Compounds useful for treating neurological disorders

a neurological disorder and compound technology, applied in the field of neurological disorders, can solve the problems of insufficient effect of neuropathic pain, inability to effectively treat general nociceptive pain, and inability to show sufficient effect on neuropathic pain

Inactive Publication Date: 2008-06-12
YISSUM RES DEV CO OF THE HEBREW UNIV OF JERUSALEM LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

These compounds demonstrate significant efficacy in reducing neuropathic pain and neuronal degeneration symptoms with improved safety profiles, offering a more effective treatment option compared to existing medications.

Problems solved by technology

Unfortunately, and unlike other types of pain, neuropathic-pain tends to respond poorly to analgesic medication.
It is known that analgesics, particularly narcotic analgesics and the like, which are effective for general nociceptive pains are hardly effective for neuropathic pain.
For example, it is known that morphine has a strong analgesic effect on nociceptive pains but does not show a sufficient effect on neuropathic pain.
Patients are usually treated empirically with tricyclic or serotonin and norephinephrine uptake inhibitors, and anticonvulsants that all have limited efficacy and undesirable side effects.
Local anaesthetic blocks targeted at trigger points, peripheral nerves, plexi, dorsal roots, and the sympathetic nervous system have useful but short lived effects; longer lasting blocks by phenol injection or cryotherapy risk irreversible functional impairment and have not been tested in placebo-controlled trials.
Chronic epidural administration of drugs such as clonidine, steroids, opiates, or midazolam is invasive, has side effects and the efficacy of these drugs has not been adequately assessed [Woolf J. et al.
Additionally, the use of Valproic acid (VPA), is limited by its considerable adverse effects including hepatotoxicity and teratogenicity and thus cannot be given to women of childbearing age and children [Baille, T. A. et al.

Method used

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  • Compounds useful for treating neurological disorders
  • Compounds useful for treating neurological disorders
  • Compounds useful for treating neurological disorders

Examples

Experimental program
Comparison scheme
Effect test

example 1

Decrease in Neuropathic Pain Following Administration of M-TMCD

[0195]Male Sprague-Dawley rats (Harlan laboratories, Jerusalem, Israel) weighing 200-225 g were used. The rats chosen feature initial lack of foot withdrawal in response to mechanical stimuli, as described in experimental A (neuropathic pain model) above. The rats underwent surgery by legating and cutting of the L5-L6 nerves, as disclosed in Experimental B (surgical procedure) above, to produce neuropathic pain as verified by tactile allodynia. Rats were divided to 3 groups including 8-10 rats per study. Each group received 2 different doses of M-TMCD i.p (selected from 20, 40, 60, 80 and 100 mg / kg) and 4 ml / kg of methyl cellulose was used as control. The doses of M-TMCD were 20, 40, 60, 80 and 100 mg / kg.

[0196]Tactile allodynia threshold was measured as base line and 30, 60, 120, 180 and 240 minutes after administration of the drug, as described in the Experimental above, the threshold being the foot withdrawal in respon...

example 2

Decrease in Neuropathic Pain Following Administration of VCD

[0198]The same experiment described in Example 1 was repeated with VCD, and the results are shown in FIG. 2.

[0199]As can be seen the rats responded in a dose dependent manner to varying dosages of VCD, with maximal effect evident 60 min after administration of the drug with an ED50 of 52.3 mg / kg.

example 3

Decrease in Neuropathic Pain Following Administration of TMCD

[0200]The same experiment described in Example 1 was repeated with TMCD, and the results are shown in FIG. 3.

[0201]As can be seen the rats responded in a dose dependent manner to varying dosages of TMCD, with maximal effect evident 60 min after administration of the drug with an ED50 of 84.5 mg / kg.

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Abstract

The invention relates to the use of compounds for the preparation of a medicament for treating neuropathic pain, migraine, psychiatric disorder and / or neuronal degeneration. The invention additionally relates to a pharmaceutical composition comprising compounds for treating neuropathic pain, migraine, psychiatric disorder and / or neuronal degeneration. A method for treating neuropathic pain, migraine, psychiatric disorder and / or neuronal degeneration is also provided.

Description

FIELD OF THE INVENTION[0001]The invention relates to compounds for the treatment of neurological disorders preferably neuropathic pain, migraine, psychiatric disorders and / or neuronal degeneration.BACKGROUND OF THE INVENTION[0002]Neuropathic pain is an intractable pain initiated or caused by a primary lesion or dysfunction in the peripheral or central nervous system. Neuropathic pain is part of the neurological disease spectrum and may be an expression of severe medical pathology [Hansson P. European J. of Pain 2002; 6; 45]. Neuropathic pain manifests itself due to neurological disorders accompanying various causes such as wound, infection, cancer, ischemia and metabolic disorders including diabetes mellitus. Though there are many unclear points on the mechanism of neuropathic pain, it is considered that abnormal continuous firing of sensory nerve and the like are the cause. Typical symptoms of neuropathic pain include allodinia, hyperalgesia, hyperesthesia and the like. Their sympt...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/19A61K31/16A61P25/00A61P25/06A61P25/18
CPCA61K31/19A61K31/16A61P25/00A61P25/06A61P25/18
InventorBIALER, MEIRYAGEN, BORISWINKLER, ILANDEVOR, MARSHALL
OwnerYISSUM RES DEV CO OF THE HEBREW UNIV OF JERUSALEM LTD