EA201891544A1 - Ингибиторы простатического специфического мембранного антигена (псма) на основе мочевины для визуализации и лечения - Google Patents

Ингибиторы простатического специфического мембранного антигена (псма) на основе мочевины для визуализации и лечения

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Publication number
EA201891544A1
EA201891544A1 EA201891544A EA201891544A EA201891544A1 EA 201891544 A1 EA201891544 A1 EA 201891544A1 EA 201891544 A EA201891544 A EA 201891544A EA 201891544 A EA201891544 A EA 201891544A EA 201891544 A1 EA201891544 A1 EA 201891544A1
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EA
Eurasian Patent Office
Prior art keywords
psma
uride
visualization
inhibitors
treatment
Prior art date
Application number
EA201891544A
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English (en)
Inventor
Ханк Ф. Кунг
Карл Плесль
Сеок Рие Чои
Чжихао Чжа
Цзехой У
Original Assignee
Файв Илевен Фарма Инк.
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Publication date
Application filed by Файв Илевен Фарма Инк. filed Critical Файв Илевен Фарма Инк.
Publication of EA201891544A1 publication Critical patent/EA201891544A1/ru

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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
    • A61K51/0474—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
    • A61K51/0474—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
    • A61K51/0478—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 complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • 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
    • A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Physics & Mathematics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Nuclear Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)

Abstract

Данное изобретение относится к соединениям формулы I и формулы IV. Данные соединения демонстрируют очень хорошую аффинность связывания с участками связывания ПСМА. Они могут быть мечены [68Ga]GaCl3 с высокими выходами и превосходной радиохимической чистотой. Данное изобретение также относится к фармацевтическим композициям, содержащим фармацевтически приемлемый носитель и соединение формулы I или формулы IV или его фармацевтически приемлемую соль.
EA201891544A 2015-12-31 2016-12-22 Ингибиторы простатического специфического мембранного антигена (псма) на основе мочевины для визуализации и лечения EA201891544A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562273786P 2015-12-31 2015-12-31
US15/385,490 US10688200B2 (en) 2015-12-31 2016-12-20 Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy
PCT/US2016/068327 WO2017116994A1 (en) 2015-12-31 2016-12-22 Urea-based prostate specific membrane antigen (psma) inhibitors for imaging and therapy

Publications (1)

Publication Number Publication Date
EA201891544A1 true EA201891544A1 (ru) 2018-11-30

Family

ID=59225798

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891544A EA201891544A1 (ru) 2015-12-31 2016-12-22 Ингибиторы простатического специфического мембранного антигена (псма) на основе мочевины для визуализации и лечения

Country Status (14)

Country Link
US (1) US10688200B2 (ru)
EP (1) EP3397968B1 (ru)
JP (1) JP6850027B2 (ru)
KR (1) KR20180098373A (ru)
CN (1) CN108541302B (ru)
AU (2) AU2016380151A1 (ru)
CA (1) CA3010295C (ru)
DK (1) DK3397968T3 (ru)
EA (1) EA201891544A1 (ru)
HK (1) HK1255215A1 (ru)
IL (1) IL260342A (ru)
MX (1) MX2018008168A (ru)
SG (1) SG11201805380YA (ru)
WO (1) WO2017116994A1 (ru)

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US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
MX2016005013A (es) 2013-10-18 2017-02-28 Deutsches Krebsforsch Inhibidores marcados de antigeno prostatico especifico de membrana (psma), su uso como agentes formadores de imagenes y agentes farmaceuticos para el tratamiento de cancer de prostata.
US10688200B2 (en) 2015-12-31 2020-06-23 Five Eleven Pharma Inc. Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy
PT3925952T (pt) * 2016-03-22 2023-12-13 Univ Johns Hopkins Agentes alvo de alta afinidade direcionados ao antigénio de membrana específica da próstata para endo radioterapia de cancro da próstata
WO2018204477A1 (en) 2017-05-02 2018-11-08 Cornell University Methods and reagents for tumor targeting with greater efficacy and less toxicity
US11478558B2 (en) * 2017-05-30 2022-10-25 The Johns Hopkins University Prostate-specific membrane antigen targeted high-affinity agents for endoradiotherapy of prostate cancer
IL274072B1 (en) 2017-12-11 2024-07-01 Univ Muenchen Tech PSMA ligands for imaging and endoradiotherapy
US20190184040A1 (en) * 2017-12-15 2019-06-20 Wisconsin Alumni Research Foundation Targeted Macrocyclic Agents for Dual Modality PET and MRI Imaging of Cancer
MX2018003175A (es) * 2018-03-14 2019-09-16 Instituto Nac De Investigaciones Nucleares 177lu-dota-hynic-ipsma como un radiofarmaco terapeutico dirigido al antigeno prostatico especifico de membrana.
CN109438517B (zh) * 2018-12-27 2021-01-08 北京久杰净化工程技术有限公司 一种与羰基金属核心配位的双功能连接剂的配合物及其制备方法
KR20220004125A (ko) * 2019-04-26 2022-01-11 파이브 일레븐 파마 인크. 진단제 및 방사성핵종 치료제로서의 전립선-특이적 막 항원 (psma) 억제제
WO2020252598A1 (en) 2019-06-21 2020-12-24 Provincial Health Services Authority Radiolabeled compounds targeting the prostate-specific membrane antigen
CN115380117A (zh) * 2020-02-18 2022-11-22 恩多塞特公司 治疗表达psma的癌症的方法
AU2021352915A1 (en) * 2020-10-01 2023-06-08 Cornell University Methods and compositions for increasing uptake, internalization, and/or retention of small molecule ligands
CN112358422B (zh) * 2020-10-16 2023-06-23 中国辐射防护研究院 一种新型螯合剂nbed的制备方法
US20240158420A1 (en) * 2021-03-17 2024-05-16 Five Eleven Pharma, Inc [18f]a1f labeled psma targeting molecular probe and preparation method therefor
CN113372285B (zh) * 2021-05-28 2024-06-18 西南医科大学附属医院 前列腺特异性膜抗原抑制剂、其放射性核素标记物及制法和应用
CN114436905A (zh) * 2022-01-24 2022-05-06 攀枝花学院 3-醛基-4-羟基苯乙酸甲酯的纯化方法
CN116514735A (zh) * 2022-01-30 2023-08-01 晶核生物医药科技(南京)有限公司 一种肽脲素衍生物、含其的药物组合物及其应用
CN114874122A (zh) * 2022-05-31 2022-08-09 南京航空航天大学 一种新的小分子抑制剂及其制备方法和应用
WO2024021556A1 (zh) * 2023-02-02 2024-02-01 北京师范大学 一种靶向前列腺特异性膜抗原的放射性金属配合物及其标记配体
CN116507630A (zh) * 2023-02-14 2023-07-28 北京师范大学 含硝基芳香杂环基团的psma靶向放射性金属配合物及其制备
CN118496299A (zh) * 2023-02-16 2024-08-16 无锡诺宇医药科技有限公司 Psma靶向放射性诊疗一体化药物及其合成和应用

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SI1472541T1 (sl) 2002-01-10 2010-12-31 Univ Johns Hopkins Prikazovalni agensi in postopek prikazovanja naaladase ali psma
US8338565B2 (en) 2008-08-20 2012-12-25 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of tumor necrosis factor alpha
CN107325127B (zh) * 2011-06-15 2020-09-01 癌靶技术有限责任公司 螯合的psma抑制剂
WO2013022797A1 (en) 2011-08-05 2013-02-14 Molecular Insight Pharmaceuticals Radiolabeled prostate specific membrane antigen inhibitors
CN104203942B (zh) * 2011-11-30 2017-04-12 约翰霍普金斯大学 前列腺特异性膜抗原(psma)的同源多价抑制剂和异源多价抑制剂以及其用途
US9636413B2 (en) * 2012-11-15 2017-05-02 Endocyte, Inc. Conjugates for treating diseases caused by PSMA expressing cells
WO2014110372A1 (en) * 2013-01-14 2014-07-17 Molecular Insight Pharmaceuticals Triazine based radiopharmaceuticals and radioimaging agents
US10406246B2 (en) 2013-10-17 2019-09-10 Deutsches Kresbsforschungszentrum Double-labeled probe for molecular imaging and use thereof
EP2862857A1 (en) * 2013-10-18 2015-04-22 Deutsches Krebsforschungszentrum Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
MX2016005013A (es) * 2013-10-18 2017-02-28 Deutsches Krebsforsch Inhibidores marcados de antigeno prostatico especifico de membrana (psma), su uso como agentes formadores de imagenes y agentes farmaceuticos para el tratamiento de cancer de prostata.
KR102457827B1 (ko) * 2013-11-14 2022-10-24 엔도사이트, 인코포레이티드 양전자 방출 단층 촬영용 화합물
CA3215134A1 (en) * 2014-05-06 2015-11-12 The Johns Hopkins University Metal/radiometal-labeled psma inhibitors for psma-targeted imaging and radiotherapy
US10688200B2 (en) 2015-12-31 2020-06-23 Five Eleven Pharma Inc. Urea-based prostate specific membrane antigen (PSMA) inhibitors for imaging and therapy

Also Published As

Publication number Publication date
DK3397968T3 (da) 2021-11-01
CA3010295C (en) 2023-09-26
EP3397968A4 (en) 2019-11-27
US10688200B2 (en) 2020-06-23
IL260342A (en) 2018-08-30
CN108541302B (zh) 2023-02-14
EP3397968B1 (en) 2021-09-29
US20170189568A1 (en) 2017-07-06
AU2016380151A1 (en) 2018-07-19
CA3010295A1 (en) 2017-07-06
HK1255215A1 (zh) 2019-08-09
JP6850027B2 (ja) 2021-03-31
JP2019508374A (ja) 2019-03-28
WO2017116994A1 (en) 2017-07-06
SG11201805380YA (en) 2018-07-30
CN108541302A (zh) 2018-09-14
EP3397968A1 (en) 2018-11-07
MX2018008168A (es) 2019-02-20
AU2023203682A1 (en) 2023-07-06
KR20180098373A (ko) 2018-09-03

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