CN101646672B - 用于诊断成像和放射治疗的叶酸轭合物和相应的金属螯合物络合物 - Google Patents

用于诊断成像和放射治疗的叶酸轭合物和相应的金属螯合物络合物 Download PDF

Info

Publication number
CN101646672B
CN101646672B CN200880002741.6A CN200880002741A CN101646672B CN 101646672 B CN101646672 B CN 101646672B CN 200880002741 A CN200880002741 A CN 200880002741A CN 101646672 B CN101646672 B CN 101646672B
Authority
CN
China
Prior art keywords
alkyl
independently
groups
complex
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN200880002741.6A
Other languages
English (en)
Chinese (zh)
Other versions
CN101646672A (zh
Inventor
R·莫泽
R·施布利
C·M·穆勒
V·格罗恩
U·米歇尔
C·斯帕尔
T·L·曼德
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck And Seay Partnership
Original Assignee
Merck Eprova AG
Eprova AG
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 Merck Eprova AG, Eprova AG filed Critical Merck Eprova AG
Publication of CN101646672A publication Critical patent/CN101646672A/zh
Application granted granted Critical
Publication of CN101646672B publication Critical patent/CN101646672B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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

Landscapes

  • 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)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (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)
  • Investigating Or Analysing Biological Materials (AREA)
  • Radiation-Therapy Devices (AREA)
  • Nuclear Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN200880002741.6A 2007-04-11 2008-04-11 用于诊断成像和放射治疗的叶酸轭合物和相应的金属螯合物络合物 Expired - Fee Related CN101646672B (zh)

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
CN101646672A CN101646672A (zh) 2010-02-10
CN101646672B true CN101646672B (zh) 2015-08-19

Family

ID=39683755

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200880002741.6A Expired - Fee Related CN101646672B (zh) 2007-04-11 2008-04-11 用于诊断成像和放射治疗的叶酸轭合物和相应的金属螯合物络合物

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
WO2008125618A1 (en) * 2007-04-11 2008-10-23 Merck Eprova Ag Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy
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
HUE068833T2 (hu) * 2011-08-17 2025-01-28 Merck & Cie Kmg Albumint megkötõ egységek folát konjugátjai
PT2864329T (pt) 2012-05-08 2019-01-10 Merck & Cie Análogos de folato/antifolato marcados com 18f
US20180016226A1 (en) * 2015-02-06 2018-01-18 Cempra Pharmaceuticals, Inc. 4-azidobutylamines and processes for preparing
JP7391847B2 (ja) 2019-06-20 2023-12-05 クワッド マイナーズ ネットワークフォレンジックシステム及びこれを用いたネットワークフォレンジック方法

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
CN1662263A (zh) * 2002-05-06 2005-08-31 恩多塞特公司 维生素－定向的显象剂
US20070280880A1 (en) * 2006-05-31 2007-12-06 Rudolf Moser Method for cell-specific targeting

Family Cites Families (3)

* 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
DE602004024879D1 (de) * 2003-04-29 2010-02-11 Univ Zuerich AN EINEM BIOMOLEKÜL GEBUNDENEN N epsilon- UND/ODER N alpha DERIVATISIERTEM UND ORGANISCH-GESCHÜTZTEM L-HISTIDIN ZUR HOCH-EFFIZIENTER MARKIERUNG MIT (M(H2O)3(CO)3)+ MITTELS FAC KOORDINIERUNG
WO2008125618A1 (en) * 2007-04-11 2008-10-23 Merck Eprova Ag Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy

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
CN1662263A (zh) * 2002-05-06 2005-08-31 恩多塞特公司 维生素－定向的显象剂
US20070280880A1 (en) * 2006-05-31 2007-12-06 Rudolf Moser Method for cell-specific targeting

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KE C-Y等.The folate receptor as a molecular target for tumor-selective radionuclide delivery.《NUCLEAR MEDICINE AND BIOLOGY》.2003,第30卷(第8期),811-817. *
Thomas L.MINDT 等.Click to chelate: synthesis and installation of metal chelates into biomolecules in a single ste.《J. AM. CHEM. SOC.》.2006,第128卷15096-15097. *

Also Published As

Publication number Publication date
JP5876527B2 (ja) 2016-03-02
CA2670385C (en) 2016-01-12
IL201250A0 (en) 2010-05-31
EP2146995A1 (en) 2010-01-27
EA200901344A1 (ru) 2010-04-30
JP2014193889A (ja) 2014-10-09
JP5710246B2 (ja) 2015-04-30
KR101605426B1 (ko) 2016-03-22
ZA200903483B (en) 2010-04-28
KR20150140415A (ko) 2015-12-15
CN101646672A (zh) 2010-02-10
AU2008237935A1 (en) 2008-10-23
KR20100016330A (ko) 2010-02-12
US20100143249A1 (en) 2010-06-10
US20170128599A1 (en) 2017-05-11
JP2010523626A (ja) 2010-07-15
AU2008237935B2 (en) 2014-03-27
WO2008125618A1 (en) 2008-10-23
CA2670385A1 (en) 2008-10-23
HK1138571A1 (zh) 2010-08-27

Similar Documents

Publication Publication Date Title
CN101657454B (zh) 18f-标记的叶酸类
JP4801348B2 (ja) ビタミンを標的とした造影剤
CN101646672B (zh) 用于诊断成像和放射治疗的叶酸轭合物和相应的金属螯合物络合物
CN104379585B (zh) 18f-标记的叶酸/抗叶酸剂类似物
US9771368B2 (en) 18F-labelled folates
HK1138571B (en) Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy
JP4801786B6 (ja) ビタミンを標的とした造影剤
HK1175169A (en) 18f-labelled folates
HK1139129B (en) 18f-labelled folates

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1138571

Country of ref document: HK

ASS Succession or assignment of patent right

Owner name: MERCK + CIE PARTNERSHIP CORPORATION

Free format text: FORMER OWNER: MERCK EPROVA AG

Effective date: 20110511

C41 Transfer of patent application or patent right or utility model
TA01 Transfer of patent application right

Effective date of registration: 20110511

Address after: Schaffhausen

Applicant after: Merck and Seay partnership

Address before: Schaffhausen

Applicant before: Merck Eprova AG

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1138571

Country of ref document: HK

CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20150819

Termination date: 20180411