CA2537113A1 - Modified protease inhibitors - Google Patents
Modified protease inhibitors Download PDFInfo
- Publication number
- CA2537113A1 CA2537113A1 CA002537113A CA2537113A CA2537113A1 CA 2537113 A1 CA2537113 A1 CA 2537113A1 CA 002537113 A CA002537113 A CA 002537113A CA 2537113 A CA2537113 A CA 2537113A CA 2537113 A1 CA2537113 A1 CA 2537113A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- conjugate
- amino acid
- peg
- polypeptide
- 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.)
- Abandoned
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- 238000002600 positron emission tomography Methods 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 1
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- 208000002815 pulmonary hypertension Diseases 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
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- 239000012857 radioactive material Substances 0.000 description 1
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- 239000000376 reactant Substances 0.000 description 1
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- 206010039073 rheumatoid arthritis Diseases 0.000 description 1
- PYWVYCXTNDRMGF-UHFFFAOYSA-N rhodamine B Chemical compound [Cl-].C=12C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C2C=1C1=CC=CC=C1C(O)=O PYWVYCXTNDRMGF-UHFFFAOYSA-N 0.000 description 1
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- 239000012146 running buffer Substances 0.000 description 1
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- 238000009738 saturating Methods 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 238000010187 selection method Methods 0.000 description 1
- 239000008299 semisolid dosage form Substances 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 208000013220 shortness of breath Diseases 0.000 description 1
- SQVRNKJHWKZAKO-OQPLDHBCSA-N sialic acid Chemical compound CC(=O)N[C@@H]1[C@@H](O)C[C@@](O)(C(O)=O)OC1[C@H](O)[C@H](O)CO SQVRNKJHWKZAKO-OQPLDHBCSA-N 0.000 description 1
- 238000002579 sigmoidoscopy Methods 0.000 description 1
- 150000004756 silanes Chemical class 0.000 description 1
- 238000002741 site-directed mutagenesis Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000000779 smoke Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- BBMHARZCALWXSL-UHFFFAOYSA-M sodium dihydrogenphosphate monohydrate Chemical compound O.[Na+].OP(O)([O-])=O BBMHARZCALWXSL-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
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- 229960000391 sorbitan trioleate Drugs 0.000 description 1
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- 230000006641 stabilisation Effects 0.000 description 1
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- 239000003381 stabilizer Substances 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000008223 sterile water Substances 0.000 description 1
- 230000001954 sterilising effect Effects 0.000 description 1
- 238000004659 sterilization and disinfection Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 238000010254 subcutaneous injection Methods 0.000 description 1
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- 125000001424 substituent group Chemical group 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- NJGWOFRZMQRKHT-UHFFFAOYSA-N surfactin Natural products CC(C)CCCCCCCCCC1CC(=O)NC(CCC(O)=O)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)NC(C(C)C)C(=O)NC(CC(O)=O)C(=O)NC(CC(C)C)C(=O)NC(CC(C)C)C(=O)O1 NJGWOFRZMQRKHT-UHFFFAOYSA-N 0.000 description 1
- NJGWOFRZMQRKHT-WGVNQGGSSA-N surfactin C Chemical compound CC(C)CCCCCCCCC[C@@H]1CC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)O1 NJGWOFRZMQRKHT-WGVNQGGSSA-N 0.000 description 1
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- 238000010189 synthetic method Methods 0.000 description 1
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- 239000006188 syrup Substances 0.000 description 1
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- 230000009885 systemic effect Effects 0.000 description 1
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- 229940126585 therapeutic drug Drugs 0.000 description 1
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- 125000003396 thiol group Chemical group [H]S* 0.000 description 1
- 108060008226 thioredoxin Proteins 0.000 description 1
- 229940094937 thioredoxin Drugs 0.000 description 1
- 230000036964 tight binding Effects 0.000 description 1
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- 108010016054 tissue-factor-pathway inhibitor 2 Proteins 0.000 description 1
- 238000004448 titration Methods 0.000 description 1
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- 230000002588 toxic effect Effects 0.000 description 1
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- 231100000759 toxicological effect Toxicity 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
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- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- QAEDZJGFFMLHHQ-UHFFFAOYSA-N trifluoroacetic anhydride Chemical compound FC(F)(F)C(=O)OC(=O)C(F)(F)F QAEDZJGFFMLHHQ-UHFFFAOYSA-N 0.000 description 1
- 239000002753 trypsin inhibitor Substances 0.000 description 1
- MDYZKJNTKZIUSK-UHFFFAOYSA-N tyloxapol Chemical compound O=C.C1CO1.CC(C)(C)CC(C)(C)C1=CC=C(O)C=C1 MDYZKJNTKZIUSK-UHFFFAOYSA-N 0.000 description 1
- 229920001664 tyloxapol Polymers 0.000 description 1
- 229960004224 tyloxapol Drugs 0.000 description 1
- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 231100000397 ulcer Toxicity 0.000 description 1
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- 239000013598 vector Substances 0.000 description 1
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- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 description 1
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- 235000012431 wafers Nutrition 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 239000001018 xanthene dye Substances 0.000 description 1
- 210000005253 yeast cell Anatomy 0.000 description 1
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- 239000011701 zinc Substances 0.000 description 1
- 229950009268 zinostatin Drugs 0.000 description 1
- 229910000859 α-Fe Inorganic materials 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/81—Protease inhibitors
- C07K14/8107—Endopeptidase (E.C. 3.4.21-99) inhibitors
- C07K14/811—Serine protease (E.C. 3.4.21) inhibitors
- C07K14/8114—Kunitz type inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
- A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/0002—General or multifunctional contrast agents, e.g. chelated agents
-
- 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
- A61P11/00—Drugs for disorders of the respiratory 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Biochemistry (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US49884503P | 2003-08-29 | 2003-08-29 | |
| US60/498,845 | 2003-08-29 | ||
| PCT/US2004/028256 WO2005021556A2 (en) | 2003-08-29 | 2004-08-30 | Modified protease inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2537113A1 true CA2537113A1 (en) | 2005-03-10 |
Family
ID=34272739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002537113A Abandoned CA2537113A1 (en) | 2003-08-29 | 2004-08-30 | Modified protease inhibitors |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20070020252A1 (https=) |
| EP (1) | EP1663279A4 (https=) |
| JP (1) | JP2007504169A (https=) |
| AU (1) | AU2004268144A1 (https=) |
| CA (1) | CA2537113A1 (https=) |
| WO (1) | WO2005021556A2 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6057287A (en) | 1994-01-11 | 2000-05-02 | Dyax Corp. | Kallikrein-binding "Kunitz domain" proteins and analogues thereof |
| WO2003103475A2 (en) | 2002-06-07 | 2003-12-18 | Dyax Corp. | Prevention and reduction of blood loss |
| US7153829B2 (en) | 2002-06-07 | 2006-12-26 | Dyax Corp. | Kallikrein-inhibitor therapies |
| PT1663281E (pt) * | 2003-08-29 | 2014-03-17 | Dyax Corp | Inibidores de proteases poli-peguilados |
| US7235530B2 (en) | 2004-09-27 | 2007-06-26 | Dyax Corporation | Kallikrein inhibitors and anti-thrombolytic agents and uses thereof |
| WO2006070012A1 (en) * | 2004-12-30 | 2006-07-06 | Ingenium Pharmaceuticals Ag | Agents useful in treating inflammatory bowel disease |
| SI1981519T1 (en) * | 2005-12-29 | 2018-05-31 | Dyax Corp. | INHIBITION PROTEAZE |
| DK1854477T3 (en) * | 2006-03-16 | 2016-11-28 | Dyax Corp | Peptide inhibitors of plasma kallikrein for use in the treatment of eye disorders |
| WO2010033226A1 (en) * | 2008-09-17 | 2010-03-25 | Nektar Therapeutics | Oligomer-protease inhibitor conjugates |
| CA2744235A1 (en) | 2009-01-06 | 2010-07-15 | Dyax Corp. | Treatment of mucositis with kallikrein inhibitors |
| JP2012530069A (ja) * | 2009-06-12 | 2012-11-29 | ネクター セラピューティックス | プロテアーゼ阻害剤、水溶性非ペプチドオリゴマーおよび親油性部分を含む共有結合体 |
| US20110094080A1 (en) * | 2009-10-27 | 2011-04-28 | William Karales | Bar soap support mat |
| EP3459564B1 (en) | 2010-01-06 | 2021-10-27 | Takeda Pharmaceutical Company Limited | Plasma kallikrein binding proteins |
| CA2823776A1 (en) | 2011-01-06 | 2012-07-12 | Dyax Corp. | Plasma kallikrein binding proteins |
| IL295414B2 (en) | 2014-03-27 | 2026-02-01 | Takeda Pharmaceuticals Co | Compositions and methods for treating macular edema due to diabetes |
| AU2016366557B2 (en) | 2015-12-11 | 2024-01-25 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof for treating hereditary angioedema attack |
| US12528880B2 (en) | 2020-01-13 | 2026-01-20 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof for treating pediatric hereditary angioedema attack |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5663143A (en) * | 1988-09-02 | 1997-09-02 | Dyax Corp. | Engineered human-derived kunitz domains that inhibit human neutrophil elastase |
| ES2229236T3 (es) * | 1994-01-11 | 2005-04-16 | Dyax Corporation | Inhibidores de la plasmina humana derivados de los dominios de kunitz. |
| US5795954A (en) * | 1994-03-04 | 1998-08-18 | Genentech, Inc. | Factor VIIa inhibitors from Kunitz domain proteins |
| EP0763055B1 (en) * | 1994-06-02 | 1999-11-03 | Merrell Pharmaceuticals Inc. | Perfluoroalkyl ketone inhibitors of elastase and processes for making the same |
| US5589359A (en) * | 1994-08-05 | 1996-12-31 | Chiron Corporation | Chimeric proteins |
| US5990237A (en) * | 1997-05-21 | 1999-11-23 | Shearwater Polymers, Inc. | Poly(ethylene glycol) aldehyde hydrates and related polymers and applications in modifying amines |
| WO2000032772A2 (en) * | 1998-11-30 | 2000-06-08 | Eli Lilly And Company | Erythropoietic compounds |
| SK8292002A3 (en) * | 1999-11-12 | 2002-12-03 | Maxygen Holdings Ltd | A conjugate exhibiting interferon gamma activity, nucleotide sequence encoding for a polypeptide fraction of conjugate, an expression vector and a host cell containing nucleotide sequence, pharmaceutical composition comprising the same and use thereof |
| US6544760B2 (en) * | 1999-12-22 | 2003-04-08 | Zymogenetics, Inc. | Kunitz domain polypeptide Zkun11 |
| US20020168323A1 (en) * | 2001-05-11 | 2002-11-14 | Igor Gonda | Optimization of the molecular properties and formulation of proteins delivered by inhalation |
| JP2004535401A (ja) * | 2001-05-21 | 2004-11-25 | ネクター セラピューティックス | 化学的に改変されたインスリンの肺投与 |
| HRP20050024A2 (en) * | 2002-07-24 | 2006-02-28 | F. Hoffmann - La Roche Ag | Pegylated t20 polypeptide |
| WO2004012773A1 (en) * | 2002-07-24 | 2004-02-12 | F. Hoffmann-La Roche Ag | Polyalkylene glycol acid additives |
| US7314613B2 (en) * | 2002-11-18 | 2008-01-01 | Maxygen, Inc. | Interferon-alpha polypeptides and conjugates |
| PT1663281E (pt) * | 2003-08-29 | 2014-03-17 | Dyax Corp | Inibidores de proteases poli-peguilados |
| US20060228331A1 (en) * | 2003-10-10 | 2006-10-12 | Novo Nordisk A/S | IL-21 Derivatives and variants |
-
2004
- 2004-08-30 WO PCT/US2004/028256 patent/WO2005021556A2/en not_active Ceased
- 2004-08-30 CA CA002537113A patent/CA2537113A1/en not_active Abandoned
- 2004-08-30 JP JP2006524951A patent/JP2007504169A/ja not_active Withdrawn
- 2004-08-30 AU AU2004268144A patent/AU2004268144A1/en not_active Abandoned
- 2004-08-30 EP EP04782687A patent/EP1663279A4/en not_active Ceased
- 2004-08-30 US US10/570,186 patent/US20070020252A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2007504169A (ja) | 2007-03-01 |
| EP1663279A2 (en) | 2006-06-07 |
| EP1663279A4 (en) | 2009-02-18 |
| US20070020252A1 (en) | 2007-01-25 |
| WO2005021556A3 (en) | 2005-12-15 |
| WO2005021556A2 (en) | 2005-03-10 |
| AU2004268144A1 (en) | 2005-03-10 |
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