AR035366A1 - Derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, sus sales de monoclorhidrato y de diclorhidrato, un proceso para su preparacion, y un metodo de utilizacion de los mismos para la elaboracion de un producto radiofarmaceutico destinado al diagnóstico de la enfermedad de alzheimer en un - Google Patents

Derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, sus sales de monoclorhidrato y de diclorhidrato, un proceso para su preparacion, y un metodo de utilizacion de los mismos para la elaboracion de un producto radiofarmaceutico destinado al diagnóstico de la enfermedad de alzheimer en un

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Publication number
AR035366A1
AR035366A1 ARP010105127A ARP010105127A AR035366A1 AR 035366 A1 AR035366 A1 AR 035366A1 AR P010105127 A ARP010105127 A AR P010105127A AR P010105127 A ARP010105127 A AR P010105127A AR 035366 A1 AR035366 A1 AR 035366A1
Authority
AR
Argentina
Prior art keywords
preparation
alzheimer
disease
derivatives
diagnosis
Prior art date
Application number
ARP010105127A
Other languages
English (en)
Inventor
Christoph-Stephan Hilger
Bernd Johannsen
Richard Horuk
Harald Dinter
Raju Mohan
Joseph E Hesselgesser
Joerg Steinbach
Peter Maeding
Meredith Halks-Miller
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 AR035366A1 publication Critical patent/AR035366A1/es

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    • 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

Derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, de fórmula (1), donde: X1 y X2 son cada uno, independientemente entre sí, halo; R1 y R2 son cada uno, independientemente entre sí, hidrógeno o alquilo, y R3 es hidrógeno, amina, monoalquilamina, dialquilamina, monoaralquilamina, alquilcarbonilamina, alquenilcarbonilamina, haloalquilcarbonilamina, arilcarbonilamina, alcoxialquilcarbonilamina, alcoxicarbonilalquilcarbonilamina, glicinamida, monoalquilglicinamida, arilcarbonilglicinamida, aminocarbonilglicinamida, (aminocarbonil)(alquil)-glicinamida, (alcoxialquilcarbonil)glicinamida, ureido, monoalquilureido, monoarilureido, monoaralquilureido, o alaninamido; y donde cualquiera de X1 o X2 se selecciona del grupo formado por 123I, 125I, 128I, 131I, 75Br, 80Br y 18F; o donde uno de los átomos de carbono en el compuesto es 11C; o una sal aceptable para uso farmacéutico de los mismos. También se describen derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, en los cuales R3 es un radical -N(R4)R5, siendo R4 hidrógeno y R5 un quelante capaz de unirse a un átomo de metal radioactivo seleccionado de 1 grupo formado por 99mTc, 186Re y 188Re. Los compuestos radiofarmacéuticos de fórmula (1) tienen la capacidad para atravesar la barrera hematoencefálica y unirse al receptor CCR1 presente en el tejido del cerebro que padecen la enfermedad de Alzheimer. Por consiguiente, son usados para la elaboración de productos radiofarmacéuticos destinados al diagnóstico de la enfermedad de Alzheimer en un ser humano.
ARP010105127A 2000-11-06 2001-11-02 Derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, sus sales de monoclorhidrato y de diclorhidrato, un proceso para su preparacion, y un metodo de utilizacion de los mismos para la elaboracion de un producto radiofarmaceutico destinado al diagnóstico de la enfermedad de alzheimer en un AR035366A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US24629900P 2000-11-06 2000-11-06

Publications (1)

Publication Number Publication Date
AR035366A1 true AR035366A1 (es) 2004-05-12

Family

ID=22930075

Family Applications (1)

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ARP010105127A AR035366A1 (es) 2000-11-06 2001-11-02 Derivados de la 2-fenoxi-1-(4-bencilpiperazin-1-il)-etan-1-ona, sus sales de monoclorhidrato y de diclorhidrato, un proceso para su preparacion, y un metodo de utilizacion de los mismos para la elaboracion de un producto radiofarmaceutico destinado al diagnóstico de la enfermedad de alzheimer en un

Country Status (29)

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

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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
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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
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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
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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
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
HUP0301710A2 (hu) 2003-11-28

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