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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: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:US20240293586A1
公开(公告)日:2024-09-05
申请号:US18293488
申请日:2022-07-29
Applicant: OSAKA UNIVERSITY
Inventor: Yoshifumi SHIRAKAMI , Kazuko KANEDA , Yuichiro KADONAGA , Tadashi WATABE , Atsushi TOYOSHIMA , Koichi FUKASE , Taku YOSHIYA
CPC classification number: A61K51/088 , A61P35/00 , A61K2121/00
Abstract: The aims of the present invention are to provide an agent that binds specifically to PSMA, is effective in the treatment and diagnosis of tumors or cancers expressing PSMA, for example, the treatment and diagnosis of prostate cancer, especially castration-resistant prostate cancer (CRPC), further especially metastatic castration-resistant prostate cancer (mCRPC), and does not exhibit side effects due to accumulation in the kidney or salivary glands. The present invention provides a radiolabeled compound represented by Formula (I) or a pharmaceutically acceptable salt thereof:
wherein each symbol is as defined in the description.-
公开(公告)号:US20240124496A1
公开(公告)日:2024-04-18
申请号:US18551674
申请日:2022-03-24
Applicant: OSAKA UNIVERSITY
Inventor: Yoshifumi SHIRAKAMI , Kazuko KANEDA , Yuichiro KADONAGA , Tadashi WATABE , Atsushi TOYOSHIMA , Koichi FUKASE , Atsushi SHINOHARA , Toshio YAMANAKA , Yutaka KONDOH
CPC classification number: C07F5/025 , B01J31/2295 , B01J31/2409 , C07B59/00 , C07C227/16 , C07F13/00 , B01J2231/40 , B01J2531/004 , B01J2531/824 , B01J2531/842 , C07B2200/05
Abstract: The invention provides a method for producing radiolabeled tyrosine derivatives with good purity and stability, by a safe method suitable for industrial production of pharmaceuticals. The invention relates to a method for producing Compound (5) and Radiolabeled Compound (6) as follows:
wherein each symbol is as defined in the description.-
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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