Enantiomers Of Tetrahydro-N,N-Dimethyl-2,2-Diphenyl-3-Furanmethanamine (Anavex2-73) And Use Thereof In The Treatment Of Alzheimer's Disease And Other Disorders Modulated By The Sigma 1 Receptor

A sigma receptor, receptor technology, applied in nervous system diseases, medical preparations containing active ingredients, instruments, etc., can solve the problems of destroying the function of interacting agonists or reversing agonists, ineffectiveness, etc.

Pending Publication Date: 2018-02-16
ANAVEX LIFE SCI CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In pharmacology, an antagonist has affinity but no potency for its cognate receptor, and binding will disrupt the interaction and inhibit the receptor's agonist function or reverse the agonist

Method used

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  • Enantiomers Of Tetrahydro-N,N-Dimethyl-2,2-Diphenyl-3-Furanmethanamine (Anavex2-73) And Use Thereof In The Treatment Of Alzheimer's Disease And Other Disorders Modulated By The Sigma 1 Receptor
  • Enantiomers Of Tetrahydro-N,N-Dimethyl-2,2-Diphenyl-3-Furanmethanamine (Anavex2-73) And Use Thereof In The Treatment Of Alzheimer's Disease And Other Disorders Modulated By The Sigma 1 Receptor
  • Enantiomers Of Tetrahydro-N,N-Dimethyl-2,2-Diphenyl-3-Furanmethanamine (Anavex2-73) And Use Thereof In The Treatment Of Alzheimer's Disease And Other Disorders Modulated By The Sigma 1 Receptor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Neuroprotection against amyloid-beta

[0113] 67-Year-Old Man Diagnosed with Early-Stage Alzheimer's Dementia Takes 10mg of Treatment, once a week, continued for three years. His mental function was tested quarterly during this period and did not decline. At autopsy, his brain was found to contain senile plaques but very low levels of amyloid oligomers.

Embodiment 2

[0115] Neuroprotection against oxidative stress

[0116] A 29-year-old female balloonist with anticipated hypoxic stress received 10 mg orally daily prior to balloon launch with little or no of Lasts 5 days. The balloonist ascended to 6,000 meters without oxygen assistance without being injured by hypoxia.

Embodiment 3

[0118] Anti-neurotoxic neuroprotection

[0119] A 37-year-old male hazardous materials engineer, predicted to have neurotoxic stress, was basically free from oral administration of 1 mg before daily exposure to tetanus toxin. of Lasts 5 days. Engineers were unharmed when exposed to 0.1 ng / kg of the neurotoxin.

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Abstract

The compound (-)-tetrahydro-N,N-dimethyl-2,2-diphenyl-3-furanmethanamine hydrochloride ((-)-ANAVEX2-73, (-)A2-73, (-)AE 37) has been found to exhibit selectivity for sigma-1 (sigma1) receptors and stronger agonist activity at the muscarinic M1 acetylcholine receptor than the (+) enantiomer of said compound. Pharmaceutical compositions comprising the (-) enantiomer are disclosed, as are methods ofusing said (-) enantiomer in the treatment of disorders associated with sigma-1 receptors and the treatment of Alzheimer's disease. Methods of classifying cells with regards to sigma receptor type using the (-) enantiomer are also disclosed.

Description

field of invention [0001] contains basically none of pharmaceutical preparations. The present invention also includes substantially free by administering a therapeutically effective amount of A method of treating Alzheimer's disease in a subject in need of such treatment. [0002] The invention also includes the method of exposing the cells to a detectable amount of substantially no of And a method for determining the level of sigma receptor binding, a method for classifying said cells by sigma receptor type. Background technique [0003] Two sigma receptor subtypes have been identified based on their pharmacological characteristics. The sigma-1 (σ-1) receptor has been cloned (Hanner et al., 1996). The sigma-2 receptor has been reported to be a separate molecular entity (Langa et al., 2003). The sigma-1 receptor has been reported to have high affinity for bezomorphas positive isoforms such as (+)-pentazocine and (+)-SKF-10,047. The sigma-2 receptor has been r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/341A61P25/28C07D307/14G01N33/567
CPCC07D231/22G01N33/5005A61K31/341A61P25/28
Inventor G·內利阿
Owner ANAVEX LIFE SCI CORP
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