AU2009335049B2 - Synthesis of 18F-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof - Google Patents

Synthesis of 18F-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof Download PDF

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Publication number
AU2009335049B2
AU2009335049B2 AU2009335049A AU2009335049A AU2009335049B2 AU 2009335049 B2 AU2009335049 B2 AU 2009335049B2 AU 2009335049 A AU2009335049 A AU 2009335049A AU 2009335049 A AU2009335049 A AU 2009335049A AU 2009335049 B2 AU2009335049 B2 AU 2009335049B2
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Prior art keywords
ethoxy
pyridin
methyl
radiolabeled
compound
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AU2009335049A
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AU2009335049A1 (en
Inventor
Tyler Benedum
Geoff Golding
Nathaniel Lim
Wei Zhang
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Avid Radiopharmaceuticals Inc
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Avid Radiopharmaceuticals Inc
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365—Lactones
    • A61K31/375—Ascorbic acid, i.e. vitamin C; Salts thereof
    • 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
    • A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M37/00—Other apparatus for introducing media into the body; Percutany, i.e. introducing medicines into the body by diffusion through the skin
    • A61M37/0069—Devices for implanting pellets, e.g. markers or solid medicaments
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Medical Informatics (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2009335049A 2008-12-31 2009-12-29 Synthesis of 18F-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof Active AU2009335049B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US14188508P 2008-12-31 2008-12-31
US61/141,885 2008-12-31
PCT/US2009/069741 WO2010078370A1 (en) 2008-12-31 2009-12-29 Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof

Publications (2)

Publication Number Publication Date
AU2009335049A1 AU2009335049A1 (en) 2011-07-21
AU2009335049B2 true AU2009335049B2 (en) 2015-07-16

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AU2009335049A Active AU2009335049B2 (en) 2008-12-31 2009-12-29 Synthesis of 18F-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof

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US (1) US20100172836A1 (enExample)
EP (1) EP2381967B1 (enExample)
JP (1) JP5717650B2 (enExample)
KR (1) KR20110119670A (enExample)
CN (1) CN102271716B (enExample)
AU (1) AU2009335049B2 (enExample)
BR (1) BRPI0923890A2 (enExample)
CA (1) CA2748705C (enExample)
CO (1) CO6341578A2 (enExample)
CR (1) CR20110410A (enExample)
CY (1) CY1118658T1 (enExample)
DK (1) DK2381967T3 (enExample)
DO (1) DOP2011000210A (enExample)
EA (1) EA023014B1 (enExample)
EC (1) ECSP11011242A (enExample)
ES (1) ES2620402T3 (enExample)
HN (1) HN2011001810A (enExample)
HR (1) HRP20170453T1 (enExample)
HU (1) HUE033649T2 (enExample)
IL (1) IL213674A (enExample)
LT (1) LT2381967T (enExample)
MA (1) MA33004B1 (enExample)
MX (1) MX2011007063A (enExample)
MY (1) MY162312A (enExample)
NZ (1) NZ593848A (enExample)
PE (1) PE20120007A1 (enExample)
PL (1) PL2381967T3 (enExample)
PT (1) PT2381967T (enExample)
RS (1) RS55674B1 (enExample)
SG (1) SG172439A1 (enExample)
SI (1) SI2381967T1 (enExample)
TN (1) TN2011000318A1 (enExample)
UA (1) UA105914C2 (enExample)
WO (1) WO2010078370A1 (enExample)
ZA (1) ZA201104824B (enExample)

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WO2010039815A1 (en) * 2008-09-30 2010-04-08 Case Western Reserve University Molecular probes for imaging of myelin
BR112012030946A2 (pt) * 2010-06-04 2016-11-01 Piramal Imaging Sa método para a produção de ligante para amiloide beta marcado com f-18
CA2801530C (en) 2010-06-04 2017-09-12 Piramal Imaging Sa Method for production of f-18 labeled amyloid beta ligands
TWI504414B (zh) * 2010-06-04 2015-10-21 Bayer Schering Pharma Ag 生產F-18標記之Aβ配位體之方法
WO2012145169A2 (en) * 2011-04-21 2012-10-26 The Regents Of The University Of California Functionalized magnetic nanoparticles and use in imaging amyloid deposits and neurofibrillary tangles
MY183997A (en) * 2011-06-21 2021-03-17 Life Molecular Imaging Sa Formulations of fluorinated stilbene suitable for pet imaging
CA2852840A1 (en) 2011-10-19 2013-04-25 Piramal Imaging Sa Improved method for production of f-18 labeled a.beta. ligands
CN102432529B (zh) * 2011-11-14 2014-03-26 江苏省原子医学研究所 一种苯乙烯基吡啶二硫二氮衍生物的制备方法
WO2013090497A1 (en) * 2011-12-15 2013-06-20 Ge Healthcare Limited Heterocyclic compounds as imaging probes of tau pathology
CN102526765B (zh) * 2011-12-31 2014-07-30 郑州泰基鸿诺药物科技有限公司 一种Aβ斑块显像剂及其制备方法
CN103965105A (zh) * 2013-01-29 2014-08-06 中山大学 苯乙烯基喹啉衍生物及其在治疗阿尔茨海默病症中的应用
CN103645254B (zh) * 2013-11-28 2015-01-07 江苏省原子医学研究所 一种Aβ斑块显像剂前体AV45的含量分析方法
WO2017014599A1 (ko) * 2015-07-22 2017-01-26 주식회사 씨코헬스케어 [18f]플루오로-도파의 방사화학적 순도를 안정화시키는 조성물 및 이의 제조방법
ES2864825T3 (es) * 2015-11-13 2021-10-14 Lilly Co Eli Derivados de azetidina para la obtención de imágenes Tau
EP3426309B1 (en) * 2016-03-09 2022-05-04 Case Western Reserve University Radioligands for myelin
CN107198780A (zh) * 2016-03-18 2017-09-26 南京江原安迪科正电子研究发展有限公司 放射性药物组合物及其制备方法、应用
CN106018575B (zh) * 2016-05-05 2018-10-19 江苏省原子医学研究所 一种PET显像剂前体TsOP-(+)-DTBZ及其光学异构体的分离测定方法
US10695450B2 (en) * 2016-07-26 2020-06-30 Laboratoires Cyclopharma Synthesis of a radioactive agent composition
DK3538161T3 (da) * 2016-11-08 2022-09-05 Univ California Fremgangsmåder til flerdosissyntese af [F-18]FDDNP til kliniske indstillinger
TW201906818A (zh) * 2017-05-31 2019-02-16 美商511製藥公司 新穎氘取代之正子發射斷層掃描(pet)顯影劑及其藥理應用
EA202091766A1 (ru) * 2018-01-24 2021-02-18 Ац Иммуне Са Композиции для диагностики для пэт-визуализации, способ получения композиции для диагностики и ее применение в диагностике
CN111499570B (zh) * 2019-01-31 2023-05-16 中国医学科学院放射医学研究所 一种av-45中间体的合成方法
CN111499544B (zh) * 2019-01-31 2022-12-02 中国医学科学院放射医学研究所 一种一锅法制备N-Boc-N-甲基-4-氨基苯乙烯的合成方法
JP7576334B2 (ja) * 2019-03-29 2024-10-31 国立研究開発法人量子科学技術研究開発機構 放射性医薬の製造方法及び放射性医薬
CN115400232A (zh) * 2021-05-26 2022-11-29 汉中汉核医疗科技有限公司 一种放射性药物合成方法
CN115403434A (zh) * 2021-05-26 2022-11-29 汉中汉核医疗科技有限公司 一种放射性药物的合成方法
CN113582885B (zh) * 2021-08-30 2023-04-21 南京克米斯璀新能源科技有限公司 一种烷基磺酸钠的生产方法
CN114805190A (zh) * 2022-06-08 2022-07-29 吉林大学第一医院 一种甲基苯胺类Aβ蛋白显像剂的双柱合成方法
KR20250107902A (ko) * 2022-11-14 2025-07-14 일라이 릴리 앤드 캄파니 플로르베타피르 전구체 av-105의 다형체 형태
CN119080714A (zh) * 2024-09-12 2024-12-06 四川大学 一种偶氮苯磺酸酯化合物及其制备方法和应用、放射性探针的制备方法

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US20070281299A1 (en) * 2004-01-19 2007-12-06 Youdim Moussa B Diagnostic Test For Parkinson's Disease
US20080038195A1 (en) * 2006-03-30 2008-02-14 The Trustees Of The University Of Pennsylvania Stryrylpyridine derivates and theur use for binding and imaging amylod plaques

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US20080038195A1 (en) * 2006-03-30 2008-02-14 The Trustees Of The University Of Pennsylvania Stryrylpyridine derivates and theur use for binding and imaging amylod plaques

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SOUZA, F., et al., The Journal of Clinical Investigations, 2006, vol. 116, pp. 1506-1513 *
ZHANG, W., et al., J. Med. Chem., 2005, vol. 48, pp. 5980-5988 *

Also Published As

Publication number Publication date
MA33004B1 (fr) 2012-01-02
WO2010078370A1 (en) 2010-07-08
BRPI0923890A2 (pt) 2015-07-28
TN2011000318A1 (en) 2012-12-17
JP5717650B2 (ja) 2015-05-13
HK1162951A1 (en) 2012-09-07
HUE033649T2 (en) 2017-12-28
CN102271716A (zh) 2011-12-07
HRP20170453T1 (hr) 2017-06-02
HN2011001810A (es) 2013-08-12
UA105914C2 (uk) 2014-07-10
SI2381967T1 (sl) 2017-03-31
EA023014B1 (ru) 2016-04-29
MX2011007063A (es) 2011-12-16
DK2381967T3 (en) 2017-03-27
ES2620402T3 (es) 2017-06-28
KR20110119670A (ko) 2011-11-02
US20100172836A1 (en) 2010-07-08
CN102271716B (zh) 2014-11-19
DOP2011000210A (es) 2011-09-15
CO6341578A2 (es) 2011-11-21
MY162312A (en) 2017-05-31
CR20110410A (es) 2011-12-08
CA2748705C (en) 2017-05-02
PL2381967T3 (pl) 2017-06-30
JP2012514007A (ja) 2012-06-21
SG172439A1 (en) 2011-07-28
IL213674A0 (en) 2011-07-31
CA2748705A1 (en) 2010-07-08
PE20120007A1 (es) 2012-01-16
ECSP11011242A (es) 2011-10-31
PT2381967T (pt) 2017-02-24
EP2381967B1 (en) 2017-01-18
EP2381967A1 (en) 2011-11-02
CY1118658T1 (el) 2017-07-12
IL213674A (en) 2016-04-21
EP2381967A4 (en) 2013-01-02
ZA201104824B (en) 2013-01-30
AU2009335049A1 (en) 2011-07-21
LT2381967T (lt) 2017-04-25
EA201170911A1 (ru) 2011-12-30
RS55674B1 (sr) 2017-06-30
NZ593848A (en) 2013-09-27

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