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经修饰的间隙子寡核苷酸及其使用方法

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摘要

本公开包含反义寡核苷酸，包含间隙子反义寡核苷酸；以及制备和使用方法，例如针对HBV。

著录项

公开/公告号CN113905744A

专利类型发明专利
公开/公告日2022-01-07

原文格式PDF
申请/专利权人阿利戈斯治疗公司;
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申请/专利号CN202080039766.4
发明设计人 L·贝格尔曼;R·K·潘迪;V·K·拉杰万什;D·B·史密斯;洪劲;
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申请日2020-05-29
分类号A61K31/7088(20060101);A61K31/7125(20060101);A61P31/20(20060101);C12N15/113(20100101);C12N15/86(20060101);C12N15/11(20060101);
代理机构11494 北京坤瑞律师事务所;
代理人封新琴
地址美国加利福尼亚州
入库时间 2023-06-19 13:33:57

法律信息

法律状态公告日

法律状态信息

法律状态
2022-06-17

实质审查的生效 IPC(主分类):A61K31/7088 专利申请号:2020800397664 申请日:20200529

实质审查的生效

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1. 经修饰的间隙子寡核苷酸及其使用方法 [P] . 中国专利： CN113905744A . 2022-01-07
2. 脂质修饰的寡核苷酸及其使用方法 [P] . 中国专利： CN114127306A . 2022-03-01
3. A compound comprising a modified oligonucleotide with a nucleobase sequence consisting of 20 linked nucleosides according to EP-B1-2563920 claim 1 (SEQ ID NO: 80), wherein the modified oligonucleotide comprises: a gap segment consisting of ten linked deoxynucleosides; a 5 'wing segment consisting of five linked nucleosides; and a 3 'wing segment consisting of five linked nucleosides; wherein the gap segment is positioned between the 5 'wing segment and the 3' wing segment, wherein each nucleoside of each wing segment comprises a 2'-O-methoxyethyl sugar; wherein each cytosine of the modified oligonucleotide is a 5-methyl cytosine, and wherein each internucleoside linkage of the modified oligonucleotide is a phosphorothioate linkage; and in particular inotersen; and derivatives thereof, such as salts thereof, including sodium salts, as protected by EP-B1-2563920. [P] . NL300963I9 . 2019-01-16

机译： 6.一种化合物，其包含具有根据20的EP-B1-2563920（SEQ ID NO：80）的具有由20个连接的核苷组成的核碱基序列的修饰的寡核苷酸，其中所述修饰的寡核苷酸包含：由十个连接的脱氧核苷组成的缺口片段;和由五个连接的核苷组成的5'翼区段; 3'翼段由五个连接的核苷组成;其中所述间隙片段位于5'侧翼片段和3'侧翼片段之间，其中每个侧翼片段的每个核苷包含2'-O-甲氧基乙基糖;其中修饰的寡核苷酸的每个胞嘧啶是5-甲基胞嘧啶，并且其中修饰的寡核苷酸的每个核苷间键是硫代磷酸酯键;特别是inotersen;及其衍生物，例如由EP-B1-2563920保护的其盐，包括钠盐。
4. A compound comprising a modified oligonucleotide with a nucleobase sequence consisting of 20 linked nucleosides according to EP-B1-2563920 claim 1 (SEQ ID NO: 80), wherein the modified oligonucleotide comprises: a gap segment consisting of ten linked deoxynucleosides; a 5 'wing segment consisting of five linked nucleosides; and a 3 'wing segment consisting of five linked nucleosides; wherein the gap segment is positioned between the 5 'wing segment and the 3' wing segment, wherein each nucleoside of each wing segment comprises a 2'-O-methoxyethyl sugar; wherein each cytosine of the modified oligonucleotide is a 5-methyl cytosine, and wherein each internucleoside linkage of the modified oligonucleotide is a phosphorothioate linkage; and in particular inotersen; and derivatives thereof, such as salts thereof, including sodium salts, as protected by EP-B1-2563920. [P] . NL300963I1 . 2019-01-08

机译： 6.一种化合物，其包含具有根据20的EP-B1-2563920（SEQ ID NO：80）的具有由20个连接的核苷组成的核碱基序列的修饰的寡核苷酸，其中所述修饰的寡核苷酸包含：由十个连接的脱氧核苷组成的缺口片段;和由五个连接的核苷组成的5'翼区段; 3'翼段由五个连接的核苷组成;其中所述间隙片段位于5'侧翼片段和3'侧翼片段之间，其中每个侧翼片段的每个核苷包含2'-O-甲氧基乙基糖;其中修饰的寡核苷酸的每个胞嘧啶是5-甲基胞嘧啶，并且其中修饰的寡核苷酸的每个核苷间键是硫代磷酸酯键;特别是inotersen;及其衍生物，例如由EP-B1-2563920保护的其盐，包括钠盐。
5. compound consisting of a modified oligonucleotide composed of 12-30 linked nucleosides, compounds comprising a modified oligonucleotide comprising at least 12 linked nucleosides, compound comprising a modified oligonucleotide comprising linked nucleosides, and use of a compound [P] . BRPI0912923A2 . 2017-10-10

机译：化合物，其包含由12-30个连接的核苷组成的修饰寡核苷酸，包含包含至少12个连接的核苷的修饰寡核苷酸的化合物，包含包含连接的核苷的修饰寡核苷酸的化合物以及该化合物的用途