FI118325B - Multikatalyyttisen proteaasin inhibiittoreita - Google Patents

Multikatalyyttisen proteaasin inhibiittoreita Download PDF

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Publication number
FI118325B
FI118325B FI972029A FI972029A FI118325B FI 118325 B FI118325 B FI 118325B FI 972029 A FI972029 A FI 972029A FI 972029 A FI972029 A FI 972029A FI 118325 B FI118325 B FI 118325B
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FI
Finland
Prior art keywords
group
mmol
compound
alkyl
carbons
Prior art date
Application number
FI972029A
Other languages
English (en)
Finnish (fi)
Swedish (sv)
Other versions
FI972029A (fi
FI972029A0 (fi
Inventor
Sankar Chatterjee
James Diebold
Mohamed Iqbal
James C Kauer
Robert Siman
Original Assignee
Cephalon Inc
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
Priority claimed from US08/337,795 external-priority patent/US5550262A/en
Application filed by Cephalon Inc filed Critical Cephalon Inc
Publication of FI972029A publication Critical patent/FI972029A/fi
Publication of FI972029A0 publication Critical patent/FI972029A0/fi
Application granted granted Critical
Publication of FI118325B publication Critical patent/FI118325B/fi

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/275Nitriles; Isonitriles
    • A61K31/277Nitriles; Isonitriles having a ring, e.g. verapamil
    • 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
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • 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
    • C07C279/00Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/30Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of guanidine groups bound to nitro or nitroso groups
    • C07C279/32N-nitroguanidines
    • C07C279/36Substituted N-nitroguanidines
    • 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
    • C07C311/01Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/09Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton the carbon skeleton being further substituted by at least two halogen atoms
    • 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
    • C07C311/45Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/47Y being a hetero atom
    • 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
    • C07C311/50Compounds containing any of the groups, X being a hetero atom, Y being any atom
    • C07C311/52Y being a hetero atom
    • C07C311/64X and Y being nitrogen atoms, e.g. N-sulfonylguanidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C337/00Derivatives of thiocarbonic acids containing functional groups covered by groups C07C333/00 or C07C335/00 in which at least one nitrogen atom of these functional groups is further bound to another nitrogen atom not being part of a nitro or nitroso group
    • C07C337/06Compounds containing any of the groups, e.g. thiosemicarbazides
    • C07C337/08Compounds containing any of the groups, e.g. thiosemicarbazides the other nitrogen atom being further doubly-bound to a carbon atom, e.g. thiosemicarbazones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/70Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with two hydrocarbon radicals attached in position 2 and elements other than carbon and hydrogen in position 6
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0207Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)4-C(=0), e.g. 'isosters', replacing two amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • C07K5/06095Arg-amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Emergency Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Macromonomer-Based Addition Polymer (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)
FI972029A 1994-11-14 1997-05-13 Multikatalyyttisen proteaasin inhibiittoreita FI118325B (fi)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US33779594 1994-11-14
US08/337,795 US5550262A (en) 1994-11-14 1994-11-14 Multicatalytic protease inhibitors
US46439895A 1995-06-05 1995-06-05
US46439895 1995-06-05
US08/552,794 US5614649A (en) 1994-11-14 1995-11-03 Multicatalytic protease inhibitors
US55279495 1995-11-03
PCT/US1995/014921 WO1996014857A1 (en) 1994-11-14 1995-11-14 Multicatalytic protease inhibitors
US9514921 1995-11-14

Publications (3)

Publication Number Publication Date
FI972029A FI972029A (fi) 1997-05-13
FI972029A0 FI972029A0 (fi) 1997-05-13
FI118325B true FI118325B (fi) 2007-10-15

Family

ID=27407222

Family Applications (1)

Application Number Title Priority Date Filing Date
FI972029A FI118325B (fi) 1994-11-14 1997-05-13 Multikatalyyttisen proteaasin inhibiittoreita

Country Status (18)

Country Link
US (3) US5614649A (ja)
EP (1) EP0789578B1 (ja)
JP (2) JP3056258B2 (ja)
KR (1) KR100420774B1 (ja)
CN (1) CN1166403C (ja)
AT (1) ATE241998T1 (ja)
BR (1) BR9509665A (ja)
CA (1) CA2202760A1 (ja)
DE (1) DE69530993T2 (ja)
DK (1) DK0789578T3 (ja)
ES (1) ES2200010T3 (ja)
FI (1) FI118325B (ja)
HK (1) HK1004638A1 (ja)
MX (1) MX9703564A (ja)
NO (1) NO324066B1 (ja)
NZ (1) NZ296479A (ja)
PT (1) PT789578E (ja)
WO (1) WO1996014857A1 (ja)

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US5614649A (en) * 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors
US6214800B1 (en) 1995-10-25 2001-04-10 Senju Pharmaceutical Co., Ltd. Angiogenesis inhibitor
ES2190139T3 (es) 1995-10-25 2003-07-16 Senju Pharma Co Inhibidor de la angiogenesis.
US6043224A (en) * 1996-09-05 2000-03-28 The Massachusetts Institute Of Technology Compositions and methods for treatment of neurological disorders and neurodegenerative diseases
US6184248B1 (en) * 1996-09-05 2001-02-06 Robert K. K. Lee Compositions and methods for treatment of neurological disorders and neurodegenerative diseases
US5939581A (en) * 1997-08-20 1999-08-17 First Chemical Corporation Processes for preparing hydrocinnamic acid
US6096778A (en) * 1997-10-07 2000-08-01 Cephalon, Inc. α-ketoamide multicatalytic protease inhibitors
US6150378A (en) * 1997-10-07 2000-11-21 Cephalon, Inc. Peptidyl-containing α-ketoamide cysteine and serine protease inhibitors
US6083944A (en) * 1997-10-07 2000-07-04 Cephalon, Inc. Quinoline-containing α-ketoamide cysteine and serine protease inhibitors
GB9723407D0 (en) * 1997-11-05 1998-01-07 Ciba Geigy Ag Organic compounds
WO1999030707A1 (en) * 1997-12-16 1999-06-24 Cephalon Inc. Multicatalytic protease inhibitors for use as anti-tumor agents
EP1052994A2 (en) 1998-02-02 2000-11-22 Trustees Of Tufts College Use of dipeptidylpetidase inhibitors to regulate glucose metabolism
US6096711A (en) * 1998-02-25 2000-08-01 Sherman; Michael Hsp72 induction and applications
US6613541B1 (en) 1998-10-20 2003-09-02 Millennium Pharmaceuticals, Inc. Method for monitoring proteasome inhibitor drug action
US20030054977A1 (en) * 1999-10-12 2003-03-20 Cell Therapeutics, Inc. Manufacture of polyglutamate-therapeutic agent conjugates
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
GB0003111D0 (en) * 2000-02-10 2000-03-29 Novartis Ag Organic compounds
DK1355910T3 (da) * 2001-01-25 2011-06-27 Us Of America Represented By The Secretary Dept Of Health And Human Services Formulering af borsyreforbindelser
US6933290B2 (en) 2001-05-30 2005-08-23 Novartis Ag 2-{N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl}-amino}-alkylboronic acid derivatives
CA2468192A1 (en) 2001-11-26 2003-06-05 Trustees Of Tufts College Peptidomimetic inhibitors of post-proline cleaving enzymes
US8410053B2 (en) 2001-11-26 2013-04-02 Trustees Of Tufts College Methods for treating autoimmune disorders, and reagents related thereto
US7223745B2 (en) * 2003-08-14 2007-05-29 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
US7468383B2 (en) * 2005-02-11 2008-12-23 Cephalon, Inc. Proteasome inhibitors and methods of using the same
FR2914920B1 (fr) 2007-04-11 2011-09-09 Clariant Specialty Fine Chem F Procede de deacetalisation d'alpha-aminoacetals.
WO2008137758A2 (en) * 2007-05-04 2008-11-13 Mdrna, Inc. Amino acid lipids and uses thereof
FR2916441B1 (fr) 2007-05-22 2009-08-28 Clariant Specialty Fine Chem Procede de racemisation d'alpha-aminoacetals optiquement actifs.
US7442830B1 (en) 2007-08-06 2008-10-28 Millenium Pharmaceuticals, Inc. Proteasome inhibitors
FR2927900B1 (fr) 2008-02-27 2010-09-17 Clariant Specialty Fine Chem Procede de preparation d'alpha-aminoacetals optiquement actifs.
BR122014008754A2 (pt) 2008-06-17 2015-11-03 Millennium Pharm Inc processos para a geração de compostos de éster boronato e ditos compostos
NO2324360T3 (ja) * 2008-08-11 2018-06-30
AR075090A1 (es) 2008-09-29 2011-03-09 Millennium Pharm Inc Derivados de acido 1-amino-2-ciclobutiletilboronico inhibidores de proteosoma,utiles como agentes anticancerigenos, y composiciones farmaceuticas que los comprenden.
WO2011041582A2 (en) 2009-09-30 2011-04-07 President And Fellows Of Harvard College Methods for modulation of autophagy through the modulation of autophagy-inhibiting gene products
CA2785300A1 (en) 2009-12-22 2011-07-21 Cephalon, Inc. Proteasome inhibitors and processes for their preparation, purification and use
US8354548B2 (en) * 2010-02-19 2013-01-15 Bristol-Myers Squibb Company Glycine chroman-6-sulfonamides for use as inhibitors of diacylglycerol lipase
MX2012011298A (es) 2010-03-31 2012-11-06 Millennium Pharm Inc Derivados del acido 1-amino-2-ciclopropiletilboronico.
UA121389C2 (uk) 2014-05-20 2020-05-25 Мілленніум Фармасьютікалз, Інк. Борвмісні інгібітори протеасом для застосування після первинної протиракової терапії
US10654843B2 (en) 2014-06-20 2020-05-19 Principia Biopharma Inc. LMP7 inhibitors

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US5614649A (en) * 1994-11-14 1997-03-25 Cephalon, Inc. Multicatalytic protease inhibitors

Also Published As

Publication number Publication date
FI972029A (fi) 1997-05-13
DE69530993D1 (de) 2003-07-10
JP2000290197A (ja) 2000-10-17
AU4110496A (en) 1996-06-06
EP0789578A4 (en) 2000-09-20
NO324066B1 (no) 2007-08-06
EP0789578B1 (en) 2003-06-04
JPH10507465A (ja) 1998-07-21
CN1164192A (zh) 1997-11-05
DK0789578T3 (da) 2003-09-22
NZ296479A (en) 1999-06-29
CA2202760A1 (en) 1996-05-23
ES2200010T3 (es) 2004-03-01
US5614649A (en) 1997-03-25
KR100420774B1 (ko) 2004-07-05
AU710437B2 (en) 1999-09-23
EP0789578A1 (en) 1997-08-20
US5830870A (en) 1998-11-03
HK1004638A1 (en) 1998-11-13
US5990083A (en) 1999-11-23
DE69530993T2 (de) 2004-05-19
MX9703564A (es) 1997-08-30
NO972104L (no) 1997-06-13
NO972104D0 (no) 1997-05-07
PT789578E (pt) 2003-10-31
FI972029A0 (fi) 1997-05-13
BR9509665A (pt) 1997-10-28
CN1166403C (zh) 2004-09-15
ATE241998T1 (de) 2003-06-15
WO1996014857A1 (en) 1996-05-23
JP3056258B2 (ja) 2000-06-26

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