公开(公告)号：US20120029209A1

公开(公告)日：2012-02-02

申请号：US13254152

申请日：2010-03-01

申请人： Hiroaki Nakanishi ,  Hidekazu Saiki ,  Hideo Saji ,  Hiroyuki Kimura ,  Hidekazu Kawashima ,  Kenji Tomatsu ,  Yuji Kuge

发明人： Hiroaki Nakanishi ,  Hidekazu Saiki ,  Hideo Saji ,  Hiroyuki Kimura ,  Hidekazu Kawashima ,  Kenji Tomatsu ,  Yuji Kuge

IPC分类号： C07D207/46

CPC分类号： C07D207/404 ,  A61K51/00 ,  C07B59/001 ,  C07B59/002

摘要： A method for synthesizing [18F]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： 公开了一种合成[18F] SFB的方法，其包括使用包括其中形成有一个通道的基板的微反应器，以使其横截面宽度为1mm以下，横截面深度为1mm以下， 所述通道在其一端连接到原料注入口和第一试剂注入口，并且在远离其一端的位置处连接到第二试剂注入口，并且连接到位于其的一端的第三试剂注入口 远离第二试剂注入口朝向其另一端的方向，并且在另一端连接到液体排出口; 并且通过使反应溶液从一端到另一端流过作为反应通道的通道而不从其一端到另一端的任何位置取出反应溶液，从而连续进行三步反应 渠道。

公开(公告)号：US20080248485A1

公开(公告)日：2008-10-09

申请号：US10593034

申请日：2005-03-18

申请人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

发明人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

IPC分类号： C07C233/75 ,  G01N33/53

CPC分类号： C07B59/001

摘要： The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter.Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.

摘要翻译： 本发明提供了一种对谷氨酸转运蛋白具有高度选择性和有效的放射性标记配体，可用于特异性检测谷氨酸转运蛋白。 具体而言，本发明提供由下式（1）表示的苯甲酰基上具有放射性取代基的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸或其酯或其盐：其中X表示取代基 含有选自直链或支链低级脂族烷基，羟基，直链或支链低级脂族烷氧基，氨基，直链或支链低级脂族酰氨基，卤素原子和 直链或支链低级脂族卤代烷基; R 1和R 2各自表示氢原子，直链或支链低级脂族烷基或乙酰氧基甲基。

公开(公告)号：US08097654B2

公开(公告)日：2012-01-17

申请号：US10593034

申请日：2005-03-18

申请人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

发明人： Keiko Shimamoto ,  Hideo Saji ,  Yuji Kuge ,  Masashi Ueda ,  Masamichi Satoh ,  Takayuki Nakagawa

IPC分类号： A61K31/166 ,  A61K31/167 ,  C07C237/40

CPC分类号： C07B59/001

摘要： The present invention provides a radiolabeled ligand which is highly selective and potent for glutamate transporters and is usable in specifically detecting the glutamate transporter.Specifically, the present invention provides a 3-[3-(benzoylamido)benzyloxy]aspartic acid having a radioactive substituent on the benzoyl group which is represented by the following formula (1), or an ester or salt thereof: wherein X represents a substituent containing a radioactive atom(s) which is selected from a straight or branched lower aliphatic alkyl group, a hydroxyl group, a straight or branched lower aliphatic alkoxy group, an amino group, a straight or branched lower aliphatic acylamido group, a halogen atom and a straight or branched lower aliphatic haloalkyl group; and R1 and R2 each represents a hydrogen atom, a straight or branched lower aliphatic alkyl group or an acetoxymethyl group.

摘要翻译： 本发明提供了一种对谷氨酸转运蛋白具有高度选择性和有效的放射性标记配体，可用于特异性检测谷氨酸转运蛋白。 具体而言，本发明提供由下式（1）表示的苯甲酰基上具有放射性取代基的3- [3-（苯甲酰氨基）苄氧基]天冬氨酸或其酯或其盐：其中X表示取代基 含有选自直链或支链低级脂族烷基，羟基，直链或支链低级脂族烷氧基，氨基，直链或支链低级脂族酰氨基，卤素原子和 直链或支链低级脂族卤代烷基; R 1和R 2各自表示氢原子，直链或支链低级脂族烷基或乙酰氧基甲基。

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。

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。

公开(公告)号：US20110033381A1

公开(公告)日：2011-02-10

申请号：US12854007

申请日：2010-08-10

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 ,  C07K14/00 ,  A61K49/00

CPC分类号： A61K51/08 ,  C07K14/435 ,  C07K14/57563 ,  Y02P20/55

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。

公开(公告)号：US09084831B2

公开(公告)日：2015-07-21

申请号：US13050672

申请日：2011-03-17

申请人： Nobuya Inagaki ,  Hideo Saji ,  Kentaro Toyoda ,  Hiroyuki Kimura ,  Konomu Hirao ,  Kenji Nagakawa

发明人： Nobuya Inagaki ,  Hideo Saji ,  Kentaro Toyoda ,  Hiroyuki Kimura ,  Konomu Hirao ,  Kenji Nagakawa

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）

公开(公告)号：US20110171129A1

公开(公告)日：2011-07-14

申请号：US13050672

申请日：2011-03-17

申请人： Nobuya Inagaki ,  Hideo Saji ,  Kentaro Toyoda ,  Hiroyuki Kimura ,  Konomu Hirao ,  Kenji Nagakawa

发明人： Nobuya Inagaki ,  Hideo Saji ,  Kentaro Toyoda ,  Hiroyuki Kimura ,  Konomu Hirao ,  Kenji Nagakawa

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）

公开(公告)号：US09278146B2

公开(公告)日：2016-03-08

申请号：US13269345

申请日：2011-10-07

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： A61K51/00 ,  A61M36/14 ,  A61K51/08 ,  C07K14/575

CPC分类号： A61K51/08 ,  A61K51/088 ,  C07K14/57563

摘要： A new peptide derivative is provided. The peptide derivative is represented by the following general formula (I), where polypeptide ExP is polypeptide that contains completely or partially the amino acid sequence of exendin-4, and a -L-Z group represents a group represented by the following formula (II) that is bonded to an amino acid side chain of or the α-amino group at the N-terminus of the polypeptide ExP,

摘要翻译： 提供了一种新的肽衍生物。 肽衍生物由以下通式（I）表示，其中多肽ExP是完全或部分含有毒蜥外泌肽-4的氨基酸序列的多肽，-LZ基团表示由下式（II）表示的基团， 与多肽ExP的N末端的氨基酸侧链或α-氨基键合，

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。