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Use of non-imidazole alkylamines histamine h3- receptor ligands in treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia

An alkyl-purpose technology, applied in the field of application of ligands of non-imidazolidinylamine histamine H3-receptors in the preparation of drugs for the treatment of Parkinson's disease and obstructive sleep apnea, which can solve problems such as poor efficacy

Active Publication Date: 2012-11-07
BIOPROJET
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

All treatments for this type of disorder by loss of circadian periodicity have been poorly effective: for example modafinil treatment has been tried in the treatment of excessive daytime sleepiness with only limited efficacy and the health authorities have not yet recognized the stimulant with an unknown mechanism of action Drug indications

Method used

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  • Use of non-imidazole alkylamines histamine h3- receptor ligands in treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia
  • Use of non-imidazole alkylamines histamine h3- receptor ligands in treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia
  • Use of non-imidazole alkylamines histamine h3- receptor ligands in treatment of parkinson's disease obstructive sleep apnea, dementia with lewy bodies, vascular dementia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0971] Example 1 : Treatment of wakefulness / sleep disturbances with histamine H3 antagonists / inverse agonists

[0972] Experimental induction of Parkinson's disease in a cohort of cats by treatment with the chemical neurotoxin MPTP (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine) and recapitulation of human PD motor impairment , the chemical neurotoxin MPTP can selectively erode dopaminergic neurons. This group of cats showed marked disorganization during the sleep-wake sequence.

[0973] With BF 2.-649 (3-(4-chlorophenyl)propyl 3-piperidine propyl ether) (a potent and selective H3-antagonist) as estimated by electromyography and EEG recordings Treatment with oral 10 mg / kg normalized the sleep-wake process. In particular, in this animal model of PD, the alternation of sleep and wakefulness is replaced by prolonged sleep, corresponding to the excess of daytime sleep experienced by most human patients, and administration of the drug of the present invention can significantly su...

Embodiment 2

[0975] Example 2 : Treatment of Obstructive Sleep Apnea with Histamine H3 Antagonists / Inverse Agonists

[0976] In a group of 10 male patients diagnosed with OSA by polysomnography in the hospital at night, with Epswoth score greater than 12 and body mass index less than 35, BF2.649 (3-(4-chlorophenyl ) Propyl 3-piperidinyl propyl ether) The effect of 3-day treatment was evaluated in a single-blind trial relative to placebo.

[0977] This treatment resulted in a significant reduction in the number of episodes of daytime sleepiness in all subjects (greater than 60% reduction) and complete prevention of episodes of daytime sleepiness. In addition, nighttime sleep duration did not decrease and its quality improved. This clinical trial is the first to determine the utility of H3 antagonists / inverse agonists in OSA.

Embodiment 3

[0978] Example 3 : Treatment of dementia with Lewy bodies with histamine H3 antagonist / inverse agonist

[0979] In general, dementia with Lewy bodies is treated with acetylcholinesterase inhibitors such as donepezil, rivastigmine or gallanthamine. These agents increase the concentration of acetylcholine in the extracellular space of the brain. Rats are tested with a compound of the invention in combination with one of these agents. Drugs selected from donepezil, rivastigmine tartrate or galantamine were administered in rats in combination with 3-(4-chlorophenyl)propyl-3-piperidinepropyl ether. Analysis of rat brains by microdialysis showed an increase in the concentration of acetylcholine by co-administration of the compounds of the present invention. Rats tolerated this combination well, especially with regard to cardiovascular parameters.

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Abstract

The present invention provides new method of treatment of Parkinson's disease, obstructive sleep apnea, narcolepsy, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamine derivatives that constitute antagonists of the H3-receptors of histamine.

Description

technical field [0001] The present invention relates to the therapeutic use of alkylamines of formula (A) as defined below for the treatment of Parkinson's disease (PD), obstructive sleep apnea (OSA), dementia with Lewy bodies (DLB) and / or vascular dementia (VD), especially for the treatment of its symptoms. Background technique [0002] known histamine H 3 - Receptor antagonists in particular increase the synthesis and release of histamine in the brain. Through this mechanism, it results in prolonged wakefulness, improved cognitive processes, decreased food intake and normalized vestibular reflexes (Schwartz et al., Physiol. Rev., 1991, 71: 1-51). [0003] known histamine H 3 - Agonists inhibit the release of several neurotransmitters, including histamine, monoamine, and neuropeptides, thereby exerting a calming and sleep-promoting effect in the brain. In peripheral tissues, H 3 - Receptor agonists exert anti-inflammatory, analgesic, gastro-intestinal, inhibitory secre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4453A61P25/28A61P25/16
CPCA61K31/4453A61P11/00A61P25/00A61P25/16A61P25/18A61P25/20A61P25/24A61P25/26A61P25/28A61P43/00
Inventor 让-夏尔·施瓦茨让娜-玛丽·勒孔特
Owner BIOPROJET
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