ES2560807T3 - Nuevos reactivos y procedimiento de conjugación de moléculas biológicas - Google Patents
Nuevos reactivos y procedimiento de conjugación de moléculas biológicas Download PDFInfo
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- ES2560807T3 ES2560807T3 ES11171786.4T ES11171786T ES2560807T3 ES 2560807 T3 ES2560807 T3 ES 2560807T3 ES 11171786 T ES11171786 T ES 11171786T ES 2560807 T3 ES2560807 T3 ES 2560807T3
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- pegylation
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- VMGAPWLDMVPYIA-HIDZBRGKSA-N n'-amino-n-iminomethanimidamide Chemical compound N\N=C\N=N VMGAPWLDMVPYIA-HIDZBRGKSA-N 0.000 description 1
- 238000000655 nuclear magnetic resonance spectrum Methods 0.000 description 1
- 230000001590 oxidative effect Effects 0.000 description 1
- 239000006174 pH buffer Substances 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 1
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 102000004196 processed proteins & peptides Human genes 0.000 description 1
- 230000004952 protein activity Effects 0.000 description 1
- 239000012460 protein solution Substances 0.000 description 1
- 238000010926 purge Methods 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- BOLDJAUMGUJJKM-LSDHHAIUSA-N renifolin D Natural products CC(=C)[C@@H]1Cc2c(O)c(O)ccc2[C@H]1CC(=O)c3ccc(O)cc3O BOLDJAUMGUJJKM-LSDHHAIUSA-N 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000017550 sodium carbonate Nutrition 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-N sulfonic acid Chemical compound OS(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-N 0.000 description 1
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- WROMPOXWARCANT-UHFFFAOYSA-N tfa trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.OC(=O)C(F)(F)F WROMPOXWARCANT-UHFFFAOYSA-N 0.000 description 1
- NJRXVEJTAYWCQJ-UHFFFAOYSA-N thiomalic acid Chemical compound OC(=O)CC(S)C(O)=O NJRXVEJTAYWCQJ-UHFFFAOYSA-N 0.000 description 1
- 238000000870 ultraviolet spectroscopy Methods 0.000 description 1
- 239000003039 volatile agent Substances 0.000 description 1
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- DGVVWUTYPXICAM-UHFFFAOYSA-N β‐Mercaptoethanol Chemical compound OCCS DGVVWUTYPXICAM-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
- C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
- C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C233/00—Carboxylic acid amides
- C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
- C07C233/67—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
- C07C233/68—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
- C07C233/73—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C317/00—Sulfones; Sulfoxides
- C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
- C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/20—Unsaturated compounds containing keto groups bound to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
- C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
- C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
- C08G65/32—Polymers modified by chemical after-treatment
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Polymers & Plastics (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Preparation (AREA)
- Polyethers (AREA)
- Peptides Or Proteins (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0813339 | 2008-07-21 | ||
| GB0813339A GB0813339D0 (en) | 2008-07-21 | 2008-07-21 | Novel reagents and method for conjugating biological molecules |
| GB0905762 | 2009-04-02 | ||
| GB0905762A GB0905762D0 (en) | 2009-04-02 | 2009-04-02 | Novel reagents and method for conjugating biological molecules |
Publications (1)
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| ES2560807T3 true ES2560807T3 (es) | 2016-02-22 |
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| ES09784718.0T Active ES2536882T3 (es) | 2008-07-21 | 2009-07-17 | Nuevos reactivos y procedimiento de conjugación de moléculas biológicas |
| ES11171786.4T Active ES2560807T3 (es) | 2008-07-21 | 2009-07-17 | Nuevos reactivos y procedimiento de conjugación de moléculas biológicas |
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| Application Number | Title | Priority Date | Filing Date |
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| ES09784718.0T Active ES2536882T3 (es) | 2008-07-21 | 2009-07-17 | Nuevos reactivos y procedimiento de conjugación de moléculas biológicas |
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| Country | Link |
|---|---|
| US (4) | US8969626B2 (OSRAM) |
| EP (2) | EP2374481B1 (OSRAM) |
| JP (2) | JP5622117B2 (OSRAM) |
| KR (1) | KR101763559B1 (OSRAM) |
| CN (1) | CN102099058B (OSRAM) |
| AU (1) | AU2009275358C1 (OSRAM) |
| DK (2) | DK2374481T3 (OSRAM) |
| ES (2) | ES2536882T3 (OSRAM) |
| PL (1) | PL2326349T3 (OSRAM) |
| WO (1) | WO2010010324A1 (OSRAM) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| GB0316294D0 (en) * | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| JP5876208B2 (ja) | 2006-12-15 | 2016-03-02 | バクスター・インターナショナル・インコーポレイテッドBaxter International Incorp0Rated | 延長されたinvivo半減期を有する第VIIa因子−(ポリ)シアル酸結合体 |
| CN102099058B (zh) * | 2008-07-21 | 2014-10-22 | 宝力泰锐克斯有限公司 | 用于缀合生物分子的新试剂和方法 |
| WO2010100430A1 (en) | 2009-03-04 | 2010-09-10 | Polytherics Limited | Conjugated proteins and peptides |
| US8642737B2 (en) | 2010-07-26 | 2014-02-04 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| JP5909755B2 (ja) | 2009-07-27 | 2016-04-27 | リポクセン テクノロジーズ リミテッド | 非血液凝固タンパク質の糖ポリシアル酸化 |
| US8809501B2 (en) | 2009-07-27 | 2014-08-19 | Baxter International Inc. | Nucleophilic catalysts for oxime linkage |
| SG178141A1 (en) | 2009-07-27 | 2012-03-29 | Baxter Int | Blood coagulation protein conjugates |
| EP3093029A1 (en) | 2009-07-27 | 2016-11-16 | Baxalta GmbH | Blood coagulation protein conjugates |
| GB201007356D0 (en) | 2010-04-30 | 2010-06-16 | Leverton Licence Holdings Ltd | Conjugated factor VIIa |
| GB201007357D0 (en) | 2010-04-30 | 2010-06-16 | Leverton Licence Holdings Ltd | Conjugated factor VIII |
| CA2811869A1 (en) * | 2010-09-21 | 2012-03-29 | Cristal Delivery B.V. | Tunable, biodegradable linker molecules for transient conjugation of components in drug delivery systems, and drug delivery systems prepared therewith |
| DK2654794T3 (da) | 2010-12-22 | 2020-06-08 | Baxalta GmbH | Materialer og fremgangsmåder til konjugering af et vandopløseligt fedtsyrederivat til et protein |
| AU2012262428C1 (en) * | 2011-05-27 | 2018-10-11 | Takeda Pharmaceutical Company Limited | Therapeutic proteins with increased half-life and methods of preparing same |
| JP5841768B2 (ja) * | 2011-08-05 | 2016-01-13 | 花王株式会社 | 脂肪蓄積抑制剤 |
| EA033469B1 (ru) | 2012-04-16 | 2019-10-31 | Cantab Biopharmaceuticals Patents Ltd | Подкожное введение конъюгатов факторов крови с полиэтиленгликолем |
| US9650331B2 (en) | 2012-06-18 | 2017-05-16 | Polytherics Limited | Conjugation reagents |
| GB201210770D0 (en) * | 2012-06-18 | 2012-08-01 | Polytherics Ltd | Novel conjugation reagents |
| KR102178606B1 (ko) | 2013-03-15 | 2020-11-13 | 자임워크스 인코포레이티드 | 세포독성 및 유사분열-억제 화합물, 및 이를 사용하는 방법 |
| EA038512B1 (ru) | 2013-03-15 | 2021-09-08 | Регенерон Фармасьютикалз, Инк. | Конъюгаты майтанзиноидов и их терапевтическое применение |
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| RU2729194C2 (ru) | 2013-12-27 | 2020-08-05 | Займворкс Инк. | Сульфонамидсодержащие связывающие системы для лекарственных конъюгатов |
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| US20250171516A1 (en) | 2023-11-03 | 2025-05-29 | Regeneron Pharmaceuticals, Inc. | Peptide acids as a glp1r agonist and antibody-drug conjugates thereof |
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| US147443A (en) * | 1874-02-10 | Improvement in lamp-extinguishers | ||
| US6552170B1 (en) | 1990-04-06 | 2003-04-22 | Amgen Inc. | PEGylation reagents and compounds formed therewith |
| US5414135A (en) | 1991-12-30 | 1995-05-09 | Sterling Winthrop Inc. | Vinyl sulfone coupling of polyoxyalkylenes to proteins |
| US5446090A (en) * | 1993-11-12 | 1995-08-29 | Shearwater Polymers, Inc. | Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules |
| US5877224A (en) | 1995-07-28 | 1999-03-02 | Rutgers, The State University Of New Jersey | Polymeric drug formulations |
| GB9713979D0 (en) | 1997-07-03 | 1997-09-10 | Univ Nottingham | Method for attaching peg to macromolecules |
| US6958212B1 (en) * | 1999-02-01 | 2005-10-25 | Eidgenossische Technische Hochschule Zurich | Conjugate addition reactions for the controlled delivery of pharmaceutically active compounds |
| US6828412B1 (en) | 1999-09-03 | 2004-12-07 | School Of Pharmacy, University Of London | Degradable polymers |
| JP4883515B2 (ja) | 1999-09-08 | 2012-02-22 | ポリセリックス リミテッド | 均一分子量ポリマー |
| KR101025143B1 (ko) | 2002-12-31 | 2011-04-01 | 넥타르 테라퓨틱스 | 가수분해상으로 안정한 말레이미드-종결 중합체 |
| JP4009721B2 (ja) * | 2003-05-23 | 2007-11-21 | 独立行政法人産業技術総合研究所 | イオン結合性ポリマー含有基板、該基板を含有する検出用センサー及び病原菌又は病原菌が生産する毒素の検出方法 |
| GB0316294D0 (en) * | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| EP1828244A2 (en) | 2004-12-22 | 2007-09-05 | Kuros Biosurgery AG | Michael-type addition reaction functionalised peg hydrogels with factor xiiia incorporated biofactors |
| DK2209494T3 (en) | 2007-10-09 | 2016-10-03 | Polytherics Ltd | New conjugated proteins and peptides |
| CN102099058B (zh) | 2008-07-21 | 2014-10-22 | 宝力泰锐克斯有限公司 | 用于缀合生物分子的新试剂和方法 |
| GB0912485D0 (en) | 2009-07-17 | 2009-08-26 | Polytherics Ltd | Improved conjugation method |
| WO2010100430A1 (en) * | 2009-03-04 | 2010-09-10 | Polytherics Limited | Conjugated proteins and peptides |
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| CN102099058B (zh) | 2014-10-22 |
| CN102099058A (zh) | 2011-06-15 |
| JP2011252167A (ja) | 2011-12-15 |
| DK2326349T3 (en) | 2015-05-26 |
| AU2009275358B2 (en) | 2015-05-28 |
| US9896412B2 (en) | 2018-02-20 |
| KR101763559B1 (ko) | 2017-08-14 |
| PL2326349T3 (pl) | 2015-08-31 |
| EP2374481B1 (en) | 2015-11-04 |
| EP2374481A3 (en) | 2012-06-13 |
| US20110262994A1 (en) | 2011-10-27 |
| US20140081047A1 (en) | 2014-03-20 |
| EP2326349B1 (en) | 2015-02-25 |
| JP5626655B2 (ja) | 2014-11-19 |
| ES2536882T3 (es) | 2015-05-29 |
| US20110136723A1 (en) | 2011-06-09 |
| WO2010010324A1 (en) | 2010-01-28 |
| AU2009275358C1 (en) | 2015-09-24 |
| KR20110053430A (ko) | 2011-05-23 |
| EP2326349A1 (en) | 2011-06-01 |
| JP5622117B2 (ja) | 2014-11-12 |
| US20150148544A1 (en) | 2015-05-28 |
| US8618333B2 (en) | 2013-12-31 |
| US8969626B2 (en) | 2015-03-03 |
| DK2374481T3 (en) | 2016-02-01 |
| JP2011528706A (ja) | 2011-11-24 |
| EP2374481A2 (en) | 2011-10-12 |
| AU2009275358A1 (en) | 2010-01-28 |
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