发明申请
WO1996014329A1 SUGAR MODIFIED NUCLEOSIDES AND THEIR USE FOR SYNTHESIS OF OLIGONUCLEOTIDES
审中-公开
基本信息:
- 专利标题： SUGAR MODIFIED NUCLEOSIDES AND THEIR USE FOR SYNTHESIS OF OLIGONUCLEOTIDES
- 专利标题（中）：糖改性核苷酸及其用于合成寡核苷酸的用途
- 申请号：PCT/US1995014600 申请日：1995-11-02
- 公开(公告)号：WO1996014329A1 公开(公告)日：1996-05-17
- 发明人： ICN PHARMACEUTICALS
- 申请人： ICN PHARMACEUTICALS , WANG, Guangyi , RAMASAMY, Kandasamy , SEIFERT, Wilfried
- 专利权人： ICN PHARMACEUTICALS,WANG, Guangyi,RAMASAMY, Kandasamy,SEIFERT, Wilfried
- 当前专利权人： ICN PHARMACEUTICALS,WANG, Guangyi,RAMASAMY, Kandasamy,SEIFERT, Wilfried
- 优先权： US8/333,545 19941102
- 主分类号： C07H19/06
- IPC分类号： C07H19/06
摘要：
A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and them converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one of the forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.
摘要（中）：
公开了一些修饰的核苷，其由在C1和C4位置含有取代基的修饰的糖部分或脱氧核糖或核糖的C3和C5位置的支链取代基组成。 将每个核苷转化为或适当保护，并将其转化为相应的亚磷酰胺。 这些亚磷酰胺用于组装寡核苷酸，其中存在至少一种预先注入的核苷。 这些糖修饰的寡核苷酸具有用作反义治疗的潜力，因为预期它们在体外或体内保持对核酸靶标的序列特异性和亲和力，从而增强核酸酶抗性和细胞摄取。
IPC结构图谱:
| C | 化学；冶金 |
| --C07 | 有机化学 |
| ----C07H | 糖类；及其衍生物；核苷；核苷酸；核酸 |
| ------C07H19/00 | 含有杂环与糖化物基团共有1个杂环原子的化合物；核苷；单核苷酸类；及其脱水衍生物 |
| --------C07H19/02 | .共有氮 |
| ----------C07H19/04 | ..仅含有氮作为杂环原子的杂环基 |
| ------------C07H19/06 | ...嘧啶基 |