Modified nucleoside compound, and oligonucleotide prepared therefrom
By introducing 2’, 3’-phosphate-linked nucleotides into the oligonucleotide, the problem of insufficient bioavailability and pharmacokinetic characteristics of existing oligonucleotide drugs is solved, and the purpose of improving activity, enzyme cleavage resistance and targeting effect is achieved.
WO2025067240A1 Publication Date: 2025-04-03CHENGDU BRILLIANT PHARMA CO LTD
12 Cites 4 Cited by
Patent Information
- Application Number
- PCT/CN2024/121099
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-09-25
- Filing Date
- 2024-09-25
- Publication Date
- 2025-04-03
AI Technical Summary
Technical Problem
The bioavailability and pharmacokinetic properties of existing oligonucleotide drugs in vivo are insufficient, making it difficult to effectively regulate target mRNA expression.
Method used
A modified nucleoside compound is developed to improve its activity and enzyme resistance by introducing 2’, 3’-phosphate-linked nucleotides (4’-modified TNAs) into the oligonucleotides, as well as improve cell membrane penetration and organ targeting.
Benefits of technology
It improves the activity and enzyme cleavage resistance of oligonucleotides, enhances its enrichment degree and pharmacokinetic properties in the target organ, and improves bioavailability and efficacy.
✦ Generated by Eureka AI based on patent content.
Abstract
A nucleoside phosphoramidite compound, which is a 2'-phosphoramidite group and 4'-modified TNA structure compound. The nucleoside phosphoramidite compound can be incorporated into the end and / or middle of an oligonucleotide, so that the modified oligonucleotide is hybridized with a portion of a target mRNA, resulting in the loss or down-regulation of the normal function of the target mRNA.
Need to check novelty before this filing date? Find Prior Art