CN100506815C - 选择性结合整联蛋白的哌啶化合物 - Google Patents

选择性结合整联蛋白的哌啶化合物 Download PDF

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Publication number
CN100506815C
CN100506815C CNB038240904A CN03824090A CN100506815C CN 100506815 C CN100506815 C CN 100506815C CN B038240904 A CNB038240904 A CN B038240904A CN 03824090 A CN03824090 A CN 03824090A CN 100506815 C CN100506815 C CN 100506815C
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base
alkyl
compound
structural formula
tetrahydrochysene
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Expired - Fee Related
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Chinese (zh)
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CN1688572A (zh
Inventor
B·德科尔特
W·A·金尼
B·E·玛利亚诺夫
S·高希
L·刘
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Janssen Pharmaceutica NV
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    • 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
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Vascular Medicine (AREA)
  • Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Materials For Medical Uses (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CNB038240904A 2002-08-16 2003-08-15 选择性结合整联蛋白的哌啶化合物 Expired - Fee Related CN100506815C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40423902P 2002-08-16 2002-08-16
US60/404,239 2002-08-16

Publications (2)

Publication Number Publication Date
CN1688572A CN1688572A (zh) 2005-10-26
CN100506815C true CN100506815C (zh) 2009-07-01

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Country Link
US (1) US20040077684A1 (enExample)
EP (1) EP1539739B1 (enExample)
JP (1) JP4554364B2 (enExample)
KR (1) KR20050031464A (enExample)
CN (1) CN100506815C (enExample)
AR (1) AR041010A1 (enExample)
AT (1) ATE489378T1 (enExample)
AU (2) AU2003259891A1 (enExample)
BR (1) BR0313534A (enExample)
CA (1) CA2496127C (enExample)
CR (1) CR7692A (enExample)
CY (1) CY1111194T1 (enExample)
DE (1) DE60335118D1 (enExample)
DK (1) DK1539739T3 (enExample)
ES (1) ES2355139T3 (enExample)
IL (1) IL166534A (enExample)
MX (1) MXPA05001859A (enExample)
NO (1) NO332036B1 (enExample)
PL (1) PL219749B1 (enExample)
PT (1) PT1539739E (enExample)
RU (1) RU2333210C2 (enExample)
SI (1) SI1539739T1 (enExample)
UA (1) UA83467C2 (enExample)
WO (1) WO2004020435A1 (enExample)

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US20040224986A1 (en) * 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
US7351711B2 (en) 2003-07-31 2008-04-01 Janssen Pharmaceutical, N.V. Tricyclic indanyls as integrin inhibitors
HRP20130782T1 (en) 2004-04-02 2013-09-30 The Regents Of The University Of California, Office Of Technology Transfer Methods and compositions for treating and preventing disease associated with alpha v beta 5 integrin
BRPI0519739A2 (pt) * 2004-12-30 2009-03-10 Cinv Ag combinaÇço compreendendo um agente fornecendo um sinal, um material de implante e uma droga
WO2006073314A1 (en) * 2005-01-06 2006-07-13 Ge Healthcare As Optical imaging
US8372399B2 (en) * 2006-08-31 2013-02-12 Cardiac Pacemakers, Inc. Bispecific antibodies and agents to enhance stem cell homing
US20080058922A1 (en) * 2006-08-31 2008-03-06 Cardiac Pacemakers, Inc. Methods and devices employing vap-1 inhibitors
US8636995B2 (en) * 2006-08-31 2014-01-28 Cardiac Pacemakers, Inc. Methods and devices to regulate stem cell homing
CN101821256A (zh) * 2007-08-02 2010-09-01 瑞蔻达蒂爱尔兰有限公司 作为mGlu5拮抗剂的新型杂环化合物
US8680278B2 (en) * 2007-10-30 2014-03-25 Janssen Pharmaceutica Nv Enantioselective process for preparing a substituted alkanoic acid
EP2217238B1 (en) * 2007-11-08 2014-03-12 The General Hospital Corporation Methods and compositions for the treatment of proteinuric diseases
EP2456460A4 (en) 2009-07-24 2013-02-20 Univ California METHOD AND COMPOSITIONS FOR TREATING AND PREVENTING DISEASES ASSOCIATED WITH AVB5 INTEGRIN
FI3929196T3 (fi) 2013-09-24 2023-10-02 Fujifilm Corp Typpeä sisältävän yhdisteen tai sen suolan tai niiden metallikompleksin farmaseuttinen koostumus
JP2019530678A (ja) 2016-09-18 2019-10-24 エイチ リー モフィット キャンサー センター アンド リサーチ インスティテュート インコーポレイテッド Yap1のoct4との相互作用を標的とするyap1阻害剤
BR112019009245A2 (pt) * 2016-11-08 2019-07-16 Bristol-Myers Squibb Company azol amidas e aminas como inibidores de alfav integrina
JP7220653B2 (ja) * 2016-11-08 2023-02-10 ブリストル-マイヤーズ スクイブ カンパニー アルファvインテグリン阻害剤としてのピロールアミド
EP3589285A4 (en) 2017-02-28 2020-08-12 Morphic Therapeutic, Inc. INHIBITORS OF INTEGRIN (ALPHA-V) (BETA-6)
CN116283977A (zh) 2017-02-28 2023-06-23 莫菲克医疗股份有限公司 αvβ6整合蛋白的抑制剂
EA202092174A1 (ru) 2018-03-14 2021-01-15 Х. Ли Моффитт Кэнсер Сентер Энд Рисерч Инститьют, Инк. Ингибиторы yap1, которые нацелены на взаимодействие yap1 с oct4
SG11202101913PA (en) 2018-08-29 2021-03-30 Morphic Therapeutic Inc INHIBITING aV ß6 INTEGRIN
CN120282949A (zh) * 2023-09-28 2025-07-08 云合智药(苏州)生物科技有限公司 靶向整合素的化合物及其在RNAi剂中的应用

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US4289772A (en) * 1977-06-03 1981-09-15 Pfizer Inc. 1-Piperidinophthalazines as cardiac stimulants
US5340798A (en) * 1992-10-14 1994-08-23 Merck & Co., Inc. Fibrinogen receptor antagonists
US6211191B1 (en) * 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists

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US5474765A (en) * 1992-03-23 1995-12-12 Ut Sw Medical Ctr At Dallas Preparation and use of steroid-polyanionic polymer-based conjugates targeted to vascular endothelial cells
US5902795A (en) * 1992-06-16 1999-05-11 Trustees Of Tufts College Oligosaccharides reactive with hyaluronan-binding protein and their methods of use
US5753659A (en) * 1993-03-29 1998-05-19 Zeneca Limited Heterocyclic compouds
US5700801A (en) * 1994-12-23 1997-12-23 Karl Thomae, Gmbh Piperazine derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
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DE19613933A1 (de) * 1996-04-06 1997-10-09 Merck Patent Gmbh Cyclische Adhäsionsinhibitoren
US5919792A (en) * 1996-10-30 1999-07-06 Merck & Co., Inc. Integrin antagonists
DE69830806T2 (de) * 1997-12-17 2006-04-27 Merck & Co., Inc. Integrinrezeptor antagonisten
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CN1308347C (zh) * 1999-04-28 2007-04-04 德克萨斯大学董事会 用于通过选择性抑制vegf来治疗癌症的组合物和方法
US6776796B2 (en) * 2000-05-12 2004-08-17 Cordis Corportation Antiinflammatory drug and delivery device

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Publication number Priority date Publication date Assignee Title
US4289772A (en) * 1977-06-03 1981-09-15 Pfizer Inc. 1-Piperidinophthalazines as cardiac stimulants
US5340798A (en) * 1992-10-14 1994-08-23 Merck & Co., Inc. Fibrinogen receptor antagonists
US6211191B1 (en) * 1997-12-17 2001-04-03 Merck & Co., Inc. Integrin receptor antagonists

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Fused bicyclic.... Fisher,Matthew.Bioorganic & Medicinal Chemistry Letters,Vol.10 No.4. 2000
Fused bicyclic.... Fisher,Matthew.Bioorganic & Medicinal Chemistry Letters,Vol.10 No.4. 2000 *

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Publication number Publication date
CN1688572A (zh) 2005-10-26
SI1539739T1 (sl) 2011-04-29
IL166534A (en) 2012-05-31
EP1539739B1 (en) 2010-11-24
CA2496127C (en) 2012-05-29
AU2010236002B2 (en) 2012-05-03
KR20050031464A (ko) 2005-04-06
PL219749B1 (pl) 2015-07-31
IL166534A0 (en) 2006-01-15
CR7692A (es) 2009-01-14
DE60335118D1 (de) 2011-01-05
PL375562A1 (en) 2005-11-28
CY1111194T1 (el) 2015-06-11
ATE489378T1 (de) 2010-12-15
AR041010A1 (es) 2005-04-27
BR0313534A (pt) 2005-07-12
CA2496127A1 (en) 2005-02-16
JP4554364B2 (ja) 2010-09-29
RU2333210C2 (ru) 2008-09-10
UA83467C2 (uk) 2008-07-25
ES2355139T3 (es) 2011-03-23
MXPA05001859A (es) 2005-06-03
AU2010236002A1 (en) 2010-11-11
JP2005539049A (ja) 2005-12-22
EP1539739A1 (en) 2005-06-15
AU2003259891A1 (en) 2004-03-19
WO2004020435A1 (en) 2004-03-11
DK1539739T3 (da) 2011-03-07
PT1539739E (pt) 2011-01-05
NO20051273L (no) 2005-05-10
NO332036B1 (no) 2012-06-04
RU2005104115A (ru) 2005-08-27
US20040077684A1 (en) 2004-04-22

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