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Method for treating diabetic peripheral neuropathic pain

a peripheral neuropathic pain and diabetic technology, applied in the direction of biocide, amide active ingredients, drug compositions, etc., can solve the problems of no survival advantage, no effective treatment available, increase of firing rate and starting or increasing spontaneous activity,

Inactive Publication Date: 2010-04-22
UCB SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention relates to the use of a group of specific amino acid derivatives for the treatment of pain, particularly allodynia, which is a common pain symptom that is often related to neuropathic pain or other chronic pain disorders. The invention specifically concerns the use of harkoseride and its derivatives for this purpose. The compounds have been previously used for the treatment of seizure disorders and have shown promising results in treating pain. The invention is based on the discovery that these compounds are effective in treating pain, particularly allodynia, which is a unique pain symptom that is often related to neuropathic pain. The compounds can be used alone or in combination with other drugs to provide better pain relief.

Problems solved by technology

The latter being maladaptive, offering no survival advantage and very often no effective treatment is available.
First, enhanced activity of afferent nociceptive neurons following sensitisation of (sleeping) neurons (e.g., inflammatory pain, cancer pain, headache, lower back pain, visceral pain, migraine) with the primary afferent nociceptive neuron remaining intact, though the receptor activity is changed and reduced thresholds, increase of firing rates and starting of or increase of spontaneous activity are typically found.
Second, ectopic activity of afferent nociceptive neurons following lesions of its axons (e.g., peripheral and central neuropathic pain), with the primary afferent neuron being damaged. This leads to irreversible peripheral and central biochemical, morphological and functional changes. Therefore, (peripheral) neuropathy is broadly defined as a disease of the (peripheral) nervous system.
The conditions listed above are known to be poorly treated by currently marketed analgesics such as opioids or nonsteroidal anti-inflammatory drugs (NSAID's) due to insufficient efficacy or limiting side effects.

Method used

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  • Method for treating diabetic peripheral neuropathic pain
  • Method for treating diabetic peripheral neuropathic pain
  • Method for treating diabetic peripheral neuropathic pain

Examples

Experimental program
Comparison scheme
Effect test

example 2

Chronic Constriction Injury

CCI, Bennett-Model

[0047]The effectiveness of harkoseride in reducing spontaneous chronic pain, mechanical allodynia, and thermal hyperalgesia was tested using the chronic constriction injury (CCI) model of peripheral neuropathy, one of the best characterised in vivo animal models used to study chronic pain due to peripheral nerve injury. In this model, loose ligatures are placed around the sciatic nerve, which produces axonal swelling and a partial deafferentation manifested as a significant but incomplete loss of axons in the distal portion of the peripheral nerve. One of the prominent behaviours seen following sciatic nerve ligation is the appearance of hind paw guarding, thought to be an indication of an ongoing spontaneous chronic pain. Support for this idea is derived from reports of increased spinal cord neural activity, and increased spontaneous neuronal discharge in spinothalamic tract neurons and in the ventrobasal thalamus in the absence of overt...

example 3

Tail Flick Test, Rat

[0057]Harkoseride was additionally tested for potential activity in acute spinal thermal nociception using the tail flick test. In this model of acute thermal spinal / reflex hyperalgesia radiant heat is applied to the animal's tail approximately 2 cm from the tip and time latency for withdrawal reaction is automatically assessed by an algometer, a defined maximal stimulus time prevents tissue damage. This test is widely used as an assay for the anti-nociceptive efficacy of pharmacological agents and is highly predictive of acute analgesic efficacy in humans. Usually pure analgesics of the opioid type are most active; neither adjuvants like amitryptiline nor anti-epileptics nor NSAIDs (non-steroidal anti-inflammatory drugs) are active.

[0058]Results for 20 and 40 mg / kg harkoseride i.p are shown in table 5 [percent anti-nociception, calculated as [{(post-drug latency)−(pre-drug-latency)} / {(max. latency)−(pre-drug latency)}×100]±SEM, n=12 / group]. A baseline or pre-dru...

example 4

The Anti-Nociceptive Activity of Harkoseride in Comparison with Gabapentin

[0060]In the following explained study the used harkoseride is hereinafter abbreviated as SPM 927 and gabapentin is hereinafter abbreviated as GBP.

Objective

[0061]The major aim of this study was to assess the anti-nociceptive activity of SPM 927 and gabapentin (GBP) in rodent models for inflammatory pain and to compare the in vivo effects of each drug with each other.

Methods:

[0062]Carrageenan-induced mechanical hyperalgesia in rats was induced by subplantar injection of a 0.1 ml of a 2% carrageenan suspension and measured 3 h afterwards by the paw pressure (Randall-Sellito) test.

[0063]Subchronic inflammatory nocicpetion in mice was induced by the subplantar injection of formalin (0.02 ml of a 5% solution). Nociceptive behaviour (paw licking) was measured and quantified between 0 and 5 min (acute pain) and between 20 and 30 min (subchronic inflammatory pain) after formalin.

[0064]Drugs and experimental design: SP...

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Abstract

The present invention concerns the novel use of compounds of the Formula I: for treating allodynia as major and unique pain symptom independent of the nature of an underlying disease, but that is often related to neuropathic pain or other different types of chronic or phantom pain.

Description

BACKGROUND OF THE INVENTION[0001]The present invention relates to the novel use of a group of specific amino acid derivatives according to Formula I for the preparation of pharmaceutical compositions useful for the treatment of allodynia as a major and unique pain symptom independent of the nature of an underlying disease, but that is often related to neuropathic pain or other different types of chronic or phantom pain. Particularly the present invention relates to the novel use of harkoseride and its derivatives for the preparation of pharmaceutical compositions useful for the treatment of allodynia as a major and unique pain symptom independent of the nature of an underlying disease, but that is often related to neuropathic pain, or other different types of chronic or phantom pain.[0002]The chemical name of SPM 927 which is also hereinafter referred to as harkoseride is (R)-2-Acetamido-N-benzyl-3-methoxypropionamide.[0003]The compounds of the Invention are known agents useful in a...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/16A61P23/00A61K31/165A61P25/02A61P25/04A61P27/16
CPCA61K31/165A61P23/00A61P25/00A61P25/02A61P25/04A61P27/16A61P29/00A61K31/16
Inventor SELVE, NORMA
Owner UCB SA
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