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1. 发明授权

US07326403B2 Radioactive iodine-labeled compound 失效
标题翻译：放射性碘标记化合物
公开(公告)号：US07326403B2
公开(公告)日：2008-02-05
申请号：US11137479
申请日：2005-05-26
申请人： Yasuhiro Magata , Hideo Saji
发明人： Yasuhiro Magata , Hideo Saji
IPC分类号： A61K51/00 , A61M36/14 , C07D417/00
CPC分类号： C07D417/14 , A61K51/0455
摘要： A radioactive iodine-labeled compound represented by the following formula (I): wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.
摘要翻译：由下式（I）表示的放射性碘标记化合物：其中X表示可以在苯环上的任意位置取代的放射性碘原子（优选<123> I等），n表示1〜3的整数，R 1和R 2各自独立地表示取代或未取代的烷基，Y表示具有1至6个碳原子的亚烷基（优选亚甲基），M表示抗衡离子，m表示中和分子的电荷所需的离子数。提供可以选择性地积聚在肿瘤细胞或肿瘤组织中的放射性碘标记的化合物和含有该化合物的闪烁显像剂。

2. 发明申请

US20050226811A1 Radioactive iodine-labeled compound 失效
标题翻译：放射性碘标记化合物
公开(公告)号：US20050226811A1
公开(公告)日：2005-10-13
申请号：US11137479
申请日：2005-05-26
申请人： Yasuhiro Magata , Hideo Saji
发明人： Yasuhiro Magata , Hideo Saji
IPC分类号： A61K51/00 , A61K51/04 , C07D417/14
CPC分类号： C07D417/14 , A61K51/0455
摘要： A radioactive iodine-labeled compound represented by the following formula (I): wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.
摘要翻译：由下式（I）表示的放射性碘标记化合物：其中X表示可以在苯环上的任意位置取代的放射性碘原子（优选<123> I等），n表示1〜3的整数，R 1和R 2各自独立地表示取代或未取代的烷基，Y表示具有1至6个碳原子的亚烷基（优选亚甲基），M表示抗衡离子，m表示中和分子的电荷所需的离子数。提供可以选择性地积聚在肿瘤细胞或肿瘤组织中的放射性碘标记的化合物和含有该化合物的闪烁显像剂。

3. 发明授权

US06916930B2 Radioactive iodine-labeled compound 失效
标题翻译：放射性碘标记化合物
公开(公告)号：US06916930B2
公开(公告)日：2005-07-12
申请号：US10665506
申请日：2003-09-22
申请人： Yasuhiro Magata , Hideo Saji
发明人： Yasuhiro Magata , Hideo Saji
IPC分类号： A61K51/00 , A61K51/04 , C07D417/14
CPC分类号： C07D417/14 , A61K51/0455
摘要： A radioactive iodine-labeled compound represented by the following formula wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.
摘要翻译：由下式表示的放射性碘标记化合物，其中X表示可在苯环上任意位置取代的放射性碘原子（优选<123>，125 I 等），n表示1〜3的整数，R 1和R 2各自独立地表示取代或未取代的烷基，Y表示具有 1〜6个碳原子（优选亚甲基），M表示抗衡离子，m表示中和分子的电荷所需的离子数。提供可以选择性地积聚在肿瘤细胞或肿瘤组织中的放射性碘标记的化合物和含有该化合物的闪烁显像剂。

4. 发明授权

US09370589B2 Switching fluorescent nanoparticle probe and fluorescent particle imaging method using same 有权
标题翻译：开关荧光纳米粒子探针和荧光颗粒成像方法使用相同
公开(公告)号：US09370589B2
公开(公告)日：2016-06-21
申请号：US13818392
申请日：2011-08-08
申请人： Isao Hara , Eiichi Ozeki , Hideo Saji , Shunsaku Kimura , Masahiro Ono , Takashi Temma
发明人： Isao Hara , Eiichi Ozeki , Hideo Saji , Shunsaku Kimura , Masahiro Ono , Takashi Temma
IPC分类号： A61K9/14 , A61K49/00
CPC分类号： A61K49/0089 , A61K49/0032 , A61K49/0093 , Y10S977/773 , Y10S977/927
摘要： The present invention provides a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye during nanoparticle preparation, and emit fluorescence during imaging). A switching fluorescent nanoparticle probe comprising: a molecular assembly composed of an amphiphilic block polymer having a hydrophilic block chain and a hydrophobic block chain; and a fluorescent dye encapsulated in the molecular assembly, wherein (a) the hydrophilic block chain comprises, as an essential hydrophilic structural unit, a unit selected from a sarcosine unit and an alkylene oxide unit, (b) the hydrophobic block chain comprises, as an essential hydrophobic structural unit, a unit selected from the group consisting of an amino acid unit and a hydroxylic acid unit, and (c) the fluorescent dye is a cyanine compound represented by the formula (I): and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.
摘要翻译：本发明提供了具有开关功能（在纳米颗粒制备期间淬灭荧光染料并在成像期间发射荧光的功能）的新型荧光纳米颗粒成像探针。一种开关荧光纳米颗粒探针，包括：由具有亲水嵌段链和疏水性嵌段链的两亲嵌段聚合物组成的分子组合; 以及包封在分子组合中的荧光染料，其中（a）所述亲水性嵌段链包含作为必需亲水性结构单元的选自肌氨酸单元和烯化氧单元的单元，（b）所述疏水性嵌段链包含：必需的疏水结构单元，选自氨基酸单元和羟基酸单元的单元，和（c）荧光染料是由式（I）表示的花青化合物：和荧光染料被封装在单分子组装中。

5. 发明授权

US08642008B2 Molecular probe for imaging of pancreatic islets and use of the same 有权
标题翻译：胰岛成像用分子探针及其用途
公开(公告)号：US08642008B2
公开(公告)日：2014-02-04
申请号：US12872837
申请日：2010-08-31
申请人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Yu Ogawa , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
发明人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Yu Ogawa , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
IPC分类号： A61K51/08
CPC分类号： A61K51/088
摘要： To provide a molecular probe for imaging of pancreatic islets. A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe includes any one of the following polypeptides: polypeptides represented by the following formulae (1), (5), and (9); and polypeptides having homology with the foregoing polypeptides: Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (5) B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (9) where X in the formulae (1) and (5) and B- in the formula (9) indicate that an amino group is labeled with a group represented by the formula (I) below having an aromatic ring, wherein A represents either an aromatic hydrocarbon group or an aromatic heterocyclic group, R1 represents a substituent that contains radioactive iodine, R2 represents either a hydrogen atom or a substituent different from that represented by R1, and R3 represents any one of a bond, a methylene group, and an oxymethylene group.
摘要翻译：为胰岛成像提供分子探针。提供了一种用于胰岛成像的分子探针。分子探针包括以下多肽之一：由下式（1），（5）和（9）表示的多肽。和与前述多肽具有同源性的多肽：Z-DLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（1）Z-DLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2（5）B-DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（9）其中式（1）和（5）中的X和式（9）表示氨基用具有芳环的下式（I）表示的基团标记，其中A表示芳香族烃基或芳香族杂环基，R 1表示含有放射性碘的取代基， R2表示氢原子或与R1表示的不同的取代基，R3表示键，亚甲基和氧亚甲基中的任一个。

6. 发明申请

US20120029209A1 METHOD FOR SYNTHESIZING [18F]SFB USING MICROSYNTHESIS TECHNIQUE 审中-公开
标题翻译：使用微结构技术合成[18 F] SFB的方法
公开(公告)号：US20120029209A1
公开(公告)日：2012-02-02
申请号：US13254152
申请日：2010-03-01
申请人： Hiroaki Nakanishi , Hidekazu Saiki , Hideo Saji , Hiroyuki Kimura , Hidekazu Kawashima , Kenji Tomatsu , Yuji Kuge
发明人： Hiroaki Nakanishi , Hidekazu Saiki , Hideo Saji , Hiroyuki Kimura , Hidekazu Kawashima , Kenji Tomatsu , Yuji Kuge
IPC分类号： C07D207/46
CPC分类号： C07D207/404 , A61K51/00 , C07B59/001 , C07B59/002
摘要： A method for synthesizing [18F]SFB is disclosed, which comprises using a microreactor including a substrate having one channel formed therein so as to have a cross-sectional width of 1 mm or less and a cross-sectional depth of 1 mm or less, the channel being connected to a raw material injection port and a first reagent injection port at one end thereof, and connected to a second reagent injection port at a position far from the one end thereof, and connected to a third reagent injection port at a position far from the second reagent injection port in a direction toward another end thereof, and connected to a liquid discharge port at the other end thereof; and continuously performing a three-step reaction by allowing a reaction solution to flow through the channel serving as a reaction channel from the one end to the other end thereof without taking out the reaction solution from anywhere between the one end and the other end of the channel.
摘要翻译：公开了一种合成[18F] SFB的方法，其包括使用包括其中形成有一个通道的基板的微反应器，以使其横截面宽度为1mm以下，横截面深度为1mm以下，所述通道在其一端连接到原料注入口和第一试剂注入口，并且在远离其一端的位置处连接到第二试剂注入口，并且连接到位于其的一端的第三试剂注入口远离第二试剂注入口朝向其另一端的方向，并且在另一端连接到液体排出口; 并且通过使反应溶液从一端到另一端流过作为反应通道的通道而不从其一端到另一端的任何位置取出反应溶液，从而连续进行三步反应渠道。

7. 发明申请

US20110081663A1 Molecular Probe for Imaging of Pancreatic Islets and Use of the Same 有权
标题翻译：胰岛成像用分子探针及其用途
公开(公告)号：US20110081663A1
公开(公告)日：2011-04-07
申请号：US12893896
申请日：2010-09-29
申请人： Hideo Saji , Nobuya Inagaki , Kentaro Toyoda , Hiroyuki Kimura , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
发明人： Hideo Saji , Nobuya Inagaki , Kentaro Toyoda , Hiroyuki Kimura , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
IPC分类号： G01N33/53 , C07K14/00
CPC分类号： A61K51/08
摘要： A molecular probe for imaging of pancreatic islets is provided. The molecular probe includes a polypeptide represented by the following formula (1), or a polypeptide that has a homology with the foregoing polypeptide. (SEQ ID NO. 1) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2 (1) Wherein “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a group represented by the following chemical formula (I), wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group; R1 represents a substituent that contains 11C, 13N, 15O, 18F, 64Cu, 67Ga, 68Ga, 75Br, 76Br, 77Br, 99mTc, 111In, 123I, 124I, 125I, or 131I; R2 represents either a hydrogen atom, or a substituent different from that represented by R1; and R3 represents any one of a bond, an alkylene group having 1 to 6 carbon atoms, and an oxyalkylene group having 1 to 6 carbon atoms.
摘要翻译：提供了用于胰岛成像的分子探针。分子探针包括由下式（1）表示的多肽，或与前述多肽具有同源性的多肽。（SEQ ID NO.1）Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH2（1）其中，“X”表示赖氨酸残基，赖氨酸残基的侧链的氨基用下述化学式（I）表示的基团标记，其中A表示芳族烃基或芳族杂环基; R1表示含有11C，13N，150C，18F，64Cu，67Ga，68Ga，75Br，76Br，77Br，99mTc，111In，123I，124I，125I或131I的取代基; R2表示氢原子或与R1表示的取代基不同的取代基; R3表示碳原子数1〜6的亚烷基，碳原子数1〜6的氧亚烷基。

8. 发明申请

US20110033381A1 MOLECULAR PROBE FOR IMAGING OF PANCREATIC ISLET AND THE PRECURSOR, AND USE OF THE SAME 审中-公开
标题翻译：用于成像胰腺和前列腺的分子探针及其用途
公开(公告)号：US20110033381A1
公开(公告)日：2011-02-10
申请号：US12854007
申请日：2010-08-10
申请人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Yu Ogawa , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
发明人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Yu Ogawa , Konomu Hirao , Kenji Nagakawa , Hirokazu Matsuda
IPC分类号： A61K51/08 , C07K14/00 , A61K49/00
CPC分类号： A61K51/08 , C07K14/435 , C07K14/57563 , Y02P20/55
摘要： A precursor of molecular probe for imaging of pancreatic islets is provided. A polypeptide represented by any one of the following formulae (1) to (4), or a polypeptide having a homology with the foregoing polypeptide. *-DLSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(1) *-LSK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(2) *-SK* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2(3) *-K* QMEEEAVRLFIEWLK* NGGPSSGAPPPSK-NH2,(4) wherein *- indicates that an α-amino group at an N-terminus is protected by a protecting group or modified with a modifying group having no electric charge; K* indicates that an amino group of a side chain of a lysine is protected by a protecting group; and —NH2 indicates that a carboxyl group at a C-terminus is amidated.
摘要翻译：提供了用于胰岛成像的分子探针的前体。由下式（1）至（4）中任一项表示的多肽或与前述多肽具有同源性的多肽。 * -DLSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPSK-NH2（1）* -LSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPSK-NH2（2）* -SK * QMEEEAVRLFIEWLK * NGGPSSGAPPPSK-NH2（3）* -K * QMEEEAVRLFIEWLK * NGGPSSGAPPPSK-NH2，（4）其中 *表示N-末端的α-氨基被保护基保护或用不带电的修饰基团修饰; K *表示赖氨酸的侧链的氨基被保护基保护; 并且-NH 2表示C末端的羧基被酰胺化。

9. 发明授权

US09084831B2 Molecular probe precursor for imaging of pancreatic islet, and use thereof 有权
标题翻译：用于胰岛成像的分子探针前体及其用途
公开(公告)号：US09084831B2
公开(公告)日：2015-07-21
申请号：US13050672
申请日：2011-03-17
申请人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Konomu Hirao , Kenji Nagakawa
发明人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Konomu Hirao , Kenji Nagakawa
IPC分类号： A61K51/08
CPC分类号： A61K51/088 , A61K51/08
摘要： A precursor of a molecular probe for imaging of pancreatic islets is provided. The precursor includes a polypeptide represented by any one of the following formulae (1) to (12), or a polypeptide having a homology with the foregoing polypeptide: *-DLSKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (1) *-LSKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (2) *-SKQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (3) *-KQMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (4) *-DLSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (5) *-LSK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (6) *-SK*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (7) *-K*QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (8) DLSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (9) LSK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (10) SK*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (11) K*QMEEEAVRLFIEWLK*NGGPSSGAPPPS-NH2 (12)
摘要翻译：提供了用于胰岛成像的分子探针的前体。前体包括由下列通式（1）至（12）中的任一个表示的多肽或与前述多肽具有同源性的多肽：* -DLSKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（1）* -LSKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（ 2）* -SKQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（3）* -KQMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（4）* -DLSK * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（5）* -LSK * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（6）* -SK * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 7）* -K * QMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（8）DLSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（9）LSK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（10）SK * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2（11）K * QMEEEAVRLFIEWLK * NGGPSSGAPPPS-NH2 12）

10. 发明申请

US20080248485A1 Radiolabeled 3-[3- (Benzoyl-Amido) Benzyloxy] Aspartic Acid Derivative and Method of Producing the Same 有权
标题翻译：放射性标记的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸衍生物及其制备方法
公开(公告)号：US20080248485A1
公开(公告)日：2008-10-09
申请号：US10593034
申请日：2005-03-18
申请人： Keiko Shimamoto , Hideo Saji , Yuji Kuge , Masashi Ueda , Masamichi Satoh , Takayuki Nakagawa
发明人： Keiko Shimamoto , Hideo Saji , Yuji Kuge , Masashi Ueda , Masamichi Satoh , Takayuki Nakagawa
IPC分类号： C07C233/75 , G01N33/53
CPC分类号： C07B59/001
摘要： The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter.Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.
摘要翻译：本发明提供了一种对谷氨酸转运蛋白具有高度选择性和有效的放射性标记配体，可用于特异性检测谷氨酸转运蛋白。具体而言，本发明提供由下式（1）表示的苯甲酰基上具有放射性取代基的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸或其酯或其盐：其中X表示取代基含有选自直链或支链低级脂族烷基，羟基，直链或支链低级脂族烷氧基，氨基，直链或支链低级脂族酰氨基，卤素原子和直链或支链低级脂族卤代烷基; R 1和R 2各自表示氢原子，直链或支链低级脂族烷基或乙酰氧基甲基。

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