Molecular probe for imaging of pancreatic islets and use of the same
    1.
    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

    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 ISLET AND THE PRECURSOR, AND USE OF THE SAME
    2.
    发明申请
    MOLECULAR PROBE FOR IMAGING OF PANCREATIC ISLET AND THE PRECURSOR, AND USE OF THE SAME 审中-公开
    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

    IPC分类号: A61K51/08 C07K14/00 A61K49/00

    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。

    Molecular Probe for Imaging of Pancreatic Islets and Use of the Same
    3.
    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

    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。

    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:US20110081663A1

    公开(公告)日:2011-04-07

    申请号:US12893896

    申请日:2010-09-29

    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。

    Molecular probe for imaging of pancreatic islets and use of the same
    5.
    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

    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
    6.
    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

    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
    7.
    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

    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 precursor for imaging of pancreatic islet, and use thereof
    8.
    发明授权
    Molecular probe precursor for imaging of pancreatic islet, and use thereof 有权
    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

    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)

    Molecular Probe Precursor for Imaging of Pancreatic Islet, and Use Thereof
    10.
    发明申请
    Molecular Probe Precursor for Imaging of Pancreatic Islet, and Use Thereof 有权
    胰岛成像用分子探针前体及其用途

    公开(公告)号:US20110171129A1

    公开(公告)日:2011-07-14

    申请号:US13050672

    申请日:2011-03-17

    IPC分类号: A61K51/08 C07K14/00 C07K1/13

    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)