CN102325880B - 丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 - Google Patents
丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 Download PDFInfo
- Publication number
- CN102325880B CN102325880B CN200980157388.3A CN200980157388A CN102325880B CN 102325880 B CN102325880 B CN 102325880B CN 200980157388 A CN200980157388 A CN 200980157388A CN 102325880 B CN102325880 B CN 102325880B
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- Prior art keywords
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- protein
- factor
- chimeric
- amino acid
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- 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
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
- C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/745—Blood coagulation or fibrinolysis factors
-
- 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
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
- C12N9/6424—Serine endopeptidases (3.4.21)
- C12N9/6429—Thrombin (3.4.21.5)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
- C12N9/6424—Serine endopeptidases (3.4.21)
- C12N9/6432—Coagulation factor Xa (3.4.21.6)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/14—Hydrolases (3)
- C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
- C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
- C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
- C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
- C12N9/6424—Serine endopeptidases (3.4.21)
- C12N9/6464—Protein C (3.4.21.69)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
- C12Y304/21—Serine endopeptidases (3.4.21)
- C12Y304/21005—Thrombin (3.4.21.5)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
- C12Y304/21—Serine endopeptidases (3.4.21)
- C12Y304/21006—Coagulation factor Xa (3.4.21.6)
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
- C12Y304/21—Serine endopeptidases (3.4.21)
- C12Y304/21069—Protein C activated (3.4.21.69)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- 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
- A61K47/62—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 a protein, peptide or polyamino acid
- A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K2319/00—Fusion polypeptide
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- General Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Hematology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Toxicology (AREA)
- Gastroenterology & Hepatology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08305990.7 | 2008-12-19 | ||
| EP08305990A EP2199387A1 (en) | 2008-12-19 | 2008-12-19 | Serine protease derivatives and uses for the prevention and/or the treatment of blood coagulation disorders |
| EP09305349.4 | 2009-04-23 | ||
| EP09305349 | 2009-04-23 | ||
| US22296009P | 2009-07-03 | 2009-07-03 | |
| US61/222,960 | 2009-07-03 | ||
| US61/222960 | 2009-07-03 | ||
| PCT/EP2009/067632 WO2010070137A1 (en) | 2008-12-19 | 2009-12-21 | Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410496015.1A Division CN104262479A (zh) | 2008-12-19 | 2009-12-21 | 丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102325880A CN102325880A (zh) | 2012-01-18 |
| CN102325880B true CN102325880B (zh) | 2014-10-01 |
Family
ID=41718355
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200980157388.3A Expired - Fee Related CN102325880B (zh) | 2008-12-19 | 2009-12-21 | 丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 |
| CN201410496015.1A Pending CN104262479A (zh) | 2008-12-19 | 2009-12-21 | 丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410496015.1A Pending CN104262479A (zh) | 2008-12-19 | 2009-12-21 | 丝氨酸蛋白酶衍生物及其在凝血功能障碍的预防或治疗中的用途 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US8436144B2 (enExample) |
| EP (1) | EP2358874B1 (enExample) |
| JP (1) | JP5833448B2 (enExample) |
| KR (1) | KR20110114587A (enExample) |
| CN (2) | CN102325880B (enExample) |
| AU (1) | AU2009329493B2 (enExample) |
| CA (1) | CA2747065A1 (enExample) |
| ES (1) | ES2629099T3 (enExample) |
| WO (1) | WO2010070137A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2008006313A (es) * | 2005-11-15 | 2008-11-06 | Philadelphia Children Hospital | Metodos y composiciones para modular la hemostasia. |
| PT3078743T (pt) | 2007-09-28 | 2020-07-15 | Portola Pharm Inc | Antídotos para inibidores do fator xa e métodos de utilização dos mesmos |
| US8455439B2 (en) | 2008-11-14 | 2013-06-04 | Portola Pharmaceuticals, Inc. | Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents |
| US8436144B2 (en) * | 2008-12-19 | 2013-05-07 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders |
| EP3604510B1 (en) | 2009-03-30 | 2025-03-26 | Alexion Pharmaceuticals, Inc. | Antidotes for factor xa inhibitors and methods of using the same |
| WO2011008885A1 (en) | 2009-07-15 | 2011-01-20 | Portola Pharmaceuticals, Inc. | Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same |
| EP2760887B1 (en) * | 2011-09-30 | 2024-10-23 | The Children's Hospital of Philadelphia | Compositions and methods for modulating hemostasis |
| AU2013293573B2 (en) * | 2012-07-25 | 2016-10-27 | Catalyst Biosciences, Inc. | Modified Factor X polypeptides and uses thereof |
| ES2761730T3 (es) | 2013-01-31 | 2020-05-20 | Pfizer | Composiciones y procedimientos para contrarrestar la inhibición del factor Xa |
| FR3001729B1 (fr) * | 2013-02-04 | 2015-03-06 | Lab Francais Du Fractionnement | Mutants du facteur x |
| JP2016510984A (ja) * | 2013-03-12 | 2016-04-14 | ノヴォ ノルディスク アー/エス | トロンビン感受性凝固第x因子分子 |
| KR101988705B1 (ko) | 2013-09-24 | 2019-06-12 | 화이자 인코포레이티드 | 재조합 인간 응고 인자 Xa 단백질의 이질적 집단을 포함하는 조성물 |
| EP3242936A1 (en) * | 2015-01-07 | 2017-11-15 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Mutated factor x polypeptides and uses thereof for the treatment of haemophilia |
| EP3328998A1 (en) * | 2015-07-27 | 2018-06-06 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Mutated factor x polypeptides and uses thereof for the treatment of haemophilia |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101006175A (zh) * | 2004-08-17 | 2007-07-25 | Csl百灵有限公司 | 经修饰的维生素k依赖性多肽 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4861719A (en) | 1986-04-25 | 1989-08-29 | Fred Hutchinson Cancer Research Center | DNA constructs for retrovirus packaging cell lines |
| US4992373A (en) | 1987-12-04 | 1991-02-12 | Eli Lilly And Company | Vectors and compounds for direct expression of activated human protein C |
| US5278056A (en) | 1988-02-05 | 1994-01-11 | The Trustees Of Columbia University In The City Of New York | Retroviral packaging cell lines and process of using same |
| US4981952A (en) | 1988-10-04 | 1991-01-01 | Eli Lilly And Company | Method for the purification of vitamin K-dependent proteins |
| US5670488A (en) | 1992-12-03 | 1997-09-23 | Genzyme Corporation | Adenovirus vector for gene therapy |
| MY110664A (en) | 1992-05-21 | 1999-01-30 | Lilly Co Eli | Protein c derivatives |
| AU6248994A (en) | 1993-02-22 | 1994-09-14 | Rockefeller University, The | Production of high titer helper-free retroviruses by transient transfection |
| FR2712812B1 (fr) | 1993-11-23 | 1996-02-09 | Centre Nat Rech Scient | Composition pour la production de produits thérapeutiques in vivo. |
| IL116816A (en) | 1995-01-20 | 2003-05-29 | Rhone Poulenc Rorer Sa | Cell for the production of a defective recombinant adenovirus or an adeno-associated virus and the various uses thereof |
| US6013516A (en) | 1995-10-06 | 2000-01-11 | The Salk Institute For Biological Studies | Vector and method of use for nucleic acid delivery to non-dividing cells |
| FR2831170B1 (fr) * | 2001-10-19 | 2004-03-19 | Inst Nat Sante Rech Med | Proteines c modifiees activables directement par la thrombine |
| FR2841904B1 (fr) | 2002-07-03 | 2004-08-20 | Inst Nat Sante Rech Med | Analogues de facteurs x clivables par la thrombine |
| WO2005007820A2 (en) | 2003-07-08 | 2005-01-27 | The Scripps Research Institute | Activated protein c variants with normal cytoprotective activity but reduced anticoagulant activity |
| RU2346996C2 (ru) | 2004-06-29 | 2009-02-20 | ЮРОПИЭН НИКЕЛЬ ПиЭлСи | Усовершенствованное выщелачивание основных металлов |
| EP1820508A1 (en) * | 2006-02-21 | 2007-08-22 | CSL Behring GmbH | Coagulation factor X polypeptides with modified activation properties |
| US8246856B2 (en) | 2007-08-01 | 2012-08-21 | Dow Global Technologies Llc | Highly efficient process for manufacture of exfoliated graphene |
| US8436144B2 (en) * | 2008-12-19 | 2013-05-07 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | Serine protease derivatives and uses in the prevention or the treatment of blood coagulation disorders |
-
2009
- 2009-12-21 US US13/139,367 patent/US8436144B2/en not_active Expired - Fee Related
- 2009-12-21 KR KR1020117016908A patent/KR20110114587A/ko not_active Ceased
- 2009-12-21 JP JP2011541497A patent/JP5833448B2/ja not_active Expired - Fee Related
- 2009-12-21 WO PCT/EP2009/067632 patent/WO2010070137A1/en not_active Ceased
- 2009-12-21 CA CA2747065A patent/CA2747065A1/en not_active Abandoned
- 2009-12-21 CN CN200980157388.3A patent/CN102325880B/zh not_active Expired - Fee Related
- 2009-12-21 CN CN201410496015.1A patent/CN104262479A/zh active Pending
- 2009-12-21 EP EP09796378.9A patent/EP2358874B1/en not_active Not-in-force
- 2009-12-21 ES ES09796378.9T patent/ES2629099T3/es active Active
- 2009-12-21 AU AU2009329493A patent/AU2009329493B2/en not_active Ceased
-
2013
- 2013-01-02 US US13/732,465 patent/US8518400B2/en not_active Expired - Fee Related
- 2013-06-04 US US13/909,323 patent/US8741286B2/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101006175A (zh) * | 2004-08-17 | 2007-07-25 | Csl百灵有限公司 | 经修饰的维生素k依赖性多肽 |
Non-Patent Citations (4)
| Title |
|---|
| Identification of the oligosaccharide structures of human coagulation factor x activation peptide at each glycosylation site;Hiroaki nakagawa et al;《Glycoconjugate Journal》;19951231;第12卷;全文 * |
| Role of the activation peptide domain in human factor x activation by the extrinsic xase complex;Robert J.Baugh et al;《The journal of biological chemistry》;19961231;第271卷(第27期);全文 * |
| The role of the factor x activation peptide:A deletion mutagenesis approach;Rudolph A E et al;《Thrombosis and haemostasis》;20021101;第88卷(第5期);全文 * |
| Thrombin-activable factor x re-establishes an intrinsic amplification in tenase-deficient plasmas;Louvain quintard virginie B et al;《Journal of biological chemistry》;20051231;第280卷(第50期);全文 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20130261060A1 (en) | 2013-10-03 |
| US8436144B2 (en) | 2013-05-07 |
| JP5833448B2 (ja) | 2015-12-16 |
| AU2009329493B2 (en) | 2014-09-18 |
| CN104262479A (zh) | 2015-01-07 |
| US8518400B2 (en) | 2013-08-27 |
| EP2358874A1 (en) | 2011-08-24 |
| JP2012512645A (ja) | 2012-06-07 |
| US20110293597A1 (en) | 2011-12-01 |
| CN102325880A (zh) | 2012-01-18 |
| KR20110114587A (ko) | 2011-10-19 |
| EP2358874B1 (en) | 2017-03-29 |
| US8741286B2 (en) | 2014-06-03 |
| US20130101570A1 (en) | 2013-04-25 |
| WO2010070137A1 (en) | 2010-06-24 |
| AU2009329493A1 (en) | 2011-07-21 |
| ES2629099T3 (es) | 2017-08-07 |
| CA2747065A1 (en) | 2010-06-24 |
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