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AR062795A1 - Marcacion con fluor radioactivo para diagnostico por imagenes - Google Patents

Marcacion con fluor radioactivo para diagnostico por imagenes

Info

Publication number
AR062795A1
AR062795A1 ARP070104086A ARP070104086A AR062795A1 AR 062795 A1 AR062795 A1 AR 062795A1 AR P070104086 A ARP070104086 A AR P070104086A AR P070104086 A ARP070104086 A AR P070104086A AR 062795 A1 AR062795 A1 AR 062795A1
Authority
AR
Argentina
Prior art keywords
aryl
heteroaryl
group
aralkyl
alkyl
Prior art date
Application number
ARP070104086A
Other languages
English (en)
Inventor
Linjing Mu
Aileen Hohne
Ulrich Klar
Ulrike Volgtmann
Ananth Sirinivasan
Simon Ametamey
Timo Stellfeld
Lutz Lehmann
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
Priority claimed from EP06076823A external-priority patent/EP1908472A1/en
Priority claimed from EP06076869A external-priority patent/EP1911452A1/en
Priority claimed from EP07090043A external-priority patent/EP1970064A1/en
Priority claimed from EP07090079A external-priority patent/EP1985624A3/en
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR062795A1 publication Critical patent/AR062795A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/13Labelling of peptides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/695Silicon compounds
    • 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
    • A61K49/085Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier conjugated systems
    • 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
    • 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
    • A61K49/14Peptides, e.g. proteins
    • 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
    • A61K51/0491Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07B59/004Acyclic, carbocyclic or heterocyclic compounds containing elements other than carbon, hydrogen, halogen, oxygen, nitrogen, sulfur, selenium or tellurium
    • 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
    • C07B59/008Peptides; Proteins
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0834Compounds having one or more O-Si linkage
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/0896Compounds with a Si-H linkage
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02Silicon compounds
    • C07F7/08Compounds having one or more C—Si linkages
    • C07F7/12Organo silicon halides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • C07K7/086Bombesin; Related peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Physics & Mathematics (AREA)
  • Optics & Photonics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nuclear Medicine (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque tiene la formula química general (1) en donde X representa un grupo saliente adecuado para fluoracion seleccionado entre el grupo que comprende hidrogeno y OR3, en donde R3 representa hidrogeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, heteroarilo o aralquilo, R1 y R2 se seleccionan, en forma independiente, entre el grupo que comprende hidrogeno, C1-10 lineal y ramificado, arilo, heteroarilo y aralquilo, -B1- se selecciona entre el grupo que comprende -[CH2]m-D-[CH2)n-A-, en donde n y m son, en forma independiente, cualquier numero entero entre 0 y 5, -D- representa una union, -S-, -O- o NR4-, en donde R4 representa hidrogeno, alquilo C1-10, arilo, heteroarilo o aralquilo, A representa alquilo, arilo sustituido o no sustituido o heteroarilo, E-Z1-Y1- representa una porcion seleccionada entre el grupo que comprende EO-C(=O)-, ENR5-C(=O)-, EC(=O)-O-, EC(=O)-NR5-, ENR5-SO2, -ESO2-NR5-, E-O-, E-(S)p-, E-NR5-, ENR6C(=O)-NR7-, ENR6-C(=O)NR7-, ENR6C(=S)-NR7-, ENR6-C(=S)NR7-, EO-C(=O)O-, EOC(=O)-O-, EOC(=S)-O-, EO-C(=S)O-, en donde el enlace simple largo que se muestra explícitamente en las formulas (2) es el enlace entre Z1 y Y1, y en donde las flechas que figuran en las formulas precedentes indican el enlace entre Z1 y Y1, R5, R6 y R7 representan, en forma independiente, hidrogeno, alquilo C1-10, arilo, heteroarilo o aralquilo lineal o ramificado, p es cualquier numero entero entre 1 y 3, y en donde E-Z1- es un radical agente de direccionamiento y E- es una biomolécula, o -B2- representa un alquil C1-10-, -aril- sustituido o no sustituido o -heteroarilo- sustituido o no sustituido, -Y2- se selecciona entre el grupo que comprende una union, - C(=O)-, -SO2-, -C(=O)-(CH2)d-, -S(=O)-, -C(=O)-C:::C-, -C(=O)-[CH2]m-D-[CH2]n-, -SO2-[CH2]m-D-[CH2]n-, -O-C(=O), -NR10-, -O-, -(S)p-, -NR12-C(=O)-, -NR12-C(=S)-, -O-C(=S)-, -cicloalquil C1-6-, -alquenil-, -heterocicloalquil-, -aril- sustituido o no sustituido, -heteroaril- sustituido o no sustituido, -aralquil-, -heteroaralquil-, -alquiloxi, -ariloxi-, -aralcoxi -NR13-SO2-, -SO2-NR13-, -O-C(=O)-NR13-, -NR12-C(=O)-NR13, -NH-NH- o -O-NH-, en donde d es un numero entero de 1 a 6, m y n son, en forma independiente, cualquier numero entero entre 0 y 5, -D- representa una union, - S-, -O- o -NR9-, en donde R9 representa hidrogeno, alquilo C1-10, arilo, heteroarilo o aralquilo, p es un numero entero de 1 a 3, R10 y R13 se seleccionan, en forma Independiente, entre el grupo que comprende hidrogeno, alquilo C1-10 sustituido o no sustituido lineal o ramificado, arilo, heteroarilo y aralquilo y R13 representa hidrogeno, alquilo C1-10 sustituido o no sustituido lineal o ramificado, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, aralquilo o heteroaralquilo, en donde E-Z2- es un agente de direccionamiento radical, en donde E es una biomolécula y Z2 representa una porcion seleccionada entre el grupo que comprende una union y un separador, en donde el separador es una secuencia de aminoácidos natural o artificial o un grupo no aminoácido y una sal aceptable para uso farmacéutico de un ácido inorgánico u orgánico del misma, un hidrato, complejo, éster, amida, solvato y prodroga del mismo.
ARP070104086A 2006-10-02 2007-09-14 Marcacion con fluor radioactivo para diagnostico por imagenes AR062795A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP06076823A EP1908472A1 (en) 2006-10-02 2006-10-02 Silicon derivatives for PET imaging
EP06076869A EP1911452A1 (en) 2006-10-11 2006-10-11 Silicon-derivates for PET-Imaging
EP07090043A EP1970064A1 (en) 2007-03-12 2007-03-12 Silicon-derivatives for pet-imaging
EP07090079A EP1985624A3 (en) 2007-04-23 2007-04-23 Single step method of radiofluorination of biologically active compounds or biomolecules

Publications (1)

Publication Number Publication Date
AR062795A1 true AR062795A1 (es) 2008-12-03

Family

ID=39030886

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070104086A AR062795A1 (es) 2006-10-02 2007-09-14 Marcacion con fluor radioactivo para diagnostico por imagenes

Country Status (21)

Country Link
US (1) US20090035215A1 (es)
EP (1) EP2074135A2 (es)
JP (1) JP2010505776A (es)
KR (1) KR20090085599A (es)
AR (1) AR062795A1 (es)
AU (1) AU2007304508A1 (es)
BR (1) BRPI0719956A2 (es)
CA (1) CA2664700A1 (es)
CO (1) CO6180444A2 (es)
CR (1) CR10703A (es)
IL (1) IL197817A0 (es)
MA (1) MA30824B1 (es)
MX (1) MX2009003617A (es)
NO (1) NO20091735L (es)
PA (1) PA8747601A1 (es)
PE (1) PE20081173A1 (es)
SV (1) SV2009003205A (es)
TN (1) TN2009000100A1 (es)
TW (1) TW200820988A (es)
UY (1) UY30596A1 (es)
WO (1) WO2008040441A2 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011089267A1 (en) * 2010-01-25 2011-07-28 Institut National De La Sante Et De La Recherche Medicale (Inserm) Silylated biomolecules
JP5717138B2 (ja) * 2011-05-23 2015-05-13 独立行政法人産業技術総合研究所 タンパク質固定化表面修飾材料
CN105452262A (zh) * 2013-06-06 2016-03-30 日产化学工业株式会社 烷氧基硅烷化合物、液晶取向剂、液晶取向膜和液晶表示元件
JP7266365B2 (ja) * 2015-05-26 2023-04-28 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 分子および生体分子の18f標識化に有用な新規な複素芳香環フッ化ケイ素アクセプタおよびその調製方法
DE112018005145T5 (de) 2017-09-15 2020-07-23 The Regents Of The University Of California Hemmung von aminoacylase 3 (aa3) bei der behandlung von krebs
WO2021226076A1 (en) * 2020-05-04 2021-11-11 The Research Foundation For The State University Of New York Positron imaging tomography imaging agent composition and method for detection of bacterial infection
US20230357100A1 (en) * 2020-09-28 2023-11-09 National Institutes for Quantum Science and Technology Method for producing radioactive labeled substance, device for producing radioactive labeled substance, and method for evaporatively concentrating radioactive metal nuclide

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5084555A (en) * 1989-08-21 1992-01-28 The Administrators Of The Tulane Educational Fund An octapeptide bombesin analog
US5732578A (en) * 1995-02-24 1998-03-31 Hyundai Metal Co., Ltd. Device for maintaining the horizontality of a door lock lever
TW432073B (en) * 1995-12-28 2001-05-01 Pfizer Pyrazolopyridine compounds
US6639076B1 (en) * 1998-08-18 2003-10-28 Eli Lilly And Company Growth hormone secretagogues
ATE303988T1 (de) * 1999-06-14 2005-09-15 Lilly Co Eli Inhibitoren von serin proteasen
WO2002044144A2 (en) * 2000-11-30 2002-06-06 Advanced Research And Technology Institute, Inc. Nucleophilic approach for preparing radiolabeled imaging agents and associated compounds
GB0206750D0 (en) * 2002-03-22 2002-05-01 Amersham Plc Radiofluorination methods
EP1597270A2 (en) * 2003-02-20 2005-11-23 University of South Florida Peptidomimetic inhibitors of stat3 activity and their medical uses
GB0305704D0 (en) * 2003-03-13 2003-04-16 Amersham Plc Radiofluorination methods
WO2005077967A1 (en) * 2004-02-13 2005-08-25 The University Of British Columbia Radiolabeled compounds and compositions, their precursors and methods for their production
US20080029548A1 (en) * 2006-05-05 2008-02-07 Ann De Wree Fabric treatment dispensing package

Also Published As

Publication number Publication date
WO2008040441A2 (en) 2008-04-10
CR10703A (es) 2009-06-25
US20090035215A1 (en) 2009-02-05
IL197817A0 (en) 2009-12-24
JP2010505776A (ja) 2010-02-25
KR20090085599A (ko) 2009-08-07
SV2009003205A (es) 2009-10-19
TW200820988A (en) 2008-05-16
WO2008040441A3 (en) 2009-01-08
AU2007304508A8 (en) 2009-05-14
PE20081173A1 (es) 2008-11-06
NO20091735L (no) 2009-06-30
PA8747601A1 (es) 2009-08-26
TN2009000100A1 (en) 2010-08-19
UY30596A1 (es) 2008-05-02
MA30824B1 (fr) 2009-10-01
BRPI0719956A2 (pt) 2014-04-29
CO6180444A2 (es) 2010-07-19
MX2009003617A (es) 2009-04-22
CA2664700A1 (en) 2008-04-10
AU2007304508A1 (en) 2008-04-10
EP2074135A2 (en) 2009-07-01

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