Indenone derivative and applications thereof as developing agent and aggregation inhibitor of amyloid protein deposit and neurofibrillary tangle

A compound and complex technology, applied in the field of preparation of labeled compounds, can solve the problems of slow clearance, large trauma and risk of biopsy
CN102180780AInactive Publication Date: 2011-09-14UNIV OF SCI & TECH OF CHINA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
UNIV OF SCI & TECH OF CHINA
Publication Date
2011-09-14
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a compound in a general formula (1), applications of pharmaceutically acceptable salt, esters, amides or predrug of the compound as a developing agent and an aggregation inhibitor of amyloid protein deposit and neurofibrillary tangle, a preparation method of a labeled compound used for development, and a method for conveying the compound to the amyloid protein deposit and the neurofibrillary tangle. When the compound is taken as the developing agent used for detecting in vivo or tissue amyloid protein deposit and neurofibrillary tangle, appropriate radioactive isotope or a contrast agent applicable to magnetic resonance detection needs to be used for labeling the compound. The compound is especially used for the diagnosis and treatment of patients with amyloid protein deposit and neurofibrillary tangle diseases including Alzheimer disease.
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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. Brain tissue autopsy confirmed a large number of senile plaques (SPs) formed by amyloid-β (Aβ) peptide aggregation and many neurofibrillary tangles (neurofibrillary tangles) formed by filaments of hyperphosphorylated tau protein. NFTs), and the loss of neurons and synapses, etc., the amyloid deposits mentioned in the present invention include but are not limited to senile plaques.

[0003] Senile plaques and neurofibrillary tangles compose...

Claims

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