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1. 发明申请

US20120178919A1 RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF 审中-公开
标题翻译：放射性核苷类似物及其制备方法及其用途
公开(公告)号：US20120178919A1
公开(公告)日：2012-07-12
申请号：US13194247
申请日：2011-07-29
申请人： HSIN-ELL WANG , CHIH-YUAN LIN , WEI-TI KUO , CHUAN-LIN CHEN , MEI-HUI WANG , HUNG-MAN YU , MAO-CHI WENG , YU CHANG , WUU-JYH LIN
发明人： HSIN-ELL WANG , CHIH-YUAN LIN , WEI-TI KUO , CHUAN-LIN CHEN , MEI-HUI WANG , HUNG-MAN YU , MAO-CHI WENG , YU CHANG , WUU-JYH LIN
IPC分类号： C07H19/067 , C07H19/09 , C07H19/073
CPC分类号： C07H19/067 , C07B59/005 , C07H19/073 , C07H19/09
摘要： A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.
摘要翻译：提供放射性标记的核苷类似物，其包括放射性碘123I / 131I和选自胞苷，胸苷，尿苷及其衍生物的核苷类似物。还提供了制备放射性标记的核苷类似物的方法及其用途。通过制备方法制备的核苷类似物，具有短的合成时间和高放射化学产率，具有长的体内生理半衰期和高血清稳定性，作为放射性药物组合物，可用于肿瘤增生诊断的发展或治疗预后评估，进一步有助于观察药物的长时间体内代谢。

2. 发明申请

US20140046045A1 METHOD FOR PREPARING PRECURSOR USED FOR LABELING HEPATOCYTE RECEPTOR AND CONTAINING TRISACCHARIDE AND DTPA LIGAND 有权
标题翻译：制备用于标记肝细胞受体和含有TRISACCHARIDE和DTPA配体的前体的方法
公开(公告)号：US20140046045A1
公开(公告)日：2014-02-13
申请号：US13571731
申请日：2012-08-10
申请人： CHIH-YUAN LIN , YU CHANG , JEN-TSUNG WANG , CHENG-FANG HSU , WEI-TI KUO , HUNG-WEN YU , WUU-JYH LIN , MEI-HUI WANG
发明人： CHIH-YUAN LIN , YU CHANG , JEN-TSUNG WANG , CHENG-FANG HSU , WEI-TI KUO , HUNG-WEN YU , WUU-JYH LIN , MEI-HUI WANG
IPC分类号： C07H15/04 , C07H1/06
CPC分类号： C07H1/06 , C07H15/04 , C07K1/13
摘要： A method for preparing a precursor used to label hepatocyte receptors is revealed. The precursor contains a bifunctional structure including trisaccharide and DTPA ligand. During synthesis processes of the precursor, silica gel columns and Reverse phase-18 (RP-18) columns are used for purification. Thus both the purification times and cost of each purification are reduced. Moreover, use diethyl ether to facilitate precipitation of products and remove a part of coupling reagent. Removing the coupling reagent helps purification of products. Furthermore, Nα,Nα-bis(carboxymethyl)-L-lysine hydrate and benzyl chloroformate are coupled to form a trisaccharide skeleton so as to ensure the yield rate of trisaccharide structure.
摘要翻译：揭示了制备用于标记肝细胞受体的前体的方法。该前体含有包括三糖和DTPA配体的双功能结构。在前体的合成过程中，使用硅胶柱和反相18（RP-18）柱进行纯化。因此，每次纯化的纯化时间和成本均降低。此外，使用乙醚促进产物沉淀并除去一部分偶联剂。去除偶联剂有助于净化产品。此外，Nalpha，Nalpha-双（羧甲基）-L-赖氨酸水合物和氯甲酸苄酯偶联形成三糖骨架，以确保三糖结构的产率。

3. 发明申请

US20110077386A1 NOVEL LIVER-TARGETING AGENTS AND THEIR SYNTHESIS 有权
标题翻译：新型肝脏靶向药物及其合成
公开(公告)号：US20110077386A1
公开(公告)日：2011-03-31
申请号：US12891004
申请日：2010-09-27
申请人： REIKO TAKASAKA LEE , YUAN-CHUAN LEE , MEI-HUI WANG , WUU-JYH LIN
发明人： REIKO TAKASAKA LEE , YUAN-CHUAN LEE , MEI-HUI WANG , WUU-JYH LIN
IPC分类号： C07H15/02 , C07C229/02
CPC分类号： C07H15/04
摘要： This invention provides novel liver targeting agents and their synthetic methods. A liver targeting agent, with a lysine based nitrilo triacetic acid structure as backbone which acquires multivalency with saccharide groups, to bind with a galactosamine chain or lactose chain is disclosed. In particular, only one amino acid L-lysine is involved to provide trivalency. All carboxyl groups in Nε-benzyloxycarbonyl-Nα-dicarboxymethyl-L-lysine can be conjugated with three glycosides of ahGalNAc or ahLac in one step. This invention also provides a hexa-lactoside. In particular, the TFA-AHA-Asp was used to conjugate 2 moles of NTA(ahLac)3. This invention also provides a method for adding a spacer between NTA and DTPA. The extended hepatocyte-specific glyco-ligand has higher 111In-radiolabelling yield than those non-extended.
摘要翻译：本发明提供新型肝靶向剂及其合成方法。公开了以赖氨酸为基础的三乙酸结构作为骨架的肝靶向剂，其以糖基取代多价，与半乳糖胺链或乳糖链结合。特别地，仅涉及一个氨基酸L-赖氨酸以提供三价值。 N，N-苄氧羰基-Nα-二羧甲基-L-赖氨酸中的所有羧基可以在一个步骤中与αGalNAc或ahLac的三种糖苷缀合。本发明还提供了六乳糖苷。特别地，TFA-AHA-Asp用于缀合2摩尔NTA（ahLac）3。本发明还提供了一种在NTA和DTPA之间添加间隔物的方法。延长的肝细胞特异性糖配体比未延长的肝细胞特异性糖配体具有更高的111In-放射性标记产率。

4. 发明申请

US20090108018A1 Automated Dispenser for Radiopharmaceuticals 有权
标题翻译：放射性药物自动分配器
公开(公告)号：US20090108018A1
公开(公告)日：2009-04-30
申请号：US11868540
申请日：2007-10-08
申请人： MING-HSIN LI , WUU-JYH LIN , TAIN-SHI ZEN
发明人： MING-HSIN LI , WUU-JYH LIN , TAIN-SHI ZEN
IPC分类号： B23Q7/12
CPC分类号： A61J1/2096 , B65B3/003 , G21G1/0005
摘要： An automated dispenser for radiopharmaceuticals is mainly for a platform to have a moving mechanism being able to move three-dimensionally back and forth, a syringe holder and a bottle holder. The syringe holder is for holding a plural number of syringes. The bottle holder has a reverse drug bottle. The moving mechanism has a syringe clamp rotatable around a horizontal axis and a syringe driving mechanism. The syringe clamp is activated to hold a syringe and move it to where the syringe needle is inserted to the drug bottle. The syringe driving mechanism and the syringe clamp are simultaneously associated with the syringe for drug-withdrawing action.
摘要翻译：用于放射性药物的自动分配器主要用于具有能够三维来回移动的移动机构的平台，注射器保持器和瓶保持器。注射器支架用于容纳多个注射器。瓶架有一个反向药瓶。移动机构具有可绕水平轴线旋转的注射器夹具和注射器驱动机构。注射器夹具被启动以保持注射器并将其移动到注射器针头插入药瓶的位置。注射器驱动机构和注射器夹具同时与注射器相关联用于吸药动作。

5. 发明申请

US20100310428A1 Synthetic method and automation device for fluorine-18-ACETATE 有权
标题翻译：氟-18-ACETATE的合成方法和自动化装置
公开(公告)号：US20100310428A1
公开(公告)日：2010-12-09
申请号：US12478787
申请日：2009-06-05
申请人： MING-HSIN LI , HSIN-EII WANG , CHUN-YI WU , WUU-JYH LIN
发明人： MING-HSIN LI , HSIN-EII WANG , CHUN-YI WU , WUU-JYH LIN
IPC分类号： G05D16/00 , B01J19/00 , G05B11/00
CPC分类号： B01J19/004
摘要： An automatic synthesis device for fluorine-18-ACETATE ([18F]fluoroacetate) consists of a machinery housing that has multiple reactors and multiple raw material containers, and uses multiple control valves between each reactor and container, and operates the control valves through a control system to charge the raw material from each container to each reactor in an automatic and sequential fashion to execute the six procedures: fluorination, azeotropic dewatering, synthesis (reaction with precursors), purification and separation, hydrolysis and neutralization, purification and collection. The operation simply requires adding raw materials to the containers in advance, turning on power, charging reactive gases. In 50 minutes, the process to produce the product will be completed. The operation is really simple and can effectively improve production efficiency.
摘要翻译：用于氟-18-乙酸酯（[18 F]氟乙酸酯）的自动合成装置由具有多个反应器和多个原料容器的机械壳体组成，并且在每个反应器和容器之间使用多个控制阀，并通过控制器操作控制阀系统，以自动和连续的方式从每个容器向每个反应器充填原料，以执行氟化，共沸脱水，合成（与前体反应），纯化和分离，水解和中和，纯化和收集的六个步骤。该操作只需要事先向容器中加入原料，打开电源，充入反应气体。 50分钟内，生产产品的过程即将完成。操作非常简单，可以有效提高生产效率。

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