SG11201810916WA - IMPROVED SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPyL - Google Patents

IMPROVED SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPyL

Info

Publication number
SG11201810916WA
SG11201810916WA SG11201810916WA SG11201810916WA SG11201810916WA SG 11201810916W A SG11201810916W A SG 11201810916WA SG 11201810916W A SG11201810916W A SG 11201810916WA SG 11201810916W A SG11201810916W A SG 11201810916WA SG 11201810916W A SG11201810916W A SG 11201810916WA
Authority
SG
Singapore
Prior art keywords
maryland
international
dcfpyl
pct
improved synthesis
Prior art date
Application number
SG11201810916WA
Other languages
English (en)
Inventor
Hayden T Ravert
Daniel P Holt
Ying Chen
Ronnie C Mease
Hong Fan
Martin G Pomper
Robert F Dannals
Original Assignee
Univ Johns Hopkins
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 Univ Johns Hopkins filed Critical Univ Johns Hopkins
Publication of SG11201810916WA publication Critical patent/SG11201810916WA/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/42Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
    • 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
    • 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
    • A61K51/0455Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
SG11201810916WA 2016-06-10 2017-06-09 IMPROVED SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPyL SG11201810916WA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662348391P 2016-06-10 2016-06-10
PCT/US2017/036681 WO2017214470A1 (en) 2016-06-10 2017-06-09 IMPROVED SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPyL

Publications (1)

Publication Number Publication Date
SG11201810916WA true SG11201810916WA (en) 2019-01-30

Family

ID=60579003

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201810916WA SG11201810916WA (en) 2016-06-10 2017-06-09 IMPROVED SYNTHESIS OF THE RADIOLABELED PROSTATE-SPECIFIC MEMBRANE ANTIGEN (PSMA) INHIBITOR [18F]DCFPyL

Country Status (8)

Country Link
US (2) US10947197B2 (ko)
EP (1) EP3481804A4 (ko)
JP (3) JP7054390B2 (ko)
KR (2) KR102558962B1 (ko)
CN (1) CN109563038A (ko)
CA (1) CA3026889A1 (ko)
SG (1) SG11201810916WA (ko)
WO (1) WO2017214470A1 (ko)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113563262A (zh) * 2008-08-01 2021-10-29 约翰.霍普金斯大学 Psma-结合剂及其用途
CN109563038A (zh) 2016-06-10 2019-04-02 约翰霍普金斯大学 放射性标记的前列腺特异性膜抗原(PSMA)抑制剂[18F]DCFPyL的改进的合成
DE102016122273B4 (de) * 2016-11-18 2018-06-21 Abx Advanced Biochemical Compounds Gmbh Präkursoren für die Radiofluorierung
DK3765097T3 (da) * 2018-03-16 2022-05-23 Univ Koeln 2-alkoxy-6-[18f]fluornicotinoylsubstituerede lys-c(o)-glu-derivater som effektive prober til billeddannelse af psma-udtrykkende væv
US20210338846A1 (en) * 2018-07-30 2021-11-04 The Johns Hopkins University Competitive prostate-specific membrane antigen (psma) binding agents for reduction of non-target organ uptake of radiolabeled psma inhibitors for psma positive tumor imaging and radiopharmaceutical therapy
US20220387635A1 (en) * 2019-11-04 2022-12-08 Board Of Regents, The University Of Texas System Pet imaging of cancerous cells using 18f-fluoroacetate
CN111548305B (zh) * 2020-05-12 2021-08-31 北京师范大学 一种可用于靶向psma的喹啉类化合物及其制备方法
CN114014843B (zh) * 2021-11-17 2022-09-20 北京大学第一医院 一种psma靶向核素/荧光双模态配体和分子探针与应用
CN114671806B (zh) * 2022-04-08 2024-03-01 上海如絮生物科技有限公司 一种亲水性吡啶衍生物、中间体、其制备方法及应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0422004D0 (en) 2004-10-05 2004-11-03 Amersham Plc Method of deprotection
CN113563262A (zh) * 2008-08-01 2021-10-29 约翰.霍普金斯大学 Psma-结合剂及其用途
WO2013173583A1 (en) * 2012-05-16 2013-11-21 Cancer Targeted Technology, Llc Psma inhibitors
US10112974B2 (en) 2014-08-24 2018-10-30 Max-Planck-Gesellschaft Zur Foerderung Der Wissenschaften E.V. Method for the production of 18F-labeled active esters and their application exemplified by the preparation of a PSMA-specific PET-tracer
CN109563038A (zh) 2016-06-10 2019-04-02 约翰霍普金斯大学 放射性标记的前列腺特异性膜抗原(PSMA)抑制剂[18F]DCFPyL的改进的合成

Also Published As

Publication number Publication date
KR20230111272A (ko) 2023-07-25
JP2022101579A (ja) 2022-07-06
JP2019521104A (ja) 2019-07-25
JP7427703B2 (ja) 2024-02-05
EP3481804A1 (en) 2019-05-15
US10947197B2 (en) 2021-03-16
US20220055991A1 (en) 2022-02-24
US20190177275A1 (en) 2019-06-13
CA3026889A1 (en) 2017-12-14
JP7054390B2 (ja) 2022-04-13
CN109563038A (zh) 2019-04-02
WO2017214470A1 (en) 2017-12-14
EP3481804A4 (en) 2019-11-13
JP2024056729A (ja) 2024-04-23
US11851407B2 (en) 2023-12-26
KR20190011804A (ko) 2019-02-07
KR102558962B1 (ko) 2023-07-21

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