专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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：

2. 发明申请

US20100056826A1 RADIOACTIVE DIAGNOSTIC IMAGING AGENT 审中-公开
标题翻译：放射性诊断成像剂
公开(公告)号：US20100056826A1
公开(公告)日：2010-03-04
申请号：US12312435
申请日：2007-08-31
申请人： Akio Hayashi , Fumie Kurosaki
发明人： Akio Hayashi , Fumie Kurosaki
IPC分类号： C07C229/28
CPC分类号： A61K51/0406
摘要： A composition comprising a radioactive fluorine-labeled amino acid compound, which is reduced in radiolysis, is provided. A composition is produced by mixing the radioactive fluorine-labeled amino acid compound with a sugar lactone in an amount effective to prevent the radiolysis As the sugar lactone, one selected from the group consisting of ascorbic acid and glucono-σ-lactone can preferably be used. The sugar lactone is preferably one selected from the compounds that are acceptable as pharmaceutical additives. The composition preferably contains the sugar lactone in an amount not less than 0.5 μmol/mL and not more than an amount acceptable for pharmaceutical additives. Preferably, the composition is prepared to have a radioactive concentration in use of 25-125 MBq/mL.
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，其被放射分解减少。通过将放射性氟标记的氨基酸化合物与糖内酯以与防止放射线分解有效的量混合来制造组合物作为糖内酯，选自抗坏血酸和葡萄糖酸 - 内酯的一种可优选为用过的。糖内酯优选选自作为药物添加剂可接受的化合物。组合物优选含有不小于0.5μmol/ mL且不大于药物添加剂可接受量的糖内酯。优选地，组合物被制备成使用25-125MBq / mL的放射性浓度。

3. 发明授权

US08758724B2 Unnatural amino acid radiolabeling precursor 有权
标题翻译：非天然氨基酸放射性标记前体
公开(公告)号：US08758724B2
公开(公告)日：2014-06-24
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： A61K51/00 , A61M36/14
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，其可以用作包括[18 F] FACBC的放射性卤素标记的氨基酸化合物的标记前体化合物，并且其防止甲醇残留在所产生的放射性卤素标记的氨基酸化合物中由此。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， R1是乙基，1-丙基或异丙基取代基; X是卤素取代基或由-OR2表示的基团; R2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，氟磺酸取代基或芳族磺酸取代基; R3为保护基。

4. 发明授权

US07910745B2 Organic compound and method for producing radioactive halogen-labeled organic compound using the same 失效
标题翻译：有机化合物及使用其的放射性卤素标记有机化合物的制造方法
公开(公告)号：US07910745B2
公开(公告)日：2011-03-22
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： C07D285/01 , C07D207/404 , 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。

5. 发明申请

US20100261931A1 PROCESS FOR PRODUCTION OF RADIOACTIVE-FLUORINE-LABELED ORGANIC COMPOUND 有权
标题翻译：生产放射性荧光标记有机化合物的方法
公开(公告)号：US20100261931A1
公开(公告)日：2010-10-14
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： C07C69/757
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。

6. 发明申请

US20090198085A1 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生产工艺
公开(公告)号：US20090198085A1
公开(公告)日：2009-08-06
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：

7. 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。

8. 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。

9. 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。

10. 发明申请

US20070036258A1 Process for producing radioactive fluorine compound 审中-公开
标题翻译：放射性氟化合物的制造方法
公开(公告)号：US20070036258A1
公开(公告)日：2007-02-15
申请号：US10573039
申请日：2004-09-28
申请人： Osamu Ito , Keiichi Hirano , Takeshi Morita , Fumie Kurosaki
发明人： Osamu Ito , Keiichi Hirano , Takeshi Morita , Fumie Kurosaki
IPC分类号： C07F5/00 , G21G1/06
CPC分类号： C07B59/00 , C07B2200/05 , C07C211/63 , C07H5/02
摘要： A process for producing a radioactive fluorine compound which comprises a step in which [18O] water containing [18F] fluoride ions is introduced into a column packed with an ion-exchange resin to collect the [18F] fluoride ions and a step in which a substrate is reacted with the [18F] fluoride ions collected, characterized in that the ion-exchange resin is a resin represented by the following general formula (1): (wherein n is an integer of 1 to 10; R represents a linear or branched, C1-8 monovalent hydrocarbon group; P represents a styrene-based copolymer; and Y represents an anion).
摘要翻译：一种放射性氟化合物的制造方法，其特征在于，将含有[[18 F] F]氟离子的[SUP] 18 O]水引入装有离子交换树脂的柱中，交换树脂以收集[F 18 F]氟化物离子，并且将底物与所收集的[SUP 18 F]氟离子反应的步骤，其特征在于，交换树脂是由以下通式（1）表示的树脂：其中n为1〜10的整数，R为直链或支链的C 1-8烷基一价烃基，P为苯乙烯基共聚物; Y表示阴离子）。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式