ECSP034547A - Derivados de pirazol para el tratamiento de enfermedades virales - Google Patents

Derivados de pirazol para el tratamiento de enfermedades virales

Info

Publication number
ECSP034547A
ECSP034547A EC2003004547A ECSP034547A ECSP034547A EC SP034547 A ECSP034547 A EC SP034547A EC 2003004547 A EC2003004547 A EC 2003004547A EC SP034547 A ECSP034547 A EC SP034547A EC SP034547 A ECSP034547 A EC SP034547A
Authority
EC
Ecuador
Prior art keywords
alkyl
optionally substituted
aryl
heterocyclyl
compounds
Prior art date
Application number
EC2003004547A
Other languages
English (en)
Inventor
Philip Stephen Jones
Brian William Dymock
John Herbert Merrett
Martin John Parratt
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP034547A publication Critical patent/ECSP034547A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10Antimycotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18One oxygen or sulfur atom
    • C07D231/20One oxygen atom attached in position 3 or 5
    • C07D231/22One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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 chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invención se refiere a nuevos y conocidos derivados de pirazol, un proceso para su elaboración, las composiciones farmacéuticas y el uso de tales compuestos en medicina, en particular, los compuestos de fórmula I son inhibidores de la enzima transcriptasa reversa del virus de inmunodeficiencia humana que esta implicada en la replicación viral. Por consiguiente los compuestos de esta invención se pueden usar favorablemente como agentes terapéuticos para los procesos mediados por el virus de inmunodeficiencia humana (VIH. Específicamente la invención describe el uso de compuestos de fórmula I en donde (Gráfico) R1 es un C1-12- alquilo sustituido opcionalmente, arilo, heterociclilo o C1-4-alquilo sustituido con fenilo opcionalmente sustituido; R3 es C1-12-alquilo o C1-4alcoxi-C1-4-alquilo; A indica un grupo seleccionado de CH2-(aril-C1-4-alquilamino), CH2-(aril-C1-4-alcoxi), C1-4-alquilo sustituido con arilo opcionalmente sustituido o con heterociclilo opccionalmente sustituido; o A indica un grupo de fórmula CH2-U-heterociclilo, en donde U representa O, S o NR", donde R" es hidrógeno o C1-4 -alquilo; oA indica un grupo de fórmula CH(V)Z, en donde V representa OH o F, y en donde Z representa arilo o heterociclilo sustituido opcionalmente; X representa SoO; para el tratamiento de enfermedades mediadas por el virus de la inmunodeficiencia humana (VIH) o para la preparación de un medicamento para dicho tratamiento.
EC2003004547A 2000-10-10 2003-04-08 Derivados de pirazol para el tratamiento de enfermedades virales ECSP034547A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0024795.7A GB0024795D0 (en) 2000-10-10 2000-10-10 Pyrazole derivatives for the treatment of viral diseases

Publications (1)

Publication Number Publication Date
ECSP034547A true ECSP034547A (es) 2003-05-26

Family

ID=9900999

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2003004547A ECSP034547A (es) 2000-10-10 2003-04-08 Derivados de pirazol para el tratamiento de enfermedades virales

Country Status (28)

Country Link
US (2) US6699887B2 (es)
EP (1) EP1326843A1 (es)
JP (1) JP4015548B2 (es)
KR (1) KR100534158B1 (es)
CN (2) CN1680333A (es)
AR (1) AR030858A1 (es)
AU (2) AU2165102A (es)
BR (1) BR0114483A (es)
CA (1) CA2423515A1 (es)
CZ (1) CZ20031297A3 (es)
EC (1) ECSP034547A (es)
GB (1) GB0024795D0 (es)
GT (1) GT200100201A (es)
HR (1) HRP20030251A2 (es)
HU (1) HUP0302722A2 (es)
IL (1) IL154875A0 (es)
MA (1) MA26951A1 (es)
MX (1) MXPA03003070A (es)
NO (1) NO20031615L (es)
NZ (1) NZ524740A (es)
PA (1) PA8530301A1 (es)
PE (1) PE20020750A1 (es)
PL (1) PL362918A1 (es)
RU (1) RU2270832C2 (es)
UY (1) UY26956A1 (es)
WO (1) WO2002030907A1 (es)
YU (1) YU27203A (es)
ZA (1) ZA200302519B (es)

Families Citing this family (27)

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Publication number Priority date Publication date Assignee Title
ATE310719T1 (de) * 2000-09-29 2005-12-15 Topotarget Uk Ltd Carbaminsäurederivate enthaltend eine amidgruppe als hdac-inhibitoren
GB0113524D0 (en) 2001-06-04 2001-07-25 Hoffmann La Roche Pyrazole derivatives
EP1556381B1 (en) 2002-09-26 2008-02-20 Pfizer Limited Pyrazole amides for treating hiv infections
MXPA05003195A (es) * 2002-09-26 2005-06-08 Pfizer Derivados de pirazol como inhibidores de la transcriptasa inversa.
US7230025B2 (en) 2002-09-26 2007-06-12 Pfizer, Inc. Pyrazole derivatives
GB0223234D0 (en) * 2002-10-07 2002-11-13 Pfizer Ltd Chemical compounds
US6933312B2 (en) 2002-10-07 2005-08-23 Agouron Pharmaceuticals, Inc. Pyrazole derivatives
GB0223232D0 (en) * 2002-10-07 2002-11-13 Pfizer Ltd Chemical compounds
TW200423930A (en) * 2003-02-18 2004-11-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitors
EP1608629A1 (en) 2003-03-24 2005-12-28 F. Hoffmann-La Roche Ag Benzyl-pyridazinons as reverse transcriptase inhibitors
US7220772B2 (en) 2003-09-05 2007-05-22 Pfizer, Inc. Pyrazole derivatives
EP1775298B1 (en) * 2004-07-01 2013-03-20 Daiichi Sankyo Company, Limited Thienopyrazole derivative having pde7 inhibitory activity
US20070005049A1 (en) * 2005-06-30 2007-01-04 Comben Richard H Apparatus and Method of Treating Urinary Incontinence by Heating Urethra
CN101511812A (zh) * 2006-07-05 2009-08-19 辉瑞产品公司 作为细胞色素p450抑制剂的吡唑衍生物
DK2057125T3 (da) 2006-08-16 2011-05-16 Hoffmann La Roche Ikke-nucleosid revers transkriptase-inhibitorer
GB0713479D0 (en) * 2007-07-11 2007-08-22 Syngenta Participations Ag Substituted aromatic heterocyclic compounds as fungicides
RU2495878C2 (ru) 2007-12-21 2013-10-20 Ф.Хоффманн-Ля Рош Аг Гетероциклические антивирусные соединения
GB0823000D0 (en) * 2008-12-17 2009-01-28 Syngenta Participations Ag Isothiazole and pyrazole derivatives with plant growth regulating properties
NZ595233A (en) 2009-02-25 2013-01-25 Daiichi Sankyo Co Ltd Tricyclic pyrazolopyrimidine derivatives
FR2951549B1 (fr) 2009-10-15 2013-08-23 Olivier Schussler Procede d'obtention de bioprotheses medicales implantables
KR20130099006A (ko) 2010-08-23 2013-09-05 다이이찌 산쿄 가부시키가이샤 3 고리성 피라졸로피리미딘 유도체의 프리체 결정
JP5701884B2 (ja) 2010-08-23 2015-04-15 第一三共株式会社 三環性ピラゾロピリミジン誘導体の結晶
WO2014074628A1 (en) * 2012-11-08 2014-05-15 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Compounds for treating hiv and methods for using the compounds
US9925190B2 (en) 2015-02-16 2018-03-27 University of Pittsburgh—of the Commonwealth System of Higher Education Small molecules targeting HIV-1 Nef
JP7301042B2 (ja) 2018-03-30 2023-06-30 住友化学株式会社 複素環化合物及びそれを含有する有害節足動物防除組成物
WO2020081856A1 (en) * 2018-10-18 2020-04-23 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Inhibitors of hiv-1 nef for the treatment of hiv disease
FR3121927B1 (fr) 2021-04-19 2023-03-31 Eiffage Genie Civil Terrassement Procédé d’inertage des boues d’excavation

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WO1993015060A1 (fr) 1992-01-22 1993-08-05 Nissan Chemical Industries, Ltd. Derive de pyrazole substitue et bactericide agrohorticole
US6005109A (en) 1997-10-30 1999-12-21 Pflizer Inc. Pyrazoles and pyrazolopyrimidines having CRF antagonistic activity
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Also Published As

Publication number Publication date
YU27203A (sh) 2006-05-25
RU2270832C2 (ru) 2006-02-27
PA8530301A1 (es) 2002-07-30
NO20031615L (no) 2003-05-23
AU2165102A (en) 2002-04-22
US20030018197A1 (en) 2003-01-23
HUP0302722A2 (hu) 2003-12-29
US7183296B2 (en) 2007-02-27
MA26951A1 (fr) 2004-12-20
JP4015548B2 (ja) 2007-11-28
KR100534158B1 (ko) 2005-12-06
UY26956A1 (es) 2002-04-26
BR0114483A (pt) 2003-07-01
ZA200302519B (en) 2004-06-30
MXPA03003070A (es) 2003-07-14
CN1191239C (zh) 2005-03-02
CN1469865A (zh) 2004-01-21
US20040192752A1 (en) 2004-09-30
CA2423515A1 (en) 2002-04-18
WO2002030907A1 (en) 2002-04-18
NO20031615D0 (no) 2003-04-09
GB0024795D0 (en) 2000-11-22
RU2003112610A (ru) 2005-02-20
GT200100201A (es) 2002-05-23
HK1061021A1 (en) 2004-09-03
KR20030046492A (ko) 2003-06-12
JP2004511469A (ja) 2004-04-15
AU2002221651B2 (en) 2006-10-19
HRP20030251A2 (en) 2005-02-28
PE20020750A1 (es) 2002-08-21
PL362918A1 (en) 2004-11-02
AR030858A1 (es) 2003-09-03
CN1680333A (zh) 2005-10-12
EP1326843A1 (en) 2003-07-16
CZ20031297A3 (cs) 2004-01-14
US6699887B2 (en) 2004-03-02
IL154875A0 (en) 2003-10-31
NZ524740A (en) 2005-09-30

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