公开(公告)号：US20180256760A1

公开(公告)日：2018-09-13

申请号：US15977522

申请日：2018-05-11

Applicant: NIHON MEDI-PHYSICS CO., LTD.

Inventor： Osamu ITO ,  Akio HAYASHI ,  Fumie KUROSAKI ,  Masahito TOYAMA ,  Toshiyuki SHINMURA ,  Arinori HARANO

IPC: A61K51/04 ,  C07C67/307 ,  C07C309/65 ,  C07B59/00

CPC classification number: A61K51/0402 ,  A61K51/0406 ,  C07B59/00 ,  C07B2200/05 ,  C07C67/307 ,  C07C309/65 ,  C07C2601/04 ,  Y02P20/55

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

公开(公告)号：US20210386873A1

公开(公告)日：2021-12-16

申请号：US17356757

申请日：2021-06-24

Applicant: NIHON MEDI-PHYSICS CO., LTD.

Inventor： Osamu ITO ,  Akio HAYASHI ,  Fumie KUROSAKI ,  Masahito TOYAMA ,  Toshiyuki SHINMURA ,  Arinori HARANO

IPC: A61K51/04 ,  C07B59/00 ,  C07C309/65 ,  C07C67/307

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

公开(公告)号：US20200282082A1

公开(公告)日：2020-09-10

申请号：US16852910

申请日：2020-04-20

Applicant: NIHON MEDI-PHYSICS CO., LTD.

Inventor： Osamu ITO ,  Akio HAYASHI ,  Fumie KUROSAKI ,  Masahito TOYAMA ,  Toshiyuki SHINMURA ,  Arinori HARANO

IPC: A61K51/04 ,  C07B59/00 ,  C07C309/65 ,  C07C67/307

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

公开(公告)号：US20160000944A1

公开(公告)日：2016-01-07

申请号：US14814185

申请日：2015-08-21

Applicant: NIHON MEDI-PHYSICS CO., LTD.

Inventor： Osamu ITO ,  Akio Hayashi ,  Fumie Kurosaki ,  Masahito Toyama ,  Toshiyuki Shinmura ,  Arinori Harano

IPC: A61K51/04

CPC classification number: A61K51/0402 ,  A61K51/0406 ,  C07B59/00 ,  C07B2200/05 ,  C07C67/307 ,  C07C309/65 ,  C07C2601/04 ,  Y02P20/55

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

公开(公告)号：US20140213817A1

公开(公告)日：2014-07-31

申请号：US14246594

申请日：2014-04-07

Applicant: Nihon-Medi-Physics Co., Ltd.

Inventor： Osamu ITO ,  Akio Hayashi ,  Fumie Kurosaki ,  Masahito Toyama ,  Toshiyuki Shinmura ,  Arinori Harano

IPC: C07C67/307

CPC classification number: A61K51/0402 ,  A61K51/0406 ,  C07B59/00 ,  C07B2200/05 ,  C07C67/307 ,  C07C309/65 ,  C07C2601/04 ,  Y02P20/55

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

Abstract translation: 旨在提供一种新的氨基酸有机化合物，其可以用作包括[18 F] FACBC的放射性卤素标记的氨基酸化合物的标记前体化合物，并且其防止甲醇残留在所产生的放射性卤素标记的氨基酸化合物中 由此。 新型氨基酸有机化合物是下式表示的化合物：其中，n为0或1〜4的整数， R1是乙基，1-丙基或异丙​​基取代基; X是卤素取代基或由-OR2表示的基团; R2是具有1至10个碳原子的直链或支链卤代烷基磺酸取代基，具有3至12个碳原子的三烷基甲锡烷基取代基，氟磺酸取代基或芳族磺酸取代基; R3为保护基。