AU2013258027B2 - 18F-labelled follate/antifolate analogues - Google Patents

18F-labelled follate/antifolate analogues Download PDF

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Publication number
AU2013258027B2
AU2013258027B2 AU2013258027A AU2013258027A AU2013258027B2 AU 2013258027 B2 AU2013258027 B2 AU 2013258027B2 AU 2013258027 A AU2013258027 A AU 2013258027A AU 2013258027 A AU2013258027 A AU 2013258027A AU 2013258027 B2 AU2013258027 B2 AU 2013258027B2
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Australia
Prior art keywords
folate
independently
acid
alkyl
aza
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AU2013258027A1 (en
Inventor
Simon Mensah Ametamey
Thomas Betzel
Viola Groehn
Rudolf Moser
Cristina Magdalena Muller
Roger Schibli
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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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/06Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/08Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/60Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Pathology (AREA)
  • Food Science & Technology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (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)
AU2013258027A 2012-05-08 2013-05-08 18F-labelled follate/antifolate analogues Active AU2013258027B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12167126 2012-05-08
EP12167126.7 2012-05-08
PCT/EP2013/059584 WO2013167653A1 (en) 2012-05-08 2013-05-08 18f-labelled folate/antifolate analogues

Publications (2)

Publication Number Publication Date
AU2013258027A1 AU2013258027A1 (en) 2014-11-13
AU2013258027B2 true AU2013258027B2 (en) 2017-11-30

Family

ID=48407549

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013258027A Active AU2013258027B2 (en) 2012-05-08 2013-05-08 18F-labelled follate/antifolate analogues

Country Status (17)

Country Link
US (1) US10357576B2 (enExample)
EP (1) EP2864329B1 (enExample)
JP (1) JP6198814B2 (enExample)
KR (1) KR102116000B1 (enExample)
CN (1) CN104379585B (enExample)
AU (1) AU2013258027B2 (enExample)
CA (1) CA2870124C (enExample)
DK (1) DK2864329T3 (enExample)
EA (1) EA201401225A1 (enExample)
ES (1) ES2703627T3 (enExample)
IL (1) IL235476B (enExample)
PL (1) PL2864329T3 (enExample)
PT (1) PT2864329T (enExample)
SG (1) SG11201406481TA (enExample)
TR (1) TR201819802T4 (enExample)
WO (1) WO2013167653A1 (enExample)
ZA (1) ZA201407266B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101646577B1 (ko) * 2014-08-14 2016-08-09 원광대학교산학협력단 엽산수용체 표적용 화합물 또는 이의 약학적으로 허용가능한 염과, 이를 유효성분으로 포함하는 암 예방, 진단 또는 치료용 조성물
CA3057042A1 (en) 2017-03-20 2018-09-27 Merck Patent Gmbh Isomerically pure 18f-labelled tetrahydrofolates
EP3671511B1 (en) 2018-12-19 2022-07-06 Rohde & Schwarz GmbH & Co. KG Communication system and method
DE102019110904B4 (de) * 2019-04-26 2022-01-20 Helmholtz-Zentrum Dresden - Rossendorf E. V. N-(4-methoxy-7-morpholinobenzo[d]thiazol-2-yl)-acetamid-Derivate und deren Verwendung
WO2021257863A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Pyrrolotriazine compounds as jak2 v617f inhibitors
WO2021257857A1 (en) 2020-06-19 2021-12-23 Incyte Corporation Naphthyridinone compounds as jak2 v617f inhibitors
US11767323B2 (en) 2020-07-02 2023-09-26 Incyte Corporation Tricyclic pyridone compounds as JAK2 V617F inhibitors
WO2022006457A1 (en) 2020-07-02 2022-01-06 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
WO2022046989A1 (en) 2020-08-27 2022-03-03 Incyte Corporation Tricyclic urea compounds as jak2 v617f inhibitors
US11919908B2 (en) 2020-12-21 2024-03-05 Incyte Corporation Substituted pyrrolo[2,3-d]pyrimidine compounds as JAK2 V617F inhibitors
WO2022182839A1 (en) 2021-02-25 2022-09-01 Incyte Corporation Spirocyclic lactams as jak2 v617f inhibitors
JP2025509672A (ja) 2022-03-17 2025-04-11 インサイト・コーポレイション Jak2 v617f阻害剤としての三環式尿素化合物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008125617A2 (en) * 2007-04-11 2008-10-23 Merck Eprova Ag 18f-labelled folates

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2007128036A (ru) 2004-12-23 2009-01-27 Пердью Рисерч Фаундейшн (Us) Способ получения изображения позитронно-эмиссионной томографией
JP4503039B2 (ja) 2006-04-27 2010-07-14 三洋電機株式会社 回路装置
EP2109466B1 (en) 2007-02-07 2014-11-12 Purdue Research Foundation Positron emission tomography imaging method
CN101646639A (zh) 2007-04-11 2010-02-10 默克阿泼洛发股份公司 18f-标记的叶酸
AU2008237935B2 (en) 2007-04-11 2014-03-27 Merck & Cie Folate-conjugates and corresponding metal-chelate complexes for use in diagnostic imaging and radiotherapy
AU2008237932C1 (en) 2007-04-11 2014-04-24 Merck & Cie 18 F-labelled folates
PT2346870E (pt) 2008-10-10 2015-10-21 Merck & Cie Folatos marcados com 18f como marcadores radioactivos de pet

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008125617A2 (en) * 2007-04-11 2008-10-23 Merck Eprova Ag 18f-labelled folates

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
ROBERTS, E. C. ET AL., J. Med. Chem., 1971, Vol. 14 (2), pages 125-130 *
ROBERTS, E. C. ET AL., J. Med. Chem., 1972, Vol. 15 (12), pages 1310-1312 *

Also Published As

Publication number Publication date
PL2864329T3 (pl) 2019-03-29
JP6198814B2 (ja) 2017-09-20
TR201819802T4 (tr) 2019-01-21
CN104379585A (zh) 2015-02-25
IL235476A0 (en) 2014-12-31
AU2013258027A1 (en) 2014-11-13
CA2870124C (en) 2021-02-16
CN104379585B (zh) 2018-07-06
SG11201406481TA (en) 2014-11-27
KR20150010970A (ko) 2015-01-29
EP2864329B1 (en) 2018-09-26
PT2864329T (pt) 2019-01-10
WO2013167653A1 (en) 2013-11-14
EP2864329A1 (en) 2015-04-29
DK2864329T3 (en) 2019-01-21
CA2870124A1 (en) 2013-11-14
EA201401225A1 (ru) 2015-04-30
IL235476B (en) 2019-09-26
HK1202548A1 (en) 2015-10-02
US10357576B2 (en) 2019-07-23
ZA201407266B (en) 2016-09-28
ES2703627T3 (es) 2019-03-11
KR102116000B1 (ko) 2020-05-29
JP2015516405A (ja) 2015-06-11
US20150125390A1 (en) 2015-05-07

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