TWI908773B - 化合物及放射性標誌化合物 - Google Patents

化合物及放射性標誌化合物

Info

Publication number
TWI908773B
TWI908773B TW110107676A TW110107676A TWI908773B TW I908773 B TWI908773 B TW I908773B TW 110107676 A TW110107676 A TW 110107676A TW 110107676 A TW110107676 A TW 110107676A TW I908773 B TWI908773 B TW I908773B
Authority
TW
Taiwan
Prior art keywords
compound
psma
formula
target molecule
group
Prior art date
Application number
TW110107676A
Other languages
English (en)
Chinese (zh)
Other versions
TW202146420A (zh
Inventor
眞矢啓史
小野正博
飯國慎平
Original Assignee
日商日本醫事物理股份有限公司
國立大學法人京都大學
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 日商日本醫事物理股份有限公司, 國立大學法人京都大學 filed Critical 日商日本醫事物理股份有限公司
Publication of TW202146420A publication Critical patent/TW202146420A/zh
Application granted granted Critical
Publication of TWI908773B publication Critical patent/TWI908773B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/004—Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • 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
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0465—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0482—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group chelates from cyclic ligands, e.g. DOTA
    • 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
    • A61K51/082—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins the peptide being a RGD-containing peptide
    • 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
    • A61K51/088—Peptides, e.g. proteins, carriers being peptides, polyamino acids, proteins conjugates with carriers being peptides, polyamino acids or proteins
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/003—Compounds containing elements of Groups 3 or 13 of the Periodic Table without C-Metal linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW110107676A 2020-03-04 2021-03-04 化合物及放射性標誌化合物 TWI908773B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2020-037150 2020-03-04
JP2020037150 2020-03-04

Publications (2)

Publication Number Publication Date
TW202146420A TW202146420A (zh) 2021-12-16
TWI908773B true TWI908773B (zh) 2025-12-21

Family

ID=77612690

Family Applications (1)

Application Number Title Priority Date Filing Date
TW110107676A TWI908773B (zh) 2020-03-04 2021-03-04 化合物及放射性標誌化合物

Country Status (9)

Country Link
US (1) US20230112418A1 (https=)
EP (1) EP4116306A4 (https=)
JP (1) JPWO2021177390A1 (https=)
KR (1) KR20220148811A (https=)
CN (1) CN115210240A (https=)
AU (1) AU2021230210A1 (https=)
CA (1) CA3174082A1 (https=)
TW (1) TWI908773B (https=)
WO (1) WO2021177390A1 (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116940557A (zh) * 2021-03-04 2023-10-24 日本医事物理股份有限公司 化合物及放射性标记化合物
AU2022228911A1 (en) * 2021-03-04 2023-09-21 Kyoto University Compound and radioactive labeling compound
WO2024249278A2 (en) * 2023-05-26 2024-12-05 Cornell University Macrocyclic chelators and methods of use for the separation of rare earth elements
WO2025189134A1 (en) * 2024-03-08 2025-09-12 ARTBIO, Inc. Methods for treating prostate cancer with radiopharmaceuticals
WO2025220711A1 (ja) * 2024-04-17 2025-10-23 日本メジフィジックス株式会社 化合物、放射性標識化合物及びその製造方法、並びに放射性医薬組成物
WO2026014283A1 (ja) * 2024-07-09 2026-01-15 日本メジフィジックス株式会社 化合物、放射性標識化合物およびその製造方法、並びに放射性医薬組成物
CN119798110B (zh) * 2025-01-02 2025-09-26 吉林大学 一种4-（对碘苯基）丁基修饰的长循环衣康酸衍生物及制备方法和医用用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2102605A1 (en) * 1991-05-23 1992-11-24 Evan C. Unger Liposoluble compounds for magnetic resonance imaging
US20060228364A1 (en) 1999-12-24 2006-10-12 Genentech, Inc. Serum albumin binding peptides for tumor targeting
GB0412181D0 (en) 2004-06-01 2004-06-30 Celltech R&D Ltd Biological products
CA2760839C (en) 2009-05-01 2019-02-12 The Trustees Of The University Of Pennsylvania Modified compstatin with peptide backbone and c-terminal modifications
DE102014115154A1 (de) * 2014-10-17 2016-04-21 SCV-SpezialChemikalien-Vertrieb GmbH Konjugierte Bisphosphonate für die Diagnostik und Therapie von Knochenerkrankungen
CN108699108B (zh) 2016-03-01 2022-04-08 国立大学法人千叶大学 放射性标记药物
US10696631B2 (en) 2016-05-09 2020-06-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents
MX2019005742A (es) 2016-11-23 2019-09-13 Cancer Targeted Tech Llc Inhibidores de antigeno de membrana especifico de la prostata (psma) de union a albumina.
US11167050B2 (en) 2017-09-26 2021-11-09 National University Corporation Chiba University Metal complex forming compound, metal complex compound formed thereof, radioactive drug containing the metal complex compound, and method of using and preparing the metal complex compound
US20200339625A1 (en) 2017-10-22 2020-10-29 Provincial Health Services Authority Novel radiometal-binding compounds for diagnosis or treatment of prostate specific membrane antigen-expressing cancer
EP3774803A1 (en) * 2018-03-30 2021-02-17 Centre national de la recherche scientifique Pyclen-based macrocyclic ligands, chelates thereof and uses thereof
BR112020023420A8 (pt) 2018-05-17 2022-07-05 Astellas Pharma Inc Complexo tendo fragmento fab de anticorpo anti-muc1 humano, peptídeo ligador e/ou ligante
SG11202103670XA (en) 2018-10-10 2021-05-28 Astellas Pharma Inc Pharmaceutical composition containing tagged site-antihuman antibody fab fragment complex
MX2021008230A (es) 2019-01-07 2021-08-11 Astellas Pharma Inc Conjugado que comprende ligando y fragmento fab de anticuerpo ceacam5.
CN114364405B (zh) * 2019-04-26 2024-07-16 五一一制药股份有限公司 作为诊断剂和放射性核素治疗剂的前列腺特异性膜抗原(psma)抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
期刊 Polasek and Caravan, "Is macrocycle a synonym for kinetic inertness in Gd(III) complexes? Effect of coordinating and non-coordinating substituents on inertness and relaxivity of Gd(III) chelates with DO3A-like ligands", Inorganic Chemistry, 2013, 52(7), pp 4084-4096.

Also Published As

Publication number Publication date
JPWO2021177390A1 (https=) 2021-09-10
EP4116306A4 (en) 2024-05-29
CA3174082A1 (en) 2021-09-10
AU2021230210A1 (en) 2022-09-22
CN115210240A (zh) 2022-10-18
US20230112418A1 (en) 2023-04-13
TW202146420A (zh) 2021-12-16
EP4116306A1 (en) 2023-01-11
KR20220148811A (ko) 2022-11-07
WO2021177390A1 (ja) 2021-09-10

Similar Documents

Publication Publication Date Title
TWI908773B (zh) 化合物及放射性標誌化合物
AU2018308699B2 (en) Dual mode radiotracer and -therapeutics
KR101314460B1 (ko) Ｒｇｄ-함유 펩티드의 방사성 표지된 접합체 및클릭-화학을 통한 그의 제조 방법
EP4303213A1 (en) Compound and radioactive labeling compound
KR20200009091A (ko) 신규 psma-결합제 및 이의 용도
JP2021513979A (ja) エバンスブルー誘導体の化学結合体ならびに前立腺癌を標的とするための放射線療法および造影剤としてのその使用
CN116981486A (zh) 双模式放射性示踪剂和治疗剂
CN113677375B (zh) 氟化硅受体取代的放射性药物及其前体
EP2996726A1 (fr) Composés dendritiques comprenant un agent chélatant, fluorochrome ou agent de reconnaissance, compositions les comprenant et leurs utilisations
US20240317780A1 (en) Radiopharmaceutical somatostatin receptor ligands and precursors thereof
JP2025514068A (ja) セラノスティックフッ化ケイ素複素芳香族系およびその方法
HK40078050A (en) Compound and radioactive labeling compound
HK40092961A (zh) 化合物及放射性标记化合物
WO2013060793A1 (en) Bifunctional ligands for radiometals
KR20240045256A (ko) 가교기로서 킬레이트기를 포함하는 리간드 화합물
CN116940557A (zh) 化合物及放射性标记化合物
WO2025220711A1 (ja) 化合物、放射性標識化合物及びその製造方法、並びに放射性医薬組成物
Bertin et al. Synthesis and characterization of a highly stable dendritic catechol-tripod bearing technetium-99m
WO2011102626A2 (ko) 폴리아자마크로사이클릭 화합물, 그 제조 방법 및 생의학적 적용
Southcott et al. Bis (amido) bis (oxinate) diamine Ligands for theranostic radiometals
WO2026014283A1 (ja) 化合物、放射性標識化合物およびその製造方法、並びに放射性医薬組成物
Lodhi Synthesis and In Vivo Biological Evaluation of 99mTc (I) Tri-carbonyl Based Radiopharmaceuticals for SPECT Imaging
WO2024051794A1 (zh) 放射性核素偶联药物及其药物组合物和应用
JP2024501947A (ja) トレーサー化合物およびその調製方法
KR20250049308A (ko) 방사성 의약품용 규소계 불화물 수용기