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Adenosine A2A receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

A receptor antagonist, adenosine technology, applied in the field of adenosine A2a receptor antagonists, can solve the problems of undiagnosed and rarely active treatment

Inactive Publication Date: 2008-12-17
SCHERING AG
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because it is often mistaken for agitation or anxiety, this common syndrome is often underdiagnosed and rarely aggressively treated

Method used

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  • Adenosine A2A receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
  • Adenosine A2A receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
  • Adenosine A2A receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders

Examples

Experimental program
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Embodiment

[0382] A population of seven capuchin monkeys previously sensitive to the chronic effects of haloperidol showed EPS when given haloperidol (0.3 mg / kg, p.o.) rapidly. Compound A was administered orally (p.o.) at a dose of 0.3 to 30 mg / kg in combination with haloperidol. Compound B was administered orally (p.o.) at a dose of 3 to 100 mg / kg in combination with haloperidol. These studies were conducted using a within-subjects design such that each monkey received all 6 treatments (vehicle and 5 doses of Compound A) in a crossover, balanced design. In all of these studies, the group of seven monkeys showed baseline levels of EPS when receiving haloperidol.

[0383] Compound A produced a dose-dependent reduction in the maximum EPS score ( Figure 1A ), and a dose-dependent delay in the onset of EPS ( Figure 1B ). Compound A at a dose of 1 mg / kg prevented EPS onset in one monkey and delayed EPS onset by 1 hour. Compound A at a dose of 3 mg / kg prevented the onset of EPS in two m...

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Abstract

There is disclosed a method for the treatment or prevention of Extra Pyramidal syndrome (EPS), dystonia, restless legs syndrome (RLS) or periodic leg movement in sleep (PLMS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS, dystonia, RLS or PLMS; also claimed are pharmaceutical compositions consisting of an adenosine A2a receptor antagonist in combination with an antipsychotic agent, an anticonvulsant agent, lithium or an opioid.

Description

field of invention [0001] The present invention relates to adenosine A 2a Use of receptor antagonists for the treatment of a variety of neurological syndromes involving the extrapyramidal motor system (ie, extrapyramidal syndromes) that occur after acute and prolonged use of almost all antipsychotic drugs. The invention also relates to adenosine A 2a Use of receptor antagonists for the treatment of other abnormal movement disorders such as restless legs syndrome (RLS) and periodic limb movements during sleep (PLMS). The present invention also relates to adenosine A 2a A receptor antagonist and an antipsychotic constitute a pharmaceutical composition useful for the treatment of EPS, and involve a 2a A pharmaceutical composition comprising a receptor antagonist and another drug useful in the treatment of other abnormal movement disorders such as RLS or PLMS. Background of the invention [0002] Extrapyramidal syndrome (EPS) is a collective term for a series of adverse neur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06
CPCA61K31/519A61K31/522A61K31/551A61K31/5513A61K45/06A61P21/02A61P25/02A61P25/16A61P25/18A61P25/24A61P25/36A61K2300/00
Inventor M·格兹拉克J·杭特A·庞德G·法堤
Owner SCHERING AG
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