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Polyvalent derivatives of emoxypine

A technology of amoxipine and its derivatives, applied in the field of treatment of synuclein disease, can solve problems such as undiscovered disease improvement treatment methods, movement disorders and mental symptoms

Pending Publication Date: 2021-10-29
ALSATECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, most drugs are metabolized before reaching the blood-brain barrier (BBB), resulting in a variety of side effects, including gastrointestinal reactions (such as anorexia, nausea, or vomiting), dyskinesias, and psychiatric symptoms
[0009] Parkinson's disease remains an incurable disease and no effective disease-modifying treatments have yet been identified

Method used

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  • Polyvalent derivatives of emoxypine
  • Polyvalent derivatives of emoxypine
  • Polyvalent derivatives of emoxypine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0217] Example 1: Experiments related to the depolymerization of α-synuclein using tetraiminoemoxipine

[0218] Depolymerization of α-synuclein by tetraiminoamoxipine.

[0219] An assay measuring the activity of tetraimino-amoxipine for solubilizing α-synuclein aggregates was performed.

Embodiment 2

[0220] Example 2: Synthesis of Tetraimino Amoxazepine Derivatives and Polyamido Amoxazepine Derivatives

[0221] The polyamido amoxazepine derivatives and the tetraimino amoxazepine derivatives of the present invention are synthesized respectively by the following formation methods:

[0222]

Embodiment 3

[0223] Example 3: Synthesis of Triimino Amoxepine Derivatives

[0224] Triimino-amoxipine (also known as MHP-trentriimine) derivatives of the present invention are synthesized via the following formation scheme:

[0225]

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PUM

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Abstract

Use of polyvalent emoxypine derivatives or related compounds in the treatment or prevention of, inter alia, Parkinson's Disease are described. The present invention provides, in one aspect, compounds and methods for treating or preventing a synucleinopathy, comprising administering an effective amount of a polyvalent derivative of emoxypine (e.g., poly-imino or poly-amido emoxypine derviatives) to a subject in need thereof, wherein the method comprises disaggregation of [alpha]-synuclein.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of U.S. Provisional Patent Application No. 62 / 802,323, filed February 7, 2019, which is hereby incorporated by reference in its entirety. technical field [0003] The present invention relates in part to the treatment of synucleinopathy. [0004] Instructions for text files submitted electronically [0005] This application contains a Sequence Listing. It has been submitted electronically via the EFS network as an ASCII text file entitled "ALS-008PC_ST25". The sequence listing is 1,438 bytes in size and was recorded around February 7, 2020. The Sequence Listing is hereby incorporated by reference in its entirety. Background technique [0006] Parkinson's disease or parkinsonism is a group of progressive neurodegenerative disorders that can significantly reduce a person's quality of life. The distinguishing features of these disorders are tremor at rest, rigidity, bradykinesia, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4412A61K31/44A61P25/28C07D213/16C07D213/24
CPCA61P25/28C07D213/65C07D213/81A61K31/444
Inventor C·尼科洛J-M·莱恩R·蒂纳德Y·阿托尼
Owner ALSATECH INC
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