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公开(公告)号：US20240316228A1
公开(公告)日：2024-09-26
申请号：US18688001
申请日：2022-08-31
发明人： Satoshi KISHIMOTO , Takuya TAKEDA , Yudai NARITA , Minoru KAWATANI , Akihiro IZAWA , Yuta TARUMIZU
CPC分类号： A61K51/1096 , A61P35/00
摘要： Provided is a conjugate of a chelating agent chelated with a radionuclide and a deglycosylated antibody, where the chelating agent site-specifically modifies the Fc region of the aforementioned antibody via a linker. The conjugate shows increased accumulation in a tumor and decreased accumulation in normal tissues. These differences in accumulation are associated with a decrease in a risk of side effects.
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公开(公告)号：US20240207464A1
公开(公告)日：2024-06-27
申请号：US18556527
申请日：2022-04-20
CPC分类号： A61K51/1096 , A61K51/1027 , A61P35/00
摘要： A conjugate of an anti-CD20 antibody and a chelating agent. The chelating agent is chelated with a metal radionuclide, the anti-CD20 antibody and the chelating agent are linked by a linker (L), and the linker (L) does not contain a thiourea bond. A radiopharmaceutical containing the conjugate as an active ingredient.
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公开(公告)号：US20240189461A1
公开(公告)日：2024-06-13
申请号：US18556582
申请日：2022-04-21
发明人： Masato YAMADA , Fumiaki TAKENAKA , Kotaro HARADA , Momoko OMURA , Mitsuhiro MATONO , Kumiko OTSUKI , Yasushi OCHIAI , Takayuki MURAKAMI
CPC分类号： A61K51/1045 , A61K51/1096 , A61P35/00
摘要： The present invention aims to provide a radionuclide-labeled anti-MUC5AC humanized antibody that is superior in the specificity for mucin subtype 5AC (MUC5AC) and accumulation in tumor. The present invention provides a conjugate of a radionuclide and an antibody, wherein the radionuclide is a nuclide that emits β-rays, and the antibody is a humanized antibody that specifically binds to mucin subtype 5AC and has a heavy chain variable region consisting of the amino acid sequence shown in any of SEQ ID NOs: 1 to 4, and a light chain variable region consisting of the amino acid sequence shown in any of SEQ ID NOs: 5 to 8.
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4.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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5.发明授权公开(公告)号：US11752223B2
公开(公告)日：2023-09-12
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
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：US20210386873A1
公开(公告)日：2021-12-16
申请号：US17356757
申请日：2021-06-24
发明人： Osamu ITO , Akio HAYASHI , Fumie KUROSAKI , Masahito TOYAMA , Toshiyuki SHINMURA , Arinori HARANO
IPC分类号： A61K51/04 , C07B59/00 , C07C309/65 , C07C67/307
摘要： 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.
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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：US10395364B2
公开(公告)日：2019-08-27
申请号：US15509244
申请日：2015-10-29
摘要： One embodiment of the present invention addresses the problem of reducing the influence of physiological accumulation in monitoring nuclear medical image data. To solve this problem, the embodiment includes: extracting a bone area from CT image data having been positioned with nuclear medical image data; in the nuclear medical image data, displaying the data of an area overlapping the bone area extracted above; and, in the nuclear medical image data, not displaying the data of an area not overlapping the bone area extracted above.
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公开(公告)号：US10189815B2
公开(公告)日：2019-01-29
申请号：US15321972
申请日：2015-06-25
发明人： Akihiro Izawa , Kei Akama , Yuki Okumura , Yurie Fukui , Nobuya Kobashi , Tsutomu Abe , Yoshihiro Doi , Miho Ikenaga , Hideo Saji , Hiroyuki Kimura , Mitsuhide Naruse
IPC分类号： C07D401/14 , A61K51/00 , A61K31/4439 , A61K51/04
摘要： Provided is a compound represented by general formula (1) or a salt thereof as well as a medicine containing the compound or the salt. In the formula, R1, R2, R3, R4, R5, X1, X2, and X3 are defined.
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![Radioactive halogen-labeled pyrido [1,2-A] benzimidazole derivative compound](/abs-image/US/2018/09/25/US10081630B2/abs.jpg.150x150.jpg)
公开(公告)号：US10081630B2
公开(公告)日：2018-09-25
申请号：US15543849
申请日：2016-02-24
发明人： Masahiro Ono , Hideo Saji , Masafumi Ihara , Hiroki Matsumoto , Ikuya Seki
IPC分类号： C07B59/00 , C07B63/04 , C07D471/04 , A61K51/04
CPC分类号： C07D471/04 , A61K51/0455 , C07B59/002 , C07B2200/05 , C07F7/0814
摘要： The present invention relates to a radioactive halogen-labeled pyrido[1,2-a]benzimidazole derivative compound represented by a specific general formula or a salt thereof, or a radiopharmaceutical comprising the same.
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