BG61693B1 - 1,3-оксатиоланови нуклеозидни аналози - Google Patents

1,3-оксатиоланови нуклеозидни аналози Download PDF

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Publication number
BG61693B1
BG61693B1 BG98616A BG9861694A BG61693B1 BG 61693 B1 BG61693 B1 BG 61693B1 BG 98616 A BG98616 A BG 98616A BG 9861694 A BG9861694 A BG 9861694A BG 61693 B1 BG61693 B1 BG 61693B1
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BG
Bulgaria
Prior art keywords
compound
compound according
enantiomer
ester
pharmaceutically acceptable
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BG98616A
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Bulgarian (bg)
English (en)
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BG98616A (bg
Inventor
Gervais Dionne
Original Assignee
Biochem Pharma Inc
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=10699340&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BG61693(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Biochem Pharma Inc filed Critical Biochem Pharma Inc
Publication of BG98616A publication Critical patent/BG98616A/bg
Publication of BG61693B1 publication Critical patent/BG61693B1/bg

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D411/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D411/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D411/04Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/16Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing two or more hetero rings
    • C12P17/167Heterorings having sulfur atoms as ring heteroatoms, e.g. vitamin B1, thiamine nucleus and open chain analogs
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P19/00Preparation of compounds containing saccharide radicals
    • C12P19/26Preparation of nitrogen-containing carbohydrates
    • C12P19/28N-glycosides
    • C12P19/38Nucleosides
    • C12P19/40Nucleosides having a condensed ring system containing a six-membered ring having two nitrogen atoms in the same ring, e.g. purine nucleosides
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P41/00Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
    • C12P41/001Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by metabolizing one of the enantiomers
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P41/00Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
    • C12P41/006Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by reactions involving C-N bonds, e.g. nitriles, amides, hydantoins, carbamates, lactames, transamination reactions, or keto group formation from racemic mixtures

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Analytical Chemistry (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
BG98616A 1991-08-01 1994-02-28 1,3-оксатиоланови нуклеозидни аналози BG61693B1 (bg)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB919116601A GB9116601D0 (en) 1991-08-01 1991-08-01 1,3-oxathiolane nucleoside analogues
PCT/CA1992/000321 WO1993003027A1 (fr) 1991-08-01 1992-07-24 Analogues de nucleosides de 1,3-oxathiolane

Publications (2)

Publication Number Publication Date
BG98616A BG98616A (bg) 1995-03-31
BG61693B1 true BG61693B1 (bg) 1998-03-31

Family

ID=10699340

Family Applications (1)

Application Number Title Priority Date Filing Date
BG98616A BG61693B1 (bg) 1991-08-01 1994-02-28 1,3-оксатиоланови нуклеозидни аналози

Country Status (41)

Country Link
US (2) US5538975A (fr)
EP (2) EP1155695B1 (fr)
JP (1) JP2960778B2 (fr)
KR (1) KR100242454B1 (fr)
CN (5) CN101066970A (fr)
AP (1) AP321A (fr)
AT (2) ATE227720T1 (fr)
AU (1) AU659668B2 (fr)
BG (1) BG61693B1 (fr)
CA (2) CA2682254C (fr)
CZ (1) CZ283765B6 (fr)
DE (2) DE69232845T2 (fr)
DK (2) DK0526253T3 (fr)
EE (1) EE03002B1 (fr)
EG (1) EG20193A (fr)
ES (2) ES2335968T3 (fr)
FI (1) FI940435A0 (fr)
GB (1) GB9116601D0 (fr)
GE (1) GEP20002094B (fr)
HK (2) HK1008672A1 (fr)
HN (1) HN1997000118A (fr)
HU (2) HUT70030A (fr)
IL (1) IL102616A (fr)
MA (1) MA22919A1 (fr)
MD (1) MD1434C2 (fr)
MX (1) MX9204474A (fr)
NO (3) NO300842B1 (fr)
NZ (1) NZ243637A (fr)
OA (1) OA09883A (fr)
PH (1) PH30983A (fr)
PT (2) PT526253E (fr)
RS (1) RS49993B (fr)
RU (1) RU2126405C1 (fr)
SG (1) SG68541A1 (fr)
SK (1) SK280131B6 (fr)
TJ (1) TJ244R3 (fr)
TN (1) TNSN92070A1 (fr)
TW (2) TWI232217B (fr)
WO (1) WO1993003027A1 (fr)
YU (1) YU49259B (fr)
ZA (1) ZA925668B (fr)

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US5914331A (en) * 1990-02-01 1999-06-22 Emory University Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
US6703396B1 (en) 1990-02-01 2004-03-09 Emory University Method of resolution and antiviral activity of 1,3-oxathiolane nuclesoside enantiomers
US5276151A (en) * 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
US5827727A (en) 1990-02-01 1998-10-27 Emory University Method of resolution of 1,3-oxathiolane nucleoside enantiomers
US5204466A (en) * 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5925643A (en) * 1990-12-05 1999-07-20 Emory University Enantiomerically pure β-D-dioxolane-nucleosides
US5444063A (en) * 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
US6812233B1 (en) * 1991-03-06 2004-11-02 Emory University Therapeutic nucleosides
US5817667A (en) * 1991-04-17 1998-10-06 University Of Georgia Research Foudation Compounds and methods for the treatment of cancer
GB9116601D0 (en) * 1991-08-01 1991-09-18 Iaf Biochem Int 1,3-oxathiolane nucleoside analogues
GB9226927D0 (en) * 1992-12-24 1993-02-17 Iaf Biochem Int Dideoxy nucleoside analogues
GB9311709D0 (en) * 1993-06-07 1993-07-21 Iaf Biochem Int Stereoselective synthesis of nucleoside analogues using bicycle intermediate
US20020120130A1 (en) 1993-09-10 2002-08-29 Gilles Gosselin 2' or 3' -deoxy and 2', 3' -dideoxy-beta-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti- viral agents
WO1995007086A1 (fr) * 1993-09-10 1995-03-16 Emory University Nucleosides a activite contre le virus de l'hepatite b
US5587362A (en) * 1994-01-28 1996-12-24 Univ. Of Ga Research Foundation L-nucleosides
IL113432A (en) * 1994-04-23 2000-11-21 Glaxo Group Ltd Process for the diastereoselective synthesis of nucleoside analogues
IL115156A (en) 1994-09-06 2000-07-16 Univ Georgia Pharmaceutical compositions for the treatment of cancer comprising 1-(2-hydroxymethyl-1,3-dioxolan-4-yl) cytosines
US5703058A (en) * 1995-01-27 1997-12-30 Emory University Compositions containing 5-fluoro-2',3'-didehydro-2',3'-dideoxycytidine or a mono-, di-, or triphosphate thereof and a second antiviral agent
US6391859B1 (en) 1995-01-27 2002-05-21 Emory University [5-Carboxamido or 5-fluoro]-[2′,3′-unsaturated or 3′-modified]-pyrimidine nucleosides
US5808040A (en) * 1995-01-30 1998-09-15 Yale University L-nucleosides incorporated into polymeric structure for stabilization of oligonucleotides
GB9506644D0 (en) * 1995-03-31 1995-05-24 Wellcome Found Preparation of nucleoside analogues
DE69636734T2 (de) 1995-06-07 2007-10-18 Emory University Nucleoside mit anti-hepatitis b virus wirksamkeit
US5753789A (en) * 1996-07-26 1998-05-19 Yale University Oligonucleotides containing L-nucleosides
ATE267198T1 (de) * 1997-03-19 2004-06-15 Univ Emory Synthese und anti-hiv und anti-hepatitis virus aktivität von 1,3-oxaselenolan nucleosiden
US6410546B1 (en) 1997-04-07 2002-06-25 Triangle Pharmaceuticals, Inc. Use of MKC-442 in combination with other antiviral agents
JP4249393B2 (ja) 1998-08-12 2009-04-02 トライアングル・ファーマシューティカルズ,インコーポレイテッド 1,3−オキサチオランヌクレオチドの製造方法
US6979561B1 (en) 1998-10-09 2005-12-27 Gilead Sciences, Inc. Non-homogeneous systems for the resolution of enantiomeric mixtures
CN1666742A (zh) 1998-11-02 2005-09-14 三角药物公司 对乙型肝炎病毒的联合治疗
US6436948B1 (en) 2000-03-03 2002-08-20 University Of Georgia Research Foundation Inc. Method for the treatment of psoriasis and genital warts
KR20080059679A (ko) 2000-03-29 2008-06-30 조지타운 유니버시티 델타형 간염 바이러스 감염의 치료방법
CA2308559C (fr) 2000-05-16 2005-07-26 Brantford Chemicals Inc. 1,3-oxathiolan-5-ones utiles pour la preparation d'analogues de nucleosides antiviraux
AU2008202336B2 (en) * 2001-03-01 2011-11-10 Abbvie Inc. Polymorphic and other crystalline forms of cis-FTC
CN102911166B (zh) * 2001-03-01 2016-08-17 基利得科学公司 顺-ftc的多晶型物及其它晶型
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TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
TWI375560B (en) 2005-06-13 2012-11-01 Gilead Sciences Inc Composition comprising dry granulated emtricitabine and tenofovir df and method for making the same
CN100360528C (zh) * 2005-08-31 2008-01-09 四川大学 4-氨基-1-(2-羟甲基-1,3-氧硫杂环戊烷-5-基)-2(1h)-嘧啶酮的制备方法
WO2007077505A2 (fr) * 2005-12-30 2007-07-12 Ranbaxy Laboratories Limited L-menthyl (2r, 5s)-5-(4-amino-5-fluoro-2-oxo-2h-pyrimidin-1-yl)[1,3]oxathiolan-2-carboxylate crystallin et procede d'elaboration correspondant
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
US8551973B2 (en) * 2008-12-23 2013-10-08 Gilead Pharmasset Llc Nucleoside analogs
EA019295B1 (ru) 2008-12-23 2014-02-28 Джилид Фармассет, Ллс. Соединения пуриновых нуклеозидов и способ их получения
EP2376088B1 (fr) 2008-12-23 2017-02-22 Gilead Pharmasset LLC Phosphoramidates de nucléosides de type 2-amino-purine 6-O-substituée
RU2537264C2 (ru) * 2009-04-03 2014-12-27 Медикал Рисерч Каунсил Мутанты индуцируемой активацией цитидиндеаминазы (aid) и способы их применения
EP2377862A1 (fr) 2010-03-29 2011-10-19 Esteve Química, S.A. Procédé pour l'obtention d'emtricitabine
JP2013527145A (ja) 2010-03-31 2013-06-27 ギリード・ファーマセット・エルエルシー リン含有活性化剤の立体選択的合成
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US5466806A (en) * 1989-02-08 1995-11-14 Biochem Pharma Inc. Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
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US5204466A (en) * 1990-02-01 1993-04-20 Emory University Method and compositions for the synthesis of bch-189 and related compounds
US5276151A (en) * 1990-02-01 1994-01-04 Emory University Method of synthesis of 1,3-dioxolane nucleosides
GB9009861D0 (en) * 1990-05-02 1990-06-27 Glaxo Group Ltd Chemical compounds
US5248776A (en) * 1990-12-05 1993-09-28 University Of Georgia Research Foundation, Inc. Process for enantiomerically pure β-L-1,3-oxathiolane nucleosides
US5444063A (en) * 1990-12-05 1995-08-22 Emory University Enantiomerically pure β-D-dioxolane nucleosides with selective anti-Hepatitis B virus activity
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Also Published As

Publication number Publication date
ZA925668B (en) 1993-04-28
AP321A (en) 1994-02-28
KR100242454B1 (ko) 2000-03-02
NZ243637A (en) 1995-03-28
GB9116601D0 (en) 1991-09-18
PT1155695E (pt) 2010-02-02
YU72303A (sh) 2006-05-25
OA09883A (en) 1994-09-15
FI940435A (fi) 1994-01-28
ATE227720T1 (de) 2002-11-15
ATE448787T1 (de) 2009-12-15
CN100542535C (zh) 2009-09-23
EP0526253A1 (fr) 1993-02-03
TNSN92070A1 (fr) 1993-06-08
CA2114221C (fr) 2009-12-22
DE69232845T2 (de) 2003-04-24
EP0526253B1 (fr) 2002-11-13
HU9400285D0 (en) 1994-05-30
TWI232217B (en) 2005-05-11
ES2186667T3 (es) 2003-05-16
MD1434B2 (en) 2000-03-31
CN101066970A (zh) 2007-11-07
CA2682254A1 (fr) 1993-02-18
RS49993B (sr) 2008-09-29
TJ244R3 (en) 1999-11-24
EP1155695A1 (fr) 2001-11-21
NO940322D0 (no) 1994-01-31
AU659668B2 (en) 1995-05-25
YU49259B (sh) 2004-12-31
US5618820A (en) 1997-04-08
CN1070191A (zh) 1993-03-24
IL102616A (en) 1996-10-31
CN1302612A (zh) 2001-07-11
NO2008009I1 (no) 2008-06-30
NO2005017I2 (no) 2007-10-01
DK0526253T3 (da) 2003-03-17
RU2126405C1 (ru) 1999-02-20
IL102616A0 (en) 1993-01-14
JP2960778B2 (ja) 1999-10-12
BG98616A (bg) 1995-03-31
YU74992A (sh) 1995-12-04
HUT70030A (en) 1995-09-28
NO940322L (no) 1994-03-21
SK10494A3 (en) 1994-12-07
CZ20394A3 (en) 1994-07-13
DE69233776D1 (de) 2009-12-31
ES2335968T3 (es) 2010-04-07
MD950114A (en) 1996-06-28
CZ283765B6 (cs) 1998-06-17
GEP20002094B (en) 2000-05-10
CA2114221A1 (fr) 1993-02-18
TW366347B (en) 1999-08-11
WO1993003027A1 (fr) 1993-02-18
PT526253E (pt) 2003-03-31
JPH07500317A (ja) 1995-01-12
EP1155695B1 (fr) 2009-11-18
SK280131B6 (sk) 1999-08-06
HK1038189A1 (en) 2002-03-08
DE69232845D1 (de) 2002-12-19
HU211333A9 (en) 1995-11-28
US5538975A (en) 1996-07-23
SG68541A1 (en) 1999-11-16
HK1008672A1 (en) 1999-05-14
AU2340892A (en) 1993-03-02
EE03002B1 (et) 1997-06-16
CN1132073A (zh) 1996-10-02
NO300842B1 (no) 1997-08-04
AP9200414A0 (en) 1992-07-31
CN1074924C (zh) 2001-11-21
CN1034810C (zh) 1997-05-07
CA2682254C (fr) 2012-02-21
MD1434C2 (ro) 2000-12-31
CN101074228A (zh) 2007-11-21
PH30983A (en) 1997-12-23
FI940435A0 (fi) 1994-01-28
DK1155695T3 (da) 2010-04-06
MA22919A1 (fr) 1993-04-01
HN1997000118A (es) 1999-11-12
NO2005017I1 (no) 2005-09-05
MX9204474A (es) 1993-12-01
EG20193A (en) 1997-10-30

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