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1.发明申请公开(公告)号：US20220370651A1
公开(公告)日：2022-11-24
申请号：US17869104
申请日：2022-07-20
发明人： Yoshio HONDA , Taku ITO , Jun ICHINOSE , Hiroaki ICHIKAWA , Tomoyuki IMAI , Kotaro NAGATSU , Hisashi SUZUKI
摘要： A method for producing an 225Ac solution includes a step (I) of irradiating a 226Ra target with particles to generate two or more actinium radioisotopes (Ac) including at least 225Ac, a step (II) of dissolving the 226Ra target after the aforementioned step to obtain a solution (1), a step (III) of separating 226Ra and Ac contained in the solution (1) to obtain a solution (2), a step (IV) of allowing Ac contained in the solution (2) other than 225Ac to decay to obtain a solution (3), and a step (V) of separating Ra and Ac contained in the solution (3) to obtain a solution (4). The solution (4) is used to produce a medicine that contains, as an active ingredient, a conjugate between a chelating agent that has formed a complex with 225Ac, and a targeting agent.
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2.发明公开公开(公告)号：US20230364275A1
公开(公告)日：2023-11-16
申请号：US18349201
申请日：2023-07-10
发明人： Yoshio HONDA , Taku ITO , Jun ICHINOSE , Hiroaki ICHIKAWA , Tomoyuki IMAI , Kotaro NAGATSU , Hisashi SUZUKI
CPC分类号： A61K51/088 , A61K51/0497
摘要： A method for producing an 225Ac solution includes a step (I) of irradiating a 226Ra target with particles to generate two or more actinium radioisotopes (Ac) including at least 225Ac, a step (II) of dissolving the 226Ra target after the aforementioned step to obtain a solution (1), a step (III) of separating 226Ra and Ac contained in the solution (1) to obtain a solution (2), a step (IV) of allowing Ac contained in the solution (2) other than 225Ac to decay to obtain a solution (3), and a step (V) of separating Ra and Ac contained in the solution (3) to obtain a solution (4). The solution (4) is used to produce a medicine that contains, as an active ingredient, a conjugate between a chelating agent that has formed a complex with 225Ac, and a targeting agent.
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公开(公告)号：US20240002411A1
公开(公告)日：2024-01-04
申请号：US18249837
申请日：2021-10-14
CPC分类号： C07F7/003 , A61K51/088 , A61K51/1096 , A61K51/0491
摘要： The present invention relates to a method for producing a radioactive zirconium-labeled complex that can realize a high labeling index in a reaction between a radioactive zirconium ion and a ligand compound. The production method of the present invention includes a step of reacting a radioactive zirconium ion with a ligand compound in a reaction solution containing water to coordinate the radioactive zirconium ion. This step is performed in a state where the pH of the reaction solution is in an acidic region. The reaction solution does not contain an organic solvent but contains a water-soluble organic compound having one or two sulfo groups or carboxy groups in its structure, separately from the ligand compound.
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公开(公告)号：US20240174622A1
公开(公告)日：2024-05-30
申请号：US18548716
申请日：2022-03-02
IPC分类号： C07D257/02 , A61K31/395 , A61K51/04 , C07B59/00
CPC分类号： C07D257/02 , A61K31/395 , A61K51/0482 , C07B59/004 , C07B2200/05
摘要： The compound of the present invention includes a structure having: a chelating part capable of coordinating with a radioactive metal ion; a first atomic group containing an albumin-binding part; and a second atomic group containing a PSMA molecule-binding part, wherein the first atomic group and the second atomic group are bonded with each other through the chelating part, or the chelating part is bonded from between the first atomic group and the second atomic group so that it makes a branch. The present invention also provides: a radiolabeled compound in which the compound is coordinated with a radioactive metal ion; and a method for manufacturing a radiolabeled compound.
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公开(公告)号：US20230390426A1
公开(公告)日：2023-12-07
申请号：US18249753
申请日：2021-10-14
CPC分类号： A61K51/1096 , A61K51/088 , A61K51/0491
摘要： A method for producing a radioactive zirconium complex of the present invention includes a step of reacting a radioactive zirconium ion, a ligand compound containing DOTA or a DOTA derivative, and an additive such as hydroxybenzoic acid and a derivative thereof with one another in a reaction solution to form a radioactive zirconium complex. As the reaction solution, a reaction solution is used in which the amount of radioactivity of the radioactive zirconium ion is 60 MBq or more at the start of the reaction and the amount of radioactivity of the radioactive zirconium ion is 5 MBq or more per 1 nmol of the ligand compound at the start of the reaction.
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![2-[5-(IMIDAZOL-1-YLMETHYL)PYRIDIN-3-YL]BENZIMIDAZOLE DERIVATIVE COMPOUND, AND MEDICAMENT INCLUDING SAME](/abs-image/US/2021/03/04/US20210060186A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210060186A1
公开(公告)日：2021-03-04
申请号：US16958427
申请日：2018-12-20
发明人： Akihiro IZAWA , Yuki OKUMURA , Yurie FUKUI , Hiroaki ICHIKAWA , Yoshifumi MAYA , Miho IKENAGA , Hiroyuki OKUDAIRA , Yoshihiro DOI , Mitsuhide NARUSE
IPC分类号： A61K51/04 , C07B59/00 , C07D401/14
摘要： Provided are a compound represented by the following formula (1): wherein X1 represents a hydrogen atom or a halogen atom, X2 represents a fluorine atom or a nitrile group, and X3 represents a radioactive halogen atom, or a salt thereof, and a medicament including the same.
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7.发明申请公开(公告)号：US20200009273A1
公开(公告)日：2020-01-09
申请号：US16491046
申请日：2018-03-05
发明人： Masato KIRIU , Hiroaki ICHIKAWA , Yuki OKUMURA , Hiroshi TANAKA
IPC分类号： A61K51/04 , C07B59/00 , C07C309/77 , C07C41/22 , C07C43/174 , C07D401/14 , C07D471/04
摘要： There is provided a labeling precursor compound represented by the general formula (2): wherein S represents a substrate, L represents a straight alkyl group having 1 to 6 carbon atoms which may contain an ether group, R1 and R2 each independently represent a straight or branched alkyl group having 1 to 30 carbon atoms, or a substituted or unsubstituted monocyclic or condensed polycyclic aryl group, R3 each independently represent an alkyl group having 1 to 4 carbon atoms or an alkoxy group having 1 to 4 carbon atoms, and p represents an integer of 0 to 4.
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公开(公告)号：US20230248854A1
公开(公告)日：2023-08-10
申请号：US17769657
申请日：2020-10-16
发明人： Akihiro IZAWA , Yu OGAWA , Hiroaki ICHIKAWA , Minoru KAWATANI , Hideaki TAKEMORI , Yuki OKUMURA
IPC分类号： A61K51/10
CPC分类号： A61K51/10
摘要： The production method of a radioactive metal-labeled antibody of the present invention includes a step of conducting a click reaction of a radioactive metal complex and an antibody site-specifically modified with a peptide to produce a radioactive metal-labeled antibody. The click reaction is performed between a first atomic group of the radioactive metal complex and a second atomic group directly or indirectly linked to the peptide. The second atomic group is an atomic group containing an azide group, or an atomic group containing trans-cyclooctene.
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