EA200901347A1 - F-меченые фолаты - Google Patents

F-меченые фолаты

Info

Publication number
EA200901347A1
EA200901347A1 EA200901347A EA200901347A EA200901347A1 EA 200901347 A1 EA200901347 A1 EA 200901347A1 EA 200901347 A EA200901347 A EA 200901347A EA 200901347 A EA200901347 A EA 200901347A EA 200901347 A1 EA200901347 A1 EA 200901347A1
Authority
EA
Eurasian Patent Office
Prior art keywords
folates
tagged
folate
treatment
synthesis
Prior art date
Application number
EA200901347A
Other languages
English (en)
Inventor
Симон Менса Аметамей
Рудольф Мозер
Тобиас Лудвиг Росс
Фибе Лам
Виола Грён
Original Assignee
Мерк Эпрова Аг
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 Мерк Эпрова Аг filed Critical Мерк Эпрова Аг
Publication of EA200901347A1 publication Critical patent/EA200901347A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • 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
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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

Landscapes

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

Abstract

Настоящее изобретение относится к новому способу синтезаF-фолатных радиофармацевтических средств, где фтор-18 присоединен к птероату (или фолату) или его производному, путем прямого введения радиоактивного изотопа с[F]фторидом, а также кF-фолатным радиофармацевтическим средствам, полученным путем такого способа синтеза, и их применению для диагностики и мониторинга лечения злокачественного новообразования и лечения воспалительных и аутоиммунных заболеваний.
EA200901347A 2007-04-11 2008-04-11 F-меченые фолаты EA200901347A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP07105976 2007-04-11
PCT/EP2008/054404 WO2008125613A1 (en) 2007-04-11 2008-04-11 18f-labelled folates

Publications (1)

Publication Number Publication Date
EA200901347A1 true EA200901347A1 (ru) 2010-04-30

Family

ID=39620260

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200901347A EA200901347A1 (ru) 2007-04-11 2008-04-11 F-меченые фолаты

Country Status (15)

Country Link
US (2) US20100111864A1 (ru)
EP (1) EP2146944B1 (ru)
JP (1) JP2010523624A (ru)
KR (2) KR20160074683A (ru)
CN (2) CN107573347A (ru)
AU (1) AU2008237930B2 (ru)
CA (1) CA2670363C (ru)
DK (1) DK2146944T3 (ru)
EA (1) EA200901347A1 (ru)
ES (1) ES2449774T3 (ru)
IL (1) IL201248A (ru)
PL (1) PL2146944T3 (ru)
PT (1) PT2146944E (ru)
WO (1) WO2008125613A1 (ru)
ZA (1) ZA200903486B (ru)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101756793B1 (ko) 2008-10-10 2017-07-11 메르크 앤드 씨에 Ｐｅｔ 방사성트레이서로서의 18ｆ-표지화된 엽산
CN103608337B (zh) 2011-05-13 2016-07-06 Futurechem株式会社 Pet放射性医疗用品的18f-标记前体及其制备方法
CA2839654C (en) 2011-08-22 2021-02-16 Merck & Cie 18f-saccharide-folates
DK2864329T3 (en) 2012-05-08 2019-01-21 Merck & Cie 18F-LABELED PHOLATE / ANTIFOLATE ANALOGS
JP6159803B2 (ja) 2012-09-04 2017-07-05 株式会社Ｎｔｔドコモ 内部相対的送受信機キャリブレーションのための方法および装置
WO2016044645A1 (en) * 2014-09-17 2016-03-24 Elmaleh David R Anticoagulant derivatives for cardiovascular imaging
RU2765573C2 (ru) 2016-08-12 2022-02-01 Телефонактиеболагет Лм Эрикссон (Пабл) Многолучевые кодовые книги с дополнительно оптимизированными издержками
WO2018029647A1 (en) 2016-08-12 2018-02-15 Telefonaktiebolaget Lm Ericsson (Publ) Configurable codebook for advanced csi feedback overhead reduction
MX2019001567A (es) 2016-08-12 2019-06-10 Ericsson Telefon Ab L M Mecanismos de notificacion ricos en informacion de estado de canal de capa 1 y capa 2.
EP3497809B1 (en) 2016-08-12 2023-03-08 Telefonaktiebolaget LM Ericsson (publ) Progressive advanced csi feedback
KR102031652B1 (ko) * 2018-01-19 2019-10-14 서울대학교산학협력단 전이체 단백질 과발현 관련 질환의 양성자방출단층촬영 방사성추적자, 형광영상 진단 및 광역학 치료를 위한 전이체 단백질 표적 리간드 및 이의 제조방법

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4202976A (en) * 1973-09-11 1980-05-13 Bayly Russell J Selenium-75 labelled derivatives of folates
GB1458978A (en) * 1973-12-11 1976-12-22 Radiochemical Centre Ltd Saturation analysis
US3989812A (en) 1974-08-09 1976-11-02 Smithkline Instruments, Inc. Folic acid derivatives and use in radio-assay
GB1501119A (en) 1974-12-20 1978-02-15 Radiochemical Centre Ltd Folate compounds
US4276280A (en) * 1976-09-29 1981-06-30 Becton, Dickinson And Company Radiolabeled derivatives of folic acid
US4298735A (en) * 1979-04-30 1981-11-03 Union Carbide Corporation Folic acid derivatives
US4337339A (en) * 1979-04-30 1982-06-29 Baker Instruments Corp. Process for preparation of folic acid derivatives
US4314988A (en) * 1979-10-31 1982-02-09 Baker Instruments Corp. Folic acid derivatives and process for preparation
JPS6144890A (ja) 1984-08-08 1986-03-04 Shionogi & Co Ltd 含フツ素メトトレキサ−ト誘導体
US4628090A (en) * 1984-08-21 1986-12-09 Rensselaer Polytechnic Institute Fluorine-containing antifolates incapable of polyglutanayte formation related compounds
US4584375A (en) * 1984-08-21 1986-04-22 Rensselaer Polytechnic Institute Fluorine-containing antifolates incapable of polyglutamate formation
US5286726A (en) 1990-04-12 1994-02-15 The Regents Of The University Of Michigan Difluoroglutamic acid conjugates with folates and anti-folates for the treatment of neoplastic diseases
US5066828A (en) 1990-04-12 1991-11-19 Merrell Dow Pharmaceuticals Inc. Difluoroglutamic acid conjugates with folates and anti-folates for the treatment of neoplastic diseases
CA2156657C (en) 1994-11-02 1999-06-15 Richard G. Beauclerc Gravity wedge for a slackless railcar connector assembly
AU1095799A (en) 1997-10-17 1999-05-10 Philip L. Fuchs Folic acid derivatives
US6093382A (en) * 1998-05-16 2000-07-25 Bracco Research Usa Inc. Metal complexes derivatized with folate for use in diagnostic and therapeutic applications
EP1389209B1 (en) 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
CN101648028B (zh) 2002-05-06 2012-11-21 恩多塞特公司 维生素-定向的显象剂
GB0407952D0 (en) * 2004-04-08 2004-05-12 Amersham Plc Fluoridation method
EP1827239B1 (en) * 2004-12-23 2019-04-17 Purdue Research Foundation Positron emission tomography imaging method
WO2006101845A2 (en) 2005-03-16 2006-09-28 Endocyte, Inc. Synthesis and purification of pteroic acid and conjugates thereof
CA2606094A1 (en) * 2005-04-27 2006-11-02 Siemens Medical Solutions Usa, Inc. The preparation of molecular imaging probes using click chemistry
US20070009434A1 (en) 2005-07-05 2007-01-11 Low Philip S Imaging and therapeutic method using monocytes
JP2009504783A (ja) 2005-08-19 2009-02-05 エンドサイト，インコーポレイテッド ビンカアルカロイド、類似体および誘導体のリガンド結合体
CN103893778A (zh) 2005-08-19 2014-07-02 恩多塞特公司 多药物配体缀合物
WO2007038346A2 (en) 2005-09-23 2007-04-05 Purdue Research Foundation Multiphoton in vivo flow cytometry method and device
US20070119258A1 (en) 2005-11-15 2007-05-31 California Institute Of Technology Resonant vibratory device having high quality factor and methods of fabricating same
WO2007139815A2 (en) 2006-05-23 2007-12-06 Purdue Research Foundation Imaging and therapeutic method using progenitor cells
US8586595B2 (en) * 2007-02-07 2013-11-19 Purdue Research Foundation Positron emission tomography imaging method
US9315506B2 (en) * 2007-04-11 2016-04-19 Merck & Cie 18F-labelled folates
CN101657454B (zh) * 2007-04-11 2013-04-24 默克和西伊公司 18f-标记的叶酸类
KR101756793B1 (ko) * 2008-10-10 2017-07-11 메르크 앤드 씨에 Ｐｅｔ 방사성트레이서로서의 18ｆ-표지화된 엽산

Also Published As

Publication number Publication date
PT2146944E (pt) 2014-03-11
EP2146944B1 (en) 2014-01-22
AU2008237930A1 (en) 2008-10-23
US20100111864A1 (en) 2010-05-06
KR20090130111A (ko) 2009-12-17
IL201248A (en) 2016-02-29
CA2670363C (en) 2015-07-21
CN101646639A (zh) 2010-02-10
DK2146944T3 (da) 2014-02-03
JP2010523624A (ja) 2010-07-15
WO2008125613A1 (en) 2008-10-23
PL2146944T3 (pl) 2014-05-30
KR101781461B1 (ko) 2017-10-23
ES2449774T3 (es) 2014-03-21
US10377756B2 (en) 2019-08-13
US20150315189A1 (en) 2015-11-05
AU2008237930B2 (en) 2014-03-27
KR20160074683A (ko) 2016-06-28
IL201248A0 (en) 2010-05-31
EP2146944A1 (en) 2010-01-27
CN107573347A (zh) 2018-01-12
CA2670363A1 (en) 2008-10-23
ZA200903486B (en) 2010-01-27

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