WO2007021858A3 - Methods of making radiolabeled tracers and precursors thereof - Google Patents

Methods of making radiolabeled tracers and precursors thereof Download PDF

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Publication number
WO2007021858A3
WO2007021858A3 PCT/US2006/031231 US2006031231W WO2007021858A3 WO 2007021858 A3 WO2007021858 A3 WO 2007021858A3 US 2006031231 W US2006031231 W US 2006031231W WO 2007021858 A3 WO2007021858 A3 WO 2007021858A3
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WO
WIPO (PCT)
Prior art keywords
radiolabeled tracers
precursors
methods
tracers
making radiolabeled
Prior art date
Application number
PCT/US2006/031231
Other languages
French (fr)
Other versions
WO2007021858A2 (en
Inventor
David S Casebier
Richard R Cesati Iii
Edward H Cheesman
Original Assignee
Bristol Myers Squibb Pharma Co
David S Casebier
Richard R Cesati Iii
Edward H Cheesman
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 Bristol Myers Squibb Pharma Co, David S Casebier, Richard R Cesati Iii, Edward H Cheesman filed Critical Bristol Myers Squibb Pharma Co
Priority to EP06801160A priority Critical patent/EP1926500A2/en
Priority to JP2008526203A priority patent/JP2009504849A/en
Priority to CA002618988A priority patent/CA2618988A1/en
Publication of WO2007021858A2 publication Critical patent/WO2007021858A2/en
Publication of WO2007021858A3 publication Critical patent/WO2007021858A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/14—Oxygen atoms
    • 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
    • A61K51/0412—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K51/0421—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • 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
    • 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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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
    • C07D237/14—Oxygen atoms
    • C07D237/16—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/42—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms in positions 2 and 4

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Physics & Mathematics (AREA)
  • Medicinal Chemistry (AREA)
  • Optics & Photonics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)

Abstract

The present disclosure relates to a solid-phase process for the production of radiolabeled tracers, in particular for the production of 18F-labeled compounds which may be used as Positron Emission Tomography (PET) radiolabeled tracers. The disclosure also relates to radiopharmaceutical kits comprising precursors to the radiolabeled tracers, which can be converted to the radiolabeled tracers using the processes described herein.
PCT/US2006/031231 2005-08-10 2006-08-09 Methods of making radiolabeled tracers and precursors thereof WO2007021858A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP06801160A EP1926500A2 (en) 2005-08-10 2006-08-09 Methods of making radiolabeled tracers and precursors thereof
JP2008526203A JP2009504849A (en) 2005-08-10 2006-08-09 Method for producing radiolabeled tracer and precursor thereof
CA002618988A CA2618988A1 (en) 2005-08-10 2006-08-09 Methods of making radiolabeled tracers and precursors thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US70688505P 2005-08-10 2005-08-10
US60/706,885 2005-08-10

Publications (2)

Publication Number Publication Date
WO2007021858A2 WO2007021858A2 (en) 2007-02-22
WO2007021858A3 true WO2007021858A3 (en) 2007-05-03

Family

ID=37667830

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2006/031231 WO2007021858A2 (en) 2005-08-10 2006-08-09 Methods of making radiolabeled tracers and precursors thereof

Country Status (6)

Country Link
US (1) US7824659B2 (en)
EP (1) EP1926500A2 (en)
JP (1) JP2009504849A (en)
CA (1) CA2618988A1 (en)
TW (1) TW200738271A (en)
WO (1) WO2007021858A2 (en)

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* Cited by examiner, † Cited by third party
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US7344702B2 (en) 2004-02-13 2008-03-18 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging
EP1448588A4 (en) * 2001-10-23 2006-10-25 Psma Dev Company L L C Psma antibodies and protein multimers
US7485283B2 (en) 2004-04-28 2009-02-03 Lantheus Medical Imaging Contrast agents for myocardial perfusion imaging
EP2257315B1 (en) * 2008-02-29 2019-10-23 Lantheus Medical Imaging, Inc. Contrast agents for applications including perfusion imaging
AU2015200027B2 (en) * 2008-02-29 2017-01-19 Lantheus Medical Imaging, Inc. Contrast agents for applications including perfusion imaging
CA2729635A1 (en) * 2008-07-03 2010-01-07 Ananth Srinivasan Compounds and processes for production of radiopharmaceuticals
CN102458396B (en) 2009-04-15 2017-05-10 兰休斯医疗成像公司 Stabilization of radiopharmaceutical compositions using ascorbic acid
CN113058046A (en) 2010-02-08 2021-07-02 兰休斯医疗成像公司 Method and apparatus for synthesizing imaging agents and intermediates thereof
BR112014005286B1 (en) 2011-09-09 2022-08-23 Lantheus Medical Imaging, Inc COMPOUNDS OF A FIRST AND A SECOND IMAGING AGENT TO DETERMINE INCOMPATIBILITY OF INNERVATION AND PERFUSION ON THE PART OF THE INDIVIDUAL
AU2011379346B2 (en) * 2011-10-21 2017-08-31 Lantheus Medical Imaging, Inc. Compositions comprising ascorbic acid and an imaging agent and related methods
CA2859773C (en) * 2011-12-22 2020-09-01 Respiratorius Ab Contrast agent for imagining myocardial perfusion
AU2013203000B9 (en) 2012-08-10 2017-02-02 Lantheus Medical Imaging, Inc. Compositions, methods, and systems for the synthesis and use of imaging agents
JP6190240B2 (en) * 2013-10-16 2017-08-30 浜松ホトニクス株式会社 Diagnostic agent for therapeutic effect on cancer
WO2015143019A2 (en) * 2014-03-18 2015-09-24 Mayo Foundation For Medical Education And Research Gaseous f-18 technologies
CN109503590B (en) * 2018-11-22 2021-06-25 四川大学华西医院 18F-PET/CT tracer with 7-deazaadenine base as mother nucleus and preparation method thereof

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WO2004056400A1 (en) * 2002-12-20 2004-07-08 Hammersmith Imanet Limited Solid-phase fluorination of uracil and cytosine
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WO2005105159A2 (en) * 2004-04-28 2005-11-10 Bristol-Myers Squibb Pharma Company Contrast agents for myocardial perfusion imaging

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WO2003002157A1 (en) * 2001-06-29 2003-01-09 Amersham Plc Solid-phase nucleophilic fluorination
WO2004056400A1 (en) * 2002-12-20 2004-07-08 Hammersmith Imanet Limited Solid-phase fluorination of uracil and cytosine
WO2005012319A1 (en) * 2003-07-31 2005-02-10 Ge Healthcare Limited Production of 2-18f-2-deoxy-d-glucose via solid-phase synthesis
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Also Published As

Publication number Publication date
US20070036716A1 (en) 2007-02-15
WO2007021858A2 (en) 2007-02-22
EP1926500A2 (en) 2008-06-04
TW200738271A (en) 2007-10-16
US7824659B2 (en) 2010-11-02
CA2618988A1 (en) 2007-02-22
JP2009504849A (en) 2009-02-05

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