ATE532781T1 - 5-(acylamino)indazol-derivate als kinase- inhibitoren - Google Patents

5-(acylamino)indazol-derivate als kinase- inhibitoren

Info

Publication number
ATE532781T1
ATE532781T1 AT04755699T AT04755699T ATE532781T1 AT E532781 T1 ATE532781 T1 AT E532781T1 AT 04755699 T AT04755699 T AT 04755699T AT 04755699 T AT04755699 T AT 04755699T AT E532781 T1 ATE532781 T1 AT E532781T1
Authority
AT
Austria
Prior art keywords
acylamino
kinase inhibitors
indazole derivatives
indazolo
tetrahydropyrimidine
Prior art date
Application number
AT04755699T
Other languages
English (en)
Inventor
David Drewry
Brian Evans
Krista Goodman
Darren Victor S Green
David Jung
Denis Lee
Robert Stavenger
Sjoerd Wadman
Original Assignee
Glaxosmithkline Llc
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 Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Application granted granted Critical
Publication of ATE532781T1 publication Critical patent/ATE532781T1/de

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P35/00—Antineoplastic agents
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    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
AT04755699T 2003-06-19 2004-06-18 5-(acylamino)indazol-derivate als kinase- inhibitoren ATE532781T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US47975303P 2003-06-19 2003-06-19
PCT/US2004/019692 WO2004112719A2 (en) 2003-06-19 2004-06-18 Chemical compounds

Publications (1)

Publication Number Publication Date
ATE532781T1 true ATE532781T1 (de) 2011-11-15

Family

ID=33539215

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04755699T ATE532781T1 (de) 2003-06-19 2004-06-18 5-(acylamino)indazol-derivate als kinase- inhibitoren

Country Status (6)

Country Link
US (1) US7560467B2 (de)
EP (1) EP1633740B1 (de)
JP (1) JP4869068B2 (de)
AT (1) ATE532781T1 (de)
ES (1) ES2374272T3 (de)
WO (1) WO2004112719A2 (de)

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EP1718638A4 (de) * 2004-02-20 2009-04-22 Smithkline Beecham Corp Neue verbindungen
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
WO2006009889A1 (en) * 2004-06-17 2006-01-26 Smithkline Beecham Corporation Novel inhibitors of rho-kinases
US20100152206A1 (en) * 2005-01-07 2010-06-17 Ralph Mazitschek Bicyclic Dihydropyrimidines and Uses Thereof
US7820821B2 (en) * 2006-02-10 2010-10-26 Transtech Pharma, Inc. Benzazole derivatives, compositions, and methods of use as aurora kinase inhibitors
WO2008061109A2 (en) * 2006-11-15 2008-05-22 Forest Laboratories Holdings Limited Indazole derivatives useful as melanin concentrating receptor ligands
BRPI0806537A2 (pt) 2007-01-10 2014-04-22 Albany Molecular Res Inc Indazóis substituídos por 5-piridinona
ATE544759T1 (de) 2007-07-21 2012-02-15 Albany Molecular Res Inc 5-pyridinon-substituierte indazole und pharmazeutische zusammensetzungen davon
JP5485391B2 (ja) * 2009-07-30 2014-05-07 エフ．ホフマン−ラ ロシュ アーゲー Ｐ２ｘ７調節薬としてのジヒドロピリミドンアミド類
EA023788B1 (ru) 2010-05-07 2016-07-29 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Производные индола и фармацевтические композиции на их основе
JP5864546B2 (ja) 2010-05-07 2016-02-17 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ インダゾール
WO2012065067A2 (en) 2010-11-12 2012-05-18 Georgetown University Immortalization of epithelial cells and methods of use
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
WO2013062945A1 (en) 2011-10-24 2013-05-02 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
CA2854447A1 (en) 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No.2) Limited Method of treatment
US10189825B2 (en) 2012-02-08 2019-01-29 Sunovion Pharmaceuticals Inc. Heteroaryl compounds and methods of use thereof
AU2013331380B2 (en) 2012-10-15 2018-03-22 Epizyme, Inc. Substituted benzene compounds
WO2015041533A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut Rock in combination with mapk-pathway
CA2953524A1 (en) 2014-06-27 2015-12-30 The Regents Of The University Of California Cultured mammalian limbal stem cells, methods for generating the same, and uses thereof
WO2016023028A2 (en) * 2014-08-08 2016-02-11 The Regents Of The University Of Michigan G protein-coupled receptor kinase 2 inhibitors and methods for use of the same
US10100285B2 (en) 2015-04-03 2018-10-16 Propagenix Inc. Ex vivo proliferation of epithelial cells
AU2016243750B2 (en) 2015-04-03 2022-02-03 Propagenix Inc. Ex vivo proliferation of epithelial cells
US10329283B2 (en) 2015-06-26 2019-06-25 The Regents Of The University Of Michigan G protein-coupled receptor kinase inhibitors and methods for use of the same
EP3347450B1 (de) 2015-09-11 2021-03-17 Propagenix Inc. Ex-vivo-proliferation von epithelzellen
AU2017301769B2 (en) 2016-07-29 2022-07-28 Pgi Drug Discovery Llc Compounds and compositions and uses thereof
SG10202100751YA (en) 2016-07-29 2021-03-30 Sunovion Pharmaceuticals Inc Compounds and compositions and uses thereof
CA3070112A1 (en) * 2017-07-21 2019-01-24 Kadmon Corporation, Llc Inhibitors of rho associated coiled-coil containing protein kinase
SG11202000669VA (en) 2017-08-02 2020-02-27 Sunovion Pharmaceuticals Inc Isochroman compounds and uses thereof
CA3107502A1 (en) 2018-08-20 2020-02-27 Chengkang ZHANG Epithelial cell spheroids
US12281308B2 (en) 2018-08-29 2025-04-22 University Of Massachusetts Inhibition of protein kinases to treat Friedreich ataxia
UY38427A (es) 2018-10-26 2020-05-29 Novartis Ag Métodos y composiciones para terapia con células oculares
JP7703449B2 (ja) 2019-03-14 2025-07-07 スミトモ・ファーマ・アメリカ・インコーポレイテッド イソクロマニル化合物の塩およびその結晶体、ならびにそれらの製造方法、治療用途および医薬組成物
US20230172929A1 (en) * 2019-08-08 2023-06-08 Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. Novel peripheral cannabinoid-1 receptor antagonists
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ATE314362T1 (de) * 1999-10-12 2006-01-15 Takeda Pharmaceutical Pyrimidin-5-carboximidverbindungen, verfahren zur herstellung derselben und deren verwendung
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
WO2002066443A2 (en) * 2001-02-21 2002-08-29 Ono Pharmaceutical Co., Ltd. 2-thioxo-1,2,3,4-tetrahydropyrimidine derivatives
AU2002255263B2 (en) 2001-04-16 2006-12-14 Eisai R&D Management Co., Ltd. Novel 1H-indazole compound
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WO2006009889A1 (en) * 2004-06-17 2006-01-26 Smithkline Beecham Corporation Novel inhibitors of rho-kinases

Also Published As

Publication number Publication date
EP1633740B1 (de) 2011-11-09
ES2374272T3 (es) 2012-02-15
EP1633740A4 (de) 2008-11-19
US20070099944A1 (en) 2007-05-03
WO2004112719A3 (en) 2005-04-07
JP4869068B2 (ja) 2012-02-01
WO2004112719A8 (en) 2005-05-26
EP1633740A2 (de) 2006-03-15
JP2007516173A (ja) 2007-06-21
US7560467B2 (en) 2009-07-14
WO2004112719A2 (en) 2004-12-29

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