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1. 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。

2. 发明授权

US08343459B2 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：US08343459B2
公开(公告)日：2013-01-01
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： A61K51/00 , 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 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。

4. 发明申请

US20100028258A1 Radioactive Diagnostic Imaging Agent 有权
标题翻译：放射诊断成像剂
公开(公告)号：US20100028258A1
公开(公告)日：2010-02-04
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： A61K51/04 , A61K101/02
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, whilst 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。

5. 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。

6. 发明授权

US06486323B1 Process for producing optically active tropinonemonocarboxylic acid derivative 有权
标题翻译：光学活性托品酮一羧酸衍生物的制备方法
公开(公告)号：US06486323B1
公开(公告)日：2002-11-26
申请号：US09806592
申请日：2001-03-30
申请人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
发明人： Manabu Node , Soichi Nakamura , Daisaku Nakamura
IPC分类号： C07D45102
CPC分类号： C12P17/10 , C12P41/00 , C12P41/005
摘要： An optically active tropinonemonocarboxylic acid ester derivative useful as an intermediate for synthesis of optically active tropane derivatives was obtained by reacting succindialdehyde with an organic amine and acetonedicarboxylic acid ester to obtain a tropinonedicarboxylic acid ester derivative, and then subjecting this derivative to enzyme-catalyzed asymmetric dealkoxy-carbonylation. Since anhydroecgonine methyl ester derived from the optically active tropinone-monocarboxylic acid ester derivative by reduction and dehydration had the same direction of optical rotation as in the case of anhydroecgonine methyl ester obtained from natural cocaine, it was proved that the obtained optically active tropinonemonocarboxylic acid ester derivative had the same absolute configuration as that of natural cocaine. The yield of the optically active tropinonemonocarboxylic acid ester derivative from the asymmetric dealkoxycarbonylation was 30 to 50 mol %, and its optical purity was 70 to 97% ee. In addition, it was found that a crystalline optically active anhydroecgonine carboxylic acid ester derivative can be obtained by reducing and then dehydrating the optically active tropinonemonocarboxylic acid ester derivative and that its optical purity can easily be increased by recrystallization.
摘要翻译：通过使琥珀醛与有机胺和丙酮二羧酸酯反应得到托品酮二羧酸酯衍生物，然后将该衍生物进行酶催化的不对称脱烷基，得到用作合成光学活性托烷衍生物的中间体的光学活性托品酮单羧酸酯衍生物羰基化。由于通过还原和脱水衍生自光学活性的托品酮 - 单羧酸酯衍生物的脱氢异君子酸甲酯具有与从天然可卡因得到的脱氢山梨醇甲酯的情况相同的旋光方向，所以证明得到的光学活性托品酮单羧酸酯衍生物具有与天然可卡因相同的绝对构型。来自不对称脱烷基羰基化反应的光学活性托品酮二羧酸酯衍生物的收率为30〜50摩尔％，光学纯度为70〜97％ee。此外，发现通过使光学活性托品酮一羧酸酯衍生物还原然后使其脱水，可以得到结晶光学活性的脱氢gon根化羧酸酯衍生物，并且可以通过重结晶容易地提高其光学纯度。

7. 发明授权

US08277777B2 Compound having affinity for amyloid 有权
标题翻译：对淀粉样蛋白具有亲和力的化合物
公开(公告)号：US08277777B2
公开(公告)日：2012-10-02
申请号：US12308715
申请日：2007-06-21
申请人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Anthony Eamon Storey , Denis Raymond Christophe Bouvet
发明人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Anthony Eamon Storey , Denis Raymond Christophe Bouvet
IPC分类号： A61K51/00 , A61M36/14 , C07D491/02
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.
摘要翻译：具有与淀粉样蛋白亲和性的化合物，显示出与正常组织的足够快速的清除，并且由下式（1）表示的毒性如诱变性被抑制：或其盐，其中R1是选自氢，羟基，羧基，硫酸根基，氨基，硝基，氰基，具有1-4个碳原子的烷基取代基或具有1-4个碳原子的烷氧基取代基; R2是放射性卤素取代基; 并且m为0〜2的整数，还提供了含有上述式所示化合物或其盐的阿尔茨海默病的低毒性诊断剂。

8. 发明申请

US20100092387A1 Novel Compound Having Affinity For Amyloid 有权
标题翻译：具有淀粉样蛋白亲和力的新型化合物
公开(公告)号：US20100092387A1
公开(公告)日：2010-04-15
申请号：US12308715
申请日：2007-06-21
申请人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Storey Anthony Eamon , Denis Raymond Christophe Bouvet
发明人： Shigeyuki Tanifuji , Akio Hayashi , Daisaku Nakamura , Shinya Takasaki , Storey Anthony Eamon , Denis Raymond Christophe Bouvet
IPC分类号： A61K51/04 , C07D471/04
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound that has affinity with amyloid, exhibits sufficiently rapid clearance from normal tissues, and is suppressed in toxicity such as mutagenicity is provided, which is represented by the following formula (1): or a salt thereof, wherein R1 is a group selected from hydrogen, hydroxyl group, carboxyl group, sulfate group, amino group, nitro group, cyano group, an alkyl substituent with one to 4 carbon atoms or an alkoxy substituent with one to 4 carbon atoms; R2 is a radioactive halogen substituent; and m is an integer of 0 to 2, and a low-toxic diagnostic agent for Alzheimer's disease comprising a compound represented by the above formula or a salt thereof is also provided.
摘要翻译：具有与淀粉样蛋白亲和性的化合物，显示出与正常组织的足够快速的清除，并且由下式（1）表示的毒性如诱变性被抑制：或其盐，其中R1是选自氢，羟基，羧基，硫酸根基，氨基，硝基，氰基，具有1-4个碳原子的烷基取代基或具有1-4个碳原子的烷氧基取代基; R2是放射性卤素取代基; 并且m为0〜2的整数，还提供了含有上述式所示化合物或其盐的阿尔茨海默病的低毒性诊断剂。

9. 发明申请

US20090252680A1 NOVEL COMPOUND WITH AFFINITY FOR AMYLOID 审中-公开
标题翻译：具有AMYLOID亲和性的新型化合物
公开(公告)号：US20090252680A1
公开(公告)日：2009-10-08
申请号：US12312596
申请日：2007-10-30
申请人： Shigeyuki Tanifuji , Daisaku Nakamura , Shinya Takasaki , Yuki Okumura
发明人： Shigeyuki Tanifuji , Daisaku Nakamura , Shinya Takasaki , Yuki Okumura
IPC分类号： A61K51/04 , C07D471/04 , A61K101/02
CPC分类号： C07B59/002 , A61K51/0455 , C07D471/04
摘要： A compound represented by the following formula or a salt thereof: wherein each of A1, A2, A3 and A4 independently represents a carbon or nitrogen; R1 is a group selected from the group consisting of hydrogen, hydroxyl group, carboxyl group, sulfuric acid group, amino group, nitro group, cyano group, non-radioactive halogen substituents, alkyl substituents with 1-4 carbon atoms and alkoxy substituents with 1-4 carbon atoms; and R2 is a radioactive halogen substituent, provided at least one of A1, A2, A3 and A4 represents a carbon, and R1 binds to a carbon represented by A1, A2, A3 or A4, is effective as an image diagnosis probe targeting amyloid and as well as a diagnostic agent for Alzheimer's disease including the compound represented by the above formula or a salt thereof.
摘要翻译：由下式表示的化合物或其盐：其中A1，A2，A3和A4各自独立地表示碳或氮; R1是选自氢，羟基，羧基，硫酸基，氨基，硝基，氰基，非放射性卤素取代基，具有1-4个碳原子的烷基取代基和具有1个 -4个碳原子; 并且R2是放射性卤素取代基，只要A1，A2，A3和A4中的至少一个代表碳，并且R1与由A1，A2，A3或A4表示的碳结合，作为靶向淀粉样蛋白的图像诊断探针是有效的，以及阿尔茨海默氏病的诊断剂，包括由上式表示的化合物或其盐。

10. 发明申请

US20100249418A1 NOVEL COMPOUND HAVING AFFINITY FOR AMYLOID 审中-公开
标题翻译：具有AMYLOID亲和性的新化合物
公开(公告)号：US20100249418A1
公开(公告)日：2010-09-30
申请号：US12739348
申请日：2008-10-24
申请人： Shigeyuki Tanifuji , Daisaku Nakamura , Shinya Takasaki , Yuki Okumura
发明人： Shigeyuki Tanifuji , Daisaku Nakamura , Shinya Takasaki , Yuki Okumura
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K51/0455
摘要： A compound effective as a probe targeting amyloid for image diagnosis and a reagent comprising the compound for detecting amyloid deposited on a biological tissue are provided. Provided are a compound represented by the following formula (1): wherein R1 is a group selected from the group consisting of a halogen substituent, alkyl substituent with 1 to 4 carbon atoms, alkoxy substituent having alkyl chain with 1 to 4 carbon atoms and hydroxyl group, R2 is a group selected from the group consisting of a cyano substituent, alkyl substituent with 1 to 4 carbon atoms and halogen substituent, R3 is a group selected from the group consisting of a hydroxyl group, halogen substituent and substituent represented by the following formula: (wherein R4 is a hydrogen, halogen substituent or hydroxyl group, and m is an integer of 1 to 4), provided that at least one of R1, R2, R3 and R4 represents a radioactive halogen, and a reagent comprising the same.
摘要翻译：提供了有效作为靶向用于图像诊断的淀粉样蛋白的探针的化合物和包含用于检测沉积在生物组织上的淀粉样蛋白的化合物的试剂。提供由下式（1）表示的化合物：其中R 1是选自卤素取代基，具有1至4个碳原子的烷基取代基，具有1至4个碳原子的烷基链的烷氧基取代基和羟基的基团基团，R 2为选自氰基取代基，具有1〜4个碳原子的烷基取代基和卤素取代基的基团，R 3为选自羟基，卤素取代基和下述基团的取代基的基团式（R 4为氢，卤素取代基或羟基，m为1〜4的整数），条件是R 1，R 2，R 3和R 4中的至少一个表示放射性卤素，和含有该卤素的试剂。

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