RU2011139219A - Реагенты и способы введения радиоактивной метки - Google Patents
Реагенты и способы введения радиоактивной метки Download PDFInfo
- Publication number
- RU2011139219A RU2011139219A RU2011139219/04A RU2011139219A RU2011139219A RU 2011139219 A RU2011139219 A RU 2011139219A RU 2011139219/04 A RU2011139219/04 A RU 2011139219/04A RU 2011139219 A RU2011139219 A RU 2011139219A RU 2011139219 A RU2011139219 A RU 2011139219A
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- Prior art keywords
- formula
- compound
- peptide
- biomolecule
- ammonium
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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
- C07D213/79—Acids; Esters
- C07D213/80—Acids; Esters 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Optics & Photonics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Physics & Mathematics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pyridine Compounds (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Abstract
1. Соединение формулы (I):2. Соединение по п.1 формулы (Ia):3. Соединение формулы (II):или его соль, где L представляет собой уходящую группу, выбранную из хлоро, бромо, йодо, нитро и три(Cалкил)аммония (например триметиламмония).4. Соединение формулы (II) или его соль по п.3, где L представляет собой три(Cалкил)аммоний (например триметиламмоний).5. Соединение формулы (II) по п.3 или 4, представляющее собой:где Xпредставляет собой противоион и предпочтительно является трифторметансульфонатом.6. СпособF-фторирования, включающий взаимодействие соединения формулы (I) или (Ia), как они определены в п.1 или 2, с соединением формулы (III):с образованиемF-продукта формулы (IV):7. Способ по п.6, где биомолекула представляет собой пептид.8. Способ по п.6, где биомолекула представляет собой пептид, выбранный из аналогов соматостатина, таких как октреотид, бомбезин, вазоактивного интестинального пептида, аналогов хемотаксического пептида, α-меланоцитостимулирующего гормона, нейротензина, пептида Arg-Gly-Asp и его аналогов, соединяющего пептида проинсулина человека, эндотелина, ангиотензина и формил-норлейцил-лейцил-фенилаланил-норлейцил-тирозил-лизина.9. Способ по п.6, где биомолекула содержит фрагмент:10. Способ по любому из пп.6-9, где биомолекула представляет собой пептид формулы (A):где Xпредставляет собой либо -NH, либогде a является целым числом от 1 до 10; предпочтительно a равен 1.
Claims (10)
4. Соединение формулы (II) или его соль по п.3, где L представляет собой три(C1-6алкил)аммоний (например триметиламмоний).
7. Способ по п.6, где биомолекула представляет собой пептид.
8. Способ по п.6, где биомолекула представляет собой пептид, выбранный из аналогов соматостатина, таких как октреотид, бомбезин, вазоактивного интестинального пептида, аналогов хемотаксического пептида, α-меланоцитостимулирующего гормона, нейротензина, пептида Arg-Gly-Asp и его аналогов, соединяющего пептида проинсулина человека, эндотелина, ангиотензина и формил-норлейцил-лейцил-фенилаланил-норлейцил-тирозил-лизина.
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16449409P | 2009-03-30 | 2009-03-30 | |
GBGB0905438.8A GB0905438D0 (en) | 2009-03-30 | 2009-03-30 | Radiolabelling reagents and methods |
GB0905438.8 | 2009-03-30 | ||
US61/164,494 | 2009-03-30 | ||
PCT/US2010/028078 WO2010114723A1 (en) | 2009-03-30 | 2010-03-22 | Radiolabelling reagents and methods |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2011139219A true RU2011139219A (ru) | 2013-05-10 |
RU2524284C2 RU2524284C2 (ru) | 2014-07-27 |
Family
ID=40671939
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2011139219/04A RU2524284C2 (ru) | 2009-03-30 | 2010-03-22 | Реагенты и способы введения радиоактивной метки |
Country Status (15)
Country | Link |
---|---|
US (1) | US8530620B2 (ru) |
EP (1) | EP2414333B1 (ru) |
JP (1) | JP2012522052A (ru) |
KR (1) | KR20110133038A (ru) |
CN (2) | CN102356069B (ru) |
AU (1) | AU2010232828A1 (ru) |
BR (1) | BRPI1011531A2 (ru) |
CA (1) | CA2757016A1 (ru) |
ES (1) | ES2404346T3 (ru) |
GB (1) | GB0905438D0 (ru) |
MX (1) | MX2011010295A (ru) |
PL (1) | PL2414333T3 (ru) |
PT (1) | PT2414333E (ru) |
RU (1) | RU2524284C2 (ru) |
WO (1) | WO2010114723A1 (ru) |
Families Citing this family (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2732632C (en) | 2008-08-01 | 2018-01-09 | The Johns Hopkins University | Psma-binding agents and uses thereof |
EP2648767B1 (en) * | 2010-12-09 | 2023-03-15 | GE Healthcare Limited | Radiotracer compositions |
WO2013048811A1 (en) | 2011-09-30 | 2013-04-04 | Ge Healthcare Limited | Imaging and radiotherapy methods for tumour stem cells |
AR097683A1 (es) * | 2013-09-26 | 2016-04-06 | Lilly Co Eli | Compuestos y uso para la preparación de agentes de formación de imagen tau y formulaciones para la formación de imagen tau |
WO2016030329A1 (en) * | 2014-08-24 | 2016-03-03 | MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. | Method for the production of 18f-labeled active esters and their application exemplified by the preparation of a psma-specific pet-tracer |
PL3356385T3 (pl) * | 2015-09-30 | 2021-06-28 | Deutsches Krebsforschungszentrum | Tagowane 18F inhibitory antygenu błonowego specyficznego dla gruczołu krokowego (PSMA) i ich zastosowanie jako środków do obrazowania w nowotworze gruczołu krokowego |
GB201518918D0 (en) * | 2015-10-26 | 2015-12-09 | Norsk Medisinsk Syklotronsenter As And Uni I Oslo | Method |
WO2018022603A1 (en) * | 2016-07-25 | 2018-02-01 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methods of making 18f-labeled precursors and peptides, labeled c-met binding peptides, and methods of use thereof |
US11628229B2 (en) | 2017-03-13 | 2023-04-18 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Method of synthesizing 18F radiolabeled biomolecular agents |
GB202019006D0 (en) | 2020-12-02 | 2021-01-13 | Vestlandets Innovasjonsselskap As | GFR targeting compounds |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
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US5242680A (en) * | 1991-08-23 | 1993-09-07 | Merck & Co., Inc. | Thiol-reactive maleimido-based radiolabeling reagents |
US5346686A (en) * | 1992-10-05 | 1994-09-13 | Mallinckrodt Medical, Inc. | Labelled interleukin-8 and medical uses thereof |
HUP9900459A3 (en) * | 1996-01-23 | 1999-11-29 | Rapigene Inc Bothell | Methods and compositions for detecting binding of ligand pair using non-fluorescent label |
EP0932417B1 (en) * | 1996-10-17 | 2003-03-05 | Immunomedics, Inc. | Non-antigenic toxin-conjugate and fusion protein of internalizing receptor system |
JP3992923B2 (ja) * | 1997-09-03 | 2007-10-17 | イムノメディクス, インコーポレイテッド | F−18陽電子放出トモグラフィー用のタン白及びペプチドのフッ素化方法 |
US6350360B1 (en) | 2000-04-07 | 2002-02-26 | Sandia Coroporation | Method of fabricating a 3-dimensional tool master |
GB0115927D0 (en) * | 2001-06-29 | 2001-08-22 | Nycomed Amersham Plc | Solid-phase nucleophilic fluorination |
WO2003006491A2 (en) * | 2001-07-10 | 2003-01-23 | Amersham Health As | Peptide-based compounds for targeting intergin receptors |
FR2841554B1 (fr) | 2002-07-01 | 2008-01-18 | Commissariat Energie Atomique | Composes de maleimides marques, leur procede de preparation et leur utilisation pour le marquage de macromolecules |
GB0305704D0 (en) | 2003-03-13 | 2003-04-16 | Amersham Plc | Radiofluorination methods |
GB0317815D0 (en) | 2003-07-30 | 2003-09-03 | Amersham Health As | Imaging agents |
GB0329716D0 (en) | 2003-12-23 | 2004-01-28 | Amersham Plc | Radical trap |
GB0420344D0 (en) * | 2004-09-14 | 2004-10-13 | Amersham Plc | Diagnostic compounds |
BRPI0813671A2 (pt) * | 2007-06-20 | 2014-12-30 | Ge Healthcare Ltd | Métodos para radiofluoração, para gerar uma imagem de um corpo humano ou animal, e para formação de imagem, composto, e, formulação radiofarmacêutica |
JP5318874B2 (ja) * | 2007-09-10 | 2013-10-16 | ジーイー・ヘルスケア・リミテッド | 放射性フッ素化方法 |
FR2926079B1 (fr) | 2008-01-03 | 2012-12-28 | Commissariat Energie Atomique | Procede de preparation d'un derive de purine marque, ledit derive et ses utilisations |
-
2009
- 2009-03-30 GB GBGB0905438.8A patent/GB0905438D0/en not_active Ceased
-
2010
- 2010-03-22 CA CA2757016A patent/CA2757016A1/en not_active Abandoned
- 2010-03-22 KR KR1020117022881A patent/KR20110133038A/ko not_active Application Discontinuation
- 2010-03-22 CN CN201080013540.3A patent/CN102356069B/zh not_active Expired - Fee Related
- 2010-03-22 RU RU2011139219/04A patent/RU2524284C2/ru not_active IP Right Cessation
- 2010-03-22 EP EP10710143A patent/EP2414333B1/en not_active Not-in-force
- 2010-03-22 WO PCT/US2010/028078 patent/WO2010114723A1/en active Application Filing
- 2010-03-22 MX MX2011010295A patent/MX2011010295A/es active IP Right Grant
- 2010-03-22 PT PT107101438T patent/PT2414333E/pt unknown
- 2010-03-22 JP JP2012503484A patent/JP2012522052A/ja not_active Ceased
- 2010-03-22 ES ES10710143T patent/ES2404346T3/es active Active
- 2010-03-22 CN CN201410441411.4A patent/CN104292155A/zh active Pending
- 2010-03-22 PL PL10710143T patent/PL2414333T3/pl unknown
- 2010-03-22 AU AU2010232828A patent/AU2010232828A1/en not_active Abandoned
- 2010-03-22 BR BRPI1011531A patent/BRPI1011531A2/pt not_active IP Right Cessation
- 2010-03-22 US US13/256,511 patent/US8530620B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
ES2404346T3 (es) | 2013-05-27 |
RU2524284C2 (ru) | 2014-07-27 |
GB0905438D0 (en) | 2009-05-13 |
BRPI1011531A2 (pt) | 2016-03-29 |
US8530620B2 (en) | 2013-09-10 |
CN102356069A (zh) | 2012-02-15 |
WO2010114723A1 (en) | 2010-10-07 |
CA2757016A1 (en) | 2010-10-07 |
PL2414333T3 (pl) | 2013-07-31 |
CN102356069B (zh) | 2014-09-24 |
CN104292155A (zh) | 2015-01-21 |
US20120022227A1 (en) | 2012-01-26 |
PT2414333E (pt) | 2013-05-07 |
EP2414333A1 (en) | 2012-02-08 |
KR20110133038A (ko) | 2011-12-09 |
AU2010232828A1 (en) | 2011-10-13 |
MX2011010295A (es) | 2012-03-26 |
EP2414333B1 (en) | 2013-02-13 |
JP2012522052A (ja) | 2012-09-20 |
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MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20150323 |