AU2008237935B2 - 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
AU2008237935B2
AU2008237935B2 AU2008237935A AU2008237935A AU2008237935B2 AU 2008237935 B2 AU2008237935 B2 AU 2008237935B2 AU 2008237935 A AU2008237935 A AU 2008237935A AU 2008237935 A AU2008237935 A AU 2008237935A AU 2008237935 B2 AU2008237935 B2 AU 2008237935B2
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alkyl
independently
hal
alkoxy
substituted
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AU2008237935A
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AU2008237935A1 (en
Inventor
Viola Groehn
Urs Michel
Thomas Leighton Mindt
Rudolf Moser
Cristina Magdalena Muller
Roger Schibli
Christof Sparr
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Merck et Cie
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Merck et Cie
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/041Heterocyclic compounds
    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0402Organic compounds carboxylic acid carriers, fatty acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0497Organic compounds conjugates with a carrier being an organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F13/00Compounds containing elements of Groups 7 or 17 of the Periodic Table
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N23/00Investigating 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
    • G01N23/22Investigating 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
    • G01N23/2204Specimen supports therefor; Sample conveying means therefore
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/82Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving vitamins or their receptors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/435Assays involving biological materials from specific organisms or of a specific nature from animals; from humans
    • G01N2333/705Assays 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nuclear Medicine (AREA)
  • Radiation-Therapy Devices (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
AU2008237935A 2007-04-11 2008-04-11 Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy Ceased AU2008237935B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP07105980.2 2007-04-11
EP07105980 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
AU2008237935A1 AU2008237935A1 (en) 2008-10-23
AU2008237935B2 true AU2008237935B2 (en) 2014-03-27

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AU2008237935A Ceased AU2008237935B2 (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) KR20150140415A (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
KR20150140415A (ko) * 2007-04-11 2015-12-15 메르크 앤드 씨에 진단 이미징 및 방사선치료에 사용하기 위한 폴레이트-컨쥬게이트 및 대응하는 금속-킬레이트 착물
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
PT2766364T (pt) * 2011-08-17 2024-09-24 Merck & Cie Conjugados de folato de entidades de ligação a albumina
AU2013258027B2 (en) 2012-05-08 2017-11-30 Merck & Cie 18F-labelled follate/antifolate analogues
JP2018504422A (ja) * 2015-02-06 2018-02-15 センプラ ファーマシューティカルズ,インコーポレイテッド 4−アジドブチルアミンおよびその調製方法
WO2020256210A1 (ko) 2019-06-20 2020-12-24 주식회사 쿼드마이너 네트워크 포렌식 시스템 및 이를 이용한 네트워크 포렌식 방법

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059640A2 (en) * 1998-05-16 1999-11-25 Bracco International B.V. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
WO2003092742A1 (en) * 2002-05-06 2003-11-13 Endocyte, Inc. Vitamin-targeted imaging agents

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
AU2004235488A1 (en) * 2003-04-29 2004-11-11 Universitat Zurich Nepsilon and/or nalpha derivatized, metal and organic protected l-histidine for coupling to biomolecules for highly efficient labeling with [M(OH2)3(CO)3]+ by fac coordination
US9265746B2 (en) * 2006-05-31 2016-02-23 Merck & Cie Method for cell-specific targeting
KR20150140415A (ko) * 2007-04-11 2015-12-15 메르크 앤드 씨에 진단 이미징 및 방사선치료에 사용하기 위한 폴레이트-컨쥬게이트 및 대응하는 금속-킬레이트 착물

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999059640A2 (en) * 1998-05-16 1999-11-25 Bracco International B.V. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
US20010004454A1 (en) * 1998-05-16 2001-06-21 Wedeking Paul W. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
WO2003092742A1 (en) * 2002-05-06 2003-11-13 Endocyte, Inc. Vitamin-targeted imaging agents

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KE CHUN-YEN et al: Nuclear Medicine & Biology, 2003, 30(8), 811-817 *
MINDT T. L. et al: J American Chem. Soc., 2006, 128, 15096-15097 *

Also Published As

Publication number Publication date
WO2008125618A1 (en) 2008-10-23
CA2670385A1 (en) 2008-10-23
CN101646672B (zh) 2015-08-19
EA200901344A1 (ru) 2010-04-30
US20170128599A1 (en) 2017-05-11
AU2008237935A1 (en) 2008-10-23
CN101646672A (zh) 2010-02-10
CA2670385C (en) 2016-01-12
ZA200903483B (en) 2010-04-28
EP2146995A1 (en) 2010-01-27
JP2014193889A (ja) 2014-10-09
IL201250A0 (en) 2010-05-31
KR20150140415A (ko) 2015-12-15
HK1138571A1 (zh) 2010-08-27
US20100143249A1 (en) 2010-06-10
KR20100016330A (ko) 2010-02-12
KR101605426B1 (ko) 2016-03-22
JP2010523626A (ja) 2010-07-15
JP5876527B2 (ja) 2016-03-02
JP5710246B2 (ja) 2015-04-30

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