CN1064685C - 四氢呋喃抗真菌剂 - Google Patents

四氢呋喃抗真菌剂 Download PDF

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Publication number
CN1064685C
CN1064685C CN94195025A CN94195025A CN1064685C CN 1064685 C CN1064685 C CN 1064685C CN 94195025 A CN94195025 A CN 94195025A CN 94195025 A CN94195025 A CN 94195025A CN 1064685 C CN1064685 C CN 1064685C
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CN
China
Prior art keywords
compound
formula
ester
ether
pharmaceutically acceptable
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
CN94195025A
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English (en)
Chinese (zh)
Other versions
CN1142828A (zh
Inventor
A·K·莎森纳
V·M·吉力扎瓦拉汉
R·G·罗韦
R·E·派克
H·Y·王
Y·T·刘
A·K·甘古利
F·本内特
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Merck Sharp & Dohme LLC
Original Assignee
Schering Corp
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22622452&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN1064685(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of CN1142828A publication Critical patent/CN1142828A/zh
Application granted granted Critical
Publication of CN1064685C publication Critical patent/CN1064685C/zh
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Dental Preparations (AREA)
  • Lubricants (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Thermal Transfer Or Thermal Recording In General (AREA)
CN94195025A 1993-12-21 1994-12-20 四氢呋喃抗真菌剂 Expired - Lifetime CN1064685C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US17108393A 1993-12-21 1993-12-21
US08/171,083 1993-12-21

Publications (2)

Publication Number Publication Date
CN1142828A CN1142828A (zh) 1997-02-12
CN1064685C true CN1064685C (zh) 2001-04-18

Family

ID=22622452

Family Applications (1)

Application Number Title Priority Date Filing Date
CN94195025A Expired - Lifetime CN1064685C (zh) 1993-12-21 1994-12-20 四氢呋喃抗真菌剂

Country Status (28)

Country Link
EP (1) EP0736030B1 (enExample)
JP (1) JP2834889B2 (enExample)
KR (1) KR0179990B1 (enExample)
CN (1) CN1064685C (enExample)
AT (1) ATE204875T1 (enExample)
AU (1) AU681753B2 (enExample)
BR (1) BR1100154B1 (enExample)
CA (1) CA2179396C (enExample)
CO (1) CO4520281A1 (enExample)
CZ (1) CZ294823B6 (enExample)
DE (2) DE69428125T2 (enExample)
DK (1) DK0736030T3 (enExample)
ES (1) ES2159623T3 (enExample)
FI (1) FI118470B (enExample)
FR (1) FR06C0009I2 (enExample)
HU (1) HU225062B1 (enExample)
IL (1) IL112081A (enExample)
LU (1) LU91216I2 (enExample)
MY (1) MY130217A (enExample)
NL (1) NL300219I2 (enExample)
NO (2) NO316173B1 (enExample)
NZ (1) NZ278713A (enExample)
PL (1) PL181193B1 (enExample)
PT (1) PT736030E (enExample)
SK (1) SK283035B6 (enExample)
TW (1) TW377349B (enExample)
WO (1) WO1995017407A1 (enExample)
ZA (1) ZA9410142B (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104370894A (zh) * 2014-10-21 2015-02-25 江苏恒盛药业有限公司 无定型泊沙康唑的制备工艺
CN106432338A (zh) * 2015-08-08 2017-02-22 陕西合成药业股份有限公司 泊沙康唑衍生物、合成和在长效制剂中的用途
CN106883221A (zh) * 2017-04-17 2017-06-23 兰州大学 一种无定形泊沙康唑及其制备方法

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SG48386A1 (en) * 1994-01-24 1998-04-17 Janssen Pharmaceutica Nv Watersoluble azole antifungals
ES2199291T3 (es) * 1995-06-02 2004-02-16 Schering Corporation Antifungicos de tetrahidrofurano.
US5698557A (en) * 1995-06-19 1997-12-16 Schering Corporation Hydroxy-substituted antifungals
MX9710270A (es) * 1995-06-19 1998-08-30 Schering Corp Fungicidas de tetrahidrofurano.
DE69616596D1 (de) * 1995-12-20 2001-12-06 Schering Corp Verfahren zur herstellung von hydraziden
US5834472A (en) * 1996-05-24 1998-11-10 Schering Corporation Antifungal composition with enhanced bioavailability
ID16956A (id) * 1996-05-24 1997-11-27 Schering Corp Komposisi antijamur dengan ketersediaan hayati yang tertingkatkan
CA2258683C (en) * 1996-06-28 2007-07-31 Schering Corporation Oral composition comprising a triazole antifungal compound
US5972381A (en) * 1996-06-28 1999-10-26 Schering Corporation Solid solution of an antifungal agent with enhanced bioavailability
US5846971A (en) * 1996-06-28 1998-12-08 Schering Corporation Oral antifungal composition
DE69730241T2 (de) * 1996-06-28 2005-08-11 Schering Corp. Feste lösung eines fungizids mit erhöhter bioverfügbarkeit
AU5251398A (en) * 1996-11-12 1998-06-03 Sepracor, Inc. (2r,4s,r,r-) and (2s,4r,r,r-)hydroxyitraconazole
EP0942907A1 (en) * 1996-11-12 1999-09-22 Sepracor, Inc. 2r, 4s, s, r- and 2s, 4r, s, r-hydroxyitraconazole
CA2269617A1 (en) * 1996-11-12 1998-05-22 Chris H. Senanayake 2r,4s,r,s- and 2s,4r,r,s-hydroxyitraconazole- and hydroxysaperconazole derivatives
JP2001504465A (ja) * 1996-11-12 2001-04-03 セプラコール，インク． ２ｒ，４ｓ，ｓ，ｓ―および２ｓ，４ｒ，ｓ，ｓ―ヒドロキシイトラコナゾール
US5684197A (en) * 1996-12-12 1997-11-04 Schering Corporation Process for preparation of hydrazides
CN1238353C (zh) * 1997-02-11 2006-01-25 詹森药业有限公司 含氨基酸酯之唑类抗真菌剂
US6043245A (en) * 1997-09-25 2000-03-28 Schering Corporation Tetrahydrofuran antifungal phosphate
SK3912000A3 (en) * 1997-09-25 2000-08-14 Schering Corp Tetrahydrofuran phosphate- and hydroxy esters, as prodrugs for the corresponding antifungal agent
WO1999018111A1 (en) * 1997-10-07 1999-04-15 Schering Corporation Crystalline antifungal glycine ester polymorph
JP2001519346A (ja) * 1997-10-07 2001-10-23 シェーリング コーポレイション 抗真菌性結晶性多形物
US6713481B1 (en) * 1997-10-17 2004-03-30 David R. Andrews Crystalline antifungal polymorph
US5883097A (en) * 1998-04-16 1999-03-16 Schering Corporation Soluble azole antifungal salt
EP0957101A1 (en) * 1998-05-14 1999-11-17 Janssen Pharmaceutica N.V. Water soluble azoles as broad-spectrum antifungals
US6147077A (en) * 1999-04-29 2000-11-14 Sepracor Inc. 2R,4S-hydroxyitraconazole isomers
BR0010279A (pt) * 1999-05-04 2002-05-14 Janssen Phamaceutica N V éteres antifúngicos
US6362172B2 (en) 2000-01-20 2002-03-26 Bristol-Myers Squibb Company Water soluble prodrugs of azole compounds
US6448401B1 (en) 2000-11-20 2002-09-10 Bristol-Myers Squibb Company Process for water soluble azole compounds
PL212985B1 (pl) * 2001-04-03 2012-12-31 Schering Corp Ciekla zawiesina zawierajaca przeciwgrzybiczo skuteczna ilosc posakonazolu oraz zastosowanie zmikronizowanych czastek posakonazolu
US7790905B2 (en) 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7446107B2 (en) 2002-02-15 2008-11-04 Transform Pharmaceuticals, Inc. Crystalline forms of conazoles and methods of making and using the same
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
EP2316468A1 (en) 2002-02-22 2011-05-04 Shire LLC Delivery system and methods for protecting and administering dextroamphetamine
IL163846A0 (en) 2002-03-01 2005-12-18 Univ South Florida Multiple-component solid phases containing at least one active pharmaceutical ingredient
EP1511490A4 (en) 2002-05-31 2009-03-11 Transform Pharmaceuticals Inc NOVEL CONAZOLE CRYSTALLINE FORMS AND RELATED METHODS, PHARMACEUTICAL COMPOSITIONS AND METHODS
IL165383A0 (en) 2002-06-21 2006-01-15 Transform Pharmaceuticals Inc Pharmaceutical compositions with improved dissolution
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
ITMI20032020A1 (it) 2003-10-17 2005-04-18 Italfarmaco Spa Nuovi agenti antifungini azolici con diminuita interazione con i citocromi metabolici
CA2576589C (en) * 2004-08-13 2013-11-12 Schering-Plough Ltd. Pharmaceutical formulation comprising an antibiotic, a triazole and a corticosteroid
JO2691B1 (en) * 2005-05-03 2013-03-03 ايساي آر آند دي مانجمنت كو.، ليمتد Monolysine salts for azole compounds
EP2130540A1 (en) * 2008-06-02 2009-12-09 Sandoz AG Pharmaceutical compositions containing a crystalline form of posaconazole
EP2141159A1 (en) * 2008-07-03 2010-01-06 Sandoz AG A Crystalline form of posaconazole
CA2767489A1 (en) 2009-07-09 2011-01-13 Sandoz Ag A crystalline form of posaconazole
WO2011158248A2 (en) * 2010-05-12 2011-12-22 Glenmark Generics Limited Process for preparation of posaconazole and crystalline polymorphic form v of posaconazole
CN102892763B (zh) * 2010-05-19 2016-03-09 桑多斯股份公司 泊沙康唑及泊沙康唑中间体的纯化
EP2571847B1 (en) * 2010-05-19 2016-09-21 Sandoz AG Process for the preparation of chiral hydrazides
AU2011254654B2 (en) * 2010-05-19 2016-01-07 Sandoz Ag Process for the preparation of chiral triazolones
US9073904B2 (en) 2010-05-19 2015-07-07 Sandoz Ag Preparation of posaconazole intermediates
PL3391890T3 (pl) 2010-06-29 2021-12-20 Merck Sharp & Dohme Corp. Preparaty dożylnego roztworu pozakonazolu stabilizowane podstawioną beta-cyklodekstryną
CN103635465A (zh) * 2011-06-16 2014-03-12 桑多斯股份公司 制备手性化合物的方法
EP2789610A1 (en) 2013-04-10 2014-10-15 Sandoz Ag Purification of Posaconazole Intermediates
WO2015011224A1 (en) * 2013-07-25 2015-01-29 Sandoz Ag Improved process for the preparation of crystalline form iv of posaconazole
ITMI20132114A1 (it) 2013-12-18 2015-06-19 Djada Pharmaceutical Sa Una forma cristallina di posaconazolo
CN105287403A (zh) * 2014-08-02 2016-02-03 陕西合成药业股份有限公司 一种泊沙康唑前体药物的冻干组合物及其制备方法和用途
WO2016087880A1 (en) 2014-12-05 2016-06-09 Pulmocide Limited Antimycotic compound
ES2790723T3 (es) * 2015-05-21 2020-10-29 Pulmocide Ltd Antifúngico 4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-il)metil)-5-(2,4-difluorofenil)tetrahidrofurano-3-il)metoxi)-3-metilfenil)piperazina-1-il)-N -(2-hidroxiciclohexil)benzamida, o una sal farmacéuticamente aceptable del mismo
CN106317032A (zh) * 2015-06-15 2017-01-11 重庆圣华曦药业股份有限公司 一种制备高纯度的泊沙康唑的方法
AU2016325733B2 (en) * 2015-09-23 2020-04-09 Biocon Limited Crystalline forms of posaconazole intermediate and process for the preparation of amorphous posaconazole
CN105606736A (zh) * 2016-01-27 2016-05-25 重庆华邦制药有限公司 分离测定泊沙康唑中间体z1及其有关物质的方法
SI3424911T1 (sl) * 2016-03-04 2021-11-30 Zhejiang Ausun Pharmaceutical Co., Ltd., Posakonazol, sestavek, intermediat, postopek priprave le-tega in uporabe le-tega
CN105949278B (zh) * 2016-03-30 2019-12-06 南京曼杰生物科技有限公司 一种取代的四氢呋喃水溶性衍生物及其应用
WO2017032908A1 (en) 2016-07-08 2017-03-02 Synthon B.V. Pharmaceutical composition comprising amorphous posaconazole
US11185548B2 (en) 2016-12-23 2021-11-30 Helmholtz Zentrum Munchen—Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) Inhibitors of cytochrome P450 family 7 subfamily B member 1 (CYP7B1) for use in treating diseases
TR201620462A2 (tr) 2016-12-31 2018-07-23 Abdi Ibrahim Ilac Sanayi Ve Ticaret Anonim Sirketi POSAKONAZOL İÇEREN FARMASÖTİK BİLEŞİMLER ve ÜRETİM YÖNTEMİ
CN106967054A (zh) * 2017-03-30 2017-07-21 成都绿林科技有限公司 一种泊沙康唑的制备方法
CN108341754A (zh) * 2018-03-12 2018-07-31 扬子江药业集团有限公司 泊沙康唑杂质及其制备方法和用途
CN110938093B (zh) * 2018-09-21 2022-08-19 华创合成制药股份有限公司 一种泊沙康唑磷酸酯单胆碱盐及其制备方法和用途
CN112778369B (zh) * 2019-11-05 2024-01-26 华创合成制药股份有限公司 一种三唑类衍生物及其制备方法和用途
GB201917867D0 (en) 2019-12-06 2020-01-22 Pulmocide Ltd Polymorphs
CN113666915B (zh) * 2021-08-27 2022-08-16 江苏海洋大学 一种泊沙康唑中间体的制备方法
CN114315811B (zh) * 2021-11-19 2024-04-30 江苏恒盛药业有限公司 一种三氮唑类似物化合物及其制备方法和应用
CN120794964A (zh) * 2025-07-03 2025-10-17 广州绿十字制药股份有限公司 泊沙康唑脂肪酸酯、泊沙康唑脂肪酸酯脂肪乳及其制备方法

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104370894A (zh) * 2014-10-21 2015-02-25 江苏恒盛药业有限公司 无定型泊沙康唑的制备工艺
CN106432338A (zh) * 2015-08-08 2017-02-22 陕西合成药业股份有限公司 泊沙康唑衍生物、合成和在长效制剂中的用途
CN106883221A (zh) * 2017-04-17 2017-06-23 兰州大学 一种无定形泊沙康唑及其制备方法

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PL181193B1 (pl) 2001-06-29
PL315169A1 (en) 1996-10-14
NZ278713A (en) 1997-12-19
ES2159623T3 (es) 2001-10-16
HU9601709D0 (en) 1996-08-28
FR06C0009I1 (enExample) 2006-05-19
WO1995017407A1 (en) 1995-06-29
FI962577A0 (fi) 1996-06-20
NO2006002I2 (no) 2011-03-07
EP0736030A1 (en) 1996-10-09
CZ294823B6 (cs) 2005-03-16
DE122006000004I2 (de) 2007-03-29
MY130217A (en) 2007-06-29
IL112081A0 (en) 1995-03-15
NO2006002I1 (no) 2006-02-20
HUT75879A (en) 1997-05-28
HK1008820A1 (en) 1999-05-21
NO316173B1 (no) 2003-12-22
CA2179396A1 (en) 1995-06-29
NO962616D0 (no) 1996-06-20
NL300219I1 (nl) 2006-04-03
HU225062B1 (en) 2006-05-29
TW377349B (en) 1999-12-21
DK0736030T3 (da) 2001-10-29
SK283035B6 (sk) 2003-02-04
NL300219I2 (nl) 2006-05-01
FR06C0009I2 (enExample) 2006-12-29
PT736030E (pt) 2002-01-30
SK82696A3 (en) 1997-03-05
CN1142828A (zh) 1997-02-12
NO962616L (no) 1996-08-07
CZ180596A3 (en) 1997-01-15
CA2179396C (en) 2001-04-17
ATE204875T1 (de) 2001-09-15
FI118470B (fi) 2007-11-30
KR0179990B1 (en) 1999-03-20
CO4520281A1 (es) 1997-10-15
FI962577L (fi) 1996-06-20
ZA9410142B (en) 1996-05-02
JPH09500658A (ja) 1997-01-21
DE69428125T2 (de) 2002-05-02
AU681753B2 (en) 1997-09-04
JP2834889B2 (ja) 1998-12-14
EP0736030B1 (en) 2001-08-29
AU1512795A (en) 1995-07-10
DE69428125D1 (de) 2001-10-04
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