Polyselenoamino acid amphiphilic block copolymer targeting glucose transporter 1 as well as preparation method and application thereof
An amphiphilic block, selenoamino acid technology, which is used in medical preparations, metabolic diseases, drug combinations, etc. of inactive ingredients, which can solve the problem of difficult control of degradation rate and cycle, poor water solubility, and difficult to achieve targeted delivery, etc. To achieve the effect of reducing toxic and side effects, reducing the frequency of administration, and improving the therapeutic effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0131] Glycosylated polyethylene glycol amine (GLU-PEG n -NH 2 )Synthesis
[0132] Take 100mg BocNH-PEG n -COOH (0.05mmol, Mn=2000) was dissolved in 5mL of DMF solution, 13mg of DCC and 9mg of NHS were added in sequence, and stirred overnight at room temperature to remove by-products to obtain BocNH-PEG activated at the carboxy-terminus n -COOH. 15mg Glucoaniline (Glu-NH 2 ) was dissolved in 1mL ultra-dry DMF solution, stirred for 5 minutes, added triethylamine, stirred for 15 minutes, and added dropwise to carboxy-terminally activated BocNH-PEG n -COOH solution, react at room temperature for 12h. After the reaction, the reaction solution was dropped dropwise into vigorously stirred anhydrous ether, centrifuged to obtain a yellow crude product, which was dissolved in THF again, precipitated with anhydrous ether, centrifuged, and finally vacuum-dried at room temperature Overnight, get Glu-PEG n -NH-Boc. 1mg Glu-PEG n -NH-Boc was dissolved in 5 mL of trifluoroacetic aci...
Embodiment 2
[0137] Glycosylated polyethylene glycol polyaspartic acid polyselenomethionine block copolymer (Glu-PEG 45 -PAsp2-PMet(Se) 2 ) of synthetic weighing 0.1g tBu-PEG 45 -NH 2 (0.05mmol, Mn=2000) was vacuum-dried in a vacuum oven for 4 hours, and then dissolved in 3ml of dried DMF as a macroinitiator. Weigh 25mg of newly prepared benzyl L-aspartate NCA (BLA-NCA) (0.1mmol) and dissolve it in 1ml of ultra-dry DMF, then mix the two reaction solutions with a syringe, place under nitrogen atmosphere, and stir the reaction 24h. After the reaction, 22.3 mg of newly prepared seleno-L-methionine NCA (0.1 mmol) was weighed and dissolved in 1 ml of ultra-dry DMF, added to the above mixed reaction solution, and the reaction was continued with stirring. After 24 hours, the reaction was complete. The three-block polymer was settled in ice anhydrous isopropyl ether, centrifuged, and dried in a vacuum oven for 24 hours to obtain the product tert-butyl acetate polyethylene glycol polyaspartic ...
Embodiment 3
[0139] Glycosylated polyethylene glycol polyaspartic acid polyselenomethionine block copolymer (Glu-PEG 45 -PAsp 2 -PMet(Se) 4 )Synthesis
[0140] Weigh 0.1g tBu-PEG-NH 2 (0.05 mmol, Mn=2000) was vacuum-dried in a vacuum oven for 4 hours, and then dissolved in 3 ml of dried DMF to be used as a macroinitiator. Weigh 25 mg of newly prepared L-benzyl-aspartate NCA (0.1 mmol) and dissolve it in 1 ml of ultra-dry DMF, then mix the two reaction solutions with a syringe, place under nitrogen atmosphere, and stir for 24 h. After the reaction, 44.6 mg of newly prepared seleno-L-methionine NCA (0.2 mmol) was weighed and dissolved in 1 ml of ultra-dry DMF, added to the above mixed reaction solution, and the reaction was continued with stirring. After 24 hours, the reaction was complete. The three-block polymer was settled in ice anhydrous isopropyl ether, centrifuged, and dried in a vacuum oven for 24 hours to obtain the product tert-butyl acetate polyethylene glycol polyaspartic ac...
PUM
Property | Measurement | Unit |
---|---|---|
particle diameter | aaaaa | aaaaa |
particle diameter | aaaaa | aaaaa |
particle diameter | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.
© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com