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21. 发明授权

US09044520B2 Compound accumulating in inflammatory site, diagnostic agent containing the compound in labeled state and its precursor compound for labeling 有权
标题翻译：化合物累积在炎症部位，含有标记状态的化合物的诊断剂及其前体化合物进行标记
公开(公告)号：US09044520B2
公开(公告)日：2015-06-02
申请号：US13434722
申请日：2012-03-29
申请人： Hideo Saji , Hiroyuki Kimura , Masahiro Ono , Ikuya Seki
发明人： Hideo Saji , Hiroyuki Kimura , Masahiro Ono , Ikuya Seki
IPC分类号： A61K51/00 , A61M36/14 , A61K51/08
CPC分类号： A61K51/088 , G01N2800/042
摘要： Embodiments of the invention provide a compound accumulating in an inflammatory site, a diagnostic agent containing the compound in labeled state and its precursor compound for labeling. Such a compound accumulating in inflammatory site may be represented by the following formula (1): Z—Y-Leu-Phe-(X)n-DLys(-(DLys)m-HalB)-(DLys)k-NH2 (1) wherein in the formula (1), Z represents a protective group for an amino group; Y represents Met or Nle; X represents a spacer consisting of one or more of amino acid and/or synthetic organic compounds; n represents 1 or 0; m represents 1 or 0; k represents 1 or 0; and HalB represents a substituted benzoic acid having a radioactive halogen in an aromatic ring.
摘要翻译：本发明的实施方案提供了一种在炎症部位中积聚的化合物，含有标记状态的化合物的诊断剂及其用于标记的前体化合物。 Z-Y-Leu-Phe-（X）n-DLys（ - （DLys）m-HalB） - （DLys）k-NH 2（1）的化合物可以由下述式（1）表示：）其中在式（1）中，Z表示氨基的保护基; Y表示Met或Nle; X表示由一种或多种氨基酸和/或合成有机化合物组成的间隔物; n表示1或0; m表示1或0; k表示1或0; HalB表示在芳香环中具有放射性卤素的取代苯甲酸。

22. 发明授权

US08980220B2 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：US08980220B2
公开(公告)日：2015-03-17
申请号：US12964486
申请日：2010-12-09
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： C07K14/605 , G01N33/74 , A61K51/08
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, (SEQ ID NO. 1) Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) (SEQ ID NO. 2) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (2) (SEQ ID NO. 3) B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (3) where, in the formulae (1) and (2), “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a radioactive nuclide, and “Z—” indicates that an α-amino group at an N-terminus is not modified, or is modified with a modifying group having no electric charge; in the formula (3), “B—” indicates that an α-amino group at an N-terminus is labeled with a radioactive nuclide; and in the formulae (1), (2), and (3), “—NH2” indicates that a carboxyl group at a 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，或与前述多肽具有同源性的多肽（SEQ ID NO.1）Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（1）（ SEQ ID NO.2）Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2（2）（SEQ ID NO.3）B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（3）其中，在式（1）和（2）中，“X”表示赖氨酸残基，赖氨酸残基的侧链的氨基被放射性核素标记，“Z-”表示N末端的α-氨基未被修饰，或者是用不具有电荷的修饰基团修饰 ; 在式（3）中，“B-”表示N末端的α-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。

23. 发明申请

US20130149252A1 SWITCHING FLUORESCENT NANOPARTICLE PROBE AND FLUORESCENT PARTICLE IMAGING METHOD USING SAME 有权
标题翻译：切换荧光纳米粒子探针和使用其的荧光颗粒成像方法
公开(公告)号：US20130149252A1
公开(公告)日：2013-06-13
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： 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。

24. 发明申请

US20120330024A1 RADIOACTIVE IODINE LABELED ORGANIC COMPOUND OR SALT THEREOF 失效
标题翻译：放射性标记有机化合物或其盐
公开(公告)号：US20120330024A1
公开(公告)日：2012-12-27
申请号：US13582047
申请日：2011-02-24
申请人： Hideo Saji , Masahiro Ono , Ikuya Seki
发明人： Hideo Saji , Masahiro Ono , Ikuya Seki
IPC分类号： C07D405/06 , C07F7/22 , C07D405/14 , C07D417/06 , C07D417/14
CPC分类号： C07D417/06 , A61K51/0453 , C07D405/06 , C07D405/14
摘要： The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.
摘要翻译：本发明是由下式（1）表示的化合物或其盐。此外，本发明是用于成像tau蛋白的成像剂，该成像剂含有下述式（1）表示的化合物或其盐。在式（1）中，R 3是放射性碘。

25. 发明申请

US20120253010A1 COMPOUND ACCUMULATING IN INFLAMMATORY SITE, DIAGNOSTIC AGENT CONTAINING THE COMPOUND IN LABELED STATE AND ITS PRECURSOR COMPOUND FOR LABELING 有权
标题翻译：包含化合物在标签状态的诊断试剂盒及其前体化合物标签中的化合物累积
公开(公告)号：US20120253010A1
公开(公告)日：2012-10-04
申请号：US13434722
申请日：2012-03-29
申请人： Hideo Saji , Hiroyuki Kimura , Masahiro Ono , Ikuya Seki
发明人： Hideo Saji , Hiroyuki Kimura , Masahiro Ono , Ikuya Seki
IPC分类号： C07K7/06
CPC分类号： A61K51/088 , G01N2800/042
摘要： Embodiments of the invention provide a compound accumulating in an inflammatory site, a diagnostic agent containing the compound in labeled state and its precursor compound for labeling. Such a compound accumulating in inflammatory site may be represented by the following formula (1): Z—Y-Leu-Phe-(X)n-DLys(-(DLys)m-HalB)-(DLys)k-NH2 (1) wherein in the formula (1), Z represents a protective group for an amino group; Y represents Met or Nle; X represents a spacer consisting of one or more of amino acid and/or synthetic organic compounds; n represents 1 or 0; m represents 1 or 0; k represents 1 or 0; and HalB represents a substituted benzoic acid having a radioactive halogen in an aromatic ring.
摘要翻译：本发明的实施方案提供了一种在炎症部位中积聚的化合物，含有标记状态的化合物的诊断剂及其用于标记的前体化合物。 Z-Y-Leu-Phe-（X）n-DLys（ - （DLys）m-HalB） - （DLys）k-NH 2（1）的化合物可以由下述式（1）表示：）其中在式（1）中，Z表示氨基的保护基; Y表示Met或Nle; X表示由一种或多种氨基酸和/或合成有机化合物组成的间隔物; n表示1或0; m表示1或0; k表示1或0; HalB表示在芳香环中具有放射性卤素的取代苯甲酸。

26. 发明申请

US20110206605A1 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：US20110206605A1
公开(公告)日：2011-08-25
申请号：US12964486
申请日：2010-12-09
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： A61K51/08 , C07K14/00 , C07K1/13 , C12Q1/02
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, (SEQ ID NO. 1) Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (1) (SEQ ID NO. 2) Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2 (2) (SEQ ID NO. 3) B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2 (3) where, in the formulae (1) and (2), “X” represents a lysine residue, an amino group of a side chain of the lysine residue being labeled with a radioactive nuclide, and “Z—” indicates that an α-amino group at an N-terminus is not modified, or is modified with a modifying group having no electric charge; in the formula (3), “B—” indicates that an α-amino group at an N-terminus is labeled with a radioactive nuclide; and in the formulae (1), (2), and (3), “—NH2” indicates that a carboxyl group at a 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，或与前述多肽具有同源性的多肽（SEQ ID NO.1）Z-HGEGTFTSDLSXQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（1）（ SEQ ID NO.2）Z-HGEGTFTSDLSKQMEEEAVRLFIEWLXNGGPSSGAPPPS-NH2（2）（SEQ ID NO.3）B-HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS-NH2（3）其中，在式（1）和（2）中，“X”表示赖氨酸残基，赖氨酸残基的侧链的氨基被放射性核素标记，“Z-”表示N末端的α-氨基未被修饰，或者是用不具有电荷的修饰基团修饰 ; 在式（3）中，“B-”表示N末端的α-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。

27. 发明申请

US20110059483A1 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：US20110059483A1
公开(公告)日：2011-03-10
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： C12Q1/04 , C07K14/00 , C12Q1/06
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; 和与上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）中的B-表示氨基被具有芳环的式（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，R 2表示氢原子或取代基与R1表示的不同，R3表示键，亚甲基和甲醛基中的任一个。

28. 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。

29. 发明授权

US09849197B2 Switching-type fluorescent nanoparticle probe, and fluorescent molecular imaging method using same 有权
公开(公告)号：US09849197B2
公开(公告)日：2017-12-26
申请号：US14002327
申请日：2012-03-01
申请人： Hideo Saji , Shunsaku Kimura , Masahiro Ono , Takashi Temma , Isao Hara , Eiichi Ozeki
发明人： Hideo Saji , Shunsaku Kimura , Masahiro Ono , Takashi Temma , Isao Hara , Eiichi Ozeki
IPC分类号： A61K9/00 , A61K49/00
CPC分类号： A61K49/0054 , A61K49/0032 , A61K49/0034 , A61K49/0069 , A61K49/0093
摘要： [Problem] To provide a novel fluorescent nanoparticle imaging probe having a switching function (a function to quench a fluorescent dye in a blood component and emit fluorescence in a tumor or an inflamed site to be imaged).[Solution] A 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 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 polylactic acid-bound cyanine compound comprising: a fluorescent group represented by the formula (I): and a polylactic acid group having 5 to 50 lactic acid units, and two or more molecules of the fluorescent dye are encapsulated in the single molecular assembly.

30. 发明授权

US08476449B2 Radioactive iodine labeled organic compound or salt thereof 失效
标题翻译：放射性碘标记的有机化合物或其盐
公开(公告)号：US08476449B2
公开(公告)日：2013-07-02
申请号：US13582047
申请日：2011-02-24
申请人： Hideo Saji , Masahiro Ono , Ikuya Seki
发明人： Hideo Saji , Masahiro Ono , Ikuya Seki
IPC分类号： C07D405/06 , C07D405/14 , C07D417/06 , C07D417/14 , C07F7/22
CPC分类号： C07D417/06 , A61K51/0453 , C07D405/06 , C07D405/14
摘要： The present invention is a compound represented by the following formula (1) or a salt thereof. Furthermore, the present invention is an imaging agent used for imaging a tau protein, the imaging agent containing a compound represented by the formula (1) below or a salt thereof. In the formula (1), R3 is a radioactive iodine.
摘要翻译：本发明是由下式（1）表示的化合物或其盐。此外，本发明是用于成像tau蛋白的成像剂，该成像剂含有下述式（1）表示的化合物或其盐。在式（1）中，R 3是放射性碘。

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