DE69840586D1 - Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien - Google Patents
Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende AgenzienInfo
- Publication number
- DE69840586D1 DE69840586D1 DE69840586T DE69840586T DE69840586D1 DE 69840586 D1 DE69840586 D1 DE 69840586D1 DE 69840586 T DE69840586 T DE 69840586T DE 69840586 T DE69840586 T DE 69840586T DE 69840586 D1 DE69840586 D1 DE 69840586D1
- Authority
- DE
- Germany
- Prior art keywords
- cyclosporine
- substitution
- disclosed
- derivatives
- cyclosporine derivatives
- 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 - Fee Related
Links
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical class CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 title abstract 9
- 239000002955 immunomodulating agent Substances 0.000 title 1
- 238000006467 substitution reaction Methods 0.000 abstract 4
- 229930105110 Cyclosporin A Natural products 0.000 abstract 3
- 108010036949 Cyclosporine Proteins 0.000 abstract 3
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 abstract 2
- 229910052805 deuterium Inorganic materials 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 230000001988 toxicity Effects 0.000 abstract 2
- 231100000419 toxicity Toxicity 0.000 abstract 2
- 108010036941 Cyclosporins Proteins 0.000 abstract 1
- 206010062016 Immunosuppression Diseases 0.000 abstract 1
- 125000003275 alpha amino acid group Chemical class 0.000 abstract 1
- 150000001413 amino acids Chemical class 0.000 abstract 1
- 229930182912 cyclosporin Natural products 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 230000000155 isotopic effect Effects 0.000 abstract 1
- 230000004060 metabolic process Effects 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/008—Peptides; Proteins
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
- C07K1/13—Labelling of peptides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
- C07K7/645—Cyclosporins; Related peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
- Y10S530/806—Antigenic peptides or proteins
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
- Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
- Y10S530/807—Hapten conjugated with peptide or protein
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Analytical Chemistry (AREA)
- Neurology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Surgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6136097P | 1997-10-08 | 1997-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DE69840586D1 true DE69840586D1 (de) | 2009-04-02 |
Family
ID=22035297
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69840586T Expired - Fee Related DE69840586D1 (de) | 1997-10-08 | 1998-10-08 | Deuterierte Cyclosporin-analoga und ihre Verwendung als immunmodulierende Agenzien |
| DE69832984T Expired - Lifetime DE69832984T2 (de) | 1997-10-08 | 1998-10-08 | DEUTERIERtE und undeuterierte CYCLOSPORIN-ANALOGA UND IHRE VERWENDUNG ALS IMMUNMODULIERENDE AGENtIEN |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69832984T Expired - Lifetime DE69832984T2 (de) | 1997-10-08 | 1998-10-08 | DEUTERIERtE und undeuterierte CYCLOSPORIN-ANALOGA UND IHRE VERWENDUNG ALS IMMUNMODULIERENDE AGENtIEN |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US6613739B1 (de) |
| EP (1) | EP0991660B8 (de) |
| JP (6) | JP4261049B2 (de) |
| KR (1) | KR100585348B1 (de) |
| AT (2) | ATE423130T1 (de) |
| AU (1) | AU750245B2 (de) |
| BR (1) | BR9811716A (de) |
| CA (1) | CA2298572C (de) |
| DE (2) | DE69840586D1 (de) |
| DK (1) | DK0991660T3 (de) |
| ES (1) | ES2256959T3 (de) |
| NO (1) | NO324042B1 (de) |
| NZ (1) | NZ502362A (de) |
| WO (1) | WO1999018120A1 (de) |
Families Citing this family (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030220234A1 (en) * | 1998-11-02 | 2003-11-27 | Selvaraj Naicker | Deuterated cyclosporine analogs and their use as immunodulating agents |
| US20050113460A1 (en) * | 1999-04-30 | 2005-05-26 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| US20060025388A1 (en) | 1999-04-30 | 2006-02-02 | Glick Gary D | Compositions and methods relating to novel compounds and targets thereof |
| US20030119029A1 (en) * | 1999-04-30 | 2003-06-26 | Regents Of The University Of Michigan | Compositions and methods relating to novel benzodiazepine compounds and targets thereof |
| US7144880B2 (en) | 1999-04-30 | 2006-12-05 | Regents Of The University Of Michigan | Compositions relating to novel compounds and targets thereof |
| US20040176358A1 (en) * | 1999-04-30 | 2004-09-09 | The Regents Of The University Of Michigan | Compositions and methods relating to novel compounds and targets thereof |
| IL146222A0 (en) * | 1999-04-30 | 2002-07-25 | Univ Michigan | Therapeutic applications of pro-apoptotic benzodiazepines |
| US6784156B2 (en) * | 2001-03-05 | 2004-08-31 | Enanta Pharmaceuticals, Inc. | Cyclosporins for the treatment of respiratory diseases |
| US6809077B2 (en) | 2001-10-12 | 2004-10-26 | Enanta Pharmaceuticals, Inc. | Cyclosporin analogs for the treatment of autoimmune diseases |
| US20030087813A1 (en) | 2001-10-12 | 2003-05-08 | Or Yat Sun | Cyclosporin analogs for the treatment of lung diseases |
| DE60231570D1 (de) * | 2001-10-19 | 2009-04-23 | Isotechnika Inc | Synthese von Cyclosporinanalogen |
| PT1435910E (pt) * | 2001-10-19 | 2009-09-07 | Isotechnika Inc | Novos pré-concentrados de microemulsão de análogos da ciclosporina |
| DK1436322T3 (da) * | 2001-10-19 | 2008-11-03 | Isotechnika Inc | Blandinger af cyclosporinanaloger og deres anvendelse som immunmodulerende midler |
| US20040110666A1 (en) * | 2002-12-04 | 2004-06-10 | Or Yat Sun | Cyclosporins for the treatment of immune disorders |
| DE10261807A1 (de) * | 2002-12-19 | 2004-07-01 | Turicum Drug Development Ag | Deuterierte Catecholaminderivate sowie diese Verbindungen enthaltende Arzneimittel |
| US7012065B2 (en) | 2003-02-07 | 2006-03-14 | Enanta Pharmaceuticals, Inc. | Cyclosporins for the treatment of immune disorders |
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| US20040266669A1 (en) * | 2003-06-20 | 2004-12-30 | Wu Frank X. H. | Cyclosporin derivatives for the treatment of immune disorders |
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| US20050272723A1 (en) * | 2004-04-27 | 2005-12-08 | The Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| US20090275099A1 (en) * | 2004-04-27 | 2009-11-05 | Regents Of The University Of Michigan | Methods and compositions for treating diseases and conditions associated with mitochondrial function |
| EP1768692B8 (de) * | 2004-07-01 | 2015-06-17 | Yale University | Mit wirkstoff beladene polymermaterialien von hoher dichte und mit zielausrichtung |
| US20060014677A1 (en) * | 2004-07-19 | 2006-01-19 | Isotechnika International Inc. | Method for maximizing efficacy and predicting and minimizing toxicity of calcineurin inhibitor compounds |
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| BRPI0517207A (pt) * | 2004-12-17 | 2008-09-30 | Isotechnika Inc | composto isolado, metabólito isolado de ciclo {{(e)- e (z)- (2s,3r,4r)-3-hidróxi-4-metil-2-(metilamino)-6,8-nonadien oil}-l-2-aminobutiril-n-metil-glicil-n-metil-l-leucil-l-v alil-n-metil-l-leucil-l-alanil-d-alanil-n-metil-l-leucil- n-metil-l-leucil-n-metil-l-valil} (isa247) e os sais e solvatos farmaceuticamente aceitáveis dos mesmos, método de preparação de metabólitos de isa247 in vitro, método de produção de um metabólito hidroxilado de isa247, metabólito hidroxilado isolado de isa247, metabólito hidroxilado isolado, método de produção de um metabólito de epóxido de isa247 in vitro, metabólito isolado de epóxido de isa247, metabólito isolado de epóxido, método de produção de um metabólito de diol de isa247 in vitro, metabólito de diol isolado de isa247, metabólito de diol isolado, método de produção de um metabólito de diol de isa247, método de produção de um metabólito de diol de isa247 e composição farmacêutica |
| US7638624B2 (en) * | 2005-01-03 | 2009-12-29 | The Regents Of The University Of Michigan | Compositions and methods relating to novel benzodiazepine compounds and derivatives |
| JP4862038B2 (ja) * | 2005-04-06 | 2012-01-25 | アボット・ラボラトリーズ | 血液検体中の免疫抑制性タクロリムス、シロリムスおよびシクロスポリンa複合体の測定方法 |
| EP1893218A4 (de) | 2005-06-01 | 2011-01-12 | Univ Michigan | Ungelöste benzodiazepin-zusammensetzungen und verfahren |
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1998
- 1998-10-08 DE DE69840586T patent/DE69840586D1/de not_active Expired - Fee Related
- 1998-10-08 WO PCT/IB1998/001693 patent/WO1999018120A1/en not_active Ceased
- 1998-10-08 KR KR1020007003743A patent/KR100585348B1/ko not_active Expired - Fee Related
- 1998-10-08 NZ NZ502362A patent/NZ502362A/en not_active IP Right Cessation
- 1998-10-08 DK DK98947718T patent/DK0991660T3/da active
- 1998-10-08 EP EP98947718A patent/EP0991660B8/de not_active Expired - Lifetime
- 1998-10-08 AT AT05024216T patent/ATE423130T1/de not_active IP Right Cessation
- 1998-10-08 BR BR9811716-5A patent/BR9811716A/pt not_active Application Discontinuation
- 1998-10-08 AT AT98947718T patent/ATE314388T1/de active
- 1998-10-08 ES ES98947718T patent/ES2256959T3/es not_active Expired - Lifetime
- 1998-10-08 CA CA002298572A patent/CA2298572C/en not_active Expired - Lifetime
- 1998-10-08 DE DE69832984T patent/DE69832984T2/de not_active Expired - Lifetime
- 1998-10-08 AU AU94542/98A patent/AU750245B2/en not_active Expired
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- 2000-02-29 NO NO20001020A patent/NO324042B1/no not_active IP Right Cessation
- 2000-08-07 US US09/634,945 patent/US6613739B1/en not_active Expired - Lifetime
- 2000-08-14 US US09/639,708 patent/US6605593B1/en not_active Expired - Lifetime
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2001
- 2001-11-07 US US09/985,997 patent/US20020132763A1/en not_active Abandoned
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- 2003-10-17 JP JP2003358524A patent/JP2004143168A/ja not_active Withdrawn
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- 2005-08-11 JP JP2005233674A patent/JP2005343904A/ja not_active Withdrawn
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- 2007-01-26 JP JP2007017196A patent/JP2007119489A/ja not_active Withdrawn
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- 2008-05-27 JP JP2008138789A patent/JP2008222724A/ja not_active Withdrawn
- 2008-05-27 JP JP2008138790A patent/JP2008222725A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| WO1999018120A1 (en) | 1999-04-15 |
| KR100585348B1 (ko) | 2006-06-01 |
| JP2008222724A (ja) | 2008-09-25 |
| JP2008222725A (ja) | 2008-09-25 |
| KR20010030978A (ko) | 2001-04-16 |
| JP2007119489A (ja) | 2007-05-17 |
| DK0991660T3 (da) | 2006-02-13 |
| ATE314388T1 (de) | 2006-01-15 |
| NO324042B1 (no) | 2007-07-30 |
| US6605593B1 (en) | 2003-08-12 |
| US6613739B1 (en) | 2003-09-02 |
| BR9811716A (pt) | 2000-07-18 |
| NO20001020L (no) | 2000-02-29 |
| EP0991660B1 (de) | 2005-12-28 |
| JP4261049B2 (ja) | 2009-04-30 |
| CA2298572A1 (en) | 1999-04-15 |
| DE69832984D1 (de) | 2006-02-02 |
| ATE423130T1 (de) | 2009-03-15 |
| NZ502362A (en) | 2001-05-25 |
| NO20001020D0 (no) | 2000-02-29 |
| HK1026432A1 (en) | 2000-12-15 |
| JP2001519355A (ja) | 2001-10-23 |
| EP0991660A1 (de) | 2000-04-12 |
| AU750245B2 (en) | 2002-07-11 |
| CA2298572C (en) | 2002-04-09 |
| DE69832984T2 (de) | 2006-09-21 |
| US20020132763A1 (en) | 2002-09-19 |
| ES2256959T3 (es) | 2006-07-16 |
| JP2005343904A (ja) | 2005-12-15 |
| EP0991660B8 (de) | 2006-04-05 |
| JP2004143168A (ja) | 2004-05-20 |
| AU9454298A (en) | 1999-04-27 |
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