
基本信息:
- 专利标题: Drug Transfer into Living Cells
- 专利标题(中):药物转移到活细胞中
- 申请号:US12681442 申请日:2008-10-02
- 公开(公告)号:US20110014196A1 公开(公告)日:2011-01-20
- 发明人: Andreas Brecht , Florent Beaufils
- 申请人: Andreas Brecht , Florent Beaufils
- 申请人地址: CH Witterswil
- 专利权人: COVALYS BIOSCIENCES AG
- 当前专利权人: COVALYS BIOSCIENCES AG
- 当前专利权人地址: CH Witterswil
- 优先权: EP07117800.8 20071003; EP08104709.4 20080710
- 国际申请: PCT/EP08/63205 WO 20081002
- 主分类号: A61K39/395
- IPC分类号: A61K39/395 ; C12N9/10 ; A61P35/00 ; C07D473/18 ; C07H21/02 ; C07H19/167 ; A61K31/713 ; A61K31/522 ; A61K31/7076 ; A61K31/538 ; A61K38/45
摘要:
The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.
摘要(中):
本发明涉及包含适当连接并进一步携带一个或多个货物实体的多个酶底物的化合物。 特别地,这样的化合物具有结构(底物)正接头(货物)m,其中“底物”是酶型蛋白质特异的底物; n为2以上; “接头”是由1至300个原子组成的连接单元; “货物”是一种药物,可由荧光检测器检测的标记物,磁共振成像(MRI),正电子发射断层扫描(PET)或闪烁扫描法,或可转化为药物或可检测标签的官能团; m为1以上。 本发明还涉及具有结构(融合蛋白)正连接体(货物)m的相应分子梭子,其中“融合蛋白”是与特定底物存在的酶型蛋白质融合的蛋白质结合实体。 蛋白质结合实体被设计为在体外或体内结合靶结构,例如细胞受体。
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K39/00 | 含有抗原或抗体的医药配制品 |
--------A61K39/395 | .抗体;免疫球蛋白;免疫血清,例如抗淋巴细胞血清 |