CA2670385C - Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy - Google Patents

Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy Download PDF

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Publication number
CA2670385C
CA2670385C CA2670385A CA2670385A CA2670385C CA 2670385 C CA2670385 C CA 2670385C CA 2670385 A CA2670385 A CA 2670385A CA 2670385 A CA2670385 A CA 2670385A CA 2670385 C CA2670385 C CA 2670385C
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Prior art keywords
alkyl
independently
alkoxy
complex
hal
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Expired - Fee Related
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CA2670385A
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English (en)
French (fr)
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CA2670385A1 (en
Inventor
Rudolf Moser
Roger Schibli
Cristina Magdalena Mueller
Viola Groehn
Urs Michel
Christof Sparr
Thomas Leighton Mindt
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Merck et Cie
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Merck et Cie
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Expired - Fee Related legal-status Critical Current
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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
    • 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
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • A61K51/0497—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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F13/00—Compounds containing elements of Groups 7 or 17 of the Periodic Table
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N23/00—Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00 – G01N17/00, G01N21/00 or G01N22/00
    • G01N23/22—Investigating or analysing materials by the use of wave or particle radiation, e.g. X-rays or neutrons, not covered by groups G01N3/00 – G01N17/00, G01N21/00 or G01N22/00 by measuring secondary emission from the material
    • G01N23/2204—Specimen supports therefor; Sample conveying means therefore
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/82—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving vitamins or their receptors
    • 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
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435—Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705—Assays involving receptors, cell surface antigens or cell surface determinants

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Pathology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • Microbiology (AREA)
  • Food Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nuclear Medicine (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
CA2670385A 2007-04-11 2008-04-11 Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy Expired - Fee Related CA2670385C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07105980 2007-04-11
EP07105980.2 2007-04-11
PCT/EP2008/054409 WO2008125618A1 (en) 2007-04-11 2008-04-11 Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy

Publications (2)

Publication Number Publication Date
CA2670385A1 CA2670385A1 (en) 2008-10-23
CA2670385C true CA2670385C (en) 2016-01-12

Family

ID=39683755

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2670385A Expired - Fee Related CA2670385C (en) 2007-04-11 2008-04-11 Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy

Country Status (11)

Country Link
US (2) US20100143249A1 (enExample)
EP (1) EP2146995A1 (enExample)
JP (2) JP5710246B2 (enExample)
KR (2) KR101605426B1 (enExample)
CN (1) CN101646672B (enExample)
AU (1) AU2008237935B2 (enExample)
CA (1) CA2670385C (enExample)
EA (1) EA200901344A1 (enExample)
IL (1) IL201250A0 (enExample)
WO (1) WO2008125618A1 (enExample)
ZA (1) ZA200903483B (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA200901344A1 (ru) * 2007-04-11 2010-04-30 Мерк Эпрова Аг Фолат-конъюгаты и соответствующие комплексы хелатов металлов для применения для диагностической визуализации и лучевой терапии
US8236284B1 (en) * 2008-04-02 2012-08-07 University Of Central Florida Research Foundation, Inc. Multimodal, multifunctional polymer coated nanoparticles
FR2942227B1 (fr) * 2009-02-13 2011-04-15 Guerbet Sa Utilisation de tampons pour la complexation de radionucleides
WO2011084571A2 (en) 2009-12-16 2011-07-14 Mallinckrodt Inc. Azide derivatives for phototherapy
DK2766364T3 (da) * 2011-08-17 2024-09-30 Merck & Cie Folatkonjugater af albumin-bindende enheder
EP2864329B1 (en) 2012-05-08 2018-09-26 Merck & Cie 18f-labelled folate/antifolate analogues
US20180016226A1 (en) * 2015-02-06 2018-01-18 Cempra Pharmaceuticals, Inc. 4-azidobutylamines and processes for preparing
WO2020256210A1 (ko) 2019-06-20 2020-12-24 주식회사 쿼드마이너 네트워크 포렌식 시스템 및 이를 이용한 네트워크 포렌식 방법

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6093382A (en) * 1998-05-16 2000-07-25 Bracco Research Usa Inc. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
WO2002085908A1 (en) * 2001-04-24 2002-10-31 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
JP4801348B2 (ja) * 2002-05-06 2011-10-26 エンドサイト，インコーポレイテッド ビタミンを標的とした造影剤
KR20060003064A (ko) * 2003-04-29 2006-01-09 유니베르시태트 취리히 〔Ｍ（ＯＨ２）３（ＣＯ）３〕+로의 ＦＡＣ 배위에 의한매우 효과적인 표지를 위해 생체분자로 커플링되는, Ｎε및（또는）Ｎα 유도체화, 금속 및 유기 보호 Ｌ-히스티딘
US9265746B2 (en) * 2006-05-31 2016-02-23 Merck & Cie Method for cell-specific targeting
EA200901344A1 (ru) * 2007-04-11 2010-04-30 Мерк Эпрова Аг Фолат-конъюгаты и соответствующие комплексы хелатов металлов для применения для диагностической визуализации и лучевой терапии

Also Published As

Publication number Publication date
JP2014193889A (ja) 2014-10-09
KR101605426B1 (ko) 2016-03-22
US20100143249A1 (en) 2010-06-10
CN101646672B (zh) 2015-08-19
EP2146995A1 (en) 2010-01-27
EA200901344A1 (ru) 2010-04-30
WO2008125618A1 (en) 2008-10-23
AU2008237935A1 (en) 2008-10-23
JP2010523626A (ja) 2010-07-15
ZA200903483B (en) 2010-04-28
HK1138571A1 (zh) 2010-08-27
KR20150140415A (ko) 2015-12-15
CN101646672A (zh) 2010-02-10
KR20100016330A (ko) 2010-02-12
CA2670385A1 (en) 2008-10-23
JP5876527B2 (ja) 2016-03-02
US20170128599A1 (en) 2017-05-11
JP5710246B2 (ja) 2015-04-30
AU2008237935B2 (en) 2014-03-27
IL201250A0 (en) 2010-05-31

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