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Sigma-1 receptor ligand with acetylcholinesterase

A carrier, an effective amount of technology, applied in the field of prevention or treatment of neurodegenerative diseases, can solve problems such as failure

Inactive Publication Date: 2006-11-15
SAMARITAN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In fact, more data highlighting the role of calcium in the pathogenesis of AD have been published, but the use of different calcium inhibitors to delay A

Method used

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  • Sigma-1 receptor ligand with acetylcholinesterase
  • Sigma-1 receptor ligand with acetylcholinesterase
  • Sigma-1 receptor ligand with acetylcholinesterase

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] The synthesis of embodiment 1.SP004

[0072] Such as figure 2 As shown, 10 grams (0.059mol) of 2,3,4-trimethoxy-benzene ( figure 2 "100" in ) was added to a suspension of aluminum chloride (35.5 g, 0.26 mol) in carbon disulfide. Keeping the temperature at about 10°C, gamma-chlorobutyryl chloride (14.7 g, 0.1 mol) was added. After the addition was complete, stirring was continued at room temperature for two hours. The reaction mixture was poured into ice and extracted with dichloromethane. The organic layer was separated, washed with water, MgSO 4 dry. The solution was concentrated under reduced pressure. The residue was used in the next step without further purification.

[0073] In the next step, the compound 4-chloro-1-(2,3,4-trimethoxy-phenyl)-butan-1-one ( figure 2 "200") (7 g, 0.026 mol) and N-ethylpiperazine (5.8 g, 0.051 mol) for seven hours. After distilling off unreacted N-ethylpiperazine, the residue was chromatographed on silica gel.

[0074] In the...

Embodiment 2

[0077] SP004 Binding Assay

[0078] Different binding studies were performed with the following SP004 concentrations:

[0079] 3E-10, 3E-9, 1E-8, 3E-8, ​​1E-7, 3E-7, 1E-6, 1E-5M.

[0080] Materials and methods

[0081] Central imidazoline-2 receptor (I 2 ). The test uses central I extracted from rat cortex 2 receptor. Each increasing concentration of SP004 and 2nM specificity I 2 receptor ligand [ 3 H]-Imidazole was incubated at 22°C for 30 minutes. Brown et al., Brit. J. Pharmacol., 99:803-809 (1990).

[0082] Muscarinic receptors (nonspecific). This test uses muscarinic receptors extracted from rat cortex. Each increasing concentration of SP004 and 0.05nM muscarinic ligand [ 3 H]-QNB was incubated at 22°C for 120 minutes. Richards, Brit. J. Pharmacol., 99:753-761 (1990).

[0083] Neuronal nicotinic α-BGTX-insensitive receptors. The assay uses neuronal nicotinic α-BGTX-insensitive receptors extracted from rat cortex. Each increasing concentration of SP004 and 1...

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PUM

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Abstract

A novel compound and method for preventing or treating neurodegenerative diseases by inhibiting acetylcholinesterase and binding the sigma-1 receptor are disclosed. Dimethylcarbamic acid 2,3-bis-dimethylcarbamoyloxy-6-[4-(4-ethyl-piperazin-yl)-butyryl]-phenyl ester and its derivatives represent a novel therapeutic strategy against beta-amyloid peptide induced neurotoxicity, in inhibiting acetylcholinesterase, in improving cholinergic transmission, in binding the sigma-l receptor, and in releasing a metabolite that is active both as a sigma-1 receptor ligand and an antioxidant.

Description

field of invention [0001] The present invention generally relates to methods of preventing or treating neurodegenerative diseases by inhibiting acetylcholinesterase, and more particularly to therapeutic compounds and pharmaceutical compositions for preventing or treating neurodegenerative diseases or conditions involving neuronal cell death. Background of the invention [0002] Nerve cell degeneration and death can cause potentially devastating and irreversible effects in an individual, and among other things, can result from stroke, heart attack, or other brain or spinal cord ischemia or trauma. Neurodegenerative disorders involving nerve cell death include Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, Down's syndrome, and Korsakov's psychosis. [0003] Alzheimer's disease (AD) is a degenerative disease of neurons in the cerebral cortex that leads to brain atrophy and dementia. AD currently affects more t...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K
CPCA61K31/495A61P25/00A61P25/28A61P43/00
Inventor 瓦西里奥斯·帕帕多珀洛斯劳伦特·莱卡奴珍妮特·格里森
Owner SAMARITAN PHARMA
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