A modified nucleoside compound and oligonucleotides made therefrom
CN122122164APending Publication Date: 2026-05-29CHENGDU BETERIMA BIOMEDICAL TECHNOLOGY CO LTD +1
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- CHENGDU BETERIMA BIOMEDICAL TECHNOLOGY CO LTD
- Filing Date
- 2024-09-25
- Publication Date
- 2026-05-29
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.
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Abstract
A nucleoside phosphoramidite compound, the compound being a 2'-phosphoramidite group, 4'-modified TNA structured compound. The nucleoside phosphoramidite compound can be used to incorporate into the first and / or last and / or intermediate of an oligonucleotide such that the modified oligonucleotide hybridizes to a portion of a target mRNA, thereby causing a loss or down-regulation of normal function of the target mRNA.
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