WO2012041292A3 - Verbindungen für die diagnostik neurodegenerativer erkrankungen an der retina - Google Patents

Verbindungen für die diagnostik neurodegenerativer erkrankungen an der retina Download PDF

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Publication number
WO2012041292A3
WO2012041292A3 PCT/DE2011/001779 DE2011001779W WO2012041292A3 WO 2012041292 A3 WO2012041292 A3 WO 2012041292A3 DE 2011001779 W DE2011001779 W DE 2011001779W WO 2012041292 A3 WO2012041292 A3 WO 2012041292A3
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WO
WIPO (PCT)
Prior art keywords
compounds
neurodegenerative diseases
retina
disease
diagnosing neurodegenerative
Prior art date
Application number
PCT/DE2011/001779
Other languages
English (en)
French (fr)
Other versions
WO2012041292A2 (de
Inventor
Boris Schmidt
Daniel Kieser
Alexander BOLÄNDER
Jochen Herms
Roland Hans Heyny-Von Haussen
Jiamin GU
Original Assignee
Klinikum Darmstadt Gmbh
Ludwig-Maximilians-Universität München
Technische Universität Darmstadt
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 Klinikum Darmstadt Gmbh, Ludwig-Maximilians-Universität München, Technische Universität Darmstadt filed Critical Klinikum Darmstadt Gmbh
Priority to EP11804932.9A priority Critical patent/EP2619590A2/de
Publication of WO2012041292A2 publication Critical patent/WO2012041292A2/de
Publication of WO2012041292A3 publication Critical patent/WO2012041292A3/de

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    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • G01N33/6893—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids related to diseases not provided for elsewhere
    • G01N33/6896—Neurological disorders, e.g. Alzheimer's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0032—Methine dyes, e.g. cyanine dyes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K49/00—Preparations for testing in vivo
    • A61K49/001—Preparation for luminescence or biological staining
    • A61K49/0013—Luminescence
    • A61K49/0017—Fluorescence in vivo
    • A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
    • A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
    • A61K49/0039—Coumarin dyes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2800/00—Detection or diagnosis of diseases
    • G01N2800/28—Neurological disorders

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Microbiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Food Science & Technology (AREA)
  • Cell Biology (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating, Analyzing Materials By Fluorescence Or Luminescence (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Gegenstand der vorliegenden Erfindung sind Verbindungen mit hoher Affinität für das Aβ-Protein, α-Synuclein oder für Tau-PHF-Aggregate, welche als vorzugsweise fluoreszente Sonden für die in vivo Diagnostik von neurodegenerativen Erkrankungen geeignet sind, wie z.B. Alzheimer Demenz und Morbus Parkinson. Die Verbindungen zeichnen sich durch geeignete physikochemische Eigenschaften (Anregungswellenlänge, Emissionswellenlänge, Stokes-Shift, Extinktion) sowie hoher Affinität und Selektivität zu den Zielproteinen aus.
PCT/DE2011/001779 2010-09-20 2011-09-20 Verbindungen für die diagnostik neurodegenerativer erkrankungen an der retina WO2012041292A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP11804932.9A EP2619590A2 (de) 2010-09-20 2011-09-20 Verbindungen für die diagnostik neurodegenerativer erkrankungen an der retina

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102010045796 2010-09-20
DE102010045796.5 2010-09-20

Publications (2)

Publication Number Publication Date
WO2012041292A2 WO2012041292A2 (de) 2012-04-05
WO2012041292A3 true WO2012041292A3 (de) 2013-03-28

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PCT/DE2011/001779 WO2012041292A2 (de) 2010-09-20 2011-09-20 Verbindungen für die diagnostik neurodegenerativer erkrankungen an der retina

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EP (1) EP2619590A2 (de)
WO (1) WO2012041292A2 (de)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10300155B2 (en) 2015-12-31 2019-05-28 Washington University Alpha-synuclein ligands
US9862682B2 (en) 2016-01-08 2018-01-09 BroadPharm Functionalized pegylated cyanine compounds, pharmaceutical compositions, and methods of use thereof
CA3031528A1 (en) * 2016-08-01 2018-02-08 Cognoptix, Inc. System and method for detecting tau protein in ocular tissue
CN107446379B (zh) * 2017-09-06 2019-03-19 江南大学 一种螺环类逆光致变色活性染料的合成
WO2023140228A1 (ja) * 2022-01-18 2023-07-27 国立大学法人東北大学 タンパク質の変性状態又は凝集状態を可視化する方法

Citations (4)

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Publication number Priority date Publication date Assignee Title
US20040152068A1 (en) * 2000-08-21 2004-08-05 Goldstein Lee E. Ocular diagnosis of Alzheimer's disease
DE102007061987A1 (de) * 2007-12-21 2009-06-25 Carl Zeiss Meditec Ag Vorrichtung und Verfahren zum Nachweisen von Molekülen im Auge
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ES2536449T3 (es) 2000-08-24 2015-05-25 University Of Pittsburgh Of The Commonwealth System Of Higher Education Derivados de tioflavina para uso en diagnosis de la enfermedad de Alzheimer
US7597878B2 (en) 2000-09-19 2009-10-06 Li-Cor, Inc. Optical fluorescent imaging
US8530483B2 (en) 2008-05-30 2013-09-10 Merck Sharp & Dohme Corp. Substituted azabenzoxazoles

Patent Citations (4)

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US20040152068A1 (en) * 2000-08-21 2004-08-05 Goldstein Lee E. Ocular diagnosis of Alzheimer's disease
DE102007061987A1 (de) * 2007-12-21 2009-06-25 Carl Zeiss Meditec Ag Vorrichtung und Verfahren zum Nachweisen von Molekülen im Auge
WO2010033861A1 (en) * 2008-09-18 2010-03-25 Cedars-Sinai Medical Center Optical method for the detection of alzheimer's disease
US20100190803A1 (en) * 2009-01-23 2010-07-29 Korea Institute Of Science And Technology Bis(styryl)pyrimidine or bis(styryl)benzene compounds, pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition for prevention or treatment of diseases featuring amyloids comprising the same as an active ingredient

Non-Patent Citations (5)

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Title
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JEYANTHY SUTHARSAN ET AL: "Rational Design of Amyloid Binding Agents Based on the Molecular Rotor Motif", CHEMMEDCHEM, vol. 5, no. 1, 4 January 2010 (2010-01-04), pages 56 - 60, XP055034870, ISSN: 1860-7179, DOI: 10.1002/cmdc.200900440 *
QIAN LI ET AL: "Styryl-Based Compounds as Potential in vivo Imaging Agents for â-Amyloid Plaques", CHEMBIOCHEM - A EUROPEAN JOURNAL OF CHEMICAL BIOLOGY, WILEY VCH, WEINHEIM, DE, vol. 8, no. 14, 24 September 2007 (2007-09-24), pages 1679 - 1687, XP002643260, ISSN: 1439-4227, [retrieved on 20070820], DOI: 10.1002/CBIC.200700154 *
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EP2619590A2 (de) 2013-07-31
WO2012041292A2 (de) 2012-04-05

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