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1. 发明公开

EP3339309A1 RADIOACTIVE HALOGEN-LABELED PYRIDO[1,2-A]BENZIMIDAZOLE DERIVATIVE COMPOUND 有权转让
公开(公告)号：EP3339309A1
公开(公告)日：2018-06-27
申请号：EP16836812.4
申请日：2016-02-24
申请人： Kyoto University , Nihon Medi-Physics Co., Ltd.
发明人： ONO Masahiro , SAJI Hideo , IHARA Masafumi , MATSUMOTO Hiroki , SEKI Ikuya
IPC分类号： C07D471/04 , A61K51/00 , A61P25/28 , C07B59/00 , C07F7/10 , C07F7/22
CPC分类号： C07D471/04 , A61K51/0455 , C07B59/002 , C07B2200/05 , C07F7/0814
摘要： The present invention relates to a radioactive halogen-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a specific general formula or a salt thereof, or a radiopharmaceutical comprising the same.

2. 发明公开

EP3266778A1 RADIOACTIVE IODINE LABELED PYRIDO[1,2-a]BENZOIMIDAZOLE DERIVATIVE COMPOUND 审中-公开
标题翻译：放射性碘标记的吡啶[1,2-a]苯并咪唑衍生物化合物
公开(公告)号：EP3266778A1
公开(公告)日：2018-01-10
申请号：EP16758812.8
申请日：2016-02-24
申请人： Kyoto University , Nihon Medi-Physics Co., Ltd.
发明人： SAJI Hideo , ONO Masahiro , IHARA Masafumi , SEKI Ikuya
IPC分类号： C07D471/04 , A61K51/00 , A61P25/28 , C07B59/00 , C07F7/10 , C07F7/22
CPC分类号： A61K51/0455 , A61K51/00 , C07B59/00 , C07B59/002 , C07B2200/05 , C07D471/04 , C07F7/0814 , C07F7/10 , C07F7/22 , C07F7/2208
摘要： The present invention relates to a radioactive iodine-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a definite general formula or a salt thereof, or a radiopharmaceutical comprising the same.
摘要翻译：本发明涉及由确定的通式表示的放射性碘标记的吡啶并[1,2-a]苯并咪唑衍生物化合物或其盐，或包含其的放射性药物。

3. 发明授权

EP2404903B1 METHOD OF SYNTHESIZING [18F]SFB USING MICROSYNTHESIS TECHNIQUE 有权
标题翻译： METHOD FOR合成[18 F] SFB的使用微型合成工艺
公开(公告)号：EP2404903B1
公开(公告)日：2013-07-17
申请号：EP10748713.4
申请日：2010-03-01
申请人： Shimadzu Corporation , Kyoto University
发明人： NAKANISHI Hiroaki , SAIKI Hidekazu , SAJI Hideo , KIMURA Hiroyuki , KAWASHIMA Hidekazu , TOMATSU Kenji , KUGE Yuji
IPC分类号： C07D207/404 , A61K51/00 , C07B59/00 , C07B61/00
CPC分类号： C07D207/404 , A61K51/00 , C07B59/001 , C07B59/002

4. 发明公开

EP2510951A1 MOLECULAR PROBE FOR IMAGING OF PANCREATIC ISLET, AND USE THEREOF 有权转让
标题翻译： MOLEKULARE SONDE ZUR BILDGEBUNG DER LANGERHANS-INSELN UND VERWENDUNG DAVON
公开(公告)号：EP2510951A1
公开(公告)日：2012-10-17
申请号：EP10836003.3
申请日：2010-12-08
申请人： Kyoto University , Arkray, Inc.
发明人： SAJI Hideo , INAGAKI Nobuya , TOYODA Kentaro , KIMURA Hiroyuki , HIRAO Konomu , NAGAKAWA Kenji , MATSUDA Hirokazu
IPC分类号： A61K51/00 , C07K1/13 , C07K14/605 , G01N33/60 , G01T1/161
CPC分类号： G01N33/74 , A61K51/088 , C07K14/605
摘要： A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide,
Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (1) (SEQ ID NO. 1)
Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH 2 (2) (SEQ ID NO. 2)
B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (3) (SEQ ID NO. 3)

where, in formulae (1) and (2), "X" represents a lysine residue, the amino group of the side chain of the lysine residue being labeled with a radioactive nuclide, and "Z-" indicates that the α-amino group at the N-terminus is not modified, or is modified with a modifying group having no electric charge; in formula (3), "B-" indicates that the α-amino group at the N-terminus is labeled with a radioactive nuclide; and in formulae (1), (2), and (3), "-NH 2 " indicates that the carboxyl group at the C-terminus is amidated.
摘要翻译：提供了一种用于胰岛成像的分子探针。分子探针包含由下式（1），（2）或（3）表示的多肽，或与前述多肽Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2（1）（SEQ ID NO.1）具有同源性的多肽， Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH 2（2）（SEQ ID NO.2）B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2（3）（SEQ ID NO.3）其中，在式（1）和（2）中，“X” 残基，用放射性核素标记赖氨酸残基侧链的氨基，“Z-”表示N末端的± - 氨基不被修饰，或者是用没有修饰的修饰基团修饰电荷; 在式（3）中，“B-”表示N末端的± - 氨基用放射性核素标记; 在式（1），（2）和（3）中，“-NH 2”表示C末端的羧基被酰胺化。

5. 发明公开

EP2510951A9 MOLECULAR PROBE FOR IMAGING OF PANCREATIC ISLET, AND USE THEREOF 有权转让
标题翻译：分子探针用于成像朗格汉斯群岛及其用途
公开(公告)号：EP2510951A9
公开(公告)日：2014-01-08
申请号：EP10836003.3
申请日：2010-12-08
申请人： Kyoto University , Arkray, Inc.
发明人： SAJI Hideo , INAGAKI Nobuya , TOYODA Kentaro , KIMURA Hiroyuki , HIRAO Konomu , NAGAKAWA Kenji , MATSUDA Hirokazu
IPC分类号： A61K51/08 , G01N33/74 , C07K1/13 , C07K14/605 , G01T1/161
CPC分类号： G01N33/74 , A61K51/088 , C07K14/605
摘要： A molecular probe for use in imaging of pancreatic islets is provided. The molecular probe comprises a polypeptide represented by the following formula (1), (2), or (3), or a polypeptide having homology with the foregoing polypeptide,
Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (1) (SEQ ID NO. 1)
Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH 2 (2) (SEQ ID NO. 2)
B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH 2 (3) (SEQ ID NO. 3)

where, in formulae (1) and (2), "X" represents a lysine residue, the amino group of the side chain of the lysine residue being labeled with a radioactive nuclide, and "Z-" indicates that the α-amino group at the N-terminus is not modified, or is modified with a modifying group having no electric charge; in formula (3), "B-" indicates that the α-amino group at the N-terminus is labeled with a radioactive nuclide; and in formulae (1), (2), and (3), "-NH 2 " indicates that the carboxyl group at the C-terminus is amidated.

6. 发明公开

EP2484386A1 MOLECULAR PROBE FOR PANCREATIC ISLET IMAGING AND USE OF SAID PROBE 有权转让
标题翻译： MOLEKULARE SONDE ZUR BILDGEBUNG DER LANGERHANS-INSELN UND VERWENDUNG DER SONDE
公开(公告)号：EP2484386A1
公开(公告)日：2012-08-08
申请号：EP10820575.8
申请日：2010-09-29
申请人： Kyoto University , Arkray, Inc.
发明人： SAJI Hideo , INAGAKI Nobuya , TOYODA Kentaro , KIMURA Hiroyuki , HIRAO Konomu , NAGAKAWA Kenji , MATSUDA Hirokazu
IPC分类号： A61K51/00 , G01T1/161
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 homology with the foregoing polypeptide.
Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH 2 (1) (SEQ I D NO. 1)
wherein "X" represents a lysine residue, the amino group of the side chain of the lysine residue being labeled with a group represented by the following formula (I),

wherein A represents an aromatic hydrocarbon group or an aromatic heterocyclic group; R 1 represents a substituent that contains 11 C, 13 N, 15 O, 18 F, 64 Cu, 67 Ga, 68 Ga, 75 Br, 76 Br, 77 Br, 99m Tc, 111 In, 123 I, 124 I, 125 I, or 131 I; R 2 represents either a hydrogen atom, or a substituent different from that represented by R 1 ; and R 3 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：提供了一种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。 Z-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPSX-NH 2（1）（SEQ ID NO.1）其中“X”表示赖氨酸残基，赖氨酸残基的侧链的氨基用下式（I）表示的基团标记，其中A表示芳族烃基或芳族杂环基; R 1表示含有11 C，13 N，15 O，18 F，64 Cu，67 Ga，68 Ga，75 Br，76 Br，77 Br，99m Tc，111 In，123 I，124 I，125 我或131我; R 2表示氢原子或与R 1表示的取代基不同的取代基; R 3表示碳原子数1〜6的亚烷基，碳原子数1〜6的氧化烯基中的任一个。

7. 发明公开

EP2404903A1 METHOD OF SYNTHESIZING [18F]SFB USING MICROSYNTHESIS TECHNIQUE 有权
标题翻译：使用显微合成技术合成[18F] SFB的方法
公开(公告)号：EP2404903A1
公开(公告)日：2012-01-11
申请号：EP10748713.4
申请日：2010-03-01
申请人： Shimadzu Corporation , Kyoto University
发明人： NAKANISHI Hiroaki , SAIKI Hidekazu , SAJI Hideo , KIMURA Hiroyuki , KAWASHIMA Hidekazu , TOMATSU Kenji , KUGE Yuji
IPC分类号： C07D207/404 , A61K51/00 , C07B59/00 , C07B61/00
CPC分类号： C07D207/404 , A61K51/00 , C07B59/001 , C07B59/002
摘要： A method for synthesizing [ 18 F]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：公开了一种用于合成[18 F] SFB的方法，其包括使用微反应器，该微反应器包括其中形成有一个通道的基板，从而具有1mm或更小的横截面宽度和1mm或更小的横截面深度，所述流路的一端与原料注入口及第一试剂注入口连接，在远离一端的位置与第二试剂注入口连接，在第三试剂注入口的位置与第二试剂注入口连接在朝向另一端的方向上远离第二试剂注入口，并且在其另一端连接到液体排出口; 而不从反应溶液的一端到另一端之间的任何地方从反应溶液的一端和另一端之间的任何位置取出反应溶液，从而使反应溶液从反应通道的一端流到另一端而连续地进行三步反应渠道。

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