NO318910B1 - Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat - Google Patents

Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat Download PDF

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Publication number
NO318910B1
NO318910B1 NO20013124A NO20013124A NO318910B1 NO 318910 B1 NO318910 B1 NO 318910B1 NO 20013124 A NO20013124 A NO 20013124A NO 20013124 A NO20013124 A NO 20013124A NO 318910 B1 NO318910 B1 NO 318910B1
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NO
Norway
Prior art keywords
methyl
carboxylic acid
azepan
amide
butyl
Prior art date
Application number
NO20013124A
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English (en)
Norwegian (no)
Other versions
NO20013124D0 (no
NO20013124L (no
Inventor
Daniel Frank Veber
Dennis Shinji Yamashita
Jr Robert Wells Marquis
Maxwell David Cummings
Yu Ru
Scott Kevin Thompson
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Smithkline Beecham Corp
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Publication date
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of NO20013124D0 publication Critical patent/NO20013124D0/no
Publication of NO20013124L publication Critical patent/NO20013124L/no
Publication of NO318910B1 publication Critical patent/NO318910B1/no

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    • 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P19/08Drugs 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
    • 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
    • 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
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06Antimalarials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00Antiparasitic agents
    • A61P33/10Anthelmintics
    • A61P33/12Schistosomicides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D223/12Nitrogen atoms not forming part of a nitro radical
    • 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
    • C07D401/10Heterocyclic 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 carbon chain containing aromatic rings
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    • 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
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    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D409/14Heterocyclic 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
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    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
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    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
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    • 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
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    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
NO20013124A 1998-12-23 2001-06-22 Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat NO318910B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11363698P 1998-12-23 1998-12-23
US16458199P 1999-11-10 1999-11-10
PCT/US1999/030730 WO2000038687A1 (fr) 1998-12-23 1999-12-21 Inhibiteurs de proteases

Publications (3)

Publication Number Publication Date
NO20013124D0 NO20013124D0 (no) 2001-06-22
NO20013124L NO20013124L (no) 2001-06-22
NO318910B1 true NO318910B1 (no) 2005-05-23

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Family Applications (1)

Application Number Title Priority Date Filing Date
NO20013124A NO318910B1 (no) 1998-12-23 2001-06-22 Proteaseinhibitorer, fremgangsmate for syntese og anvendelse derav samt farmasoytisk preparat

Country Status (24)

Country Link
US (2) US20020147188A1 (fr)
EP (1) EP1158986A4 (fr)
JP (1) JP2002533397A (fr)
KR (1) KR100630986B1 (fr)
CN (1) CN1253441C (fr)
AT (1) ATE411294T1 (fr)
AU (1) AU768565B2 (fr)
BR (1) BR9916488A (fr)
CA (1) CA2356671A1 (fr)
CZ (1) CZ20012277A3 (fr)
DE (1) DE69939752D1 (fr)
DZ (1) DZ2977A1 (fr)
ES (1) ES2315456T3 (fr)
GC (1) GC0000178A (fr)
HK (1) HK1043536A1 (fr)
HU (1) HUP0104768A3 (fr)
IL (2) IL143142A0 (fr)
NO (1) NO318910B1 (fr)
NZ (1) NZ511710A (fr)
PE (1) PE20001340A1 (fr)
PL (1) PL350132A1 (fr)
TR (1) TR200101869T2 (fr)
UY (1) UY25874A1 (fr)
WO (1) WO2000038687A1 (fr)

Families Citing this family (39)

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US20030144175A1 (en) 1998-12-23 2003-07-31 Smithkline Beecham Corporation Protease inhibitors
JP2003513924A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
AU1474601A (en) * 1999-11-10 2001-06-06 Smithkline Beecham Corporation Protease inhibitors
WO2001034566A2 (fr) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Inhibiteurs de la protease
EP1232155A4 (fr) * 1999-11-10 2002-11-20 Smithkline Beecham Corp Inhibiteurs de protease
JP2003513956A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
JP2003513928A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害剤
WO2001034600A1 (fr) 1999-11-10 2001-05-17 Smithkline Beecham Corporation Inhibiteurs de protease
EP1231922A4 (fr) * 1999-11-10 2004-06-23 Smithkline Beecham Corp Inhibiteurs de protease
EP1231921A4 (fr) * 1999-11-10 2004-06-23 Smithkline Beecham Corp Inhibiteurs de proteases
WO2001034154A1 (fr) * 1999-11-10 2001-05-17 Smithkline Beecham Corporation Inhibiteurs de protease
JP2003513925A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
JP2003513921A (ja) * 1999-11-10 2003-04-15 スミスクライン・ビーチャム・コーポレイション プロテア−ゼ阻害剤
SK13632002A3 (sk) * 2000-03-21 2003-02-04 Smithkline Beecham Corporation C1-6-alkyl-4-amino-azepán-3-ónové zlúčeniny, spôsob ich prípravy, farmaceutický prostriedok s ich obsahom, ich použitie a medziprodukty
CO5280088A1 (es) * 2000-04-18 2003-05-30 Smithkline Beecham Corp Inhibidores de proteasa
CO5280093A1 (es) * 2000-04-18 2003-05-30 Smithkline Beecham Corp Metodos de tratamiento
CA2412353A1 (fr) * 2000-06-14 2001-12-20 Smithkline Beecham Corporation Inhibiteurs de proteases
AU2001286983A1 (en) * 2000-09-01 2002-03-13 Smith Kline Beecham Corporation Method of treatment
PL366232A1 (en) * 2000-11-22 2005-01-24 Smithkline Beecham Corporation Protease inhibitors
US7709510B2 (en) 2001-02-20 2010-05-04 Chugai Seiyaku Kabushiki Kaisha Azoles as malonyl-CoA decarboxylase inhibitors useful as metabolic modulators
JP4155351B2 (ja) 2001-02-20 2008-09-24 中外製薬株式会社 代謝調節剤として有用なマロニル−CoA脱炭酸酵素阻害剤としてのアゾール
JP2004527575A (ja) * 2001-05-17 2004-09-09 スミスクライン・ビーチャム・コーポレイション プロテアーゼ阻害物質
US6982263B2 (en) 2001-06-08 2006-01-03 Boehringer Ingelheim Pharmaceuticals, Inc. Nitriles useful as reversible inhibitors of cysteine proteases
US20050256100A1 (en) * 2002-05-22 2005-11-17 Jeong Jae U Protease inhibitors
WO2003099844A2 (fr) * 2002-05-22 2003-12-04 Smithkline Beecham Corporation Inhibiteurs de protease
KR100962972B1 (ko) 2002-07-26 2010-06-09 주식회사유한양행 1-페닐피페리딘-3-온 유도체 및 그의 제조방법
JP2006504719A (ja) * 2002-10-08 2006-02-09 メルク フロスト カナダ アンド カンパニー 骨粗しょう症の治療において有用なカテプシンk阻害剤としての4−アミノ−アゼパン−3−オン化合物
ZA200508298B (en) 2003-04-11 2007-01-31 Ptc Therapeutics Inc 1,2,4-oxadiazole benzoic acid compounds
ATE400272T1 (de) 2003-08-01 2008-07-15 Chugai Pharmaceutical Co Ltd Piperidin-verbindungen als malonyl-coa decarboxylase-hemmer
US7696365B2 (en) 2003-08-01 2010-04-13 Chugai Seiyaku Kabushiki Kaisha Heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors
EP2208495B1 (fr) 2003-08-01 2011-12-14 Chugai Seiyaku Kabushiki Kaisha Composes azole a base de cyanoguanidine-utilises comme inhibiteurs de malonyl-coa decarboxylase
JP2007517810A (ja) * 2004-01-08 2007-07-05 メルク フロスト カナダ リミテツド カテプシンシステインプロテアーゼ阻害剤
US20070293477A1 (en) * 2004-09-07 2007-12-20 Smithkline Beecham Corporation Novel Compounds
WO2007012180A1 (fr) * 2005-07-26 2007-02-01 Merck Frosst Canada Ltd. Inhibiteurs de la cystéine protéase de la famille de la papaïne pour le traitement des maladies parasitaires
MX2008012515A (es) 2006-03-30 2008-11-19 Ptc Therapeutics Inc Metodos para la produccion de proteina funcional a partir de adn que tiene una mutacion sin sentido y el tratamiento de trastornos asociados con la misma.
US9943522B2 (en) 2011-05-16 2018-04-17 Bayer Intellectual Property Gmbh Use of cathepsin K inhibition for the treatment and/or prophylaxis of pulmonary hypertension and/or heart failure
CN103275070A (zh) * 2013-05-10 2013-09-04 郑彪 调节单核细胞增殖的四环化合物及其应用
TWI695717B (zh) 2014-03-06 2020-06-11 美商 Ptc 治療公司 1,2,4-二唑苯甲酸之鹽及醫藥組合物
JP2018531975A (ja) 2015-10-30 2018-11-01 ピーティーシー セラピューティクス,インコーポレーテッド てんかんの治療方法

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DE69321087T2 (de) * 1992-12-25 1999-05-20 Mitsubishi Chem Corp Alpha-aminoketon Derivate
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CN1350458A (zh) 2002-05-22
HUP0104768A3 (en) 2002-05-28
CA2356671A1 (fr) 2000-07-06
PE20001340A1 (es) 2001-01-28
TR200101869T2 (tr) 2002-01-21
ATE411294T1 (de) 2008-10-15
CZ20012277A3 (cs) 2001-11-14
HK1043536A1 (zh) 2002-09-20
UY25874A1 (es) 2001-08-27
GC0000178A (en) 2006-03-29
KR100630986B1 (ko) 2006-10-09
PL350132A1 (en) 2002-11-04
DE69939752D1 (de) 2008-11-27
JP2002533397A (ja) 2002-10-08
IL143142A0 (en) 2002-04-21
BR9916488A (pt) 2001-10-09
NZ511710A (en) 2003-12-19
HUP0104768A2 (hu) 2002-04-29
IL143142A (en) 2006-08-20
US20030225061A1 (en) 2003-12-04
ES2315456T3 (es) 2009-04-01
DZ2977A1 (fr) 2004-03-15
EP1158986A1 (fr) 2001-12-05
NO20013124D0 (no) 2001-06-22
AU1941100A (en) 2000-07-31
CN1253441C (zh) 2006-04-26
KR20010089677A (ko) 2001-10-08
US20020147188A1 (en) 2002-10-10
AU768565B2 (en) 2003-12-18
EP1158986A4 (fr) 2002-03-27
NO20013124L (no) 2001-06-22
WO2000038687A1 (fr) 2000-07-06

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