HUP0301710A2 - Alzheimer-kór diagnosztizálására szolgáló radioaktív izotóppal jelzett gyógyszerkészítmények - Google Patents

Alzheimer-kór diagnosztizálására szolgáló radioaktív izotóppal jelzett gyógyszerkészítmények

Info

Publication number
HUP0301710A2
HUP0301710A2 HU0301710A HUP0301710A HUP0301710A2 HU P0301710 A2 HUP0301710 A2 HU P0301710A2 HU 0301710 A HU0301710 A HU 0301710A HU P0301710 A HUP0301710 A HU P0301710A HU P0301710 A2 HUP0301710 A2 HU P0301710A2
Authority
HU
Hungary
Prior art keywords
atom
glycineamido
hydrogen atom
disease
99mtc
Prior art date
Application number
HU0301710A
Other languages
English (en)
Inventor
Harald Dinter
Meredith Halks-Miller
Joseph E. Hesselgesser
Christoph-Stephan Hilger
Richard Horuk
Bernd Johannsen
Raju Mohan
Peter Mäding
Jörg Steinbach
Original Assignee
Schering 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 Schering Ag. filed Critical Schering Ag.
Publication of HUP0301710A2 publication Critical patent/HUP0301710A2/hu
Publication of HUP0301710A3 publication Critical patent/HUP0301710A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • 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
    • A61K51/041—Heterocyclic compounds
    • A61K51/044—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0459—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
    • 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
    • A61K51/0474—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group
    • A61K51/0478—Organic compounds complexes or complex-forming compounds, i.e. wherein a radioactive metal (e.g. 111In3+) is complexed or chelated by, e.g. a N2S2, N3S, NS3, N4 chelating group complexes from non-cyclic ligands, e.g. EDTA, MAG3
    • 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Optics & Photonics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)

Abstract

A találmány tárgya (I) és (II) általános képletű vegyületek ahol aképletekben X1 és X2 jelentése egymástól függetlenül halogénatom; R1és R2 jelentése egymástól függetlenül hidrogénatom vagy alkilcsoport;és R3 jelentése hidrogénatom, amino, monoalkil-amino, dialkilamino,monoaralkil-amino, alkil-karbonil-amino, alkenil-karbonil-amino,halogénezett-alkil-karbonil-amino, aril-karbonil-amino, alkoxi-alkil-karbonil-amino, alkoxi-karbonil-alkil-karbonil-amino, glicin-amido,monoalkil-glicin-amido, aril-karbonil-glicin-amido, amino-karbonil-glicin-amido, (amino-karbonil)-(alkil)-glicin-amido, (alkoxi-alkil-karbonil)-glicin-amido, ureido, monoalkil-ureido, monoaril-ureido,monoaralkil-ureido- vagy alanin-amido-csoport; és ahol X1 vagy X2egyikének jelentése 123 J, 125 J, 128 J, 131J, 75Br, 76Br, 80Br vagy18F atom; vagy ahol a vegyület egyik szénatomja 11C atom; R4 jelentésehidrogénatom; és R5 jelentése egy kelátképző szer, amely egyradioaktív fématomhoz, így 99mTC, 186Re, vagy 188Re atomhoz képeskötődni; vagy 99mTC, 186Re, vagy 188Re atommal képzett komplexeik; -vagy gyógyászatilag alkalmazható sóik. A találmány szerinti vegyületekaz Alzheimer-kór diagnosztizálásában alkalmazhatók. Ó
HU0301710A 2000-11-06 2001-11-01 Radiopharmaceuticals for diagnosing alzheimer's disease HUP0301710A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24629900P 2000-11-06 2000-11-06
PCT/EP2001/012607 WO2002036581A1 (en) 2000-11-06 2001-11-01 Radiopharmaceuticals for diagnosing alzheimer's disease

Publications (2)

Publication Number Publication Date
HUP0301710A2 true HUP0301710A2 (hu) 2003-11-28
HUP0301710A3 HUP0301710A3 (en) 2007-03-28

Family

ID=22930075

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0301710A HUP0301710A3 (en) 2000-11-06 2001-11-01 Radiopharmaceuticals for diagnosing alzheimer's disease

Country Status (29)

Country Link
US (2) US6676926B2 (hu)
EP (1) EP1332138B1 (hu)
JP (1) JP4234425B2 (hu)
KR (1) KR20030045167A (hu)
CN (1) CN1473158A (hu)
AR (1) AR035366A1 (hu)
AT (1) ATE314354T1 (hu)
AU (2) AU1403402A (hu)
BG (1) BG107762A (hu)
BR (1) BR0115150A (hu)
CA (1) CA2424598A1 (hu)
DE (1) DE60116365T2 (hu)
EA (1) EA006199B1 (hu)
EE (1) EE200300216A (hu)
HR (1) HRP20030459A2 (hu)
HU (1) HUP0301710A3 (hu)
IL (1) IL155191A0 (hu)
JO (1) JO2207B1 (hu)
MX (1) MXPA03003759A (hu)
NO (1) NO20032007L (hu)
NZ (1) NZ525303A (hu)
PE (1) PE20020531A1 (hu)
PL (1) PL361631A1 (hu)
SK (1) SK287495B6 (hu)
TW (1) TWI238820B (hu)
UY (1) UY27003A1 (hu)
WO (1) WO2002036581A1 (hu)
YU (1) YU33203A (hu)
ZA (1) ZA200304409B (hu)

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UY27003A1 (es) * 2000-11-06 2002-07-31 Schering Ag Productos radiofarmacéuticos para el diagnóstico de la enfermedad de alzheimer
BR0213452A (pt) 2001-10-22 2004-11-09 Pfizer Prod Inc Derivados de piperazina com atividade antagonista receptora de ccr1
JP5082033B2 (ja) 2001-12-21 2012-11-28 エグゼリクシス パテント カンパニー エルエルシー Ｌｘｒのモジュレーター
US7482366B2 (en) 2001-12-21 2009-01-27 X-Ceptor Therapeutics, Inc. Modulators of LXR
PL1620373T3 (pl) * 2003-05-07 2008-09-30 Bayer Schering Pharma Ag Urządzenie i sposób fluorowania nukleofilowego
US8257680B1 (en) 2004-02-24 2012-09-04 The General Hospital Corporation Catalytic radiofluorination
US9017724B2 (en) 2004-02-24 2015-04-28 The General Hospital Corporation Catalytic radiofluorination
AU2005216949B2 (en) * 2004-02-24 2011-09-22 The General Hospital Corporation Catalytic radiofluorination
GB0409236D0 (en) * 2004-04-26 2004-05-26 Novartis Ag Organic compounds
US7833513B2 (en) 2004-12-03 2010-11-16 Rhode Island Hospital Treatment of Alzheimer's Disease
KR100778888B1 (ko) * 2005-11-29 2007-11-28 재단법인서울대학교산학협력재단 베타아밀로이드 펩타이드 플라크의 영상화를 위한벤질리덴아닐린 계열의 유도체 및 그의 방사성 동위원소표지화합물
ES2399147T3 (es) 2006-09-08 2013-03-26 Rhode Island Hospital Tratamiento, prevención y reversión de una enfermedad hepática alcohólica
JP2010502719A (ja) 2006-09-08 2010-01-28 ロード アイランド ホスピタル アルコール誘発性脳疾患の治療、予防および回復
CN101563305A (zh) * 2006-12-21 2009-10-21 哈默史密斯网上成像有限公司 放射性标记方法
GB0625523D0 (en) 2006-12-21 2007-01-31 Ge Healthcare Ltd In vivo imaging agents
JP2011502966A (ja) * 2007-10-31 2011-01-27 アルセレス ファーマシューティカルズ， インコーポレイテッド ドーパミントランスポーターレベルを評価することによるレビー小体型認知症の診断およびレビー小体型認知症の処置のモニタリングのための方法
MX2010010314A (es) 2008-03-21 2011-04-12 Gen Hospital Corp Compuestos y composiciones para la deteccion y el tratamiento de la enfermedad de alzheimer y trastornos relacionados.
EP2161256A1 (en) * 2008-09-08 2010-03-10 Atomic Energy Council - Institute of Nuclear Energy Research Compound containing carboxylate ester and N2S2 ligand bi-functional groups and manufacturing method thereof
EP2163541A1 (en) * 2008-09-12 2010-03-17 Bayer Schering Pharma Aktiengesellschaft Piperazine derivatives for binding and imaging amyloid plaques and their use
WO2011041470A2 (en) * 2009-09-30 2011-04-07 Mallinckrodt Inc. Sustained-release opiate and opiate derivative compositions
TW201201846A (en) * 2010-02-08 2012-01-16 Bayer Schering Pharma Ag Iodo precursor for a PET imaging agent of amyloid plaques
WO2011110511A1 (en) * 2010-03-11 2011-09-15 Bayer Pharma Aktiengesellschaft Spect imaging agents of amyloid plaques
WO2012159107A1 (en) 2011-05-19 2012-11-22 Rhode Island Hospital Inhibition of renal fibrosis
EP4321165A2 (en) 2013-12-27 2024-02-14 National University Corporation Tokyo Medical and Dental University Method for diagnosis of alzheimer's disease and frontotemporal lobar degeneration, diagnostic agent, therapeutic agent, and screening method for said agents
US10137211B2 (en) 2015-08-28 2018-11-27 Chdi Foundation, Inc. Probes for imaging Huntingtin protein

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JPH06510021A (ja) 1991-03-13 1994-11-10 ザ リージェンツ オブ ザ ユニバーシティ オブ ミネソタ アルツハイマー病検出用の放射性薬剤
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Also Published As

Publication number Publication date
KR20030045167A (ko) 2003-06-09
EP1332138A1 (en) 2003-08-06
MXPA03003759A (es) 2003-07-28
UY27003A1 (es) 2002-07-31
PL361631A1 (en) 2004-10-04
TWI238820B (en) 2005-09-01
DE60116365D1 (de) 2006-02-02
AU1403402A (en) 2002-05-15
HUP0301710A3 (en) 2007-03-28
US20020131932A1 (en) 2002-09-19
US6676926B2 (en) 2004-01-13
PE20020531A1 (es) 2002-06-15
US6872381B1 (en) 2005-03-29
JP2004513123A (ja) 2004-04-30
BG107762A (en) 2004-03-31
EA006199B1 (ru) 2005-10-27
AR035366A1 (es) 2004-05-12
JP4234425B2 (ja) 2009-03-04
EE200300216A (et) 2003-08-15
EP1332138B1 (en) 2005-12-28
YU33203A (sh) 2006-05-25
JO2207B1 (en) 2004-10-07
NZ525303A (en) 2004-10-29
DE60116365T2 (de) 2006-08-24
SK5472003A3 (en) 2003-10-07
IL155191A0 (en) 2003-11-23
SK287495B6 (sk) 2010-12-07
CA2424598A1 (en) 2002-05-10
HRP20030459A2 (en) 2005-04-30
CN1473158A (zh) 2004-02-04
NO20032007L (no) 2003-07-02
AU2002214034B2 (en) 2006-01-05
EA200300507A1 (ru) 2003-12-25
WO2002036581A1 (en) 2002-05-10
BR0115150A (pt) 2003-12-30
ZA200304409B (en) 2004-09-06
ATE314354T1 (de) 2006-01-15
NO20032007D0 (no) 2003-05-05

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