WO2012105814A3 - 개선된 플루오르-18 표지를 위한 트리아자노난 유도체 또는 이의 약학적으로 허용가능한 염 - Google Patents

개선된 플루오르-18 표지를 위한 트리아자노난 유도체 또는 이의 약학적으로 허용가능한 염 Download PDF

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Publication number
WO2012105814A3
WO2012105814A3 PCT/KR2012/000790 KR2012000790W WO2012105814A3 WO 2012105814 A3 WO2012105814 A3 WO 2012105814A3 KR 2012000790 W KR2012000790 W KR 2012000790W WO 2012105814 A3 WO2012105814 A3 WO 2012105814A3
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WO
WIPO (PCT)
Prior art keywords
labeling
triazanonane
derivative
pharmaceutically acceptable
acceptable salt
Prior art date
Application number
PCT/KR2012/000790
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English (en)
French (fr)
Other versions
WO2012105814A2 (ko
Inventor
정재민
셰티디네쉬
이동수
정준기
이명철
Original Assignee
서울대학교 산학협력단
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 서울대학교 산학협력단 filed Critical 서울대학교 산학협력단
Priority to US13/983,053 priority Critical patent/US9012604B2/en
Publication of WO2012105814A2 publication Critical patent/WO2012105814A2/ko
Publication of WO2012105814A3 publication Critical patent/WO2012105814A3/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
    • C07D255/02—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 not condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Optics & Photonics (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

본 발명은 하기 화학식 1로 표시되는 트리아자노난 유도체, 또는 이의 약학 적으로 허용가능한 염 및 이의 제조방법에 관한 것으로, 본 발명에 따른 트리아자 노난 유도체는 금속-플루오라이드와 착체를 형성하여 F-18을 표지할 때 표지효율을 78~90%까지 높이는 효과를 나타냄으로써, 다양한 방사성 의약품 표지에 널리 이용 될 수 있다. [화학식 1] (상기 화학식 1에서, R1, R2, A. E. X, n 및 m은 본 명세서에서 정의한 바와 같다.)
PCT/KR2012/000790 2011-02-01 2012-02-01 개선된 플루오르-18 표지를 위한 트리아자노난 유도체 또는 이의 약학적으로 허용가능한 염 WO2012105814A2 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US13/983,053 US9012604B2 (en) 2011-02-01 2012-02-01 Triazanonane derivatives or pharmaceutically acceptable salt thereof for enhanced fluorine-18 labeling

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020110010202A KR101142153B1 (ko) 2011-02-01 2011-02-01 개선된 플루오르-18 표지를 위한 트리아자노난 유도체 또는 이의 약학적으로 허용가능한 염
KR10-2011-0010202 2011-02-01

Publications (2)

Publication Number Publication Date
WO2012105814A2 WO2012105814A2 (ko) 2012-08-09
WO2012105814A3 true WO2012105814A3 (ko) 2012-11-01

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2012/000790 WO2012105814A2 (ko) 2011-02-01 2012-02-01 개선된 플루오르-18 표지를 위한 트리아자노난 유도체 또는 이의 약학적으로 허용가능한 염

Country Status (3)

Country Link
US (1) US9012604B2 (ko)
KR (1) KR101142153B1 (ko)
WO (1) WO2012105814A2 (ko)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8545809B2 (en) 2007-01-11 2013-10-01 Immunomedics, Inc. Methods and compositions for improved 18F labeling of proteins, peptides and other molecules
CA2814953A1 (en) * 2010-12-13 2012-06-21 Immunomedics, Inc. Methods and compositions for improved f-18 labeling of proteins, peptides and other molecules
CN103787998B (zh) * 2014-02-25 2015-09-23 江苏省原子医学研究所 一种双功能螯合剂p-SCN-NODA的合成方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050120494A1 (en) * 2003-09-26 2005-06-09 Laurent Vidal Triazacyclononane derivatives substituted on at least one of the nitrogen atoms with a substituted or unsubstituted 4'-aminophenyl group, for dyeing keratin fibres
WO2009079024A1 (en) * 2007-12-19 2009-06-25 Immunomedics, Inc. Improved methods and compositions for f-18 labeling of proteins, peptides and other molecules
US20090246130A1 (en) * 2007-01-11 2009-10-01 Immunomedics, Inc. Methods and Compositions for F-18 Labeling of Proteins, Peptides and Other Molecules

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7993626B2 (en) 2007-01-11 2011-08-09 Immunomedics, Inc. Methods and compositions for F-18 labeling of proteins, peptides and other molecules
US7563433B2 (en) 2007-01-11 2009-07-21 Immunomedics, Inc. Methods and compositions for F-18 labeling of proteins, peptides and other molecules
EP2117604B1 (en) 2007-01-11 2017-07-26 Immunomedics, Inc. Methods and compositions for improved f-18 labeling of proteins, peptides and other molecules

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050120494A1 (en) * 2003-09-26 2005-06-09 Laurent Vidal Triazacyclononane derivatives substituted on at least one of the nitrogen atoms with a substituted or unsubstituted 4'-aminophenyl group, for dyeing keratin fibres
US20090246130A1 (en) * 2007-01-11 2009-10-01 Immunomedics, Inc. Methods and Compositions for F-18 Labeling of Proteins, Peptides and Other Molecules
WO2009079024A1 (en) * 2007-12-19 2009-06-25 Immunomedics, Inc. Improved methods and compositions for f-18 labeling of proteins, peptides and other molecules

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DINESH SHETTY ET AL.: "Stable aluminium fluoride chelates with triazacyclononane derivatives proved by X-ray crystallography and 18F-labling study", CHEMICAL COMMUNICATIONS, vol. 47, no. 34, 14 September 2011 (2011-09-14), pages 9732 - 9734 *
SHUANG LIU: "Radiolabeled Cyclic RGD Peptides as Integrin uvp3-Targeted Radiotracers:MaximizingBindingAffmityviaBivalency", BIOCONJUGATE CHEMISTRY, vol. 20, no. 12, 2009, pages 2199 - 2213 *

Also Published As

Publication number Publication date
US9012604B2 (en) 2015-04-21
US20130317196A1 (en) 2013-11-28
KR101142153B1 (ko) 2012-05-10
WO2012105814A2 (ko) 2012-08-09

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