AR073843A1 - Acido l-glutamico marcado con (f-18) y derivados de l-glutamina marcada con (f-18) (ii) su uso y procedimientos para su preparacion y composiciones farmaceuticas - Google Patents

Acido l-glutamico marcado con (f-18) y derivados de l-glutamina marcada con (f-18) (ii) su uso y procedimientos para su preparacion y composiciones farmaceuticas

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Publication number
AR073843A1
AR073843A1 ARP090101803A ARP090101803A AR073843A1 AR 073843 A1 AR073843 A1 AR 073843A1 AR P090101803 A ARP090101803 A AR P090101803A AR P090101803 A ARP090101803 A AR P090101803A AR 073843 A1 AR073843 A1 AR 073843A1
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AR
Argentina
Prior art keywords
unbranched
branched
alkyl
alkoxy
alkynyl
Prior art date
Application number
ARP090101803A
Other languages
English (en)
Inventor
Ludger Dinkelborg
Keith Graham
Heribert Schmitt-Willich
Lutz Lehmann
Mathias Berndt
Norman Koglin
Matthias Friebe
Original Assignee
Bayer Schering Pharma Ag
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.)
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Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR073843A1 publication Critical patent/AR073843A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/18—Heterocyclic 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
    • C07D207/22—Heterocyclic 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/273—2-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
    • C07D207/277—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D207/28—2-Pyrrolidone-5- carboxylic acids; Functional derivatives thereof, e.g. esters, nitriles
    • 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
    • A61K51/0402—Organic compounds carboxylic acid carriers, fatty acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds 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
    • C07C229/04—Compounds 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
    • C07C229/24—Compounds 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds 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
    • C07C229/28—Compounds 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 saturated and containing rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds 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
    • C07C229/34—Compounds 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 containing six-membered aromatic rings
    • C07C229/36—Compounds 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters 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
    • C07C271/22—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/04—Systems containing only non-condensed rings with a four-membered ring
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (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)
  • Physics & Mathematics (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)

Abstract

Compuestos y síntesis de ácido L-glutámico marcado [F-18], L-glutamato marcado [F-18], sus derivados de acuerdo con la formula (1) y su uso. Reivindicacion 1: Compuestos caracterizados porque responden a la formula general (1) en donde A representa: a) hidroxilo, b) alcoxi C1-5 ramificado o no ramificado, c) hidroxi-alcoxi C1-5 ramificado o no ramificado, d) O-alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado, e) N(alquilo C1-5)2, f) NH2, g) N(H)-L, h) O-L o i) O-Z; G representa: a) hidroxilo, b) O-Z, c) O-alquilo C1-5 ramificado o no ramificado, d) O-alquenilo C2-5 ramificado o no ramificado, e) O-alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado, f) O-alquinilo C2-5 ramificado o no ramificado o g) trifenilmetoxi; R1 y R2 representan: a) hidrogeno, b) 18F-alcoxi C6-10 ramificado o no ramificado, c) 18F-alquilo C6-10 ramificado o no ramificado, d) 18F-alquenilo C6-10 ramificado o no ramificado, e) 18F-alquinilo C6-10 ramificado o no ramificado, f) hidroxilo, g) alquilo C1-5 ramificado o no ramificado o h) alcoxi C1-5 ramificado o no ramificado, con la condicion de que uno de los sustituyentes R1 o R2 contenga un isotopo de 18F y el otro sustituyente no contenga isotopo de 18F; L representa: a) alquilo C1-5 ramificado o no ramificado, b) alquenilo C2-5 ramificado o no ramificado, c) alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado o d) alquinilo C2-5 ramificado o no ramificado; y Z representa un equivalente de un cation metálico, en donde n = 0, 1, 2 o 3; y comprenden todos los diastereomeros y enantiomeros. Reivindicacion 3: Método para obtener compuestos de la formula general (1) de la reivindicacion 1 caracterizado porque comprende disociar uno o varios grupos protectores presentes de un compuesto de la formula (2) de acuerdo con la reivindicacion 4. Reivindicacion 8: Uso de compuestos de la formula (3) caracterizado porque es para preparar compuestos de la formula (1) o (2) en donde A'' representa: a) alcoxi C1-5 ramificado o no ramificado, b) hidroxi-alcoxi C1-5 ramificado o no ramificado, c) O-alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado, d) N(alquilo C1-5)2, e) NH2, f) N(H)-L'' o g) O-L''; G'' representa: a) O-alquilo C1-5 ramificado o no ramificado, b) O-alquenilo C2-5 ramificado o no ramificado, c) O-alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado, d) O-alquinilo C2-5 ramificado o no ramificado o e) trifenilmetoxi; R3 y R4 representa: a) hidrogeno, b) E-alcoxi C6-10 ramificado o no ramificado, c) E-alquilo C6-10 ramificado o no ramificado, d) E-alquenilo C6-10 ramificado o no ramificado, e) E-alquinilo C6-10 ramificado o no ramificado, f) hidroxilo, g) alquilo C1-5 ramificado o no ramificado o h) alcoxi C1-5 ramificado o no ramificado, con la condicion de que uno de los sustituyentes R3 o R4 contenga un E y el otro sustituyente no contenga E; E representa un grupo lábil; Q' representa: a) N(H)-ter-butoxicarbonilo, b) N(H)-aliloxicarbonilo, c) N(H)-benciloxicarbonilo, d) N(H)-etoxicarbonilo, e) N(H)-metoxicarbonilo, f) N(H)-propoxicarbonilo, g) N(H)-2,2,2-tricloroetoxicarbonilo, h) N(H)-1,1-dimetilpropinilo, i) N(H)-1-metil-1-fenil-etoxicarbonilo, j) N(H)-1-metil-1-(4-bifenilil)-etoxicarbonilo, k) N(H)-ciclobutilcarbonilo, l) N(H)-1-metilciclobutilcarbonilo, m) N(H)-vinilcarbonilo, n) N(H)-alilcarbonilo, o) N(H)-adamantilcarbonilo, p) N(H)-difenilmetilcarbonilo, q) N(H)-cinamilcarbonilo, r) N(H)-formilo, s) N(H)-benzoilo, t) N(H)-tritilo, u) N(H)-p-metoxifenil-difenilmetilo, v) N(H)-di-(p-metoxifenil)-fenilmetilo, w) -N=CX'X'' o x) N-(ter-butoxicarbonilo)2; L'' representa: a) alquilo C1-5 ramificado o no ramificado, b) alquenilo C2-5, ramificado o no ramificado, c) alquilo C1-5-(O-alquilo C1-4)n-O-alquilo C1-4 ramificado o no ramificado o d) alquinilo C2-5 ramificado o no ramificado; X' y X'' representan, independientemente entre sí, a) alquilo C1-5 ramificado o no ramificado, b) arilo sustituido o no sustituido, c) alquilarilo sustituido o no sustituido o d) heteroarilo sustituido o no sustituido; y en donde n = 0, 1, 2 o 3; y comprenden todos los diastereomeros y enantiomeros. Reivindicacion 12: Composiciones farmacéuticas caracterizadas porque contienen compuestos de la formula general (1), (2), (3) o (4) y vehículos farmacéuticos apropiados.
ARP090101803A 2008-05-20 2009-05-20 Acido l-glutamico marcado con (f-18) y derivados de l-glutamina marcada con (f-18) (ii) su uso y procedimientos para su preparacion y composiciones farmaceuticas AR073843A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08075508A EP2123619A1 (de) 2008-05-20 2008-05-20 Neue [F-18]-Markierte L-Glutaminsäure-und L-Glutaminderivate (II), ihre Verwendung sowie Verfahren zu ihrer Herstellung

Publications (1)

Publication Number Publication Date
AR073843A1 true AR073843A1 (es) 2010-12-09

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ID=39767162

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Application Number Title Priority Date Filing Date
ARP090101803A AR073843A1 (es) 2008-05-20 2009-05-20 Acido l-glutamico marcado con (f-18) y derivados de l-glutamina marcada con (f-18) (ii) su uso y procedimientos para su preparacion y composiciones farmaceuticas

Country Status (13)

Country Link
US (1) US20110104057A1 (es)
EP (2) EP2123619A1 (es)
JP (1) JP2011522799A (es)
KR (1) KR20110009166A (es)
CN (1) CN102036936A (es)
AR (1) AR073843A1 (es)
CA (1) CA2723459A1 (es)
CL (1) CL2009001238A1 (es)
PA (1) PA8827201A1 (es)
PE (1) PE20100140A1 (es)
TW (1) TW201008586A (es)
UY (1) UY31836A (es)
WO (1) WO2009141079A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2009004686A (es) * 2006-11-01 2009-09-28 Bayer Schering Pharma Ag Acido l-glutamico marcado con [f-18], l-glutamina marcada con [f-18], sus derivados y su uso, asi como procedimientos para su preparacion.
CN102471235A (zh) * 2009-07-11 2012-05-23 拜耳医药股份有限公司 利用环烷基的放射性标记方法
RU2012124810A (ru) * 2009-11-17 2013-12-27 Байер Фарма Акциенгезельшафт Способ получения f-18 меченных производных глутаминовой кислоты
EP2520556A1 (en) * 2011-05-03 2012-11-07 Bayer Pharma Aktiengesellschaft Radiolabeled amino acids for diagnostic imaging
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
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1461184A (fr) 1964-12-23 1966-01-07 Takeda Chemical Industries Ltd Procédé de préparation d'isoxazolidones substituées en position 5
GB1474377A (en) 1973-09-11 1977-05-25 Beecham Group Ltd Naphthalene derivatives
EA002755B1 (ru) 1998-01-21 2002-08-29 Мерк Шарп Энд Домэ Лимитед Производные триазолопиридазина в качестве лигандов для гамк рецепторов
AU2001278945A1 (en) * 2000-08-10 2002-02-25 Eli Lilly And Company 4-substituted d-glutamic acid derivatives for use as antibiotic
KR20050033067A (ko) * 2002-08-02 2005-04-08 말린크로트, 인코포레이티드 방사성 라벨된 아미노산 유사체, 그 제조방법 및 용도
MX2009004686A (es) * 2006-11-01 2009-09-28 Bayer Schering Pharma Ag Acido l-glutamico marcado con [f-18], l-glutamina marcada con [f-18], sus derivados y su uso, asi como procedimientos para su preparacion.

Also Published As

Publication number Publication date
PE20100140A1 (es) 2010-03-21
EP2280915A1 (de) 2011-02-09
WO2009141079A1 (de) 2009-11-26
CA2723459A1 (en) 2009-11-26
KR20110009166A (ko) 2011-01-27
UY31836A (es) 2010-01-05
EP2123619A1 (de) 2009-11-25
US20110104057A1 (en) 2011-05-05
JP2011522799A (ja) 2011-08-04
CN102036936A (zh) 2011-04-27
PA8827201A1 (es) 2009-12-16
TW201008586A (en) 2010-03-01
CL2009001238A1 (es) 2010-06-04
WO2009141079A8 (de) 2010-11-18

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