Beta-hydroxyl butyryl-amino acid compound, preparing method and application
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A technology of hydroxybutyryl and amino acid, which is applied in the field of compounds, can solve the problems of different doses, different effects, low bioavailability, ketoacidosis in blood vessels, etc.
Active Publication Date: 2018-05-11
郑州海斯威生物技术有限公司
View PDF4 Cites 5 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
However, BHB is very unstable in the human body. Whether BHB or BHB salt is introduced, it will not only cause great damage to the gastrointestinal digestive system, resulting in low bioavailability, but also cause differences in dosage due to differences in each person's physique. The effects are different; at the same time, BHB cannot be injected routinely, and it is easy to cause intravascular ketoacidosis poisoning, which limits the application of BHB
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
Embodiment A1
[0122] β-Hydroxybutyryl-leucine pseudo-dipeptide
[0123] (1) Preparation of intermediate tert-butyldimethylsilyl ether β-hydroxybutyric acid
[0124] synthetic route:
[0125]
[0126]Ethyl β-hydroxybutyrate (132g, 1mol) and imidazole (136g, 2mol) were dissolved in 200mL of dichloromethane, cooled to 0-5°C, tert-butyldimethylsilyl chloride (195.8g, 1.3mol) was dissolved in 200 mL of dichloromethane was added dropwise into the reaction solution. After the dropwise addition, the ice bath was removed, and the reaction was carried out overnight at room temperature. After the gas chromatography monitors that the reaction is complete, add water to quench the reaction. After liquid separation, the organic phase is washed once with 50mL of 0.1M dilute hydrochloric acid and 50mL of saturated sodium chloride aqueous solution, and dried and concentrated to obtain tert-butyldimethylsilyl ether β-hydroxyl Crude ethyl butyrate. Add 2 times the volume of ethanol to the protected crude...
[0137] The synthetic route can refer to the synthetic route of Example A1, which is prepared from the intermediate tert-butyldimethylsiloxane β-hydroxybutyric acid and ethyl phenylalanine hydrochloride, with a yield of 67.8%.
[0142] The synthetic route can refer to the synthetic route of Example A1, which is prepared from the intermediate tert-butyldimethylsilyl ether β-hydroxybutyric acid and isoleucine ethyl ester hydrochloride, with a yield of 62.8%.
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 the technical field of compounds, in particular to a beta-hydroxyl butyryl-amino acid compound, a preparing method and application. The compound comprises compounds with the structural formulas shown in the formulas I, II, III, IV, V, VI, VII, VIII, IX and X, pharmaceutically-accepted salts or solvates of the compounds and pharmaceutically-accepted esterification products.Through rat experiments, cell experiments and safety evaluation, it is proved that the compound can be metabolized into BHB, amino acids and pseudopeptide metabolites in a human body, has an in-vivometabolism time half-life period of 4-6 hours, is safe and free of toxin and side effects, has high stability and certain anti-cancer activity (commonly 30-80 for esophageal cancer cell lines IC50), has good functions for reducing weight, resisting ageing, treating Alzheimer's disease and epilepsy and reducing blood fat and blood pressure, and is expected to become a novel food material for supplementing energy and being developed into different healthcare foods or pharmaceutically-accepted OTC medicines.
Description
technical field [0001] The invention relates to the technical field of compounds, in particular to a β-hydroxybutyryl-amino acid compound and its preparation method and application. Background technique [0002] In recent years, the development of pharmaceutical science has shown a rapid development in the direction of improving the body's own immunity and using the body's own immunity to treat various diseases. The research on endogenous substances, such as amino acids, small molecule active peptides, polypeptides etc. have become one of the mainstream and hot spots in the development of pharmaceutical science. The research on the medicinalization of endogenous substances is in the ascendant and developing in depth. The progress and breakthroughs in this area not only directly promote the industry of new drugs and new health care products, but also have important significance for the study of the material basis of human life and the code of life activities. [0003] β-hyd...
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.