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    Molecular probe for imaging of pancreatic islets and use of the same
    2.
    发明授权
    Molecular probe for imaging of pancreatic islets and use of the same 有权
    胰岛成像用分子探针及其用途

    公开(公告)号：US09238083B2

    公开(公告)日：2016-01-19

    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： A61K51/08 ,  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。

    Molecular probe for imaging of pancreatic islets and use of the same
    3.
    发明授权
    Molecular probe for imaging of pancreatic islets and use of the same 有权
    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。

    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same
    4.
    发明申请
    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same 有权
    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。

    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same
    5.
    发明申请
    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same 有权
    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。

    Method for Producing Radioactively Labeled Polypeptide
    6.
    发明申请
    Method for Producing Radioactively Labeled Polypeptide 审中-公开
    生产放射性标记多肽的方法

    公开(公告)号：US20130052132A1

    公开(公告)日：2013-02-28

    申请号：US13369903

    申请日：2012-02-09

    申请人： Hideo Saji ,  Nobuya Inagaki ,  Hiroyuki Kimura ,  Kentaro Toyoda ,  Konomu Hirao ,  Hirokazu Matsuda

    发明人： Hideo Saji ,  Nobuya Inagaki ,  Hiroyuki Kimura ,  Kentaro Toyoda ,  Konomu Hirao ,  Hirokazu Matsuda

    IPC分类号： C07K14/00 ,  A61K51/08

    CPC分类号： C07K14/57563 ,  A61K51/088 ,  C07K1/13

    摘要： The present invention relates to a method for producing a polypeptide. The method includes labeling a molecular probe precursor represented by an amino acid sequence of the formula (1) using a labeling compound capable of labeling a lysine or lysine derivative: (1) Y1-Leu-Ser-Xaa12-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg- Leu-Phe-Ile-Glu-Trp-Leu-Xaa27-Asn-Gly-Y2 where Y1 represents an amino acid sequence represented by the formula (2) or the amino acid sequence represented by the formula (2) with 1 to 8 amino acids from the N-terminus being deleted, Xaa12 represents a lysine or lysine derivative, Xaa27 represents a basic amino acid having no functional group at its side chain that reacts with the labeling compound or represents methyl lysine or acetylated lysine, and Y2 represents an amino acid sequence represented by the formula (3) or the amino acid sequence represented by the formula (3) with 1 to 9 amino acids from the C-terminus being deleted: (2) His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp (3) Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser

    摘要翻译： 本发明涉及一种生产多肽的方法。 该方法包括使用能够标记赖氨酸或赖氨酸衍生物的标记化合物来标记由式（1）的氨基酸序列表示的分子探针前体：（1）Y1-Leu-Ser-Xaa12-Gln-Met-Glu- Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Xaa27-Asn-Gly-Y2，其中Y1表示由式（2）表示的氨基酸序列或由 缺失N末端1〜8个氨基酸的式（2），Xaa12表示赖氨酸或赖氨酸衍生物，Xaa27表示其侧链上没有与标记化合物反应的官能团的碱性氨基酸， 赖氨酸或乙酰化赖氨酸，Y2表示由式（3）表示的氨基酸序列或由式（3）表示的氨基酸序列，其中C末端具有1至9个氨基酸缺失：（2）His- Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp（3）Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro

    Molecular probe for imaging of pancreatic islets and use of the same
    9.
    发明授权
    Molecular probe for imaging of pancreatic islets and use of the same 有权
    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。

    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same
    10.
    发明申请
    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same 有权
    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。