WO2013081091A1 - Médicament pour la fabrication de polypeptide radiomarqué réduisant une accumulation rénale non spécifique - Google Patents

Médicament pour la fabrication de polypeptide radiomarqué réduisant une accumulation rénale non spécifique Download PDF

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Publication number
WO2013081091A1
WO2013081091A1 PCT/JP2012/081033 JP2012081033W WO2013081091A1 WO 2013081091 A1 WO2013081091 A1 WO 2013081091A1 JP 2012081033 W JP2012081033 W JP 2012081033W WO 2013081091 A1 WO2013081091 A1 WO 2013081091A1
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WO
WIPO (PCT)
Prior art keywords
polypeptide
acceptable salt
group
compound
pharmacologically acceptable
Prior art date
Application number
PCT/JP2012/081033
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English (en)
Japanese (ja)
Inventor
泰 荒野
知也 上原
宏史 花岡
千恵 鈴木
Original Assignee
国立大学法人 千葉大学
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Publication date
Application filed by 国立大学法人 千葉大学 filed Critical 国立大学法人 千葉大学
Priority to JP2013547226A priority Critical patent/JP6164556B2/ja
Publication of WO2013081091A1 publication Critical patent/WO2013081091A1/fr

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/08—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins
    • A61K51/10—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody
    • A61K51/1093—Antibodies or immunoglobulins; Fragments thereof, the carrier being an antibody, an immunoglobulin or a fragment thereof, e.g. a camelised human single domain antibody or the Fc fragment of an antibody conjugates with carriers being antibodies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Abstract

L'invention concerne un médicament radiomarqué qui contient un composé exprimé dans la formule suivante (I) ; le composé auquel un polypeptide est lié qui est capable d'être lié à un site cible, ou un sel pharmaceutiquement acceptable du composé ; et un complexe qui comprend une structure complexe qui contient le composé auquel le polypeptide est lié qui est capable d'être lié au site cible, ou le sel pharmaceutiquement acceptable de celui-ci, et un radioisotope. Dans la formule (I), R1 représente un atome d'hydrogène, un groupe méthyle ou un groupe carboxyméthyle ; R2 représente CH2-CH2-NH-CH2-COOH, CH2-CH2-N(CH2-COOH)2, CH2-CH2-NH2, CH2-CH2-NHR3, le groupe carboxyméthyle ou CH2-CH2-NR3R4 ; R3 et R4 représentent des groupes alkyle qui peuvent être différents ; X, Y et Z représentent des acides aminés qui peuvent être différents ; et F représente un groupe fonctionnel qui est capable d'être lié au polypeptide. A l'aide du composé selon la présente invention, le médicament radiomarqué est fourni, lequel est préparé par une opération simple, a une accumulation élevée vis-à-vis du site cible et réduit une accumulation rénale non spécifique.
PCT/JP2012/081033 2011-12-01 2012-11-30 Médicament pour la fabrication de polypeptide radiomarqué réduisant une accumulation rénale non spécifique WO2013081091A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2013547226A JP6164556B2 (ja) 2011-12-01 2012-11-30 非特異的腎集積が低減された放射性標識ポリペプチド作製用薬剤

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2011263647 2011-12-01
JP2011-263647 2011-12-01

Publications (1)

Publication Number Publication Date
WO2013081091A1 true WO2013081091A1 (fr) 2013-06-06

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Application Number Title Priority Date Filing Date
PCT/JP2012/081033 WO2013081091A1 (fr) 2011-12-01 2012-11-30 Médicament pour la fabrication de polypeptide radiomarqué réduisant une accumulation rénale non spécifique

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JP (1) JP6164556B2 (fr)
WO (1) WO2013081091A1 (fr)

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013224283A (ja) * 2012-04-23 2013-10-31 Nipro Corp 腎臓集積性を示すペプチド、薬物担体、製剤、医薬組成物
JP2015532295A (ja) * 2012-10-02 2015-11-09 エピセラピューティックス・エイ・ピー・エス ヒストン脱メチル化酵素の阻害剤
WO2017150549A1 (fr) * 2016-03-01 2017-09-08 国立大学法人 千葉大学 Médicament radiomarqué
WO2019203191A1 (fr) 2018-04-16 2019-10-24 日本メジフィジックス株式会社 Anticorps modifié et anticorps marqué par un métal radioactif
WO2020145228A1 (fr) 2019-01-07 2020-07-16 アステラス製薬株式会社 Composite constitué d'un ligand et d'un fragment fab d'un anticorps ｃｅａｃａｍ５
JPWO2019065774A1 (ja) * 2017-09-26 2021-01-28 国立大学法人千葉大学 放射性薬剤
US11667724B2 (en) 2017-07-07 2023-06-06 Astellas Pharma Inc. Anti-human CEACAM5 antibody Fab fragment
US11679166B2 (en) 2016-11-18 2023-06-20 Astellas Pharma Inc. Anti-human MUC1 antibody Fab fragment

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112135841A (zh) 2018-05-17 2020-12-25 安斯泰来制药株式会社 包含抗人MUC1抗体Fab片段、肽接头和/或配体的复合物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002293796A (ja) * 2001-03-30 2002-10-09 Canon Inc 標識ペプチドによるシトクロムｃの造影・検出試薬
JP2005047821A (ja) * 2003-07-30 2005-02-24 Nihon Medi Physics Co Ltd シクロペンタジエニルカルボニル基を含む放射性化合物を用いた診断及び治療用薬剤
WO2011040574A1 (fr) * 2009-09-30 2011-04-07 国立大学法人京都大学 Procédé pour produire un dérivé d'azétidinylméthoxypyridine et utilisation du dérivé d'azétidinylméthoxypyridine

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2002293796A (ja) * 2001-03-30 2002-10-09 Canon Inc 標識ペプチドによるシトクロムｃの造影・検出試薬
JP2005047821A (ja) * 2003-07-30 2005-02-24 Nihon Medi Physics Co Ltd シクロペンタジエニルカルボニル基を含む放射性化合物を用いた診断及び治療用薬剤
WO2011040574A1 (fr) * 2009-09-30 2011-04-07 国立大学法人京都大学 Procédé pour produire un dérivé d'azétidinylméthoxypyridine et utilisation du dérivé d'azétidinylméthoxypyridine

Cited By (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013224283A (ja) * 2012-04-23 2013-10-31 Nipro Corp 腎臓集積性を示すペプチド、薬物担体、製剤、医薬組成物
JP2015532295A (ja) * 2012-10-02 2015-11-09 エピセラピューティックス・エイ・ピー・エス ヒストン脱メチル化酵素の阻害剤
US10189787B2 (en) 2012-10-02 2019-01-29 Gilead Sciences, Inc. Inhibitors of histone demethylases
US10221139B2 (en) 2012-10-02 2019-03-05 Gilead Sciences, Inc. Inhibitors of histone demethylases
US10960089B2 (en) 2016-03-01 2021-03-30 National University Corporation Chiba University Radiolabeled drug
WO2017150549A1 (fr) * 2016-03-01 2017-09-08 国立大学法人 千葉大学 Médicament radiomarqué
JPWO2017150549A1 (ja) * 2016-03-01 2019-01-10 国立大学法人千葉大学 放射性標識薬剤
US11679166B2 (en) 2016-11-18 2023-06-20 Astellas Pharma Inc. Anti-human MUC1 antibody Fab fragment
US11667724B2 (en) 2017-07-07 2023-06-06 Astellas Pharma Inc. Anti-human CEACAM5 antibody Fab fragment
JP7207740B2 (ja) 2017-09-26 2023-01-18 国立大学法人千葉大学 放射性薬剤
JPWO2019065774A1 (ja) * 2017-09-26 2021-01-28 国立大学法人千葉大学 放射性薬剤
WO2019203191A1 (fr) 2018-04-16 2019-10-24 日本メジフィジックス株式会社 Anticorps modifié et anticorps marqué par un métal radioactif
KR20200143366A (ko) 2018-04-16 2020-12-23 니혼 메디피직스 가부시키가이샤 수식 항체 및 방사성 금속 표지 항체
US11701440B2 (en) 2018-04-16 2023-07-18 Nihon Medi-Physics Co., Ltd. Modified antibody and radioactive metal-labelled antibody
WO2020145227A1 (fr) 2019-01-07 2020-07-16 アステラス製薬株式会社 Composite constitué d'un ligand, d'un espaceur, d'un lieur peptidique et d'une biomolécule
KR20210113202A (ko) 2019-01-07 2021-09-15 아스텔라스세이야쿠 가부시키가이샤 배위자, 스페이서, 펩티드 링커 및 생물 분자를 포함하는 복합체
KR20210113201A (ko) 2019-01-07 2021-09-15 아스텔라스세이야쿠 가부시키가이샤 배위자 및 CEACAM5 항체 Fab 프래그먼트를 포함하는 복합체
WO2020145228A1 (fr) 2019-01-07 2020-07-16 アステラス製薬株式会社 Composite constitué d'un ligand et d'un fragment fab d'un anticorps ｃｅａｃａｍ５

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JPWO2013081091A1 (ja) 2015-04-27

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