WO2002016333A3 - Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease - Google Patents

Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease Download PDF

Info

Publication number
WO2002016333A3
WO2002016333A3 PCT/US2001/026427 US0126427W WO0216333A3 WO 2002016333 A3 WO2002016333 A3 WO 2002016333A3 US 0126427 W US0126427 W US 0126427W WO 0216333 A3 WO0216333 A3 WO 0216333A3
Authority
WO
WIPO (PCT)
Prior art keywords
disease
diagnosis
derivatives
alzheimer
theraphy
Prior art date
Application number
PCT/US2001/026427
Other languages
French (fr)
Other versions
WO2002016333A2 (en
Inventor
William E Klunk
Chester A Mathis Jr
Yanming Wang
Original Assignee
Univ Pittsburgh
William E Klunk
Chester A Mathis Jr
Yanming Wang
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 to JP2002521434A priority Critical patent/JP5022554B2/en
Priority to BRPI0113470-1 priority patent/BRPI0113470B8/en
Application filed by Univ Pittsburgh, William E Klunk, Chester A Mathis Jr, Yanming Wang filed Critical Univ Pittsburgh
Priority to HU1500560A priority patent/HU230581B1/en
Priority to SI200131017T priority patent/SI1334091T1/en
Priority to EP01966165A priority patent/EP1334091B1/en
Priority to ES01966165T priority patent/ES2395721T3/en
Priority to CA2419420A priority patent/CA2419420C/en
Priority to AU2001286702A priority patent/AU2001286702B2/en
Priority to HU0302956A priority patent/HU230375B1/en
Priority to DK01966165.1T priority patent/DK1334091T3/en
Priority to AU8670201A priority patent/AU8670201A/en
Priority to PL360550A priority patent/PL215711B1/en
Publication of WO2002016333A2 publication Critical patent/WO2002016333A2/en
Publication of WO2002016333A3 publication Critical patent/WO2002016333A3/en
Priority to NO20030860A priority patent/NO330176B1/en
Priority to HK04100858.7A priority patent/HK1058041A1/en
Priority to AU2008202626A priority patent/AU2008202626B9/en
Priority to LTPA2015001C priority patent/LTC1334091I2/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles condensed with carbocyclic rings
    • 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
    • A61K51/0497—Organic compounds conjugates with a carrier being an organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C07D277/66—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2 with aromatic rings or ring systems directly attached in position 2
    • 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

Abstract

This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, ∫i⊃in vivo∫/i⊃ imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The Disease, familial Alzheimer's Disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.
PCT/US2001/026427 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease WO2002016333A2 (en)

Priority Applications (16)

Application Number Priority Date Filing Date Title
HU0302956A HU230375B1 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and treatment of alzheimer's disease
AU2001286702A AU2001286702B2 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease
HU1500560A HU230581B1 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and treatment of alzheimer's disease
SI200131017T SI1334091T1 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and therapy of alzheimer's disease
EP01966165A EP1334091B1 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and therapy of alzheimer's disease
ES01966165T ES2395721T3 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and therapy of Alzheimer's disease
BRPI0113470-1 BRPI0113470B8 (en) 2000-08-24 2001-08-24 amyloid binding compound, pharmaceutical composition and methods of compound synthesis, of in vivo detection of amyloid deposits in an individual and in human or animal tissue, of quantification of amyloid deposit in biopsy or postmortem tissue, and of distinguishing a brain from disease alzheimer of a normal brain
JP2002521434A JP5022554B2 (en) 2000-08-24 2001-08-24 Thioflavin derivatives for prenatal diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposits
CA2419420A CA2419420C (en) 2000-08-24 2001-08-24 Thioflavin derivatives for use in antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition
AU8670201A AU8670201A (en) 2000-08-24 2001-08-24 Thioflavin derivatives for use in antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition
DK01966165.1T DK1334091T3 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in the diagnosis and therapy of Alzheimer's disease
PL360550A PL215711B1 (en) 2000-08-24 2001-08-24 Thioflavin derivatives for use in antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition
NO20030860A NO330176B1 (en) 2000-08-24 2003-02-24 Amyloid Binding Compounds, Methods of Preparation and Use, Pharmaceutical Composition for In Vivo Imaging and Use thereof
HK04100858.7A HK1058041A1 (en) 2000-08-24 2004-02-09 Thioflavin derivatives and their use in diagnosis and therapy of alzheimer's disease
AU2008202626A AU2008202626B9 (en) 2000-08-24 2008-06-13 Thioflavin derivatives and their use in diagnosis and therapy of Alzheimer's disease
LTPA2015001C LTC1334091I2 (en) 2000-08-24 2015-01-19 Thioflavin derivatives and their use for diagnosis and therapy of Alzheimer's disease

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22760100P 2000-08-24 2000-08-24
US60/227,601 2000-08-24

Publications (2)

Publication Number Publication Date
WO2002016333A2 WO2002016333A2 (en) 2002-02-28
WO2002016333A3 true WO2002016333A3 (en) 2002-05-30

Family

ID=22853739

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/026427 WO2002016333A2 (en) 2000-08-24 2001-08-24 Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease

Country Status (19)

Country Link
US (5) US20020133019A1 (en)
EP (2) EP1334091B1 (en)
JP (2) JP5022554B2 (en)
CN (1) CN1285582C (en)
AU (3) AU8670201A (en)
BR (1) BRPI0113470B8 (en)
CA (1) CA2419420C (en)
CY (1) CY1113311T1 (en)
DK (2) DK2264018T3 (en)
ES (2) ES2536449T3 (en)
HK (2) HK1058041A1 (en)
HU (2) HU230375B1 (en)
LT (1) LTC1334091I2 (en)
NO (1) NO330176B1 (en)
PL (1) PL215711B1 (en)
PT (2) PT1334091E (en)
RU (1) RU2324686C2 (en)
SI (1) SI1334091T1 (en)
WO (1) WO2002016333A2 (en)

Families Citing this family (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6689753B1 (en) * 1999-11-05 2004-02-10 Axonyx, Inc. β sheet breaker peptide analogs that inhibit β pleated sheet formation in amyloid β-peptide
EP1266884A4 (en) * 2000-03-22 2003-04-23 Bf Res Inst Inc Image diagnosis probe based on substituted azobenzene or analogue thereof for disease attributable to amyloid accumulation and composition for image diagnosis containing the same
AU8517001A (en) 2000-08-21 2002-03-04 Gen Hospital Corp Methods for diagnosing a neurodegenerative condition
US7297326B2 (en) * 2000-08-21 2007-11-20 The General Hospital Corporation Ocular diagnosis of Alzheimer's disease
WO2002016333A2 (en) * 2000-08-24 2002-02-28 University Of Pittsburgh Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease
US7270800B2 (en) 2000-08-24 2007-09-18 University Of Pittsburgh Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
WO2002064084A2 (en) * 2000-11-02 2002-08-22 Cornell Research Foundation, Inc. In vivo multiphoton diagnostic detection and imaging of a neurodegenerative disease
WO2002051821A1 (en) * 2000-12-22 2002-07-04 Astrazeneca Ab Therapeutic compounds
GB0106953D0 (en) 2001-03-20 2001-05-09 Univ Aberdeen Neufofibrillary labels
US20060106074A1 (en) * 2001-11-28 2006-05-18 Peter Bernstein Er-b-selective ligands
US6774248B2 (en) 2001-12-18 2004-08-10 Wyeth Substituted 2-phenyl benzofurans as estrogenic agents
EP1820806A1 (en) * 2006-02-16 2007-08-22 Crossbeta Biosciences B.V. Affinity regions
AU2003239508A1 (en) 2002-05-21 2003-12-12 Bristol-Myers Squibb Company Indole compounds useful as impdh inhibitors
AU2003242233A1 (en) * 2002-06-12 2003-12-31 Bf Research Institute, Inc. Probe compound for image diagnosis of disease with amyloid accumulation, compound for staining age spots/diffuse age spots, and remedy for disease with amyloid accumulation
US20070003552A1 (en) * 2002-07-09 2007-01-04 Gebbink Martijn F B Cross-beta structure comprising amyloid binding proteins and methods for detection of the cross-beta structure, for modulating cross-beta structures fibril formation and for modulating cross-beta structure-mediated toxicity and method for interfering with blood coagulation
EP1380290A1 (en) * 2002-07-09 2004-01-14 Universitair Medisch Centrum Utrecht Cross-beta structure pathway and its therapeutic relevance
WO2004035522A1 (en) * 2002-08-30 2004-04-29 Bf Research Institute, Inc. Diagnostic probes and remedies for diseases with accumulation of prion protein, and stains for prion protein
PT1587821E (en) 2002-12-19 2008-09-23 Scripps Research Inst Compositions and methods for stabilizing transthyretin and inhibiting transthyretin misfolding
GB0229686D0 (en) 2002-12-20 2003-01-29 Amersham Plc Solid-phase fluorination of benzothiazoles
CA2438032C (en) * 2003-03-14 2013-05-07 University Of Pittsburgh Benzothiazole derivative compounds, compositions and uses
CN1784392A (en) * 2003-03-14 2006-06-07 匹兹堡大学 Benzothiazole derivative compounds,compositions and uses
GB0307855D0 (en) * 2003-04-04 2003-05-14 Novartis Ag Organic compounds
WO2004100998A2 (en) 2003-05-07 2004-11-25 General Electric Company Compositions and methods for non-invasive imaging of soluble beta-amyloid
US20040223912A1 (en) * 2003-05-07 2004-11-11 Montalto Michael Christopher Compositions and methods for non-invasive imaging of soluble beta-amyloid
AU2004265174A1 (en) * 2003-08-13 2005-02-24 Bf Research Institute, Inc. Probe for diseases in which amyloid accumulates, agents for staining amyloid, drugs for treatment and prophylaxis of diseases with accumulated amyloid, and probes for diagnosis of neurofibrillary tangles and agents for staining neurofibrillary tangles.
WO2005016384A1 (en) * 2003-08-13 2005-02-24 Bf Research Institute, Inc. Probe for disease with amyloid deposit, amyloid-staining agent, remedy and preventive for disease with amyloid deposit and diagnostic probe and staining agent for neurofibril change
US8236282B2 (en) 2003-08-22 2012-08-07 University of Pittsburgh—of the Commonwealth System of Higher Education Benzothiazole derivative compounds, compositions and uses
WO2005042461A1 (en) * 2003-10-30 2005-05-12 Dojindo Laboratories Compound with amyloid affinity
EP1719529A4 (en) * 2004-02-25 2008-05-21 Astellas Pharma Inc Contrast medium for thrombus formation
CA2563063C (en) 2004-04-27 2014-06-03 Wyeth Purification of progesterone receptor modulators
GB0410448D0 (en) 2004-05-11 2004-06-16 Hammersmith Imanet Ltd Purification methods
EP1755585A4 (en) 2004-05-20 2009-04-01 Scripps Research Inst Transthyretin stabilization
CA2587248C (en) 2004-07-02 2014-01-07 William E. Klunk Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies
WO2006014382A1 (en) * 2004-07-02 2006-02-09 University Of Pittsburgh A method of diagnosing prodromal forms of diseases associated with amyloid deposition
US7772271B2 (en) 2004-07-14 2010-08-10 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
MX2007000481A (en) 2004-07-14 2007-03-29 Ptc Therapeutics Inc Methods for treating hepatitis c.
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
CA2573819A1 (en) * 2004-07-15 2006-02-23 The General Hospital Corporation Heterocyclic dye compounds for in vivo imaging and diagnosis of alzheimer's disease
MX2007000762A (en) 2004-07-22 2007-04-02 Ptc Therapeutics Inc Thienopyridines for treating hepatitis c.
US8114832B2 (en) 2005-07-13 2012-02-14 Crossbeta Biosciences B.V. Method for detecting and/or removing a protein comprising a cross-beta structure from a pharmaceutical composition
US20070015133A1 (en) * 2005-07-13 2007-01-18 Umc Utrecht Holding B.V. Method for detecting and/or removing protein and/or peptide comprising a cross-beta structure from an aqueous solution comprising a protein
BRPI0613525A2 (en) * 2005-07-13 2011-05-31 Crossbeta Biosciences Bv methods for producing an immunogenic composition, for enhancing the immunogenicity of a composition, for enhancing the immunogenicity of a vaccine composition, and for determining the amount of beta-cross structures in a vaccine composition, uses of beta-cross structures, and an immunogenic composition, subunit vaccine, and immunogenic composition
CA2615028A1 (en) * 2005-07-13 2007-01-18 Crossbeta Biosciences B.V. Cross-.beta. structure binding compounds
US20080305040A1 (en) * 2005-09-16 2008-12-11 University Of Pittsburgh In Vivo or in Vitro Method For Detecting Amyloid Deposits Having at Least One Amyloidogenic Protein
KR100778888B1 (en) * 2005-11-29 2007-11-28 재단법인서울대학교산학협력재단 Benzylideneaniline derivatives and their radioisotope labeled compounds for binding and imaging of ?-amyloid plaques
EP1956013B1 (en) 2005-11-30 2016-04-13 Fujifilm RI Pharma Co., Ltd. Diagnostic and remedy for disease caused by amyloid aggregation and/or deposition
WO2007064773A2 (en) * 2005-12-01 2007-06-07 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Isotopically-labeled benzothiazole compounds as imaging agents for amyloidogenic proteins
WO2007075595A2 (en) * 2005-12-20 2007-07-05 Vertex Pharmacueticals Incorporated Biofilm assay
US7781187B2 (en) * 2005-12-30 2010-08-24 Corning Incorporated Fluorescent dyes
TW201018678A (en) 2006-01-27 2010-05-16 Astrazeneca Ab Novel heteroaryl substituted benzothiazoles
KR101426093B1 (en) 2006-02-10 2014-08-01 서미트 코포레이션 피엘씨 Treatment of duchenne muscular dystrophy
JP5182747B2 (en) * 2006-03-28 2013-04-17 国立大学法人滋賀医科大学 Diagnostic imaging for intractable neurological diseases
TW200803903A (en) 2006-04-28 2008-01-16 Nihon Mediphysics Co Ltd Novel compound having affinity to amyloid
WO2008118122A2 (en) * 2006-05-08 2008-10-02 Molecular Neuroimaging, Llc Compounds and amyloid probes thereof for therapeutic and imaging uses
US8303935B2 (en) 2006-05-19 2012-11-06 Nihon Medi-Physics Co., Ltd. Alkoxy substituted imidazo[1,2-a]pyridines having affinity for amyloid
TW200813035A (en) 2006-06-19 2008-03-16 Astrazeneca Ab Novel heteroaryl substituted benzoxazoles
WO2007148755A1 (en) 2006-06-21 2007-12-27 Nihon Medi-Physics Co., Ltd. Novel compound having affinity for amyloid
WO2008015391A1 (en) * 2006-08-03 2008-02-07 Hammersmith Imanet Limited Method for the purification of radiolabelled compounds
JP5180838B2 (en) 2006-11-30 2013-04-10 日本メジフィジックス株式会社 Novel amyloid affinity compound
CN101668560A (en) * 2006-12-07 2010-03-10 宾夕法尼亚大学理事会 Acetylene derivatives and their use for binding and imaging amyloid plaques
AU2008211786B2 (en) * 2007-01-30 2014-07-03 Ge Healthcare Limited Tools for aiding in the diagnosis of neurodegenerative diseases
WO2008099800A1 (en) 2007-02-13 2008-08-21 Nihon Medi-Physics Co., Ltd. Method for production of radiation diagnostic imaging agent
TW200901998A (en) 2007-03-06 2009-01-16 Astrazeneca Ab Novel 2-heteroaryl substituted benzothiophenes and benzofuranes
CN101293878B (en) * 2007-04-25 2010-12-15 中国科学院上海应用物理研究所 Benzothiazole amino benzenes compounds, preparation method and application thereof
TW200911237A (en) 2007-08-03 2009-03-16 Summit Corp Plc Drug combinations for the treatment of duchenne muscular dystrophy
KR101571572B1 (en) * 2007-08-30 2015-11-24 지이 헬쓰케어 리미티드 Radiopharmaceutical composition
EP2213672A4 (en) * 2007-10-24 2012-05-02 Nihon Mediphysics Co Ltd Novel compound having affinity for amyloid
CA2704027A1 (en) 2007-10-26 2009-04-30 Nihon Medi-Physics Co., Ltd. Novel compound having affinity for amyloid
WO2009057575A1 (en) * 2007-10-30 2009-05-07 Nihon Medi-Physics Co., Ltd. Use of novel compound having affinity for amyloid, and process for production of the same
KR20100101577A (en) 2007-10-30 2010-09-17 니혼 메디피직스 가부시키가이샤 Utilization of novel compounds with amyloid affinity and method of producing the same
US20090123373A1 (en) * 2007-11-05 2009-05-14 Yanming Wang Amyloid-imaging agents
EP2058000A1 (en) * 2007-11-08 2009-05-13 Crossbeta Biosciences B.V. Immunogenic compositions capable of activating T cells
EP2058001A1 (en) * 2007-11-08 2009-05-13 Crossbeta Biosciences B.V. Enhancement of immunogenicity of antigens
AU2009253046A1 (en) * 2008-05-30 2009-12-03 Foster Wheeler Energia Oy Method of and system for generating power by oxyfuel combustion
EP2296474A1 (en) * 2008-05-30 2011-03-23 Merck Sharp & Dohme Corp. Novel substituted indoles
CA2725940A1 (en) 2008-05-30 2009-12-23 Merck Sharp & Dohme Corp. Novel substituted azabenzoxazoles
NZ588442A (en) * 2008-06-09 2013-01-25 Univ Muenchen L Maximilians Pyrazole, isoxazole and imidazole derivatives for treating diseases linked to protein aggregation and neurodegenerative diseases
US20100099609A1 (en) * 2008-07-28 2010-04-22 Buck Institute For Age Research eAPP AND DERIVATIVES FOR TREATMENT OF ALZHEIMER'S DISEASE
WO2010039815A1 (en) 2008-09-30 2010-04-08 Case Western Reserve University Molecular probes for imaging of myelin
EP2365974B1 (en) * 2008-11-06 2013-12-25 SNU R&DB Foundation Fluorinated benzothiazole derivatives, preparation method thereof and imaging agent for diagnosing altzheimer's disease using the same
US20100129290A1 (en) * 2008-11-26 2010-05-27 I.S.T. Corporation Smart contrast agent and detection method for detecting transition metal ions
CN101598703B (en) * 2009-07-03 2012-08-22 中国人民解放军第三军医大学第一附属医院 Application of dGTpase protein in preparing medicament for identifying and diagnosing Down syndrome foetus
FR2948685A1 (en) * 2009-07-30 2011-02-04 Biomerieux Sa NEW SUBSTRATES
US20110081428A1 (en) * 2009-09-16 2011-04-07 The Buck Institute For Age Research Use of thioflavin-like compounds to increase life span and/or health span
WO2012041292A2 (en) 2010-09-20 2012-04-05 Klinikum Darmstadt Gmbh Compounds for diagnosing neurodegenerative diseases at the retina
DE102010045797A1 (en) 2010-09-20 2012-03-22 Klinikum Darmstadt Gmbh Compounds for the diagnosis of neurodegenerative diseases of the olfactory epithelium
TWI528977B (en) 2011-05-20 2016-04-11 Nihon Mediphysics Co Ltd New amyloid affinity products
US9211350B2 (en) 2011-06-24 2015-12-15 Nihon Medi-Physics Co., Ltd. Compound with amyloid affinity
JPWO2013027694A1 (en) * 2011-08-24 2015-03-19 国立大学法人京都大学 Molecular imaging probe for conformation disease diagnosis
MX2014003043A (en) 2011-09-16 2015-02-05 Pfizer Solid forms of a transthyretin dissociation inhibitor.
CN102526765B (en) * 2011-12-31 2014-07-30 郑州泰基鸿诺药物科技有限公司 Abeta plaque developing agent and preparation method thereof
KR20130111082A (en) * 2012-03-30 2013-10-10 한미약품 주식회사 Aminostyrylbenzofuran derivatives as inhibitors against beta-amyloid fibril formation, and pharmaceutical composition comprising same
EP2890700B1 (en) * 2012-08-28 2017-12-13 Eberhard Karls Universität Tübingen Medizinische Fakultät Halogenated benzoxazines and their use
DK2890700T3 (en) 2012-08-28 2018-03-12 Univ Tuebingen Medizinische Fakultaet HALOGENATED BENZOXAZINES AND THEIR USE
WO2014097474A1 (en) 2012-12-21 2014-06-26 独立行政法人放射線医学総合研究所 Novel compound for imaging tau protein accumulated in the brain
US9246108B2 (en) 2012-12-28 2016-01-26 Dow Global Technologies Llc Quinoline-benzoxazole derived compounds for electronic films and devices
WO2014127365A1 (en) 2013-02-15 2014-08-21 Case Western Reserve University Psma ligands and uses thereof
CN105579453B (en) 2013-09-26 2017-12-22 豪夫迈·罗氏有限公司 The amine of imidazo [1,2 a] pyridine 7 as imaging tool
WO2015051188A1 (en) 2013-10-02 2015-04-09 Washington University Heterocyclic molecules for biomedical imaging and therapeutic applications
WO2015162870A1 (en) 2014-04-24 2015-10-29 想い出創造株式会社 Amyloid fiber formation limiter or inhibitor
CN104059028B (en) * 2014-06-06 2020-10-16 北京智博高科生物技术有限公司 Fluoro-2-aryl benzo heterocyclic compound with affinity with Abeta plaque and substituted chiral side chain, and preparation method and application thereof
JP6498412B2 (en) * 2014-10-17 2019-04-10 国立大学法人群馬大学 Novel thioflavin T derivative and use thereof
US9842938B2 (en) 2015-03-24 2017-12-12 Semiconductor Energy Laboratory Co., Ltd. Semiconductor device and display device including semiconductor device
WO2017156303A1 (en) 2016-03-09 2017-09-14 Case Western Reserve University Radioligands for myelin
ES2905539T3 (en) * 2016-03-11 2022-04-11 Ac Immune Sa Bicyclic compounds for diagnosis and therapy
CN109790184B (en) 2016-09-29 2021-06-29 韩国原子力研究院 Curcumin derivative, method for producing the same, and photoacoustic imaging agent for detecting β -amyloid plaques comprising curcumin derivative
SG11202009438UA (en) 2018-04-18 2020-11-27 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
US11167283B2 (en) 2018-05-04 2021-11-09 University Of South Carolina Dot blot box and use thereof
WO2019226491A1 (en) 2018-05-21 2019-11-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TWI759962B (en) 2019-11-13 2022-04-01 香港商新旭生技股份有限公司 Compounds for degrading tau protein aggregates and uses thereof
KR102426160B1 (en) 2020-07-13 2022-07-29 (주)바이오액츠 Novel fluorescent dyes for diagonizing Alzheimer and the preparation method thereof

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3257204A (en) * 1958-08-22 1966-06-21 Azoplate Corp Electrophotographic reproduction material
EP0081141A1 (en) * 1981-12-05 1983-06-15 BASF Aktiengesellschaft Urea derivatives, process for their preparation and their use in combating undesired plant growth
EP0118086A2 (en) * 1983-03-02 1984-09-12 Hoechst Aktiengesellschaft Two-component diazo type material
EP0287909A1 (en) * 1987-04-08 1988-10-26 Salutar, Inc. Amyloidosis and Alzheimer's disease diagnostic assay and reagents therefor
WO1995006469A1 (en) * 1993-08-28 1995-03-09 Cancer Research Campaign Technology Limited Benzazole compounds for use in therapy
WO1997026919A2 (en) * 1996-01-24 1997-07-31 Warner-Lambert Company Method of imaging amyloid deposits
WO1998017267A1 (en) * 1996-10-23 1998-04-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA241942A (en) 1924-08-05 Martinetto Vittorio Asynchronous machine
US4666829A (en) 1985-05-15 1987-05-19 University Of California Polypeptide marker for Alzheimer's disease and its use for diagnosis
US4933156A (en) * 1987-04-08 1990-06-12 Salutar, Inc. Amyloidosis and Alzheimer's disease diagnostic assay and reagents therefor
US5231000A (en) 1987-10-08 1993-07-27 The Mclean Hospital Antibodies to A4 amyloid peptide
CA1339014C (en) 1987-10-08 1997-03-25 Ronald E. Majocha Antibodies to a4 amyloid peptide
US5297562A (en) 1991-04-01 1994-03-29 President And Fellows Of Harvard College Method for detecting and treating Alzheimer's disease
US5434050A (en) 1991-08-13 1995-07-18 Regents Of The University Of Minnesota Labelled β-amyloid peptide and methods of screening for Alzheimer's disease
AU692237B2 (en) 1994-02-03 1998-06-04 Picower Institute For Medical Research, The Compositions and methods for advanced glycosylation endproduct-mediated modulation of amyloidosis
US6168776B1 (en) * 1994-07-19 2001-01-02 University Of Pittsburgh Alkyl, alkenyl and alkynyl Chrysamine G derivatives for the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
US6417178B1 (en) * 1994-07-19 2002-07-09 University Of Pittsburgh Amyloid binding nitrogen-linked compounds for the antemortem diagnosis of alzheimer's disease, in vivo imaging and prevention of amyloid deposits
GB9503946D0 (en) * 1995-02-28 1995-04-19 Cancer Res Campaign Tech Benzazole compounds
NZ307369A (en) 1995-05-01 1999-11-29 Univ Pittsburgh Azocompounds for the antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition
AU5354398A (en) 1996-11-22 1998-06-10 Elan Pharmaceuticals, Inc. N-(aryl/heteroaryl) amino acid derivatives, pharmaceutical compositions compri sing same, and methods for inhibiting beta-amyloid peptide release and/or it s synthesis by use of such compounds
CA2310330A1 (en) * 1997-11-20 1999-06-03 Teijin Limited Biphenylamidine derivatives
AU1089900A (en) 1998-06-30 2000-01-24 Kevin Mcclung Controlled-penetration projectile
GB9919673D0 (en) 1999-08-20 1999-10-20 Cancer Res Campaign Tech 2-Arlybenzazole compounds
US7270800B2 (en) 2000-08-24 2007-09-18 University Of Pittsburgh Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
WO2002016333A2 (en) * 2000-08-24 2002-02-28 University Of Pittsburgh Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease
WO2002051821A1 (en) 2000-12-22 2002-07-04 Astrazeneca Ab Therapeutic compounds
JP4317955B2 (en) 2001-04-23 2009-08-19 ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルバニア Amyloid plaque aggregation inhibitor and diagnostic contrast agent
GB0229686D0 (en) 2002-12-20 2003-01-29 Amersham Plc Solid-phase fluorination of benzothiazoles
CN1784392A (en) * 2003-03-14 2006-06-07 匹兹堡大学 Benzothiazole derivative compounds,compositions and uses
US8236282B2 (en) * 2003-08-22 2012-08-07 University of Pittsburgh—of the Commonwealth System of Higher Education Benzothiazole derivative compounds, compositions and uses
CA2587248C (en) * 2004-07-02 2014-01-07 William E. Klunk Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies
WO2007047204A1 (en) * 2005-10-11 2007-04-26 University Of Pittsburgh Isotopically-labeled benzofuran compounds as imagingagents foramyloidogenic proteins

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3257204A (en) * 1958-08-22 1966-06-21 Azoplate Corp Electrophotographic reproduction material
EP0081141A1 (en) * 1981-12-05 1983-06-15 BASF Aktiengesellschaft Urea derivatives, process for their preparation and their use in combating undesired plant growth
EP0118086A2 (en) * 1983-03-02 1984-09-12 Hoechst Aktiengesellschaft Two-component diazo type material
EP0287909A1 (en) * 1987-04-08 1988-10-26 Salutar, Inc. Amyloidosis and Alzheimer's disease diagnostic assay and reagents therefor
WO1995006469A1 (en) * 1993-08-28 1995-03-09 Cancer Research Campaign Technology Limited Benzazole compounds for use in therapy
WO1997026919A2 (en) * 1996-01-24 1997-07-31 Warner-Lambert Company Method of imaging amyloid deposits
WO1998017267A1 (en) * 1996-10-23 1998-04-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions

Non-Patent Citations (14)

* Cited by examiner, † Cited by third party
Title
BOGERT M T ET AL: "Researches on thiazoles. XVII. An investigation of the connection between constitution and color in the thioflavine group", COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 3, 1931, pages 480 - 498, XP002189040 *
CHEMICAL ABSTRACTS, vol. 86, no. 15, 11 April 1977, Columbus, Ohio, US; abstract no. 106455t, VAZ C J F ET AL: "6-Substituted 2-(p-aminostyryl)benzothiazole derivatives" page 499; XP002189043 *
CUADRO A ET AL: "Styryl and azastyryl 1,3-benzazoles with antihelmitic activity", IL FARMACO, vol. 47, no. 4, April 1992 (1992-04-01), pages 477 - 488, XP002189036 *
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; May 2001 (2001-05-01), MATHIS C A ET AL: "Lipophilic 11C-labelled thioflavin-T analogues for imaging amyloid plaques in Alzheimer's disease.", XP002189045, Database accession no. PREV200100390957 *
DATABASE BIOSIS [online] BIOSCIENCES INFORMATION SERVICE, PHILADELPHIA, PA, US; May 2001 (2001-05-01), WANG Y ET AL: "Synthesis and evaluation of a radioiodinated benzothiazole derivative as a radioligand for in vivo quantitation of beta-amyloid deposits in aging and Alzheimer's disease.", XP002189044, Database accession no. PREV200100392640 *
DRYANSKA V ET AL: "Alpha-hydroxybenzylation and benzylidenation of the methyl group in 2-methyl-1,3-benzoxazole and 2-methyl-1,3-benzothiazole", SYNTHESIS, no. 1, January 1976 (1976-01-01), pages 37 - 38, XP002189039 *
FOKKEN B ET AL: "Beitrag zur Darstellung von Verbindungen mit Amidino- bzw. Amidoximstruktur", PHARMAZIE, vol. 32, no. 10, October 1977 (1977-10-01), pages 566 - 569, XP002189037 *
GROZINGER K G ET AL: "Heterocyclic ethenyloxanilates as orally ative antiallergic agents", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY - CHIMICA THERAPEUTICA, vol. 20, no. 6, 1985, pages 487 - 491, XP002189038 *
INDIAN J. CHEM., SECT. B, vol. 14B, no. 9, 1976, pages 709 - 711 *
JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 44, no. Supplement 1, May 2001 (2001-05-01), Fourteenth International Symposium on Radiopharmaceutical Chemistry;Interlaken, Switzerland; June 10-15, 2001, pages S239 - S241, ISSN: 0362-4803 *
JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, vol. 44, no. Supplement 1, May 2001 (2001-05-01), Fourteenth International Symposium on Radiopharmaceutical Chemistry;Interlaken, Switzerland; June 10-15, 2001, pages S26 - S28, ISSN: 0362-4803 *
KLUNK W E ET AL: "Uncharged thioflavin-T derivatives bind to amyloid-beta protein with high affinity and readily enter the brain", LIFE SCIENCES, vol. 69, no. 13, 17 August 2001 (2001-08-17), pages 1471 - 1484, XP002189042 *
MARTVON A ET AL: "2-Phenyl-6-benzothiazolyl isothiocyanates", COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, vol. 39, no. 5, 1974, pages 1356 - 1365, XP002189041 *
SHI D-F ET AL: "Antitumor benzothiazoles. 3. Synthesis of 2-(4-aminophenyl) benzothiazoles and evaluation of their activities against breast cancer cell lines in vitro and in vivo", JOURNAL OF MEDICINAL CHEMISTRY, vol. 39, no. 17, 16 August 1996 (1996-08-16), pages 3375 - 3384, XP002189035 *

Also Published As

Publication number Publication date
WO2002016333A2 (en) 2002-02-28
DK2264018T3 (en) 2015-05-11
US9833458B2 (en) 2017-12-05
HUP1500560A2 (en) 2003-12-29
SI1334091T1 (en) 2013-01-31
JP2012102106A (en) 2012-05-31
HK1146725A1 (en) 2011-07-08
BR0113470A (en) 2003-12-30
CN1535268A (en) 2004-10-06
ES2536449T3 (en) 2015-05-25
AU8670201A (en) 2002-03-04
HUP0302956A2 (en) 2003-12-29
NO20030860D0 (en) 2003-02-24
CN1285582C (en) 2006-11-22
HU230581B1 (en) 2017-01-30
US20120095235A1 (en) 2012-04-19
BRPI0113470B1 (en) 2019-04-16
LTC1334091I2 (en) 2018-05-25
EP2264018A3 (en) 2012-04-25
US20150190400A1 (en) 2015-07-09
AU2008202626B9 (en) 2010-02-11
EP1334091B1 (en) 2012-09-19
US20080154042A1 (en) 2008-06-26
CY1113311T1 (en) 2016-04-13
CA2419420A1 (en) 2002-02-28
CA2419420C (en) 2011-08-02
AU2008202626A1 (en) 2008-07-03
DK1334091T3 (en) 2012-10-15
LTPA2015001I1 (en) 2015-02-25
EP1334091A2 (en) 2003-08-13
PL360550A1 (en) 2004-09-06
ES2395721T3 (en) 2013-02-14
HUP0302956A3 (en) 2006-05-29
EP2264018A2 (en) 2010-12-22
NO20030860L (en) 2003-04-24
AU2008202626B2 (en) 2010-02-04
US7351401B2 (en) 2008-04-01
US20050043377A1 (en) 2005-02-24
RU2324686C2 (en) 2008-05-20
BRPI0113470B8 (en) 2021-05-25
PL215711B1 (en) 2014-01-31
US20020133019A1 (en) 2002-09-19
AU2001286702B2 (en) 2008-03-13
JP5022554B2 (en) 2012-09-12
EP2264018B1 (en) 2015-02-11
PT2264018E (en) 2015-06-03
PT1334091E (en) 2013-01-07
HK1058041A1 (en) 2004-04-30
HU230375B1 (en) 2016-03-29
JP2004506723A (en) 2004-03-04
NO330176B1 (en) 2011-02-28

Similar Documents

Publication Publication Date Title
WO2002016333A3 (en) Thioflavin derivatives and their use in diagnosis and theraphy of alzheimer's disease
SI2527315T1 (en) Compounds, compositions and methods for the treatment of amyloid diseases and synucleinopathies such as Alzheimer's disease, type 2 diabetes and Parkinson's disease
CA2171882A1 (en) Inhibitors of .beta.-amyloid protein production
CA2427227A1 (en) Lactam compound
MX2009005279A (en) N- (methyl) -1h- pyrazol- 3 -amine, n- (methyl) -pyridin-2-amine and n- (methyl) -thiaz0l-2-amine derivatives for the treatment of diseases associated with amyloid or amyloid-like proteins, like e.g. alzheimer's.
WO2003053330A3 (en) Use of oxindole derivatives in the treatment of dementia related diseases, alzheimer’s disease and conditions associated with glycogen synthase kinase-3
WO2001009118A3 (en) Dithiolthione compounds for the treatment of neurological disorders and for memory enhancement
WO2008118122A3 (en) Compounds and amyloid probes thereof for therapeutic and imaging uses
IL188506A0 (en) Use of an immunogen for preparation of pharmaceutical composition for treating alzheimer's disease
EA200400881A1 (en) AZAARILPIPERAZINS
WO2001060826A3 (en) SUCCINOYLAMINO CARBOCYCLES AND HETEROCYCLES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
WO2005063745A8 (en) Novel spiroindoline or spiroisoquinoline compounds, methods of use and compositions thereof
WO2002096415A3 (en) Use of azetidinone substituted derivatives in the treatment of alzheimer's disease
DE69912808D1 (en) Use of hymenialdisine and its derivatives for the preparation of therapeutic agents
WO2005014041A3 (en) Use of an amyloid beta dna vaccine for the treatment and/or prevention of amyloid diseases
WO2003040183A3 (en) Compounds for the diagnosis/prevention/treatment of alzheimer's disease
ATE367387T1 (en) USE OF OXINDOL DERIVATIVES FOR THE TREATMENT OF DEMENTIA-RELATED DISEASES, ALZHEIMER'S DISEASE AND GLYCOGEN SYNTHASE KINASE-3-ASSOCIATED CONDITIONS
WO2004064869A3 (en) Amyloid-binding, metal-chelating agents
WO2005003103A3 (en) 2, 4, 6-tri-substituted 6-membered heterocycles and their use in the treatment of neurodegenerative diseases
HK1104280A1 (en) Derivatives of 1-phenylalkanecarboxylic acids for the treatment of neurodegenerative diseases
WO2006019685A3 (en) Compounds and their preparation for the treatment of alzheimer's disease by inhibiting beta-amyloid peptide production
BRPI0408274A (en) amyloid binding compounds, pharmaceutical composition and in vivo amyloid deposit detection method
WO2001062799A3 (en) Method for inhibiting angiogenesis using molecules that enhance plasmin activity
WO2005012330A3 (en) AMYLOID β-PEPTIDE AND METHODS OF USE
WO2005000406A3 (en) Treatment of amyloid- and epileptogenesis-associated diseases

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PH PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
WWE Wipo information: entry into national phase

Ref document number: 2002521434

Country of ref document: JP

Ref document number: 2419420

Country of ref document: CA

Ref document number: 2001286702

Country of ref document: AU

WWE Wipo information: entry into national phase

Ref document number: 2001966165

Country of ref document: EP

ENP Entry into the national phase

Country of ref document: RU

Kind code of ref document: A

Format of ref document f/p: F

Ref document number: 2003108256

Country of ref document: RU

Kind code of ref document: A

Format of ref document f/p: F

WWE Wipo information: entry into national phase

Ref document number: 018178847

Country of ref document: CN

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

WWP Wipo information: published in national office

Ref document number: 2001966165

Country of ref document: EP