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

Info

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.)
Filing date
Publication date
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR073844A1 publication Critical patent/AR073844A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/16—Preparation 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
    • A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
    • A61K49/10—Organic compounds
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C07B59/001—Acyclic or carbocyclic compounds
    • 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
    • C07C229/34—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
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic 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
    • C07C237/04—Carboxylic 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
    • C07C237/06—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • 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

Landscapes

  • 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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Magnetic Resonance Imaging Apparatus (AREA)
  • Pyridine Compounds (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
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.
US8747809B2 (en) * 2009-08-14 2014-06-10 The Trustees Of The University Of Pennsylvania Single diastereomers of 4-fluoroglutamine and methods of their preparation and use
RU2012124810A (ru) * 2009-11-17 2013-12-27 Байер Фарма Акциенгезельшафт Способ получения f-18 меченных производных глутаминовой кислоты
EP2322171A3 (en) * 2009-11-17 2011-06-01 Bayer Schering Pharma Aktiengesellschaft Fluorine labeled L-glutamic acid derivatives
EP2520556A1 (en) * 2011-05-03 2012-11-07 Bayer Pharma Aktiengesellschaft Radiolabeled amino acids for diagnostic imaging
EP2520557A1 (en) * 2011-05-03 2012-11-07 Bayer Pharma Aktiengesellschaft Novel precursors of glutamate derivatives
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
KR20210100169A (ko) * 2018-12-18 2021-08-13 시엔펑 펑 글루타민 유도체가 동물 사료 첨가제의 제조에 있어서의 응용
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
CA2421507A1 (en) * 2000-09-01 2002-03-07 Karina Aprico 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
US7837982B2 (en) * 2005-06-23 2010-11-23 Emory University Imaging agents
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
US20140227191A1 (en) 2014-08-14
WO2009141090A1 (en) 2009-11-26
CN102083773A (zh) 2011-06-01
EP2282981A1 (en) 2011-02-16
CA2723594A1 (en) 2009-11-26
JP2011520931A (ja) 2011-07-21
PE20091926A1 (es) 2010-01-24
WO2009141090A8 (en) 2010-10-28
WO2009141090A9 (en) 2010-03-25
EP2123620A1 (en) 2009-11-25
UY31834A (es) 2010-01-05
US20110064673A1 (en) 2011-03-17
TW201010733A (en) 2010-03-16
KR20110013411A (ko) 2011-02-09

Similar Documents

Publication Publication Date Title
AR073844A1 (es) Acido l-glutamico y derivado l-glutamina (iii) uso de los mismos y metodo para obtenerlos , composiciones farmaceuticas y métodos de diagnostico de enfermedades
AR075583A1 (es) Derivados de isoxazol/o-piridina con eslabon etilo o etenilo
MX2010001189A (es) Derivados de naftiridina como modulares del canal de potasio.
MA45223B1 (fr) Nouveaux dérivés de pipéridinyle subsitués par (hétéro)aryle, leur procédé de préparation et compositions pharmaceutiques les contenant
AR064304A1 (es) Formulaciones de ansamicina y sus metodos de uso
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
AR074622A1 (es) Derivados de acido ciclopentanocarboxilico condensados sustituidos con acilamino y su uso como productos farmaceuticos
AR047972A1 (es) Derivado de bencimidazol, proceso de obtencion y composiciones farmaceuticas.
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR037983A1 (es) Derivados de pirido [2,1-a] isoquinolina
AR084976A1 (es) Compuestos de bifenileno sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
UY27666A1 (es) Nuevos derivados de piridina y quinolina
AR038843A1 (es) Derivados de fenetanolamina para el tratamiento de enfermedades respiratorias
HRP20070505B1 (hr) Spiro-oksindol spojevi i njihove upotrebe kao terapijska sredstva
AR070395A1 (es) Derivados de 4,5-dihidro-oxazol-2-il- amina
MX2015015893A (es) 2-fenilimidazo[1,2-a]pirimidinas como agentes formadores de imagen.
AR058379A1 (es) Derivados de arilpropionamida arilacrilamida arilpropinamida o arilmetilurea como inhibidores del factor xia. proceso de obtencion y composiciones farmaceuticas.
RU2008107733A (ru) Ингибиторы gsk-3
AR058546A1 (es) Derivados de 2- adamantilurea como inhibidores selectivos de 11 beta - hsd1
PE20090880A1 (es) Compuestos heterociclicos como inhibidores de fosfatidilinositol 3-cinasa
UY39032A (es) Compuestos heterocíclicos como agentes antivirales
AR063988A1 (es) Derivados heterociclicos, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
AR084011A1 (es) Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen
AR053526A1 (es) Derivados del acido alcanoico arilcicloalqui-sustituidos, composicion farmaceutica y procedimiento para su preparacion
WO2012101065A3 (en) Pyrimidine biaryl amine compounds and their use as cdk9 inhibitors

Legal Events

Date Code Title Description
FB Suspension of granting procedure