EA201001766A1 - Новые[f-18]-меченые производные l-глутаминовой кислоты и l-глутамина (i), их применение, а также способ их получения - Google Patents

Новые[f-18]-меченые производные l-глутаминовой кислоты и l-глутамина (i), их применение, а также способ их получения

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Publication number
EA201001766A1
EA201001766A1 EA201001766A EA201001766A EA201001766A1 EA 201001766 A1 EA201001766 A1 EA 201001766A1 EA 201001766 A EA201001766 A EA 201001766A EA 201001766 A EA201001766 A EA 201001766A EA 201001766 A1 EA201001766 A1 EA 201001766A1
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EA
Eurasian Patent Office
Prior art keywords
glutamine
new
production
way
acid
Prior art date
Application number
EA201001766A
Other languages
English (en)
Other versions
EA025217B1 (ru
Inventor
Лудгер Динкельборг
Матиас Берндт
Маттиас Фрибе
Хериберт Шмитт-Виллих
Детлев Зюльцле
Норман Коглин
Original Assignee
Байер Шеринг Фарма Акциенгезельшафт
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39970942&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201001766(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Байер Шеринг Фарма Акциенгезельшафт filed Critical Байер Шеринг Фарма Акциенгезельшафт
Publication of EA201001766A1 publication Critical patent/EA201001766A1/ru
Publication of EA025217B1 publication Critical patent/EA025217B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/04X-ray contrast preparations
    • A61K49/0433X-ray contrast preparations containing an organic halogenated X-ray contrast-enhancing agent
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations 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
    • A61K51/04Organic compounds
    • A61K51/0402Organic compounds carboxylic acid carriers, fatty acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/001Acyclic or carbocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions not involving the amino or carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/24Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one carboxyl group bound to the carbon skeleton, e.g. aspartic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63Esters of sulfonic acids
    • C07C309/64Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms
    • C07C309/65Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to acyclic carbon atoms of a saturated carbon skeleton
    • C07C309/66Methanesulfonates
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24Oxygen or sulfur atoms
    • C07D207/262-Pyrrolidones
    • C07D207/2732-Pyrrolidones 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 other ring carbon atoms
    • C07D207/277Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/282-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Описаны соединения и синтез [F-18]-меченой L-глутаминовой кислоты, [F-18]-меченого L-глутамата, их производные согласно формуле (I) и их применение.
EA201001766A 2008-05-20 2009-05-14 [f-18]-меченые производные l-глутаминовой кислоты и l-глутамина (i), их применение, а также способ их получения EA025217B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08075510A EP2123621A1 (de) 2008-05-20 2008-05-20 Neue {F-18}-markierte L-Glutaminsäure- und L-Glutaminderivate (I), ihre Verwendung sowie Verfahren zu ihrer Herstellung
PCT/EP2009/003420 WO2009141091A1 (de) 2008-05-20 2009-05-14 Neue [f-18] -markierte l-glutaminsäure- und l-glutaminderivate (i), ihre verwendung sowie verfahren zu ihrer herstellung

Publications (2)

Publication Number Publication Date
EA201001766A1 true EA201001766A1 (ru) 2011-12-30
EA025217B1 EA025217B1 (ru) 2016-12-30

Family

ID=39970942

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201001766A EA025217B1 (ru) 2008-05-20 2009-05-14 [f-18]-меченые производные l-глутаминовой кислоты и l-глутамина (i), их применение, а также способ их получения

Country Status (25)

Country Link
US (3) US20110165076A1 (ru)
EP (2) EP2123621A1 (ru)
JP (2) JP2011520932A (ru)
KR (1) KR101636245B1 (ru)
CN (2) CN104356019A (ru)
AR (1) AR073845A1 (ru)
AU (1) AU2009250130B2 (ru)
BR (1) BRPI0913128A2 (ru)
CA (1) CA2723596C (ru)
CL (1) CL2009001240A1 (ru)
CO (1) CO6331330A2 (ru)
CR (1) CR11800A (ru)
DO (1) DOP2010000358A (ru)
EA (1) EA025217B1 (ru)
EC (1) ECSP10010617A (ru)
HK (1) HK1205099A1 (ru)
IL (1) IL208662A0 (ru)
MX (1) MX2010012636A (ru)
NZ (1) NZ589350A (ru)
PA (1) PA8827401A1 (ru)
PE (1) PE20091956A1 (ru)
SV (1) SV2010003739A (ru)
TW (2) TW201008585A (ru)
UY (1) UY31835A (ru)
WO (1) WO2009141091A1 (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2667395C (en) 2006-11-01 2016-05-10 Bayer Schering Pharma Aktiengesellschaft [f-18]-labeled l-glutamic acid, [f-18]-labeled l-glutamine, their derivatives and their use and processes for their preparation
EP2123621A1 (de) 2008-05-20 2009-11-25 Bayer Schering Pharma Aktiengesellschaft Neue {F-18}-markierte L-Glutaminsäure- und L-Glutaminderivate (I), ihre Verwendung sowie Verfahren zu ihrer Herstellung
JP2013510891A (ja) * 2009-11-17 2013-03-28 バイエル・ファルマ・アクチェンゲゼルシャフト F−18標識のグルタミン酸誘導体の製造法
DE102010036356A1 (de) * 2010-07-12 2012-01-12 Abx Advanced Biochemical Compounds Gmbh Vorrichtung zur Synthese radioaktiv markierter Verbindungen
DE102010063974B4 (de) * 2010-12-22 2021-10-07 Thomas Rühl Pharmakologische Wirkstoffe und Radiodiagnostika mit 18F-markierter 3-Aryl- oder 3-Heteroaryl-1,2,4-oxadiazoleinheit und Verfahren zu deren Herstellung
EP2520557A1 (en) 2011-05-03 2012-11-07 Bayer Pharma Aktiengesellschaft Novel precursors of glutamate derivatives
EP2520556A1 (en) 2011-05-03 2012-11-07 Bayer Pharma Aktiengesellschaft Radiolabeled amino acids for diagnostic imaging
US8784774B2 (en) * 2011-09-16 2014-07-22 General Electric Company Labeled molecular imaging agents and methods of use
CN103333079B (zh) * 2013-07-03 2016-08-17 广东回旋医药科技股份有限公司 亚氨基酸类pet显像剂及其制备方法与应用
US9468693B2 (en) 2014-01-23 2016-10-18 General Electric Company Labeled molecular imaging agents and methods of use
US9468692B2 (en) 2014-01-23 2016-10-18 General Electric Company Labeled molecular imaging agents and methods of use
CN106631863B (zh) * 2016-09-06 2018-08-17 中山大学附属第一医院 亚谷氨酸类pet显像剂的放射合成方法
CN109369445B (zh) * 2018-11-20 2021-10-15 首都医科大学 用于诊断和治疗的放射性谷氨酰胺衍生物及其制备方法
WO2023229997A1 (en) * 2022-05-23 2023-11-30 Board Of Regents, The University Of Texas System Cgmp-compliant automated [18f]fspg production for clinical examination

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DE1620522A1 (de) 1964-12-23 1970-04-23 Takeda Chemical Industries Ltd Verfahren zur Herstellung von 5-substituierten Isoxazolidonverbindungen
FR1461184A (fr) 1964-12-23 1966-01-07 Takeda Chemical Industries Ltd Procédé de préparation d'isoxazolidones substituées en position 5
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CA2421507A1 (en) 2000-09-01 2002-03-07 Karina Aprico Screen for glutamate reuptake inhibitors, stimulators, and modulators
DE10223451A1 (de) 2002-05-25 2003-12-24 Abx Gmbh Verfahren zur Herstellung von 18F-fluorierten alpha-Aminosäuren
WO2004110500A1 (en) 2002-08-02 2004-12-23 Mallinckrodt Inc. Radioactively labelled amino acid analogues, their preparation and use
US7483732B2 (en) 2004-04-15 2009-01-27 Boston Scientific Scimed, Inc. Magnetic resonance imaging of a medical device and proximate body tissue
EP1923382A1 (de) * 2006-11-18 2008-05-21 Bayer Schering Pharma Aktiengesellschaft [F-18] markierte L-Glutaminsäure, [F-18] markiertes Glutamin, ihre Derivate und ihre Verwendung sowie Verfahren zu ihrer Herstellung
EP2123621A1 (de) 2008-05-20 2009-11-25 Bayer Schering Pharma Aktiengesellschaft Neue {F-18}-markierte L-Glutaminsäure- und L-Glutaminderivate (I), ihre Verwendung sowie Verfahren zu ihrer Herstellung
CA2667395C (en) * 2006-11-01 2016-05-10 Bayer Schering Pharma Aktiengesellschaft [f-18]-labeled l-glutamic acid, [f-18]-labeled l-glutamine, their derivatives and their use and processes for their preparation
EP2123620A1 (en) 2008-05-20 2009-11-25 Bayer Schering Pharma Aktiengesellschaft {F-19}-labeled L-Glutamic acid and L-Glutamine derivative (III), use thereof and method for obtaining them

Also Published As

Publication number Publication date
HK1205099A1 (en) 2015-12-11
CA2723596A1 (en) 2009-11-26
CO6331330A2 (es) 2011-10-20
CN102083772A (zh) 2011-06-01
MX2010012636A (es) 2010-12-06
IL208662A0 (en) 2010-12-30
UY31835A (es) 2010-01-05
WO2009141091A1 (de) 2009-11-26
US20140154183A1 (en) 2014-06-05
US20110165076A1 (en) 2011-07-07
NZ589350A (en) 2012-08-31
TW201008585A (en) 2010-03-01
BRPI0913128A2 (pt) 2016-01-05
CN104356019A (zh) 2015-02-18
AR073845A1 (es) 2010-12-09
CA2723596C (en) 2016-08-02
ECSP10010617A (es) 2010-12-30
KR20110009165A (ko) 2011-01-27
JP2011520932A (ja) 2011-07-21
PE20091956A1 (es) 2010-02-05
CR11800A (es) 2011-01-12
DOP2010000358A (es) 2010-12-31
AU2009250130B2 (en) 2014-08-21
SV2010003739A (es) 2011-04-06
JP2015042671A (ja) 2015-03-05
PA8827401A1 (es) 2009-12-16
US9308282B2 (en) 2016-04-12
EP2282982A1 (de) 2011-02-16
US20100290991A1 (en) 2010-11-18
AU2009250130A1 (en) 2009-11-26
EA025217B1 (ru) 2016-12-30
KR101636245B1 (ko) 2016-07-07
WO2009141091A8 (de) 2010-11-11
TW201439043A (zh) 2014-10-16
CL2009001240A1 (es) 2010-07-19
EP2123621A1 (de) 2009-11-25

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