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1. 发明申请

US20050137421A1 Method for making fluorine labled L-Dopa 有权
标题翻译：制造氟化合物的方法
公开(公告)号：US20050137421A1
公开(公告)日：2005-06-23
申请号：US10742023
申请日：2003-12-19
申请人： Joseph Walsh , Henry Padgett
发明人： Joseph Walsh , Henry Padgett
IPC分类号： C07C227/32 , C07C229/36 , C07C269/06 , C07C271/22
CPC分类号： C07C271/22 , C07B2200/05 , C07B2200/07 , C07C227/32 , C07C229/36 , C07C269/06
摘要： The invention relates to a method for preparing F-Dopa and 18F-Dopa and intermediates that are useful in the method. The invention is a method that synthesizes F-Dopa and 18F-Dopa in good yield with high enantiopurity without the need for further transformations. The method includes the step of reacting a benzaldehyde derivative with a phosphonic acid derivative to produces an olefin intermediate that can be asymmetrically hydrogenated to produce the desired enantiomer.
摘要翻译：本发明涉及一种制备在该方法中有用的F-多巴和十八氟多卡因和中间体的方法。本发明是以高的对映体纯度合成F-Dopa和16 F-多巴的方法，而不需要进一步的转化。该方法包括使苯甲醛衍生物与膦酸衍生物反应以产生不对称氢化以产生所需对映异构体的烯烃中间体的步骤。

2. 发明申请

US20070077198A1 Method for preparing radiolabeled thymidine having low chromophoric byproducts 有权
公开(公告)号：US20070077198A1
公开(公告)日：2007-04-05
申请号：US11603703
申请日：2006-11-22
申请人： Joseph Walsh , Henry Padgett , Tanea Ysaguirre
发明人： Joseph Walsh , Henry Padgett , Tanea Ysaguirre
IPC分类号： A61K51/00 , C07H19/12
CPC分类号： A61K51/0491 , C07H19/048 , Y02P20/55
摘要： The invention is a method and related precursor for preparing 18F-FLT. The precursor has a butoxycarbonyl protecting group at the 5′-position that results in low amounts of chromophoric byproducts being formed during deprotection. The method for preparing 18F-FLT is efficient and makes the final purification step less complicated.

3. 发明申请

US20050131224A1 Method for preparing radiolabeled thymidine 审中-公开
标题翻译：制备放射性标记的胸苷的方法
公开(公告)号：US20050131224A1
公开(公告)日：2005-06-16
申请号：US10736084
申请日：2003-12-15
申请人： Joseph Walsh , Henry Padgett
发明人： Joseph Walsh , Henry Padgett
IPC分类号： A61K20060101 , A61K31/70 , C07H19/06
CPC分类号： C07H19/06
摘要： The invention is a novel method and precursor for preparing radiolabeled nucleosides. In particular, the invention is useful for preparing 3′-[18F]fluorothymidine. The method uses an enol group that is attached to the 2-position on the pyrimidine ring. The enol group attenuates thymidines activity so that the thymidine is easily radiolabeled in short number of steps with good yield.
摘要翻译：本发明是制备放射性标记核苷的新方法和前体。特别地，本发明可用于制备3' - [[18 F]氟胸苷。该方法使用连接在嘧啶环上2位上的烯醇基团。烯醇基团减少胸腺嘧啶的活性，使得胸苷容易以短的步骤以良好的产率放射标记。

4. 发明申请

US20050131223A1 Method for preparing radiolabeled thymidine having low chromophoric byproducts 有权
标题翻译：制备具有低发色副产物的放射性标记的胸苷的方法
公开(公告)号：US20050131223A1
公开(公告)日：2005-06-16
申请号：US10736087
申请日：2003-12-15
申请人： Joseph Walsh , Henry Padgett , Tanea Ysaguirre
发明人： Joseph Walsh , Henry Padgett , Tanea Ysaguirre
IPC分类号： A61K20060101 , A61K51/00 , A61K51/04 , A61M36/14 , C07H19/048
CPC分类号： A61K51/0491 , C07H19/048 , Y02P20/55
摘要： The invention is a method and related precursor for preparing 18F-FLT. The precursor has a butoxycarbonyl protecting group at the 5′-position that results in low amounts of chromophoric byproducts being formed during deprotection. The method for preparing 18F-FLT is efficient and makes the final purification step less complicated.
摘要翻译：本发明是一种用于制备F-FL-FLT的方法和相关前体。该前体在5'-位具有丁氧羰基保护基，导致在脱保护期间形成少量的发色副产物。制备 F-FLT的方法是有效的，并且使得最终的纯化步骤不那么复杂。

5. 发明申请

US20050232861A1 Microfluidic apparatus and method for synthesis of molecular imaging probes including FDG 审中-公开
标题翻译：用于合成包括FDG的分子成像探针的微流体装置和方法
公开(公告)号：US20050232861A1
公开(公告)日：2005-10-20
申请号：US10827992
申请日：2004-04-20
申请人： Charles Buchanan , Henry Padgett , Thomas Collier
发明人： Charles Buchanan , Henry Padgett , Thomas Collier
IPC分类号： A61K51/00 , C07B59/00 , C07F5/00
CPC分类号： C07B59/00 , A61K51/0491 , C07B59/005 , C07B2200/05
摘要： The invention provides a method and apparatus for preparation of radiochemicals wherein the reaction that couples the radioactive isotope to the reactive precursor to form a positron-emitting molecular imaging probe is performed in a microfluidic environment. The method comprises: providing a micro reactor; introducing a liquid reactive precursor dissolved in a polar aprotic solvent into an inlet port of the micro reactor, the reactive precursor adapted for reaction with a radioactive isotope to form a radiochemical; introducing a solution comprising a radioactive isotope dissolved in a polar aprotic solvent into another inlet port of the micro reactor; contacting the reactive precursor with the isotope-containing solution in a microchannel of the micro reactor; reacting the reactive precursor with the isotope-containing solution as the reactive precursor and isotope-containing solution flow through the microchannel of the micro reactor, wherein the reacting step is conducted at a temperature above the boiling point of the polar aprotic solvent at 1 atm and at a pressure sufficient to maintain the polar aprotic solvent in liquid form; and collecting the resulting radiochemical from the micro reactor.
摘要翻译：本发明提供了一种用于制备放射化学物质的方法和装置，其中在微流体环境中进行将放射性同位素与反应性前体耦合以形成正电子发射分子成像探针的反应。该方法包括：提供微反应器; 将溶解在极性非质子溶剂中的液体反应性前体引入微反应器的入口端口，所述反应性前体适于与放射性同位素反应以形成放射化学物质; 将包含溶解在极性非质子溶剂中的放射性同位素的溶液引入微反应器的另一入口; 在微反应器的微通道中使反应性前体与含同位素的溶液接触; 使反应性前体与含有同位素的溶液反应，作为反应性前体，同位素溶液流过微反应器的微通道，其中反应步骤在高于大气压极性非质子传递溶剂沸点的温度下进行，在足以保持极性非质子溶剂为液体形式的压力下; 并从微反应器收集所得的放射化学物质。

6. 发明申请

US20050232387A1 Microfluidic apparatus and method for synthesis of molecular imaging probes 审中-公开
标题翻译：用于合成分子成像探针的微流控装置和方法
公开(公告)号：US20050232387A1
公开(公告)日：2005-10-20
申请号：US10827893
申请日：2004-04-20
申请人： Henry Padgett , Charles Buchanan , Thomas Collier , Joseph Matteo , Charles Alvord
发明人： Henry Padgett , Charles Buchanan , Thomas Collier , Joseph Matteo , Charles Alvord
IPC分类号： A61M36/14
CPC分类号： A61K51/0491
摘要： The invention provides a method and apparatus for preparation of radiochemicals, such as PET molecular imaging probes, wherein the reaction step or steps that couple the radioactive isotope to an organic or inorganic compound to form a positron-emitting molecular imaging probe are performed in a microfluidic environment. The method for synthesizing a radiochemical in a microfluidic environment comprises: i) providing a micro reactor comprising a first inlet port, a second inlet port, an outlet port, and at least one microchannel in fluid communication with the first and second inlet ports and the outlet port; ii) introducing a reactive precursor into the first inlet port of the micro reactor, the reactive precursor adapted for reaction with a radioactive isotope to form a radiochemical; iii) introducing a solution comprising a radioactive isotope into the second inlet port of the micro reactor; iv) contacting the reactive precursor with the isotope-containing solution in the microchannel of the micro reactor; v) reacting the reactive precursor with the isotope-containing solution as the reactive precursor and isotope-containing solution flow through the microchannel of the micro reactor, the reacting step resulting in formation of a radiochemical; and vi) collecting the radiochemical from the outlet port of the micro reactor.
摘要翻译：本发明提供了一种用于制备放射化学物质的方法和装置，例如PET分子成像探针，其中将放射性同位素与有机或无机化合物偶联以形成正电子发射分子成像探针的反应步骤或步骤在微流体环境。用于在微流体环境中合成放射化学的方法包括：i）提供微反应器，其包括与第一和第二入口端口流体连通的第一入口端口，第二入口端口，出口端口和至少一个微通道，出口口 ii）将反应性前体引入微反应器的第一入口，反应性前体适于与放射性同位素反应以形成放射化学物质; iii）将包含放射性同位素的溶液引入微反应器的第二入口; iv）使反应性前体与微反应器的微通道中的含同位素溶液接触; v）使反应性前体与含有同位素的溶液反应，作为反应性前体，并且含同位素的溶液流过微反应器的微通道，反应步骤导致形成放射化学; 和vi）从微反应器的出口收集放射化学物质。

7. 发明申请

US20130022525A1 METHODS AND COMPOSITIONS FOR DRYING IN THE PREPARATION OF RADIOPHARMACEUTICALS 审中-公开
标题翻译：用于干燥放射性核素制备的方法和组合物
公开(公告)号：US20130022525A1
公开(公告)日：2013-01-24
申请号：US13550188
申请日：2012-07-16
申请人： Dennis B. ESHIMA , Mehmet Husnu , Henry Padgett , Thomas A. Klausing , Chad E. Bouton , Herman Benecke , Daniel B. Garbark
发明人： Dennis B. ESHIMA , Mehmet Husnu , Henry Padgett , Thomas A. Klausing , Chad E. Bouton , Herman Benecke , Daniel B. Garbark
IPC分类号： C01B7/00 , C09K3/00
CPC分类号： C07B59/00
摘要： A method of drying a radioisotope solution having radioisotopes includes passing the radioisotope solution through a solid phase extraction column containing an anion exchange group, thereby trapping the radioisotopes in the column. The method also includes passing an eluent through the column, thereby removing the radioisotopes from the column. The eluent includes a cation trapping agent/salt complex, less than 4% water, and the remainder is a solvent. A method of producing the eluent includes reacting a cation trapping agent with a salt in the presence of less than 4% water and a solvent to form solubilized cation trapping agent/salt complex, wherein one of the cation trapping agent and the salt is present in en excess of a stoichiometric amount and ending the reaction when a predetermined amount of solubilized cation trapping agent/salt complex has been formed.
摘要翻译：干燥具有放射性同位素的放射性同位素溶液的方法包括使放射性同位素溶液通过含有阴离子交换基团的固相萃取塔，从而将放射性同位素捕集在柱中。该方法还包括使洗脱液通过柱，从而从柱中除去放射性同位素。洗脱液包括阳离子捕获剂/盐络合物，小于4％的水，其余为溶剂。制备洗脱液的方法包括在小于4％的水和溶剂的存在下使阳离子捕获剂与盐反应形成溶解的阳离子捕获剂/盐络合物，其中阳离子捕获剂和盐之一存在于超过化学计量量，并且当已经形成预定量的溶解的阳离子捕获剂/盐络合物时结束反应。

8. 发明申请

US20130102772A1 SYSTEMS, METHODS AND DEVICES FOR PRODUCING, MANUFACTURING AND CONTROL OF RADIOPHARMACEUTICALS-FULL 审中-公开
标题翻译：用于生产，制造和控制放射线照相的系统，方法和装置
公开(公告)号：US20130102772A1
公开(公告)日：2013-04-25
申请号：US13550425
申请日：2012-07-16
申请人： Dennis ESHIMA , Mehmet Husnu , Jim Stone , Derrick Alcaide , Henry Padgett , Joseph E. Zambanini , Thomas A. Klausing , Chad E. Bouton , Brian C. Kelley , Scott N. Danhof , David A. Holley , Jeffrey T. Stroup , James B. Gleeson , Eric Hassenpflug , James A. Prescott , Herman Benecke , Daniel B. Garbark
发明人： Dennis ESHIMA , Mehmet Husnu , Jim Stone , Derrick Alcaide , Henry Padgett , Joseph E. Zambanini , Thomas A. Klausing , Chad E. Bouton , Brian C. Kelley , Scott N. Danhof , David A. Holley , Jeffrey T. Stroup , James B. Gleeson , Eric Hassenpflug , James A. Prescott , Herman Benecke , Daniel B. Garbark
IPC分类号： B01J19/00 , B65B1/00
CPC分类号： B01J19/0006 , A61J3/002 , A61K51/0491 , B01J19/004 , B01J19/0046 , B01J2219/00049 , B01J2219/00351 , B01J2219/00355 , B01J2219/00585 , B01J2219/00693 , B01J2219/00702 , B01J2219/0072 , B01J2219/00722 , B01J2219/00759 , B65B1/00 , B65B3/003 , G21G1/10 , G21G2001/0015
摘要： Systems, methods, and devices for generating radionuclides for use in production of radiopharmaceuticals; synthesizing the radionuclides generated and removing any unwanted products; measuring the quantity and activity level of the synthesized radionuclides; distributively delivering the radionuclides in appropriate quantities to modular cassette synthesis units in a modular cassette subsystem for contemporaneous/parallel production of radiopharmaceutical output and that allow reuse and/or quick, safe, and disposable replacement of portions of the subsystem; delivering non-radionuclide components to the modular cassette synthesis units as part of production of radiopharmaceutical output; measuring the quantity and activity level of each stream of radiopharmaceutical output; purifying the radiopharmaceutical output; dispensing individual doses in sterile vial(s); automatically producing labeling and dose related information; performing automated quality control on extracted samples of produced radiopharmaceutical output; and providing software and hardware controls for overall and sub-portion operation for optional remote data collection, communication, and/or control.
摘要翻译：用于产生用于放射性药物生产的放射性核素的系统，方法和装置; 合成生成的放射性核素并除去任何不需要的产物; 测量合成放射性核素的数量和活度水平; 将放射性核素分配递送到模块化盒式系统中的模块化盒式合成单元，用于同时/并行生产放射性药物输出，并允许重复使用和/或快速，安全和一次性更换子系统的一部分; 将非放射性核素组分作为放射性药物输出生产的一部分提供给模块化盒式合成单元; 测量每个放射性药物输出流量的数量和活动水平; 净化放射性药物输出; 在无菌小瓶中分配单个剂量; 自动生成标签和剂量相关信息; 对提取的放射性药物输出样品进行自动化质量控制; 并为可选的远程数据收集，通信和/或控制提供用于整体和子部分操作的软件和硬件控制。

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