RU2008126209A - Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами - Google Patents
Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами Download PDFInfo
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- RU2008126209A RU2008126209A RU2008126209/04A RU2008126209A RU2008126209A RU 2008126209 A RU2008126209 A RU 2008126209A RU 2008126209/04 A RU2008126209/04 A RU 2008126209/04A RU 2008126209 A RU2008126209 A RU 2008126209A RU 2008126209 A RU2008126209 A RU 2008126209A
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- 102000004196 processed proteins & peptides Human genes 0.000 title claims abstract 5
- 108090000765 processed proteins & peptides Proteins 0.000 title claims abstract 5
- 102000004169 proteins and genes Human genes 0.000 title claims abstract 5
- 108090000623 proteins and genes Proteins 0.000 title claims abstract 5
- 230000021615 conjugation Effects 0.000 title claims abstract 3
- 229920000642 polymer Polymers 0.000 claims abstract 8
- 230000000269 nucleophilic effect Effects 0.000 claims abstract 6
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims abstract 4
- 102400001368 Epidermal growth factor Human genes 0.000 claims abstract 2
- 101800003838 Epidermal growth factor Proteins 0.000 claims abstract 2
- 102000003951 Erythropoietin Human genes 0.000 claims abstract 2
- 108090000394 Erythropoietin Proteins 0.000 claims abstract 2
- 102000004269 Granulocyte Colony-Stimulating Factor Human genes 0.000 claims abstract 2
- 108010017080 Granulocyte Colony-Stimulating Factor Proteins 0.000 claims abstract 2
- 102100040018 Interferon alpha-2 Human genes 0.000 claims abstract 2
- 108010079944 Interferon-alpha2b Proteins 0.000 claims abstract 2
- 108010023197 Streptokinase Proteins 0.000 claims abstract 2
- 230000004913 activation Effects 0.000 claims abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims abstract 2
- 229940116977 epidermal growth factor Drugs 0.000 claims abstract 2
- 229940105423 erythropoietin Drugs 0.000 claims abstract 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims abstract 2
- 229920001184 polypeptide Polymers 0.000 claims abstract 2
- OXCMYAYHXIHQOA-UHFFFAOYSA-N potassium;[2-butyl-5-chloro-3-[[4-[2-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanol Chemical compound [K+].CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C2=N[N-]N=N2)C=C1 OXCMYAYHXIHQOA-UHFFFAOYSA-N 0.000 claims abstract 2
- 229960005202 streptokinase Drugs 0.000 claims abstract 2
- VBEQCZHXXJYVRD-GACYYNSASA-N uroanthelone Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CS)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C(C)C)[C@@H](C)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@H](CCSC)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CS)NC(=O)CNC(=O)[C@H]1N(CCC1)C(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(N)=O)C(C)C)[C@@H](C)CC)C1=CC=C(O)C=C1 VBEQCZHXXJYVRD-GACYYNSASA-N 0.000 claims abstract 2
- 0 CCCCC(*NC)N*OC Chemical compound CCCCC(*NC)N*OC 0.000 description 1
Classifications
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- 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
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
- C08G65/26—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 from cyclic ethers and other compounds
-
- 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
- C08G65/321—Polymers modified by chemical after-treatment with inorganic compounds
- C08G65/325—Polymers modified by chemical after-treatment with inorganic compounds containing nitrogen
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Polymers & Plastics (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Inorganic Chemistry (AREA)
- Communicable Diseases (AREA)
- Peptides Or Proteins (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Polyethers (AREA)
- Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
Abstract
1. Полимерная дендример-подобная структура, включающая четыре ветви монометоксиполиэтиленгликоля, которая может быть представлена как: ! ! для получения конъюгатов, представляющих фармацевтический интерес. ! 2. Полимерная структура по п.1, где молекулярная масса каждой ПЭГ-цепи находится между 5000 и 30000 Д, а общая молекулярная масса находится между 20000 и 120000 Д. ! 3. Полимерная структура по п.2, активированная для конъюгирования с нуклеофильными группами, полученная функциональной активацией карбоксильной группы. ! 4. Конъюгат, включающий полимерную структуру по п.1 и нуклеофильную группу. ! 5. Конъюгат по п.4, где нуклеофильная группа содержится в биомолекуле, выбранной из группы, состоящей из белков, пептидов и полипептидов. ! 6. Конъюгат по п.5, где белок выбран из группы, состоящей из интерферона альфа 2-b, стрептокиназы, гранулоцитарного колониестимулирующего фактора, эритропоэтина и эпидермального ростового фактора.
Claims (6)
1. Полимерная дендример-подобная структура, включающая четыре ветви монометоксиполиэтиленгликоля, которая может быть представлена как:
для получения конъюгатов, представляющих фармацевтический интерес.
2. Полимерная структура по п.1, где молекулярная масса каждой ПЭГ-цепи находится между 5000 и 30000 Д, а общая молекулярная масса находится между 20000 и 120000 Д.
3. Полимерная структура по п.2, активированная для конъюгирования с нуклеофильными группами, полученная функциональной активацией карбоксильной группы.
4. Конъюгат, включающий полимерную структуру по п.1 и нуклеофильную группу.
5. Конъюгат по п.4, где нуклеофильная группа содержится в биомолекуле, выбранной из группы, состоящей из белков, пептидов и полипептидов.
6. Конъюгат по п.5, где белок выбран из группы, состоящей из интерферона альфа 2-b, стрептокиназы, гранулоцитарного колониестимулирующего фактора, эритропоэтина и эпидермального ростового фактора.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CU20050241A CU23556A1 (es) | 2005-11-30 | 2005-11-30 | Estructura polimérica semejante a dendrímero para la obtención de conjugados de interés farmacéutico |
| CU2005-0241 | 2005-11-30 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2008126209A true RU2008126209A (ru) | 2010-01-10 |
| RU2409389C2 RU2409389C2 (ru) | 2011-01-20 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008126209/05A RU2409389C2 (ru) | 2005-11-30 | 2006-11-20 | Дендример-пэг с четырьмя ветками для конъюгирования с белками и пептидами |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8703893B2 (ru) |
| EP (1) | EP1967212B1 (ru) |
| JP (1) | JP5123201B2 (ru) |
| KR (1) | KR101134983B1 (ru) |
| CN (2) | CN101389354A (ru) |
| AR (1) | AR058841A1 (ru) |
| AU (1) | AU2006319636B2 (ru) |
| BR (1) | BRPI0604313A (ru) |
| CA (1) | CA2631335C (ru) |
| CU (1) | CU23556A1 (ru) |
| EG (1) | EG26619A (ru) |
| MY (1) | MY150739A (ru) |
| RU (1) | RU2409389C2 (ru) |
| UA (1) | UA91575C2 (ru) |
| UY (1) | UY29981A1 (ru) |
| WO (1) | WO2007062610A2 (ru) |
| ZA (1) | ZA200804694B (ru) |
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| JPH0688453B2 (ja) | 1986-10-03 | 1994-11-09 | 富士写真フイルム株式会社 | 感熱記録材料 |
| WO2007082331A1 (en) * | 2006-01-20 | 2007-07-26 | Starpharma Pty Limited | Modified macromolecule |
| US8252834B2 (en) * | 2008-03-12 | 2012-08-28 | The Regents Of The University Of Michigan | Dendrimer conjugates |
| WO2010039861A2 (en) * | 2008-09-30 | 2010-04-08 | The Regents Of The University Of Michigan | Dendrimer conjugates |
| WO2010054321A2 (en) | 2008-11-07 | 2010-05-14 | The Regents Of The University Of Michigan | Methods of treating autoimmune disorders and/or inflammatory disorders |
| US20100158850A1 (en) * | 2008-12-23 | 2010-06-24 | The Regents Of The University Of Michigan | Dendrimer based modular platforms |
| WO2011059609A2 (en) * | 2009-10-13 | 2011-05-19 | The Regents Of The University Of Michigan | Dendrimer compositions and methods of synthesis |
| US8912323B2 (en) | 2009-10-30 | 2014-12-16 | The Regents Of The University Of Michigan | Multifunctional small molecules |
| RU2441036C1 (ru) * | 2010-09-30 | 2012-01-27 | Общество с ограниченной ответственностью Научно-производственное объединение "Перспектива" (ООО НПО "Перспектива") | Способ получения активированного полиэтиленоксида |
| WO2013085718A1 (en) | 2011-12-08 | 2013-06-13 | The Regents Of The University Of Michigan | Multifunctional small molecules |
| CN104105508B (zh) * | 2011-12-21 | 2017-10-24 | 加利福尼亚大学董事会 | 药物递送增强的末端树枝状聚合物 |
| US9642916B2 (en) | 2012-12-12 | 2017-05-09 | The Regents Of The University Of California | Porphyrin modified telodendrimers |
| AU2014226741B2 (en) * | 2013-03-05 | 2018-10-18 | Hanmi Pharm. Co., Ltd. | Improved preparation method for high-yield production of physiologically active polypeptide conjugate |
| EP2786766A1 (en) * | 2013-04-05 | 2014-10-08 | Ufpeptides S.r.l. | Supramolecular aggregates comprising maleimido cores |
| US9630909B2 (en) | 2013-06-27 | 2017-04-25 | Mylan Laboratories Ltd | Process for the preparation of nepafenac |
| CU20140003A7 (es) * | 2014-01-08 | 2015-08-27 | Ct De Inmunología Molecular Biofarmacuba | Conjugado que comprende eritropoyetina y una estructura polimérica ramificada |
| WO2017030563A1 (en) | 2014-08-19 | 2017-02-23 | Biogen Ma Inc | Pegylation method |
| CN107949565A (zh) * | 2015-06-11 | 2018-04-20 | 安姆生物制药有限责任公司 | 聚乙二醇化粒细胞集落刺激因子(gcsf) |
| WO2017094897A1 (ja) | 2015-12-04 | 2017-06-08 | 全薬工業株式会社 | 血中滞留性を改善した抗ｉｌ－１７アプタマー |
| WO2017118707A1 (en) | 2016-01-08 | 2017-07-13 | Ascendis Pharma Growth Disorders A/S | Controlled-release cnp agonists with reduced side-effects |
| CN115177720A (zh) | 2016-01-08 | 2022-10-14 | 阿森迪斯药物生长障碍股份有限公司 | 具有低npr-c结合的控制释放cnp激动剂 |
| WO2017118693A1 (en) * | 2016-01-08 | 2017-07-13 | Ascendis Pharma Growth Disorders A/S | Cnp prodrugs with large carrier moieties |
| CA3008015A1 (en) | 2016-01-08 | 2017-07-13 | Ascendis Pharma Growth Disorders A/S | Controlled-release c-type natriuretic peptide agonists with increased neutral endopeptidase stability |
| NZ743488A (en) | 2016-01-08 | 2023-02-24 | Ascendis Pharma Growth Disorders As | Controlled-release cnp agonists with low initial npr-b activity |
| AU2017205688C1 (en) | 2016-01-08 | 2022-03-10 | Ascendis Pharma Growth Disorders A/S | Cnp prodrugs with carrier attachment at the ring moiety |
| EP3512569A4 (en) | 2016-09-15 | 2020-09-23 | The Regents of The University of California | ENHANCED HYBRID TELODENDRIMERS |
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2005
- 2005-11-30 CU CU20050241A patent/CU23556A1/es active IP Right Grant
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2006
- 2006-10-19 BR BRPI0604313-5A patent/BRPI0604313A/pt not_active Application Discontinuation
- 2006-11-20 US US12/095,335 patent/US8703893B2/en not_active Expired - Fee Related
- 2006-11-20 RU RU2008126209/05A patent/RU2409389C2/ru not_active IP Right Cessation
- 2006-11-20 CN CNA2006800491651A patent/CN101389354A/zh active Pending
- 2006-11-20 WO PCT/CU2006/000014 patent/WO2007062610A2/es not_active Ceased
- 2006-11-20 MY MYPI20081872 patent/MY150739A/en unknown
- 2006-11-20 AU AU2006319636A patent/AU2006319636B2/en not_active Ceased
- 2006-11-20 EP EP06817995.1A patent/EP1967212B1/en active Active
- 2006-11-20 UA UAA200808587A patent/UA91575C2/ru unknown
- 2006-11-20 JP JP2008542584A patent/JP5123201B2/ja not_active Expired - Fee Related
- 2006-11-20 KR KR1020087015901A patent/KR101134983B1/ko not_active Expired - Fee Related
- 2006-11-20 CA CA2631335A patent/CA2631335C/en not_active Expired - Fee Related
- 2006-11-20 CN CN201510340715.6A patent/CN104906594B/zh not_active Expired - Fee Related
- 2006-11-28 AR ARP060105233A patent/AR058841A1/es not_active Application Discontinuation
- 2006-11-30 UY UY29981A patent/UY29981A1/es not_active Application Discontinuation
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- 2008-06-01 EG EG2008060905A patent/EG26619A/en active
Also Published As
| Publication number | Publication date |
|---|---|
| US20090082537A1 (en) | 2009-03-26 |
| US8703893B2 (en) | 2014-04-22 |
| CN101389354A (zh) | 2009-03-18 |
| AR058841A1 (es) | 2008-02-27 |
| CA2631335A1 (en) | 2007-06-07 |
| CA2631335C (en) | 2013-07-16 |
| AU2006319636A1 (en) | 2007-06-07 |
| CU23556A1 (es) | 2010-07-20 |
| AU2006319636B2 (en) | 2012-10-18 |
| WO2007062610A3 (es) | 2007-09-20 |
| EG26619A (en) | 2014-04-08 |
| JP5123201B2 (ja) | 2013-01-23 |
| JP2009517414A (ja) | 2009-04-30 |
| CN104906594A (zh) | 2015-09-16 |
| BRPI0604313A (pt) | 2007-01-30 |
| KR101134983B1 (ko) | 2012-04-09 |
| KR20080072960A (ko) | 2008-08-07 |
| EP1967212A2 (en) | 2008-09-10 |
| UA91575C2 (ru) | 2010-08-10 |
| MY150739A (en) | 2014-02-28 |
| UY29981A1 (es) | 2007-06-29 |
| EP1967212B1 (en) | 2016-09-21 |
| WO2007062610A2 (es) | 2007-06-07 |
| ZA200804694B (en) | 2009-03-25 |
| CN104906594B (zh) | 2016-12-28 |
| RU2409389C2 (ru) | 2011-01-20 |
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