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1. 发明申请

WO2012160450A2 MODULAR TRANSPORT PLATFORM FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于定向递送治疗药物的模块化运输平台
公开(公告)号：WO2012160450A2
公开(公告)日：2012-11-29
申请号：PCT/IB2012/050624
申请日：2012-02-13
申请人： CONTANGO PARTNERS GROUP, INC. , SOBOLEV, Alexander, S. , ROSENKRANZ, Audrey, A. , JANS, David, A. , LUNIN, Vladimir, G.
发明人： SOBOLEV, Alexander, S. , ROSENKRANZ, Audrey, A. , JANS, David, A. , LUNIN, Vladimir, G.
CPC分类号： A61K47/48269 , A61K41/0071 , A61K47/6415 , A61K47/642 , A61K47/6445 , A61K51/081 , A61K51/088
摘要： The invention relates to a modular transport platform (MTP) for delivering active, diagnostic or research substances to predesigned intracellular compartments of target cells. The MTP includes functional modules within one molecule to accomplish one or more of the following: penetration of the modular transport platform into a target cell type, pH-dependent membrane disruption activity within the target cell, directed intracellular transport into preselected intracellular compartment, and delivery of a substance to be transported to the intracellular compartment. The modular transport platform includes the following modules: (1) a ligand module to target a specific receptor on the surface of the target cell; (2) an endosomolytic module that provides pH-dependent membrane disruption activity within the target cell; (3) an intracellular transport module to cause delivery of the MTP to a particular subcellular compartment; (4) a module for intracellular retention to ensure retention of the MTP within the subcellular compartment of the target cell; (5) a module for subcellular recognition; (6) a substance to be transported by the MTP; and (7) a carrier module for unifying the modules and coupling the modules with the transported substance.
摘要翻译：本发明涉及用于将活性，诊断或研究物质递送到靶细胞的预先设计的细胞内区室的模块化转运平台（MTP）。 MTP包括一个分子内的功能模块，以实现以下一个或多个：模块化传输平台渗透到靶细胞类型中，靶细胞内的pH依赖性膜破坏活性，定向细胞内转运到预选的细胞内区室和递送的物质被运送到细胞内隔室。模块化运输平台包括以下模块：（1）靶靶细胞表面上特定受体的配体模块; （2）在靶细胞内提供pH依赖性膜破坏活性的内体分解模块; （3）细胞内转运模块，以使MTP递送至特定的亚细胞室; （4）用于细胞内保留的模块以确保MTP在靶细胞的亚细胞间隔内的保留; （5）用于亚细胞识别的模块; （六）中期计划运输的物质; 和（7）用于统一模块并将模块与输送的物质耦合的载体模块。

2. 发明申请

WO2012160450A3 MODULAR TRANSPORT PLATFORM FOR TARGETED DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于定向递送治疗药物的模块化运输平台
公开(公告)号：WO2012160450A3
公开(公告)日：2013-01-17
申请号：PCT/IB2012050624
申请日：2012-02-13
申请人： CONTANGO PARTNERS GROUP INC , SOBOLEV ALEXANDER S , ROSENKRANZ AUDREY A , JANS DAVID A , LUNIN VLADIMIR G
发明人： SOBOLEV ALEXANDER S , ROSENKRANZ AUDREY A , JANS DAVID A , LUNIN VLADIMIR G
IPC分类号： A61K47/48 , A61K41/00 , A61K51/08 , A61P35/00
CPC分类号： A61K47/48269 , A61K41/0071 , A61K47/6415 , A61K47/642 , A61K47/6445 , A61K51/081 , A61K51/088
摘要： The invention relates to a modular transport platform (MTP) for delivering active, diagnostic or research substances to predesigned intracellular compartments of target cells. The MTP includes functional modules within one molecule to accomplish one or more of the following: penetration of the modular transport platform into a target cell type, pH-dependent membrane disruption activity within the target cell, directed intracellular transport into preselected intracellular compartment, and delivery of a substance to be transported to the intracellular compartment. The modular transport platform includes the following modules: (1) a ligand module to target a specific receptor on the surface of the target cell; (2) an endosomolytic module that provides pH-dependent membrane disruption activity within the target cell; (3) an intracellular transport module to cause delivery of the MTP to a particular subcellular compartment; (4) a module for intracellular retention to ensure retention of the MTP within the subcellular compartment of the target cell; (5) a module for subcellular recognition; (6) a substance to be transported by the MTP; and (7) a carrier module for unifying the modules and coupling the modules with the transported substance.
摘要翻译：本发明涉及用于将活性，诊断或研究物质递送到靶细胞的预先设计的细胞内区室的模块化转运平台（MTP）。 MTP包括一个分子内的功能模块，以实现以下一个或多个：模块化传输平台渗透到靶细胞类型中，靶细胞内的pH依赖性膜破坏活性，定向细胞内转运到预选的细胞内区室和递送的物质被运送到细胞内隔室。模块化运输平台包括以下模块：（1）靶靶细胞表面上特定受体的配体模块; （2）在靶细胞内提供pH依赖性膜破坏活性的内体分解模块; （3）细胞内转运模块，以使MTP递送至特定的亚细胞室; （4）用于细胞内保留的模块以确保MTP在靶细胞的亚细胞间隔内的保留; （5）用于亚细胞识别的模块; （六）中期计划运输的物质; 和（7）用于统一模块并将模块与输送的物质耦合的载体模块。

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