ATE534622T1 - Aspartylprotease-inhibitoren - Google Patents

Aspartylprotease-inhibitoren

Info

Publication number
ATE534622T1
ATE534622T1 AT06009072T AT06009072T ATE534622T1 AT E534622 T1 ATE534622 T1 AT E534622T1 AT 06009072 T AT06009072 T AT 06009072T AT 06009072 T AT06009072 T AT 06009072T AT E534622 T1 ATE534622 T1 AT E534622T1
Authority
AT
Austria
Prior art keywords
protease inhibitors
aspartyl protease
aspartyl
inhibitors
protease
Prior art date
Application number
AT06009072T
Other languages
English (en)
Inventor
Michael Hale
Roger Tung
Stephen Price
Robin David Wilkes
Wayne Schairer
Ashley Nicholas Jarvis
Andrew Spaltenstein
Eric Steven Furfine
Vicente Samano
Istvan Kaldor
John Miller
Michael Stephen Brieger
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE534622T1 publication Critical patent/ATE534622T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed 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
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A61K31/36Compounds containing methylenedioxyphenyl groups, e.g. sesamin
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/16Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • C07C311/18Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/39Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/06Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08Systems containing only non-condensed rings with a five-membered ring the ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
AT06009072T 1999-06-11 2000-06-08 Aspartylprotease-inhibitoren ATE534622T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13907099P 1999-06-11 1999-06-11
US19021100P 2000-03-17 2000-03-17

Publications (1)

Publication Number Publication Date
ATE534622T1 true ATE534622T1 (de) 2011-12-15

Family

ID=26836833

Family Applications (2)

Application Number Title Priority Date Filing Date
AT00941279T ATE325091T1 (de) 1999-06-11 2000-06-08 Aspartyl-protease inhibitoren
AT06009072T ATE534622T1 (de) 1999-06-11 2000-06-08 Aspartylprotease-inhibitoren

Family Applications Before (1)

Application Number Title Priority Date Filing Date
AT00941279T ATE325091T1 (de) 1999-06-11 2000-06-08 Aspartyl-protease inhibitoren

Country Status (31)

Country Link
EP (2) EP1686113B1 (de)
JP (2) JP4503896B2 (de)
KR (1) KR100762188B1 (de)
CN (2) CN101245058A (de)
AR (1) AR031520A1 (de)
AT (2) ATE325091T1 (de)
AU (1) AU779994B2 (de)
BR (1) BR0011745A (de)
CA (1) CA2380858C (de)
CO (1) CO5160337A1 (de)
CY (1) CY1112632T1 (de)
CZ (1) CZ303052B6 (de)
DE (1) DE60027722T2 (de)
DK (2) DK1194404T3 (de)
ES (2) ES2263478T3 (de)
HK (1) HK1046899B (de)
HU (1) HUP0300385A3 (de)
IL (3) IL146918A0 (de)
MX (1) MXPA01012808A (de)
MY (1) MY137777A (de)
NO (1) NO323951B1 (de)
NZ (1) NZ516003A (de)
PE (1) PE20010230A1 (de)
PL (1) PL210227B1 (de)
PT (2) PT1686113E (de)
SI (1) SI1194404T1 (de)
TN (1) TNSN00129A1 (de)
TR (3) TR200202528T2 (de)
TW (3) TW593248B (de)
WO (1) WO2000076961A1 (de)
ZA (1) ZA200110177B (de)

Families Citing this family (28)

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PT1086076E (pt) 1998-06-19 2005-05-31 Vertex Pharma Inibidores de sulfonamida de aspartil protease
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion
US7659404B2 (en) 2001-02-14 2010-02-09 Tibotec Pharmaceuticals Ltd. Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors
US7285566B2 (en) * 2002-01-07 2007-10-23 Erickson John W Resistance-repellent retroviral protease inhibitors
MY142238A (en) 2002-03-12 2010-11-15 Tibotec Pharm Ltd Broadspectrum substituted benzimidazole sulfonamide hiv protease inhibitors
WO2003091264A2 (en) * 2002-04-26 2003-11-06 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors
US6632816B1 (en) * 2002-12-23 2003-10-14 Pharmacor Inc. Aromatic derivatives as HIV aspartyl protease inhibitors
WO2005000249A2 (en) * 2003-06-27 2005-01-06 Smithkline Beecham Corporation Preparation of chemical compounds
PL1658277T3 (pl) * 2003-08-18 2012-10-31 H Lundbeck As Sól bursztynianowa i malonianowa trans-4-((1R,3S)-6-chloro-3-fenyloindan-1-ylo)-1,2,2-tri-metylopiperazyny i zastosowanie jako lek
EP2335701B1 (de) * 2003-12-15 2012-07-11 Schering Corporation Heterocyclische Aspartyl-Protease Inhibitoren
JP2007528423A (ja) 2004-03-11 2007-10-11 セコイア、ファーマシューティカルズ、インコーポレイテッド 耐性防止レトロウイルスプロテアーゼ阻害薬
TWI383975B (zh) 2004-03-31 2013-02-01 悌柏泰克醫藥有限公司 製備(3R,3aS,6aR)六氫-呋喃并〔2,3-b〕呋喃-3-醇之方法
US7388008B2 (en) 2004-08-02 2008-06-17 Ambrilia Biopharma Inc. Lysine based compounds
TWI453198B (zh) 2005-02-16 2014-09-21 Lundbeck & Co As H 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s)-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法
TWI376373B (en) 2005-02-16 2012-11-11 Lundbeck & Co As H Crystalline base of a pharmaceutical compound
JP2008533017A (ja) * 2005-03-11 2008-08-21 スミスクライン ビーチャム コーポレーション Hivプロテアーゼ阻害薬
ES2452718T3 (es) 2005-11-30 2014-04-02 Taimed Biologics, Inc. Profármacos a base de lisina de inhibidores de la aspartil proteasa y procesos para su preparación
WO2008013834A1 (en) * 2006-07-24 2008-01-31 Gilead Sciences, Inc., Bisfuranyl protease inhibitors
CN102432621B (zh) 2006-11-09 2016-02-17 爱尔兰詹森科学公司 六氢呋喃并[2,3-b]呋喃-3-醇的制备方法
EP2120562A4 (de) * 2006-11-21 2010-01-13 Purdue Research Foundation Verfahren und zusammensetzungen zur behandlung von hiv-infektionen
WO2008132154A1 (en) 2007-04-27 2008-11-06 Tibotec Pharmaceuticals Ltd. Methods for the preparation of n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide derivatives
GB2452952A (en) * 2007-09-20 2009-03-25 Npil Pharmaceuticals N-[2-Hydroxy-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-sulphonamide derivatives via N-[2-oxo-3-(hydroxycarbonylamino)-3-methyl]-N-methyl-imine skeleton
US8592487B2 (en) 2007-10-26 2013-11-26 Concert Pharmaceuticals, Inc. Deuterated darunavir
AU2010299959B2 (en) 2009-09-22 2016-07-21 Tibotec Pharmaceuticals Treatment and prevention of HIV infection
WO2011061590A1 (en) 2009-11-17 2011-05-26 Hetero Research Foundation Novel carboxamide derivatives as hiv inhibitors
WO2016039403A1 (ja) * 2014-09-11 2016-03-17 塩野義製薬株式会社 持続性hivプロテアーゼ阻害剤
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors

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DE3635907A1 (de) * 1986-10-22 1988-04-28 Merck Patent Gmbh Hydroxy-aminosaeurederivate
CA2032259A1 (en) * 1989-12-18 1991-06-19 Wayne J. Thompson Hiv protease inhibitors useful for the treatment of aids
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US5475013A (en) * 1990-11-19 1995-12-12 Monsanto Company Retroviral protease inhibitors
ES2123065T3 (es) * 1992-08-25 1999-01-01 Searle & Co Hidroxietilamino-sulfonamidas utiles como inhibidores de proteasas retroviricas.
US5723490A (en) * 1992-09-08 1998-03-03 Vertex Pharmaceuticals Incorporated THF-containing sulfonamide inhibitors of aspartyl protease
IS2334B (is) * 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
EP0885880A3 (de) * 1992-10-30 1999-10-06 G.D. Searle & Co. Sulfonylalkanoylaminohydroxyethylaminosulfamidsäuren verwendbar als retrovirale Proteasehemmer
EP0715618B1 (de) * 1993-08-24 1998-12-16 G.D. Searle & Co. Hydroxyaminosulfonamide verwendbar als inhibitoren retroviraler proteasen
CA2210889C (en) * 1995-01-20 2007-08-28 G.D. Searle & Co. Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors
US5756533A (en) * 1995-03-10 1998-05-26 G.D. Searle & Co. Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5705500A (en) * 1995-03-10 1998-01-06 G.D. Searle & Co. Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
BR9607625A (pt) * 1995-03-10 1999-06-15 Searle & Co Inibidores de protease retroviral sulfonamida hidroxietilamino de aminoácido heterociclocarbonila
US6150556A (en) * 1995-03-10 2000-11-21 G. D. Dearle & Co. Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
US5691372A (en) * 1995-04-19 1997-11-25 Vertex Pharmaceuticals Incorporated Oxygenated-Heterocycle containing sulfonamide inhibitors of aspartyl protease
US5753660A (en) * 1995-11-15 1998-05-19 G. D. Searle & Co. Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
GB9712504D0 (en) * 1997-06-17 1997-08-20 Dundee Teaching Hospitals Nhs Thermal imaging method and apparatus
WO1999010374A1 (en) * 1997-08-26 1999-03-04 Wisconsin Alumni Research Foundation Cyclosporin a conjugates and uses therefor
AR031520A1 (es) * 1999-06-11 2003-09-24 Vertex Pharma Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion

Also Published As

Publication number Publication date
CA2380858C (en) 2011-12-06
HK1046899B (en) 2007-03-02
PE20010230A1 (es) 2001-03-15
PL352830A1 (pl) 2003-09-08
CZ20014431A3 (cs) 2002-06-12
TR200603871T2 (tr) 2007-01-22
AR031520A1 (es) 2003-09-24
TR200202528T2 (tr) 2003-02-21
CN1361765A (zh) 2002-07-31
TWI299000B (en) 2008-07-21
DK1194404T3 (da) 2006-09-04
TR200200407T2 (tr) 2002-08-21
CO5160337A1 (es) 2002-05-30
TNSN00129A1 (fr) 2005-11-10
CN101245058A (zh) 2008-08-20
TW200804252A (en) 2008-01-16
HUP0300385A3 (en) 2007-05-29
KR100762188B1 (ko) 2007-10-04
IL146918A (en) 2010-06-16
TW200425891A (en) 2004-12-01
ES2263478T3 (es) 2006-12-16
ES2375823T3 (es) 2012-03-06
EP1686113A1 (de) 2006-08-02
PL210227B1 (pl) 2011-12-30
AU5600600A (en) 2001-01-02
IL202633A (en) 2013-02-28
ATE325091T1 (de) 2006-06-15
TWI318116B (en) 2009-12-11
TW593248B (en) 2004-06-21
SI1194404T1 (sl) 2006-10-31
CA2380858A1 (en) 2000-12-21
NO20016034L (no) 2002-01-18
NO20016034D0 (no) 2001-12-10
PT1194404E (pt) 2006-08-31
JP4503896B2 (ja) 2010-07-14
IL146918A0 (en) 2002-08-14
IL202633A0 (en) 2010-06-30
EP1194404A1 (de) 2002-04-10
CY1112632T1 (el) 2016-02-10
PT1686113E (pt) 2012-02-20
HK1046899A1 (en) 2003-01-30
MXPA01012808A (es) 2002-07-22
EP1686113B1 (de) 2011-11-23
DK1686113T3 (da) 2012-02-20
EP1194404B1 (de) 2006-05-03
ZA200110177B (en) 2003-01-13
DE60027722T2 (de) 2007-04-26
WO2000076961A1 (en) 2000-12-21
MY137777A (en) 2009-03-31
BR0011745A (pt) 2002-03-19
JP2009046493A (ja) 2009-03-05
HUP0300385A2 (hu) 2003-07-28
JP2003502309A (ja) 2003-01-21
NO323951B1 (no) 2007-07-23
AU779994B2 (en) 2005-02-24
DE60027722D1 (en) 2006-06-08
KR20020033642A (ko) 2002-05-07
NZ516003A (en) 2004-02-27
CZ303052B6 (cs) 2012-03-14
CN100516034C (zh) 2009-07-22

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