CN1072210C - 对神经紧张素受体有活性的1－苯基－3－吡唑甲酰胺类化合物 - Google Patents

对神经紧张素受体有活性的1－苯基－3－吡唑甲酰胺类化合物 Download PDF

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Publication number
CN1072210C
CN1072210C CN96193871A CN96193871A CN1072210C CN 1072210 C CN1072210 C CN 1072210C CN 96193871 A CN96193871 A CN 96193871A CN 96193871 A CN96193871 A CN 96193871A CN 1072210 C CN1072210 C CN 1072210C
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China
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mixture
acid
preparation
vacuo
compound
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Expired - Fee Related
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CN96193871A
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English (en)
Chinese (zh)
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CN1184469A (zh
Inventor
B·拉比尤
D·古利
F·杰杰
J·C·莫里马德
R·伯吉格拉恩
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Sanofi SA
Sanofi Aventis France
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Sanofi SA
Sanofi Synthelabo SA
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Publication of CN1184469A publication Critical patent/CN1184469A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/10—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/10—Hydrazines
    • C07C243/22—Hydrazines having nitrogen atoms of hydrazine groups bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/63—Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C255/65—Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms
    • C07C255/66—Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to nitrogen atoms having cyano groups and nitrogen atoms being part of hydrazine or hydrazone groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/45—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/45—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton
    • C07C309/47—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton having at least one of the sulfo groups bound to a carbon atom of a six-membered aromatic ring being part of a condensed ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides 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
    • C07C311/15—Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C311/21—Sulfonamides 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 a carbon atom of a six-membered aromatic ring
    • 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
    • C07D231/14—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 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN96193871A 1995-04-11 1996-04-11 对神经紧张素受体有活性的1－苯基－3－吡唑甲酰胺类化合物 Expired - Fee Related CN1072210C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR9504350A FR2732967B1 (fr) 1995-04-11 1995-04-11 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant
FR95/04350 1995-04-11

Publications (2)

Publication Number Publication Date
CN1184469A CN1184469A (zh) 1998-06-10
CN1072210C true CN1072210C (zh) 2001-10-03

Family

ID=9478010

Family Applications (1)

Application Number Title Priority Date Filing Date
CN96193871A Expired - Fee Related CN1072210C (zh) 1995-04-11 1996-04-11 对神经紧张素受体有活性的1－苯基－3－吡唑甲酰胺类化合物

Country Status (26)

Country Link
US (6) US5723483A (2)
EP (2) EP0820444A1 (2)
JP (1) JP3061644B2 (2)
KR (1) KR100366118B1 (2)
CN (1) CN1072210C (2)
AR (1) AR003940A1 (2)
AU (1) AU709119B2 (2)
CA (1) CA2220827A1 (2)
CZ (1) CZ292255B6 (2)
EE (1) EE9700264A (2)
FR (1) FR2732967B1 (2)
HU (1) HUP9801435A3 (2)
IL (1) IL117860A0 (2)
IN (1) IN185700B (2)
IS (1) IS4582A (2)
MY (1) MY114424A (2)
NO (1) NO310071B1 (2)
NZ (1) NZ307227A (2)
PL (1) PL188077B1 (2)
RU (1) RU2195455C2 (2)
SK (1) SK136797A3 (2)
TR (1) TR199701146T1 (2)
TW (1) TW411332B (2)
UA (1) UA66750C2 (2)
WO (1) WO1996032382A1 (2)
ZA (1) ZA962886B (2)

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FR2732967B1 (fr) 1995-04-11 1997-07-04 Sanofi Sa 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant
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ATE329909T1 (de) 2002-11-27 2006-07-15 Boehringer Ingelheim Pharma 1,2,3-triazolamid-derivate als cytokininhibitoren
US7078419B2 (en) 2003-03-10 2006-07-18 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
RU2337099C2 (ru) * 2003-04-03 2008-10-27 Мерк Патент Гмбх Карбонильные соединения
US20060079566A1 (en) * 2003-10-03 2006-04-13 Ching-Shih Chen PDK-1/Akt signaling inhibitors
GB0323584D0 (en) * 2003-10-08 2003-11-12 Glaxo Group Ltd Compounds
GB0323585D0 (en) * 2003-10-08 2003-11-12 Glaxo Group Ltd Compounds
EP1675585A2 (en) * 2003-10-17 2006-07-05 Tanabe Seiyaku Co., Ltd. Large conductance calcium-activated k channel opener
EP1692116B1 (en) 2003-12-03 2011-03-09 Boehringer Ingelheim Pharmaceuticals Inc. 1,2,3-triazole amide derivatives as inhibitors of cytokine production
BRPI0507786A (pt) * 2004-02-20 2007-07-17 Astrazeneca Ab composto e sais farmaceuticamente aceitáveis do mesmo, formulação farmacêutica, uso de um composto, método de tratar uma doença, e, processo para a preparação de compostos
SI1725544T1 (sl) 2004-03-09 2009-10-31 Boehringer Ingelheim Pharma 3-(4-heterociklil-1,2,3-triazol-1-il)-N-aril-benzamidi kot inhibitorji proizvodnje citokinov za zdravljenje kroničnih vnetnih bolezni
CA2560387C (en) 2004-05-03 2013-09-24 Boehringer Ingelheim Pharmaceuticals, Inc. Cytokine inhibitors
GB0410121D0 (en) * 2004-05-06 2004-06-09 Glaxo Group Ltd Compounds
US7485657B2 (en) * 2004-05-12 2009-02-03 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
US7531560B2 (en) * 2004-11-10 2009-05-12 Boehringer Ingelheim Pharmaceuticals, Inc. Anti-cytokine heterocyclic compounds
JP2008525404A (ja) * 2004-12-23 2008-07-17 アストラゼネカ アクチボラグ 治療剤
RU2304967C2 (ru) * 2005-05-26 2007-08-27 Государственное общеобразовательное учреждение высшего профессионального образования Казанский государственный медицинский университет Способ лечения язвенной болезни желудка и двенадцатиперстной кишки
GB0514738D0 (en) * 2005-07-19 2005-08-24 Astrazeneca Ab Therapeutic agents
SI1999114T1 (sl) * 2006-03-22 2015-10-30 F. Hoffmann-La Roche Ag Pirazoli kot 11-beta-hsd-1
WO2008072724A1 (ja) * 2006-12-14 2008-06-19 Taisho Pharmaceutical Co., Ltd. ピラゾール誘導体
RU2440989C2 (ru) * 2007-07-17 2012-01-27 Ф.Хоффманн-Ля Рош Аг ИНГИБИТОРЫ 11β-ГИДРОКСИСТЕРОИДНОЙ ДЕГИДРОГЕНАЗЫ
US8586043B2 (en) 2009-01-07 2013-11-19 Inserm ( Institut National De La Sante Et De La Recherche Medicale) Methods for treating breast cancer with inhibitors of neurotensin activation of NTSR1
JPWO2011007819A1 (ja) 2009-07-17 2012-12-27 塩野義製薬株式会社 ラクタムまたはベンゼンスルホンアミド化合物を含有する医薬
US20110028624A1 (en) * 2009-07-30 2011-02-03 Genovique Specialties Holdings Corporation Polymer Compositions That Include High Solvating Plasticizer And Surfactant
EP2740726A1 (en) 2012-12-07 2014-06-11 3B Pharmaceuticals GmbH Neurotensin receptor ligands
WO2015148465A1 (en) * 2014-03-25 2015-10-01 Research Triangle Institute Pyrazole compounds selective for neurotensin 2 receptor
PE20170664A1 (es) 2014-06-06 2017-06-10 Res Triangle Inst Agonistas del receptor de apelina(apj) y usos de los mismos
AU2015273934B2 (en) * 2014-06-10 2020-08-20 3B Pharmaceuticals Gmbh Conjugate comprising a neurotensin receptor ligand and use thereof
EP2954933A1 (en) 2014-06-10 2015-12-16 3B Pharmaceuticals GmbH Conjugate comprising a neurotensin receptor ligand
EP2954934A1 (en) 2014-06-11 2015-12-16 3B Pharmaceuticals GmbH Conjugate comprising a neurotensin receptor ligand and use thereof
PE20190258A1 (es) 2015-12-09 2019-02-25 Res Triangle Inst Antagonistas del receptor de la apelina (apj) mejorados y usos de los mismos
EP3279197A1 (en) 2016-08-03 2018-02-07 Friedrich-Alexander-Universität Erlangen-Nürnberg Diagnosis, treatment and prevention of neurotensin receptor-related conditions
GB201815695D0 (en) 2018-09-26 2018-11-07 Mereo Biopharma 1 Ltd Synthetic method
GB201815696D0 (en) * 2018-09-26 2018-11-07 Mereo Biopharma 1 Ltd Synthetic method
IL314786A (en) * 2022-02-18 2024-10-01 Full Life Tech Hk Limited Compounds and radioligands for targeting neurotensin receptor and uses thereof
US12091454B2 (en) 2022-12-28 2024-09-17 Development Center For Biotechnology Humanized anti-human neurotensin receptor 1 antibodies and their uses
WO2025146126A1 (en) * 2024-01-04 2025-07-10 Full-Life Technologies Hk Limited Preparation method of compounds targeting neurotensin receptor

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EP0477049A1 (fr) * 1990-08-20 1992-03-25 Sanofi Dérivés d'amido-3 pyrazole, procédé pour leur préparation et compositions pharmaceutiques les contenant

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FR2711140B1 (fr) * 1993-10-12 1996-01-05 Sanofi Sa 1-Naphtylpyrazole-3-carboxamides substitués actifs sur la neurotensine, leur préparation, les compositions pharmaceutiques en contenant.
FR2732967B1 (fr) 1995-04-11 1997-07-04 Sanofi Sa 1-phenylpyrazole-3-carboxamides substitues, actifs sur la neurotensine, leur preparation, les compositions pharmaceutiques en contenant

Patent Citations (1)

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RU2195455C2 (ru) 2002-12-27
EP1097921A1 (fr) 2001-05-09
SK136797A3 (en) 1998-07-08
JPH11504624A (ja) 1999-04-27
UA66750C2 (en) 2004-06-15
ZA962886B (en) 1996-10-15
HUP9801435A3 (en) 1998-12-28
KR100366118B1 (ko) 2003-03-15
CZ292255B6 (cs) 2003-08-13
TR199701146T1 (xx) 1998-02-21
NO974702D0 (no) 1997-10-10
PL322723A1 (en) 1998-02-16
EP0820444A1 (fr) 1998-01-28
US5965579A (en) 1999-10-12
IN185700B (2) 2001-04-07
WO1996032382A1 (fr) 1996-10-17
HUP9801435A2 (hu) 1998-10-28
AR003940A1 (es) 1998-09-30
CZ323297A3 (cs) 1998-02-18
AU709119B2 (en) 1999-08-19
US6172239B1 (en) 2001-01-09
AU5651696A (en) 1996-10-30
TW411332B (en) 2000-11-11
MY114424A (en) 2002-10-31
CA2220827A1 (en) 1996-10-17
US5925661A (en) 1999-07-20
JP3061644B2 (ja) 2000-07-10
IS4582A (is) 1997-10-09
CN1184469A (zh) 1998-06-10
US5939449A (en) 1999-08-17
FR2732967B1 (fr) 1997-07-04
NO310071B1 (no) 2001-05-14
FR2732967A1 (fr) 1996-10-18
NZ307227A (en) 2000-01-28
IL117860A0 (en) 1996-08-04
NO974702L (no) 1997-12-10
EE9700264A (et) 1998-04-15
US5936123A (en) 1999-08-10
US5723483A (en) 1998-03-03
PL188077B1 (pl) 2004-12-31

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