a side effect of L-DOPA and / or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.

Description

TECHNICAL FIELD[0001]The present invention relates to an agent for the treatment and / or prophylaxis of a movement disorder, an agent for the treatment and / or prophylaxis of Parkinson's disease and the like.BACKGROUND ART[0002]Parkinson's disease is a brain disease characterized by tremor, bradykinesia, difficulty in gait and coordinated movement and the like. This disease is associated with damage of a part of brain which governs muscle movements. Generally, the first symptom of Parkinson's disease is a limb tremor (shaking or trembling) particularly when the body is at rest. Tremor often begins in the hemibody, and frequently occurs in one of the hands. Other common symptoms include slow movement (bradykinesia), an inability to move (akinesia), a rigidity of trunk and limbs, a shuffling gait, and a stooped posture and the like. Patients with Parkinson's disease are poor in facial expression, and tend to speak in a soft voice. Parkinson's disease can cause secondary symptoms such as...

Claims

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Application Information

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IPC IPC(8): A61K31/5377A61K31/506A61K31/427A61K31/4355A61K31/4709A61K31/436A61K31/435A61K31/4365C07D417/14C07D491/048C07D491/052C07D495/04A61P25/14A61P25/16A61K31/4439
CPCA61K31/435A61K31/4355A61K31/436A61K31/4365A61K31/4439C07D495/04A61K31/506A61K31/5377C07D417/14C07D491/048C07D491/052A61K31/4709A61K31/198A61K31/427A61P21/00A61P25/00A61P25/14A61P25/16A61P43/00
Inventor UESAKA, NORIAKISAWADA, TAKASHIKANDA, TOMOYUKI
Owner KYOWA HAKKO KIRIN CO LTD
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