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公开(公告)号:US20230331640A1
公开(公告)日:2023-10-19
申请号:US18337623
申请日:2023-06-20
Applicant: OSAKA UNIVERSITY
Inventor: Yoshifumi SHIRAKAMI , Hayato IKEDA , Yasukazu KANAI , Eku SHIMOSEGAWA , Jun HATAZAWA , Tadashi WATABE , Kazuko KANEDA
CPC classification number: C07B59/001 , C07F13/00 , C07B59/004 , C07F5/025 , C07F13/005 , C07B2200/05
Abstract: The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is 211At, 210At, 123I, 124I, 125I, or 131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 211At, 210At, 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.
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公开(公告)号:US20210000988A1
公开(公告)日:2021-01-07
申请号:US16979346
申请日:2019-02-22
Applicant: OSAKA UNIVERSITY
Inventor: Koichi FUKASE , Atsushi SHINOHARA , Yoshikatsu KANAI , Kazuya KABAYAMA , Kazuko KANEDA , Zijian ZHANG , Jun HATAZAWA , Yoshifumi SHIRAKAMI , Atsushi SHIMOYAMA , Yoshiyuki MANABE
Abstract: To develop a compound which is highly accumulated in cancer cells and capable of emitting an α-ray and provide a pharmaceutical composition for cancer treatment including the compound.
A pharmaceutical composition for cancer treatment including a compound having a structure in which 211At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.-
公开(公告)号:US20200369578A1
公开(公告)日:2020-11-26
申请号:US16636236
申请日:2018-08-03
Applicant: OSAKA UNIVERSITY
Inventor: Yoshifumi SHIRAKAMI , Hayato IKEDA , Yasukazu KANAI , Eku SHIMOSEGAWA , Jun HATAZAWA , Tadashi WATABE , Kazuko KANEDA
Abstract: The invention relates to a method of producing the radiolabeled aryl compound (I) Ar—X, or a salt thereof, wherein X is 211At, 210At, 123I, 124I, 125I, or 131I. The method involves reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 211At, 210At, 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from an alkali metal iodide, an alkali metal bromide, N-bromosuccinimide, N-chlorosuccinimide and hydrogen peroxide, in water.
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公开(公告)号:US20230302169A1
公开(公告)日:2023-09-28
申请号:US18317224
申请日:2023-05-15
Applicant: OSAKA UNIVERSITY
Inventor: Yoshifumi SHIRAKAMI , Tadashi WATABE , Kazuko KANEDA , Eku SHIMOSEGAWA , Atsushi SHINOHARA , Jun HATAZAWA
CPC classification number: A61K51/121 , A61K47/22
Abstract: The invention provides a method for producing a solution containing 211At− (astatide ion) at a high radiochemical purity by using 211At obtained by a nuclear reaction as a starting material, including a step of adding a reducing agent to a solution containing an impurity derived from 211At. The invention also provides a solution containing 211At− (astatide ion) at a radiochemical purity of not less than 30%.
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公开(公告)号:US20220387636A1
公开(公告)日:2022-12-08
申请号:US17882708
申请日:2022-08-08
Applicant: OSAKA UNIVERSITY
Inventor: Koichi FUKASE , Atsushi SHINOHARA , Yoshikatsu KANAI , Kazuya KABAYAMA , Kazuko KANEDA , Zijian ZHANG , Jun HATAZAWA , Yoshifumi SHIRAKAMI , Atsushi SHIMOYAMA , Yoshiyuki MANABE
IPC: A61K51/04
Abstract: To develop a compound which is highly accumulated in cancer cells and capable of emitting an α-ray and provide a pharmaceutical composition for cancer treatment including the compound.
A pharmaceutical composition for cancer treatment including a compound having a structure in which 211At is introduced as a substituent into an amino acid derivative having an affinity with an amino acid transporter LAT1 or a pharmaceutically acceptable salt of the compound.
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