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1. 发明授权

US10358434B2 2-(3-pyridinyl)-1H-benzimidazole derivative compound and medicament containing same 有权
公开(公告)号：US10358434B2
公开(公告)日：2019-07-23
申请号：US16211434
申请日：2018-12-06
申请人： NIHON MEDI-PHYSICS CO., LTD. , Kyoto University , National Hospital Organization
发明人： Akihiro Izawa , Kei Akama , Yuki Okumura , Yurie Fukui , Nobuya Kobashi , Tsutomu Abe , Yoshihiro Doi , Miho Ikenaga , Hideo Saji , Hiroyuki Kimura , Mitsuhide Naruse
IPC分类号： C07D401/14 , A61K51/04 , A61K31/4439 , A61K51/00
摘要： Provided is a medicament comprising the compound represented by the following general formula (1) or a salt thereof: In the formula, R1, R2, R3, R4, R5, X1, X2, and X3 are defined. Methods for producing various radioactive compounds are also provided.

2. 发明授权

US10189815B2 2-(3-pyridinyl)-1H-benzimidazole derivative compound and medicine containing same 有权
公开(公告)号：US10189815B2
公开(公告)日：2019-01-29
申请号：US15321972
申请日：2015-06-25
申请人： NIHON MEDI-PHYSICS CO., LTD. , Kyoto University , National Hospital Organization
发明人： Akihiro Izawa , Kei Akama , Yuki Okumura , Yurie Fukui , Nobuya Kobashi , Tsutomu Abe , Yoshihiro Doi , Miho Ikenaga , Hideo Saji , Hiroyuki Kimura , Mitsuhide Naruse
IPC分类号： C07D401/14 , A61K51/00 , A61K31/4439 , A61K51/04
摘要： Provided is a compound represented by general formula (1) or a salt thereof as well as a medicine containing the compound or the salt. In the formula, R1, R2, R3, R4, R5, X1, X2, and X3 are defined.

3. 发明授权

US10080812B2 Radioactive iodine labeled pyrido[1,2-a]benzoimidazole derivative compound 有权
公开(公告)号：US10080812B2
公开(公告)日：2018-09-25
申请号：US15543857
申请日：2016-02-24
申请人： KYOTO UNIVERSITY , NIHON MEDI-PHYSICS CO., LTD.
发明人： Hideo Saji , Masahiro Ono , Masafumi Ihara , Ikuya Seki
IPC分类号： C07B59/00 , C07B63/04 , C07D471/04 , A61K51/04 , 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.

4. 发明申请

US20140088306A1 RADIOACTIVE FLUORINE-LABELED QUINOXALINE COMPOUND 审中-公开
标题翻译：放射性荧光标记喹啉化合物
公开(公告)号：US20140088306A1
公开(公告)日：2014-03-27
申请号：US13975980
申请日：2013-08-26
申请人： Nihon Medi-Physics Co., Ltd. , KYOTO UNIVERSITY
发明人： Hideo Saji , Masahiro Ono , Masafumi Ihara , Ikuya Seki
IPC分类号： A61K51/04
CPC分类号： A61K51/0459
摘要： Provided is a compound effective as a diagnostic imaging probe targeting amyloid and an agent for Alzheimer's disease diagnosis including the compound.
摘要翻译：提供了作为靶向淀粉样蛋白的诊断性成像探针和用于阿尔茨海默病诊断的试剂的化合物，包括该化合物。

5. 发明授权

US10081630B2 Radioactive halogen-labeled pyrido [1,2-A] benzimidazole derivative compound 有权
公开(公告)号：US10081630B2
公开(公告)日：2018-09-25
申请号：US15543849
申请日：2016-02-24
申请人： KYOTO UNIVERSITY , NIHON MEDI-PHYSICS CO., LTD.
发明人： Masahiro Ono , Hideo Saji , Masafumi Ihara , Hiroki Matsumoto , Ikuya Seki
IPC分类号： C07B59/00 , C07B63/04 , C07D471/04 , A61K51/04
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.

6. 发明申请

US20140187784A1 RADIOACTIVE QUINOLINONE DERIVATIVE AND PHARMACEUTICAL DRUG COMPRISING THE SAME 审中-公开
标题翻译：放射性喹诺酮酮衍生物和药物包装物
公开(公告)号：US20140187784A1
公开(公告)日：2014-07-03
申请号：US14134400
申请日：2013-12-19
申请人： Nihon Medi-Physics Co., Ltd. , Kyoto University
发明人： Hideo Saji , Hiroyuki Kimura , Masahiro Ono , Hiroki Matsumoto
IPC分类号： A61K51/04
CPC分类号： A61K51/0455 , C07D471/04
摘要： It is intended to provide a radioactive compound that has higher selectivity for CYP11B2 than that for CYP11B1, exhibits highly selective accumulation in the adrenal gland compared with blood and organs adjacent to the adrenal gland, and permits commercial supply. The present invention provides a radioactive quinolinone derivative represented by the predetermined general formula or a salt thereof.
摘要翻译：旨在提供对CYP11B2具有比CYP11B1更高选择性的放射性化合物，与邻近肾上腺的血液和器官相比，在肾上腺中表现出高度选择性的积累，并且允许商业供应。本发明提供由预定的通式表示的放射性喹啉酮衍生物或其盐。

7. 发明申请

US20140127128A1 Molecular Probe for Imaging of Pancreatic Islets and Use of the Same 审中-公开
标题翻译：胰岛成像用分子探针及其用途
公开(公告)号：US20140127128A1
公开(公告)日：2014-05-08
申请号：US14109769
申请日：2013-12-17
申请人： ARKRAY, INC. , Kyoto University
发明人： Nobuya Inagaki , Hideo Saji , Kentaro Toyoda , Hiroyuki Kimura , Yu Ogawa
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。（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。

8. 发明授权

US10029022B2 Nuclear medicine diagnostic imaging agent 有权
公开(公告)号：US10029022B2
公开(公告)日：2018-07-24
申请号：US15140572
申请日：2016-04-28
申请人： Kyoto University , ARKRAY, Inc.
发明人： Hideo Saji , Hiroyuki Kimura , Hirokazu Matsuda , Shuichi Nakanishi
IPC分类号： A61K51/04 , C07B59/00 , C07D471/04
摘要： Provided is a radioactive labeled compound capable of detecting a secondary mutation of an epidermal growth factor receptor, where the compound is represented by Formula (1) or a pharmaceutically acceptable salt thereof, where Y, L1, R1 and R2 are as defined.

9. 发明申请

US20170000913A1 Nuclear Medicine Diagnostic Imaging Agent 审中-公开
标题翻译：核医学诊断成像剂
公开(公告)号：US20170000913A1
公开(公告)日：2017-01-05
申请号：US15200346
申请日：2016-07-01
申请人： Kyoto University , ARKRAY, Inc.
发明人： Hideo Saji , Hiroyuki Kimura , Anna Miyazaki , Hirokazu Matsuda , Shuichi Nakanishi
IPC分类号： A61K51/04 , C07D495/14 , A61K49/00
摘要： Provided is a radioactive labeled compound capable of detecting a secondary mutation of an epidermal growth factor receptor, where the compound is represented by Formula (1) or a pharmaceutically acceptable salt thereof, where R1, R2, and Y are as defined.
摘要翻译：本发明提供能够检测表皮生长因子受体的二次突变的放射性标记化合物，其为式（1）表示的化合物或其药学上可接受的盐。式（1）中，R 1为式（a），（b）或（c）所示的基团，R 2为式（d）或（e）所示的基团，Y为-NH-或 - O-。

10. 发明申请

US20150352233A1 Polypeptide and Imaging Method 有权
标题翻译：多肽和成像方法
公开(公告)号：US20150352233A1
公开(公告)日：2015-12-10
申请号：US14648467
申请日：2013-11-29
申请人： KYOTO UNIVERSITY , ARKRAY, INC.
发明人： Hideo Saji , Nobuya Inagaki , Hiroyuki Kimura , Kentaro Toyoda , Hirokazu Matsuda , Mikako Ioroi , Asami Kon
IPC分类号： A61K51/08 , C07K14/00
CPC分类号： A61K51/08 , A61K49/0423 , B82Y5/00 , C07K1/13 , C07K14/001 , C07K14/605 , C07K14/705 , G01N33/50 , G01N2800/042
摘要： A peptide that can be used as an imaging probe for GLP-1R is provided. In an embodiment, a polypeptide is represented by the following formula (3); (Sequence ID No. 3) Xaa1-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg- Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser- Ser-Gly-Ala-Pro-Pro-Pro-Ser (3) where Xaa1 represents an aspartic acid in which a —Y—X′ group binds to an α-amino group, X′ includes a chelating site and a radioactive metal nuclide chelated by the chelating site, the chelating site being diethylenetriaminepentaacetic dianhydride (DTPA) or 1,4,7-triazacyclononnane-N,N′,N″-triacetic acid (NOTA), and Y represents a linker including a group selected from the group consisting of —CH2—(C6H4)—, —NH—C(═S)—, —NH—(CH2)5—C(═O)—, and a combination thereof.
摘要翻译：提供了可用作GLP-1R成像探针的肽。在一个实施方案中，多肽由下式（3）表示; （序列号3）Xaa1-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly -Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser（3）其中Xaa1表示-Y-X'基团与α-氨基结合的天冬氨酸，X'包括螯合位点和由螯合位点螯合的放射性金属核素，螯合位点是二亚乙基三胺五乙酸二酐（DTPA）或1,4,7-三氮杂环壬烷-N，N'，N“ - 三乙酸（NOTA），Y表示连接体，基团选自-CH 2 - （C 6 H 4） - ， - NH-C（= S） - ， - NH-（CH 2）5 -C（= O） - 及其组合。

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