Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A technology of residues and compounds, applied in the field of dihydroxyphenylalanine derivatives, can solve problems such as the inability to ensure the formation of a sufficient amount of the chemical messenger dopamine
Inactive Publication Date: 2008-06-25
ELLNEUROXX LTD
View PDF0 Cites 58 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
Therefore, the formation of sufficient amounts of t
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
example 1
[0095] Example 1: Synthesis of O,O'-Diacetyl-L-DOPA-ethylene glycol lipoate (Diacetyl-DOPA-ethylene glycol lipoate; Compound 1)
[0096]
[0097] Lipoic acid is converted to lipoic acid monoethylene glycol ester using excess ethylene glycol and DCC. Conversion of L-DOPA to Fmoc-L-DOPA by Fmoc-succinimide, and acetylation of Fmoc-L-DOPA to N-Fmoc via acetic anhydride under Schotten-Baumann conditions -O,O'-diacetyl-L-DOPA. The coupling product N-Fmoc-O,O'-diacetyl-L-DOPA ethylene glycol-racemic (rac)-lipoate was obtained by converting the above lipoic acid monoethylene glycol ester with DDC. The Fmoc protecting group was cleaved via tetrabutylammonium fluoride in DMF.
[0098] Purity (HPLC): 81-85%, clear yellow oil
[0099] 13 C-NMR (100.6MHz, d 4 - Methanol), δ (ppm):
[0101] Example 2: Synthesis of O,O'-diacetyl-L-DOPA-(R,S)-lipoic acid amide (Diacetyl-DOPA-lipoic acid amide; Compound 2)
[0102]
[0103] O, O'-diacetyl-L-DOPA-rac-lipoic acid amide is obtained by reacting L-DOPA-rac-lipoic acid amide with acetic anhydride under mild alkaline reaction conditions.
[0107] Example 3: Synthesis of L-DOPA-(D,L)-lipoic acid amide (DOPA-lipoic acid amide; compound 3)
[0108]
[0109] L-DOPA-rac-ac- Lipoic acid amide. Lipoyl chloride is obtained from lipoic acid and oxalyl chloride, and lipoic acid succinimide ester is obtained from lipoic acid, hydroxysuccinimide and DCC.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
PUM
Login to view more
Abstract
The invention relates to dihydroxyphenylalanine derivatives, the production thereof, and pharmaceutical compositions containing said dihydroxyphenylalanine derivatives. The invention further relates to the use of said dihydroxyphenylalanine derivatives and pharmaceutical compositions for the treatment and prevention of movement disorders, neurodegenerative diseases, Alzheimer, Parkinson's disease, hemiatrophy hemiparkinsonism, Parkinson's syndrome, Lewy bodies disease, frontotemporal dementia, Lytico-Bodig disease (Parkinsonism-dementia-amyotrophic lateral sclerosis, striatonigral degeneration, Shy-Drager syndrome, sporadic olivopontocerebellar degeneration, progressive pallidal atrophy, progressive supranuclear palsy, Hallervorden-Spatz disease, Huntington's disease, X chromosome-linked dystonia (Morbus Lubag), mitochondrial cytopathy with striatal necrosis, neuroacanthocytosis, restless leg syndrome, Wilson's disease.
Description
technical field [0001] The present invention relates to a dihydroxyphenylalanine derivative, a synthesis method thereof, an application thereof and a pharmaceutical composition comprising the dihydroxyphenylalanine derivative. Background technique [0002] DOPA is named 2-amino-3-(3,4-dihydroxyphenyl)-propionic acid by the International Union of Pure and Applied Chemistry (IUPAC), commonly known as Levodopa and used especially in the treatment of Parkinson's sick. [0003] Parkinson's disease, also known as Parkinson's syndrome, is a chronic disease that still cannot be cured. The course of the disease is characterized by the slow death of nerve cells that do not contain the chemical messenger dopamine in the substantia nigra (black matter) of the brain. Therefore, sufficient amounts of the chemical messenger dopamine cannot be guaranteed to be formed. Mutations (eg, Lewy bodies) can also be found in other parts of the brain, such as the nucleus coeruleus, raphe nucleus, ...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to view more 
Login to view more