Cyclic ketone derivatives and applications thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles

A technology of derivatives and cyclic ketones, which is applied in the field of preparation of labeled compounds, can solve the problems of large trauma, risk and slow clearance of biopsy

Inactive Publication Date: 2012-07-11
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Both methods have obvious disadvantages: biopsy has greater trauma and risk, autopsy can only be used for postmortem diagnosis, etc.
18 Deficiency in FDDNP is slower to clear from normal brain regions

Method used

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  • Cyclic ketone derivatives and applications thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles
  • Cyclic ketone derivatives and applications thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles
  • Cyclic ketone derivatives and applications thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0321] Embodiment 1, the synthetic method of symmetrical cyclic ketone derivatives:

[0322]

[0323] Synthesis method of symmetrical cyclic ketone derivatives: Under the catalysis of sodium hydroxide solution, carry out Aldol condensation dehydration of cyclopentanone or cyclohexanone and corresponding benzaldehyde to obtain the target compound.

Embodiment 2

[0324] Embodiment 2, the synthetic method of asymmetric cyclic ketone derivatives:

[0325]

[0326] The synthesis method of asymmetric cyclic ketone derivatives: firstly, react with different substituted benzaldehydes and excess cyclopentanone or cyclohexanone to obtain a single chalcone-based reaction product, after separation and purification, react with the corresponding benzene Formaldehyde reacts to obtain the target substance.

Embodiment 3

[0327] Embodiment three, cyclic ketone derivatives 11 C radioactive isotope labeling method:

[0328]

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PUM

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Abstract

The invention relates to applications of compounds of formulas (1)-(58), or pharmaceutically-acceptable salts, esters, amides or prodrugs thereof as developers and aggregation inhibitors of amyloid protein sediments and neurofibrillary tangles, a preparation method labeled compounds for imaging, and a method for transporting the compounds to amyloid protein sediments and neurofibrillary tangles. When serving as the developers used to detect the amyloid protein sediments and neurofibrillary tangles in body and tissue, the compounds need to use appropriate radioisotopes or contrast agents suitable for magnetic resonance detection to be labeled. The compounds of the invention are applied to diagnose and treat patients suffering from amyloid protein sediments and neurofibrillary tangles and Alzheimer disease.

Description

field of invention [0001] The present invention relates to a new biologically active compound and its application, a method for diagnosis and treatment using a radioactive isotope or magnetic resonance contrast agent-labeled compound, and a preparation method for the labeled compound. Background technique [0002] Alzheimer's disease (AD) is a neurodegenerative disease with insidious onset and progressive aggravation. The main clinical manifestations are cognitive decline, irreversible memory loss, disorientation and language dysfunction. Autopsy confirmed that there are a large number of senile plaques (Senile plaques) formed by the aggregation of amyloid-β (Aβ) peptides and many neurofibrillary tangles (neurofibrillary tangles) formed by highly phosphorylated tau protein filaments in the brain tissue. As well as the loss of neurons and synapses, etc., the amyloid deposits mentioned in the present invention include senile plaques, and also include amyloid deposits such as D...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C225/22C07C221/00C07C45/74C07C229/52C07C227/16C07C233/43C07C231/12C07C65/38C07C51/373C07C49/747C07C49/753C07C49/697A61K51/04A61K49/10A61K31/196A61K31/194A61K31/167A61K31/136A61K31/122A61P25/28A61P43/00A61P35/00A61P3/10A61P9/00A61P25/00
Inventor 周江宁乔金平甘昌胜汪琛玮葛金芳南豆豆
Owner UNIV OF SCI & TECH OF CHINA
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