CN102271716B - 由甲苯磺酸酯前体合成18f-放射性标记的苯乙烯基吡啶及其稳定的药物组合物 - Google Patents

由甲苯磺酸酯前体合成18f-放射性标记的苯乙烯基吡啶及其稳定的药物组合物 Download PDF

Info

Publication number
CN102271716B
CN102271716B CN200980153414.5A CN200980153414A CN102271716B CN 102271716 B CN102271716 B CN 102271716B CN 200980153414 A CN200980153414 A CN 200980153414A CN 102271716 B CN102271716 B CN 102271716B
Authority
CN
China
Prior art keywords
ethyoxyl
vinyl
pyridin
methyl
radiopharmaceutical composition
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN200980153414.5A
Other languages
English (en)
Chinese (zh)
Other versions
CN102271716A (zh
Inventor
T.贝内杜姆
G.戈尔丁
N．林
W.张
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Avid Radiopharmaceuticals Inc
Original Assignee
Avid Radiopharmaceuticals Inc
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 Avid Radiopharmaceuticals Inc filed Critical Avid Radiopharmaceuticals Inc
Publication of CN102271716A publication Critical patent/CN102271716A/zh
Application granted granted Critical
Publication of CN102271716B publication Critical patent/CN102271716B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Neurosurgery (AREA)
  • Neurology (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)
CN200980153414.5A 2008-12-31 2009-12-29 由甲苯磺酸酯前体合成18f-放射性标记的苯乙烯基吡啶及其稳定的药物组合物 Active CN102271716B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US14188508P 2008-12-31 2008-12-31
US61/141885 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
CN102271716A CN102271716A (zh) 2011-12-07
CN102271716B true CN102271716B (zh) 2014-11-19

Family

ID=42310197

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980153414.5A Active CN102271716B (zh) 2008-12-31 2009-12-29 由甲苯磺酸酯前体合成18f-放射性标记的苯乙烯基吡啶及其稳定的药物组合物

Country Status (35)

Country Link
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)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010039815A1 (en) * 2008-09-30 2010-04-08 Case Western Reserve University Molecular probes for imaging of myelin
LT2579902T (lt) 2010-06-04 2017-09-25 Piramal Imaging Sa Gamybos būdas amiloido beta ligandų, žymėtų f-18
SG185785A1 (en) 2010-06-04 2013-01-30 Piramal Imaging Sa Method for production of f-18 labeled amyloid beta ligand
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
CN103491870B (zh) * 2011-04-21 2016-12-28 加利福尼亚大学董事会 官能化磁性纳米颗粒及在淀粉样沉积物和神经原纤维缠结成像中用途
CN105833303A (zh) * 2011-06-21 2016-08-10 皮拉莫尔影像股份公司 适用于pet成像的氟化茋的制剂
BR112014009013A2 (pt) 2011-10-19 2017-05-02 Piramal Imaging Sa método melhorado para a produção de ligandos aß rotulados por f-18
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
JP2015507617A (ja) * 2011-12-15 2015-03-12 ジーイー・ヘルスケア・リミテッド タウ病理のイメージングプローブとしての複素環式化合物
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
PL3374358T3 (pl) * 2015-11-13 2021-07-12 Eli Lilly And Company Pochodne azetydyny do obrazowania białka tau
US10765763B2 (en) 2016-03-09 2020-09-08 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
CN109922837A (zh) * 2016-11-08 2019-06-21 加利福尼亚大学董事会 用于临床应用的[f-18]fddnp的多剂量合成方法
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
BR112020014594A8 (pt) * 2018-01-24 2022-12-13 Ac Immune Sa Composições de diagnóstico para imageamento pet, método para fabricar composição de diagnóstico e seu uso em diagnóstico
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
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
US20220175973A1 (en) * 2019-03-29 2022-06-09 National Institutes for Quantum Science and Technology Method for producing radiopharmaceutical and radiopharmaceutical
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
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
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
CN120187703A (zh) * 2022-11-14 2025-06-20 伊莱利利公司 氟贝他吡前体av-105的多晶型物
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA012334B1 (ru) * 2004-12-17 2009-08-28 Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания Производные стильбена и их применение для связывания и визуализации амилоидных бляшек

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
"F-18 Stilbenes as PET Imaging Agents for Detecting Beta-Amyloid Plaques in the Brain.;ZHANG ET AL.;《 JOURNAL OF MEDICINAL CHEMISTRY》;20050823;第48卷;第5980-5988页 *
"Longitudinal noninvasive PET-based Beta cell ";SOUZA ET AL.;《 JOURNAL OF CLINICAL INVESTIGATION》;20060630;第116卷;第1506-1513页 *

Also Published As

Publication number Publication date
JP2012514007A (ja) 2012-06-21
AU2009335049B2 (en) 2015-07-16
DOP2011000210A (es) 2011-09-15
MX2011007063A (es) 2011-12-16
ES2620402T3 (es) 2017-06-28
DK2381967T3 (en) 2017-03-27
BRPI0923890A2 (pt) 2015-07-28
UA105914C2 (uk) 2014-07-10
HN2011001810A (es) 2013-08-12
IL213674A0 (en) 2011-07-31
HRP20170453T1 (hr) 2017-06-02
AU2009335049A1 (en) 2011-07-21
MA33004B1 (fr) 2012-01-02
HUE033649T2 (en) 2017-12-28
US20100172836A1 (en) 2010-07-08
EP2381967B1 (en) 2017-01-18
RS55674B1 (sr) 2017-06-30
HK1162951A1 (en) 2012-09-07
SI2381967T1 (sl) 2017-03-31
ECSP11011242A (es) 2011-10-31
WO2010078370A1 (en) 2010-07-08
TN2011000318A1 (en) 2012-12-17
IL213674A (en) 2016-04-21
PT2381967T (pt) 2017-02-24
JP5717650B2 (ja) 2015-05-13
CY1118658T1 (el) 2017-07-12
CR20110410A (es) 2011-12-08
CN102271716A (zh) 2011-12-07
EA201170911A1 (ru) 2011-12-30
EP2381967A4 (en) 2013-01-02
NZ593848A (en) 2013-09-27
LT2381967T (lt) 2017-04-25
KR20110119670A (ko) 2011-11-02
MY162312A (en) 2017-05-31
PE20120007A1 (es) 2012-01-16
PL2381967T3 (pl) 2017-06-30
CA2748705C (en) 2017-05-02
EA023014B1 (ru) 2016-04-29
CO6341578A2 (es) 2011-11-21
CA2748705A1 (en) 2010-07-08
ZA201104824B (en) 2013-01-30
EP2381967A1 (en) 2011-11-02
SG172439A1 (en) 2011-07-28

Similar Documents

Publication Publication Date Title
CN102271716B (zh) 由甲苯磺酸酯前体合成18f-放射性标记的苯乙烯基吡啶及其稳定的药物组合物
AU2016201367B2 (en) Stabilization of radiopharmaceutical compositions using ascorbic acid
US20090004106A1 (en) Radioligands for the 5 -Ht1b Receptor
Li et al. Translating the concept of peptide labeling with 5-deoxy-5-[18 F] fluororibose into preclinical practice: 18 F-labeling of Siglec-9 peptide for PET imaging of inflammation
KR101602912B1 (ko) [18ｆ]플루오르메틸기가 도입된 뇌신경염증 표적 양성자방출단층촬영 방사성추적자, 이의 합성 및 그를 이용한 생물학적 결과 평가 방법
US20110263819A1 (en) Simplified one-pot synthesis of [18f]sfb for radiolabeling
Nguyen et al. IBETA: A new aβ plaque positron emission tomography imaging agent for Alzheimer’s disease
Rahman et al. Synthesis of ([11C] carbonyl) raclopride and a comparison with ([11C] methyl) raclopride in a monkey PET study
Andersson et al. Radiosynthesis of the candidate β‐amyloid radioligand [11C] AZD2184: Positron emission tomography examination and metabolite analysis in cynomolgus monkeys
Pathuri et al. Synthesis and in vivo evaluation of gallium‐68‐labeled glycine and hippurate conjugates for positron emission tomography renography
Foged et al. Development of 123I-labelled NNC 13-8241 as a radioligand for SPECT visualization of benzodiazepine receptor binding
Vercouillie et al. Automated production of [18F] FDDNP using a TRACERlab MXFDG
HK1162951B (en) Synthesis of 18f-radiolabeled styrylpyridines from tosylate precursors and stable pharmaceutical compositions thereof
Nguyen et al. [124I] BETA, a new beta-amyloid plaque PET imaging agent for Alzheimer's disease
Ott Selective neuropeptide and opioid receptor radioligands for imaging studies in vivo by positron emission tomography (PET)
US20150297760A1 (en) 18f labeled bodipy dye and its derivatives for pet imaging of heart perfusion and others
Liang et al. A one-step fully automated radio-synthesis of a dopamine transporter PET imaging agent 18F-FECNT and its in vivo evaluations
JP5128293B2 (ja) 橋頭標識化合物およびその使用方法
CN117865858A (zh) 靶向大麻素2型受体的新型pet显像剂及其制备方法和应用
JPH0871413A (ja) 芳香族フルオロ体とニトロ体の分離
HK1170672A (en) Stabilization of radiopharmaceutical compositions using ascorbic acid
HK1170672B (en) Stabilization of radiopharmaceutical compositions using ascorbic acid

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1162951

Country of ref document: HK

C14 Grant of patent or utility model
GR01 Patent grant
REG Reference to a national code

Ref country code: HK

Ref legal event code: GR

Ref document number: 1162951

Country of ref document: HK