NZ589360A - Radiohalogen 18F substituted on a pyridine arboxamide compound - Google Patents

Radiohalogen 18F substituted on a pyridine arboxamide compound

Info

Publication number
NZ589360A
NZ589360A NZ589360A NZ58936009A NZ589360A NZ 589360 A NZ589360 A NZ 589360A NZ 589360 A NZ589360 A NZ 589360A NZ 58936009 A NZ58936009 A NZ 58936009A NZ 589360 A NZ589360 A NZ 589360A
Authority
NZ
New Zealand
Prior art keywords
compound
substituted
leaving group
precursor
ring
Prior art date
Application number
NZ589360A
Inventor
Andrew Katsifis
Ivan Greguric
Original Assignee
Crc For Biomedical Imaging Dev Ltd
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
Priority claimed from AU2008901989A external-priority patent/AU2008901989A0/en
Application filed by Crc For Biomedical Imaging Dev Ltd filed Critical Crc For Biomedical Imaging Dev Ltd
Publication of NZ589360A publication Critical patent/NZ589360A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K51/0455—Heterocyclic 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
    • 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
    • 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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms 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
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pyridine Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

A compound comprising a pyridine carboxamide structure wherein an aromatic ring in the structure is substituted radio halogen atom 18F (fluorine) and wherein the substitution on the amide nitrogen atom is: a hydrogen atom and a tertiary aminoalkyl group; or such that the amide nitrogen is a member of a saturated ring structure having a second nitrogen atom in the ring; or a pharmaceutically acceptable salt of said compound. A structural representation of a possible compound is shown in formula (I). R3 and R4 can form an aryl ring fused to the pyridine ring. Also disclosed is a process for making a compound comprising the step of treating a precursor comprising a leaving group so as to replace said leaving group with the radiohalogen atom18F, said precursor comprising a pyridine carboxamide structure wherein an aromatic ring in the structure is substituted with said leaving group and wherein the substitution on the amide nitrogen atom is a hydrogen atom and a tertiary aminoalkyl group; or the process includes the step of treating a solution of a precursor comprising a chloro leaving group in dimethylformamide with K[18F]-K2.2.2 K2CO3, and heating the mixture at 150 degrees C for 10 minutes; said precursor comprising a pyridine carboxamide structure wherein an aromatic ring in the structure is substituted with said leaving group and wherein the substitution on the amide nitrogen atom is a hydrogen atom and a tertiary aminoalkyl group, such that the compound binds to melanin.
NZ589360A 2008-04-22 2009-04-22 Radiohalogen 18F substituted on a pyridine arboxamide compound NZ589360A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
AU2008901989A AU2008901989A0 (en) 2008-04-22 Nicotinamide derivatives
PCT/AU2009/000504 WO2009129573A1 (en) 2008-04-22 2009-04-22 Nicotinamide derivatives

Publications (1)

Publication Number Publication Date
NZ589360A true NZ589360A (en) 2012-08-31

Family

ID=41216339

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ589360A NZ589360A (en) 2008-04-22 2009-04-22 Radiohalogen 18F substituted on a pyridine arboxamide compound

Country Status (6)

Country Link
EP (1) EP2285778A4 (en)
CN (1) CN102232067A (en)
AU (1) AU2009240785A1 (en)
CA (1) CA2753532A1 (en)
NZ (1) NZ589360A (en)
WO (1) WO2009129573A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120107240A1 (en) * 2010-11-03 2012-05-03 The Board Of Trustees Of The Leland Stanford Junior University Probes and methods of melanoma imaging
US20150023877A1 (en) * 2013-07-18 2015-01-22 The Board Of Trustees Of The Leland Stanford Junior University Methods of parkinsons disease diagnosis and monitoring treatment
JP2015193545A (en) * 2014-03-31 2015-11-05 国立大学法人京都大学 2-(3-pyridinyl)-1h-benzimidazole derivative compound, and radioactive pharmaceuticals containing the same
CN107556236B (en) * 2017-08-25 2020-01-21 华中科技大学同济医学院附属协和医院 Isotope-substituted targeted melanoma positron imaging agent and preparation method and application thereof
KR102302065B1 (en) * 2018-06-28 2021-09-15 전남대학교 산학협력단 A novel radioactive compound for treating melanoma and use thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2904317A1 (en) * 2006-07-27 2008-02-01 Inst Nat Sante Rech Med ANALOGUES OF HALOGENOBENZAMIDES BRANDED AS RADIOPHARMACEUTICALS
EP2085390A1 (en) * 2008-01-31 2009-08-05 Institut National De La Sante Et De La Recherche Medicale (Inserm) Labelled analogues of halobenzamides as multimodal radiopharmaceuticals and their precursors

Also Published As

Publication number Publication date
WO2009129573A1 (en) 2009-10-29
CA2753532A1 (en) 2009-10-29
AU2009240785A1 (en) 2009-10-29
EP2285778A4 (en) 2011-05-11
CN102232067A (en) 2011-11-02
EP2285778A1 (en) 2011-02-23

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Legal Events

Date Code Title Description
RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 22 APR 2016 BY FREEHILLS PATENT ATTORNEYS

Effective date: 20130709

LAPS Patent lapsed