AR073844A1 - Acido l-glutamico y derivado l-glutamina (iii) uso de los mismos y metodo para obtenerlos , composiciones farmaceuticas y métodos de diagnostico de enfermedades - Google Patents

Acido l-glutamico y derivado l-glutamina (iii) uso de los mismos y metodo para obtenerlos , composiciones farmaceuticas y métodos de diagnostico de enfermedades

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Publication number
AR073844A1
AR073844A1 ARP090101804A ARP090101804A AR073844A1 AR 073844 A1 AR073844 A1 AR 073844A1 AR P090101804 A ARP090101804 A AR P090101804A AR P090101804 A ARP090101804 A AR P090101804A AR 073844 A1 AR073844 A1 AR 073844A1
Authority
AR
Argentina
Prior art keywords
unbranched
branched
alkyl
substituted
general formula
Prior art date
Application number
ARP090101804A
Other languages
English (en)
Inventor
Ludger Dinkelborg
Heribert Schmitt-Willich
Keith Graham
Matthias Friebe
Mathias Berndt
Norman Koglin
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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Publication date
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR073844A1 publication Critical patent/AR073844A1/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00Preparations for testing in vivo
    • A61K49/06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10Organic compounds
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • 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
    • C07C229/34Compounds 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
    • C07C229/36Compounds 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
    • 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
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/04Systems containing only non-condensed rings with a four-membered ring

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Radiology & Medical Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Hematology (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)
  • Pyridine Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Magnetic Resonance Imaging Apparatus (AREA)

Abstract

Acido glutámico fluorado (glutamato) y derivados de glutamina en donde el átomo de fluor es 19F. El ácido glutámico (glutamato) y derivados de glutamina son los compuestos de la formula general (1) que abarcan todos los posibles derivados de diastereoisomeros y/o enantiomeros o mezclas de los mismos. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula general (1) donde A es 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(alquil C1-5)2, f) NH2, g) N(H)-L, h) O-L o i) O-Z; y G es 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, o f) O-alquinilo C2-5 ramificado o no ramificado; y R1 y/o R2, son independientemente en forma separada, a) hidrogeno, b) 19F-alcoxi C1-10 ramificado o no ramificado, c) 19F-alquilo C1-10 ramificado o no ramificado, d) 19F-alquenilo C2-10 ramificado o no ramificado, e) 19F-alquinilo C2-10 ramificado o no ramificado, f) 19F-arilo C6-10 mono o bicíclico sustituido o no sustituido, g) 19F-alquil C6-10 arilo mono o bicíclico sustituido o no sustituido, h) 19F-heteroarilo C5-10 mono o bicíclico sustituido o no sustituido, i) 19F-alquil-heteroarilo C5-10 mono o bicíclico sustituido o no sustituido, j) 19F-cicloalquilo C3-6 sustituido o no sustituido, k) 19F-alquil-cicloalquilo C3-6 sustituido o no sustituido, l) hidroxilo, m) alquilo C1-5 ramificado o no ramificado o n) alcoxi C1-5 ramificado o no ramificado, donde alquilo se interrumpe opcionalmente o se reemplaza con O, S o N; con la salvedad de que uno de los sustituyentes R1 o R2 comprende un átomo de 19F y el otro sustituyente no comprende un átomo de 19F; y L es a) alquilo C1-5 ramificado o no ramificado, b) 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) alquinilo C2-5 ramificado o no ramificado; y Z es un ion metálico equivalente, con el significado de n = 0, 1, 2 o 3; y donde se comprenden las mezclas de todos los diastereomeros y/o enantiomeros posibles así como también los compuestos enantioméricamente puros y sales farmacéuticas de los mismos. Reivindicacion 4: Una composicion farmacéutica caracterizada porque comprende uno o más compuestos de la formula general (1) y un vehículo farmacéuticamente aceptable. Reivindicacion 5: Un método para obtener uno o más compuestos de la formula general (1) de acuerdo con la reivindicacion 1, caracterizado porque comprende la reaccion de un compuesto de la formula (1) no fluorado con un átomo de fluor o un derivado del mismo. Reivindicacion 14: Un método para el diagnostico por imágenes de enfermedades proliferativas, caracterizado porque comprende administrarle a un individuo que lo necesita una cantidad terapéuticamente eficaz de uno o más compuestos de la formula general (1) segun se definio en cualquiera de las reivindicaciones 1 a 3.
ARP090101804A 2008-05-20 2009-05-20 Acido l-glutamico y derivado l-glutamina (iii) uso de los mismos y metodo para obtenerlos , composiciones farmaceuticas y métodos de diagnostico de enfermedades AR073844A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08075509A EP2123620A1 (en) 2008-05-20 2008-05-20 {F-19}-labeled L-Glutamic acid and L-Glutamine derivative (III), use thereof and method for obtaining them

Publications (1)

Publication Number Publication Date
AR073844A1 true AR073844A1 (es) 2010-12-09

Family

ID=39967400

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090101804A AR073844A1 (es) 2008-05-20 2009-05-20 Acido l-glutamico y derivado l-glutamina (iii) uso de los mismos y metodo para obtenerlos , composiciones farmaceuticas y métodos de diagnostico de enfermedades

Country Status (11)

Country Link
US (2) US20110064673A1 (es)
EP (2) EP2123620A1 (es)
JP (1) JP2011520931A (es)
KR (1) KR20110013411A (es)
CN (1) CN102083773A (es)
AR (1) AR073844A1 (es)
CA (1) CA2723594A1 (es)
PE (1) PE20091926A1 (es)
TW (1) TW201010733A (es)
UY (1) UY31834A (es)
WO (1) WO2009141090A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2008052788A1 (de) * 2006-11-01 2008-05-08 Bayer Schering Pharma Aktiengesellschaft [f-18] markierte l-glutaminsäure, [f-18] markiertes l-glutamin, ihre derivate und ihre verwendung sowie verfahren zu ihrer herstellung
KR20120089846A (ko) * 2009-08-14 2012-08-14 더 트러스티스 오브 더 유니버시티 오브 펜실바니아 4-플루오로글루타민의 단일 부분입체이성질체, 및 그의 제조 및 사용 방법
EP2322171A3 (en) * 2009-11-17 2011-06-01 Bayer Schering Pharma Aktiengesellschaft Fluorine labeled L-glutamic acid derivatives
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
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
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
CN109467514B (zh) * 2018-11-15 2020-11-24 西北师范大学 一种α-胺基-γ-羰基庚二酸酯类化合物的合成方法
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
CN110582207B (zh) * 2018-12-18 2022-11-11 广州英赛特生物技术有限公司 一种谷氨酰胺衍生物在制备动物饲料添加剂中的应用
WO2021011492A1 (en) * 2019-07-12 2021-01-21 University Of Mississippi L-y-methyleneglutamine compounds and methods of use

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9324872D0 (en) * 1993-12-03 1994-01-19 Univ Pasteur Pharmaceutical compounds
US5721265A (en) * 1994-08-05 1998-02-24 Sri International Fluorinated 2-nitroimidazole analogs for detecting hypoxic tumor cells
AU2001278945A1 (en) * 2000-08-10 2002-02-25 Eli Lilly And Company 4-substituted d-glutamic acid derivatives for use as antibiotic
EP1314041A2 (en) * 2000-09-01 2003-05-28 Annovis, Inc. Screen for glutamate reuptake inhibitors, stimulators, and modulators
KR20050033067A (ko) * 2002-08-02 2005-04-08 말린크로트, 인코포레이티드 방사성 라벨된 아미노산 유사체, 그 제조방법 및 용도
US7483732B2 (en) * 2004-04-15 2009-01-27 Boston Scientific Scimed, Inc. Magnetic resonance imaging of a medical device and proximate body tissue
JP2009505947A (ja) * 2005-06-23 2009-02-12 エモリー・ユニバーシティ 画像化剤
WO2008052788A1 (de) * 2006-11-01 2008-05-08 Bayer Schering Pharma Aktiengesellschaft [f-18] markierte l-glutaminsäure, [f-18] markiertes l-glutamin, ihre derivate und ihre verwendung sowie verfahren zu ihrer herstellung

Also Published As

Publication number Publication date
PE20091926A1 (es) 2010-01-24
UY31834A (es) 2010-01-05
EP2123620A1 (en) 2009-11-25
JP2011520931A (ja) 2011-07-21
US20110064673A1 (en) 2011-03-17
WO2009141090A1 (en) 2009-11-26
WO2009141090A8 (en) 2010-10-28
TW201010733A (en) 2010-03-16
CA2723594A1 (en) 2009-11-26
WO2009141090A9 (en) 2010-03-25
CN102083773A (zh) 2011-06-01
US20140227191A1 (en) 2014-08-14
EP2282981A1 (en) 2011-02-16
KR20110013411A (ko) 2011-02-09

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