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1. 发明授权

US08269035B2 Process for production of radioactive-fluorine-labeled organic compound 有权
标题翻译：放射性氟标记有机化合物的制备方法
公开(公告)号：US08269035B2
公开(公告)日：2012-09-18
申请号：US12747726
申请日：2008-12-16
申请人： Fumie Kurosaki , Masahito Toyama , Akio Hayashi
发明人： Fumie Kurosaki , Masahito Toyama , Akio Hayashi
IPC分类号： C07C69/74
CPC分类号： C07B59/00 , C07B59/001 , C07B2200/05 , C07C269/06 , C07C2601/04 , Y02P20/55 , C07C271/24
摘要： A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1): (wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.7 or more relative to the compound of the formula (1), and the concentration of the compound of the formula (1) in the inert organic solvent is 50 mmol/L or more.
摘要翻译：提供了可以提高放射性氟化产率的放射性氟标记的有机化合物的制造方法。本发明提供下述式（1）表示的化合物：其中，R 1为碳原子数为1〜10的直链或支链烷基或芳香族取代基的化合物，R2为直链或支链的卤代烷基磺酸取代基， 10个碳原子，具有1-10个碳原子的直链或支链烷基磺酸取代基，氟磺酸取代基或芳族磺酸取代基，并且R 3是保护基））在搅拌下在惰性有机溶剂中，在相转移催化剂，18F离子和钾离子，以便用放射性氟进行标记，其中加热温度为40-90℃，相转移催化剂在惰性有机溶剂中的浓度为70mmol / L 或者更多。相对于式（1）化合物，相转移催化剂的摩尔比优选为0.7以上，惰性有机溶剂中式（1）化合物的浓度为50mmol / L以上。

2. 发明申请

US20100119448A1 METHOD FOR PRODUCTION OF RADIATION DIAGNOSTIC IMAGING AGENT 有权
标题翻译：辐射诊断成像剂的生产方法
公开(公告)号：US20100119448A1
公开(公告)日：2010-05-13
申请号：US12526667
申请日：2008-02-12
申请人： Daisaku Nakamura , Soichi Nakamura , Masahito Toyama , Akio Hayashi
发明人： Daisaku Nakamura , Soichi Nakamura , Masahito Toyama , Akio Hayashi
IPC分类号： A61K51/04
CPC分类号： C07C229/48 , A61K9/0019 , A61K47/26 , A61K51/0402 , A61K51/0406 , C07B59/001 , C07B63/04 , C07B2200/05 , C07C2601/04
摘要： A method for producing a radioactive diagnostic imaging agent which contains a radioactive halogen-labeled amino acid compound as an effective ingredient and has a composition that can inhibit radiolysis of the effective ingredient, thereby further improving stability, is provided. Disclosed is a method for producing a radioactive diagnostic imaging agent, comprising a solution preparation step of preparing a solution containing a radioactive halogen-labeled amino acid compound, and a dilution step of diluting the solution containing the radioactive fluorine-labeled organic compound in order to adjust radioactive concentration thereof, which further comprises an acid addition step of adding an acid to the solution containing the radioactive fluorine-labeled organic compound, after the solution preparation step and before the dilution step, wherein the acid is added in the acid addition step in an amount sufficient to adjust the pH of the solution resulting from the dilution step to 2.0-5.9, for example, in an amount corresponding to 0.40-2.8 mmol per 1 L of the solution resulting from the dilution step.
摘要翻译：提供了含有放射性卤素标记的氨基酸化合物作为有效成分并具有能够抑制有效成分的放射线析出，从而进一步提高稳定性的组成的放射性诊断显像剂的制造方法。本发明公开了一种放射性诊断显像剂的制造方法，其特征在于，包括：制备含有放射性卤素标记的氨基酸化合物的溶液的溶液制备工序，以及稀释含有放射性氟标记的有机化合物的溶液的稀释步骤，调整其放射性浓度，其还包括在溶液制备步骤之后和稀释步骤之前在含有放射性氟标记的有机化合物的溶液中加入酸的酸添加步骤，其中在酸添加步骤中加入酸足以将由稀释步骤得到的溶液的pH调节至2.0-5.9的量，例如，相对于每1L由稀释步骤得到的溶液为0.40-2.8mmol的量。

3. 发明申请

US20100016626A1 PROCESS FOR PRODUCTION OF PRECURSOR COMPOUND FOR RADIOACTIVE HALOGEN-LABELED ORGANIC COMPOUND 有权
标题翻译：用于生产放射性标记有机化合物的前体化合物的方法
公开(公告)号：US20100016626A1
公开(公告)日：2010-01-21
申请号：US12448311
申请日：2007-12-17
申请人： Masahito Toyama , Akio Hayashi
发明人： Masahito Toyama , Akio Hayashi
IPC分类号： C07C69/74
CPC分类号： G21H5/02 , A61K51/0406 , C07B59/001 , C07B2200/09 , C07C303/28 , C07C303/44 , C07C2601/04 , Y02P20/55 , C07C309/73 , C07C309/65 , C07C309/66
摘要： A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.
摘要翻译：提供了一种制备可用于制备放射性氟标记的氨基酸化合物的标记前体的方法。在用于将离去基团引入到FACBC的正构形式和抗体形式的混合物的反应步骤中，允许碱在反应体系中存在以产生与碱不反应的合成离去基团加合物，并且是高度稳定的抗离析基加合物，其可以与碱反应形成水溶性化合物。通过使用利用这种溶解度差异的纯化方法，可以选择性地分离出合成离去基加成物。碱可以是具有1-10个碳原子的直链或支链伯 - 叔烷基胺，具有2-20个碳原子的含氮杂环化合物和具有2-20个碳原子的含氮杂芳族化合物。

4. 发明申请

US20080281121A1 Precursor Compound of Radioactive Halogen-Labeled Organic Compound 有权
标题翻译：放射性标记有机化合物的前体化合物
公开(公告)号：US20080281121A1
公开(公告)日：2008-11-13
申请号：US12085679
申请日：2006-11-28
申请人： Osamu Ito , Akio Hayashi , Fumie Kurosaki , Masahito Toyama , Toshiyuki Shinmura , Arinori Harano
发明人： Osamu Ito , Akio Hayashi , Fumie Kurosaki , Masahito Toyama , Toshiyuki Shinmura , Arinori Harano
IPC分类号： C07C69/74
CPC分类号： A61K51/0402 , A61K51/0406 , C07B59/00 , C07B2200/05 , C07C67/307 , C07C309/65 , C07C2601/04 , Y02P20/55
摘要： It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
摘要翻译：旨在提供一种新的氨基酸有机化合物，其可用作用于放射性卤素标记的氨基酸化合物的标记前体化合物，包括[SUP 18 F] FACBC，并且其防止甲醇残留在由其制备的放射性卤素标记的氨基酸化合物。新型氨基酸有机化合物是下式表示的化合物：其中，n为0或1〜4的整数， R 1是乙基，1-丙基或异丙基取代基; X是卤素取代基或由-OR 2表示的基团。 R 2是具有1至10个碳原子的直链或支链卤代烷基磺酸取代基，具有3至12个碳原子的三烷基甲锡烷基取代基，氟代磺酸取代基或芳族磺酸取代基; R 3是保护基。

5. 发明申请

US20090105489A1 NOVEL ORGANIC COMPOUND AND METHOD FOR PRODUCING RADIOACTIVE HALOGEN-LABELED ORGANIC COMPOUND USING THE SAME 失效
标题翻译：新型有机化合物及其制造使用其的放射性标记有机化合物的方法
公开(公告)号：US20090105489A1
公开(公告)日：2009-04-23
申请号：US11915267
申请日：2006-05-15
申请人： Masahito Toyama , Fumie Kurosaki , Akio Hayashi , Osamu Ito
发明人： Masahito Toyama , Fumie Kurosaki , Akio Hayashi , Osamu Ito
IPC分类号： C07D209/48 , C07C61/04
CPC分类号： C07D209/48 , A61K51/0406 , Y02P20/55
摘要： It is intended to provide a labeling precursor compound used for selectively producing radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acids, and to provide a process for producing a radioactive halogen-substituted syn-1-amino-3-cyclobutane-carboxylic acid using the labeling precursor compound. A labeling precursor is used in which a phthalimide group is used as a protective group for protecting the amino group. The syn-form of the radioactive halogen-substituted 1-amino-3-cyclobutane-carboxylic acid can be selectively produced by labeling the labeling precursor with a radioactive halogen followed by deprotecting.
摘要翻译：旨在提供用于选择性地制备放射性卤素取代的顺式-1-氨基-3-环丁烷羧酸的标记前体化合物，并提供一种制备放射性卤素取代的顺式-1-氨基-3- 使用标记前体化合物的环丁烷羧酸。使用标记前体，其中使用邻苯二甲酰亚胺基作为保护氨基的保护基。放射性卤素取代的1-氨基-3-环丁烷羧酸的合成形式可以通过用放射性卤素标记前述标记前体，然后脱保护来选择性地制备。

6. 发明授权

US08790620B2 Radioactive diagnostic imaging agent 有权
标题翻译：放射诊断成像剂
公开(公告)号：US08790620B2
公开(公告)日：2014-07-29
申请号：US12518307
申请日：2007-11-20
申请人： Akio Hayashi , Toshiyuki Shinmura , Daisaku Nakamura , Soichi Takasaki , Shinji Tokunaga , Emi Kaneko , Masahito Toyama
发明人： Akio Hayashi , Toshiyuki Shinmura , Daisaku Nakamura , Soichi Takasaki , Shinji Tokunaga , Emi Kaneko , Masahito Toyama
IPC分类号： A61K51/00 , A61M36/14 , A61K49/04 , A61K47/26 , A61K51/04
CPC分类号： A61K49/0433 , A61K47/26 , A61K51/04 , A61K51/0406 , C07B59/001
摘要： A composition including a radioactive fluorine-labeled amino acid compound is provided, which can be prevented from radiolysis. Disclosed is a composition which includes a solution containing a radioactive fluorine-labeled amino acid compound as an effective ingredient, in which the pH value of the solution is kept at 2.0-5.9, more preferably 2.0-4.9 in order to inhibit radiolysis. Also, it is possible to further inhibit radiolysis by adding thereto a pharmaceutical additive capable of inhibiting radiolysis, such as a sugar, a sugar alcohol and a sugar lactone, while the pH is kept at 2.0-5.9.
摘要翻译：提供了包含放射性氟标记的氨基酸化合物的组合物，其可以防止放射分解。公开了含有放射性氟标记的氨基酸化合物作为有效成分的溶液的组合物，其中溶液的pH值保持在2.0-5.9，更优选为2.0-4.9，以抑制放射分解。此外，通过在pH保持在2.0〜5.9的同时向其中添加能够抑制放射线分解的药物添加剂，例如糖，糖醇和糖内酯，可以进一步抑制放射分解。

7. 发明授权

US08658132B2 Method for production of radiation diagnostic imaging agent 有权
标题翻译：辐射诊断成像剂生产方法
公开(公告)号：US08658132B2
公开(公告)日：2014-02-25
申请号：US13565204
申请日：2012-08-02
申请人： Daisaku Nakamura , Soichi Nakamura , Masahito Toyama , Akio Hayashi
发明人： Daisaku Nakamura , Soichi Nakamura , Masahito Toyama , Akio Hayashi
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： C07C229/48 , A61K9/0019 , A61K47/26 , A61K51/0402 , A61K51/0406 , C07B59/001 , C07B63/04 , C07B2200/05 , C07C2601/04
摘要： A method for producing a radioactive diagnostic imaging agent containing a radioactive 18 fluorine-labeled organic compound represented by the following formula (1): as an effective ingredient in which radiolysis of the effective ingredient is inhibited, involves providing a solution containing the radioactive 18fluorine-labeled organic compound represented by the above formula (1), adding an acid to the solution obtained in the first step in an amount sufficient for the solution to be kept within a pH of 2.0-5.9 in the following third step, and diluting the solution obtained in the second step in order to adjust the solution to a desired radioactive concentration within a pH of 2.0-5.9.
摘要翻译：一种含有下式（1）表示的放射性18氟标记有机化合物的放射性诊断显像剂的制造方法：作为有效成分的有效成分被抑制的有效成分，提供含有放射性18- 标记的由上述式（1）表示的有机化合物，在第三步中向第一步骤中获得的溶液中加入酸，其量足以使溶液保持在2.0-5.9的pH范围内，并稀释溶液在第二步中获得，以便将溶液调节到2.0-5.9的pH范围内的所需放射性浓度。

8. 发明申请

US20120301399A1 METHOD FOR PRODUCTION OF RADIATION DIAGNOSTIC IMAGING AGENT 有权
标题翻译：辐射诊断成像剂的生产方法
公开(公告)号：US20120301399A1
公开(公告)日：2012-11-29
申请号：US13565204
申请日：2012-08-02
申请人： Daisaku NAKAMURA , Soichi Nakamura , Masahito Toyama , Akio Hayashi
发明人： Daisaku NAKAMURA , Soichi Nakamura , Masahito Toyama , Akio Hayashi
IPC分类号： A61K51/04
CPC分类号： C07C229/48 , A61K9/0019 , A61K47/26 , A61K51/0402 , A61K51/0406 , C07B59/001 , C07B63/04 , C07B2200/05 , C07C2601/04
摘要： A method for producing a radioactive diagnostic imaging agent containing a radioactive 18 fluorine-labeled organic compound represented by the following formula (1): as an effective ingredient in which radiolysis of the effective ingredient is inhibited, involves providing a solution containing the radioactive 18fluorine-labeled organic compound represented by the above formula (1), adding an acid to the solution obtained in the first step in an amount sufficient for the solution to be kept within a pH of 2.0-5.9 in the following third step, and diluting the solution obtained in the second step in order to adjust the solution to a desired radioactive concentration within a pH of 2.0-5.9.
摘要翻译：一种含有下式（1）表示的放射性18氟标记有机化合物的放射性诊断显像剂的制造方法：作为有效成分的有效成分被抑制的有效成分，提供含有放射性18- 标记的由上述式（1）表示的有机化合物，在第三步中向第一步骤中获得的溶液中加入酸，其量足以使溶液保持在2.0-5.9的pH范围内，并稀释溶液在第二步中获得，以便将溶液调节到2.0-5.9的pH范围内的所需放射性浓度。

9. 发明授权

US07897811B2 Process for production of radioactive fluorine-labeled organic compound 有权
标题翻译：放射性氟标记有机化合物的生产工艺
公开(公告)号：US07897811B2
公开(公告)日：2011-03-01
申请号：US12227240
申请日：2007-05-07
申请人： Akio Hayashi , Fumie Kurosaki , Masahito Toyama , Toshiyuki Shinmura , Emi Kaneko
发明人： Akio Hayashi , Fumie Kurosaki , Masahito Toyama , Toshiyuki Shinmura , Emi Kaneko
IPC分类号： C07C61/04
CPC分类号： C07C227/18 , C07B59/001 , C07B2200/05 , C07C227/20 , C07C2601/04 , Y02P20/55 , C07C229/48
摘要： A process is provided for producing [18F]FACBC, which can reduce the production amount of impurities. Disclosed is a process for producing a radioactive fluorine-labeled organic compound, including a deesterification step of retaining, in a reverse-phase column, a compound represented by Formula (1): wherein R1 is a linear or branched C1-C10-alkyl chain or an aromatic substituent, and R2 is a protecting group; charging the column with an alkaline solution to deesterify the compound, and subsequently discharging the alkaline solution from the column to obtain a compound represented by Formula (2): wherein X is sodium or potassium; and a deprotection step of deprotecting the amino-protecting group of the compound obtained in the deesterification step to obtain a compound represented by Formula (3):
摘要翻译：提供了用于生产[18F] FACBC的方法，其可以降低杂质的产生量。公开了一种放射性氟标记的有机化合物的制备方法，包括在反相柱中保留由式（1）表示的化合物的脱酯化步骤：其中R 1是直链或支链的C 1 -C 10 - 烷基链或芳香族取代基，R2为保护基; 用碱性溶液装入柱子以使化合物脱酯化，然后从柱中排出碱性溶液，得到由式（2）表示的化合物：其中X是钠或钾; 和脱甲基化工序中得到的化合物的氨基保护基脱保护，得到式（3）表示的化合物：

10. 发明授权

US08563771B2 Process for production of precursor compound for radioactive halogen-labeled organic compound 有权
标题翻译：用于放射性卤素标记的有机化合物的前体化合物的制备方法
公开(公告)号：US08563771B2
公开(公告)日：2013-10-22
申请号：US12448311
申请日：2007-12-17
申请人： Masahito Toyama , Akio Hayashi
发明人： Masahito Toyama , Akio Hayashi
IPC分类号： C07C61/04
CPC分类号： G21H5/02 , A61K51/0406 , C07B59/001 , C07B2200/09 , C07C303/28 , C07C303/44 , C07C2601/04 , Y02P20/55 , C07C309/73 , C07C309/65 , C07C309/66
摘要： A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.
摘要翻译：提供了一种制备可用于制备放射性氟标记的氨基酸化合物的标记前体的方法。在用于将离去基团引入到FACBC的正构形式和抗体形式的混合物的反应步骤中，允许碱在反应体系中存在以产生与碱不反应的合成离去基团加合物，并且是高度稳定的抗脱离基加合物，其可与碱反应形成水溶性化合物。通过使用利用这种溶解度差异的纯化方法，可以选择性地分离出合成离去基加成物。碱可以是具有1-10个碳原子的直链或支链伯 - 叔烷基胺，具有2-20个碳原子的含氮杂环化合物和具有2-20个碳原子的含氮杂芳族化合物。

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