AU2013279099A1 - Novel process for preparation of antibody conjugates and novel antibody conjugates - Google Patents

Novel process for preparation of antibody conjugates and novel antibody conjugates Download PDF

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Publication number
AU2013279099A1
AU2013279099A1 AU2013279099A AU2013279099A AU2013279099A1 AU 2013279099 A1 AU2013279099 A1 AU 2013279099A1 AU 2013279099 A AU2013279099 A AU 2013279099A AU 2013279099 A AU2013279099 A AU 2013279099A AU 2013279099 A1 AU2013279099 A1 AU 2013279099A1
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AU
Australia
Prior art keywords
antibody
ser
pro
group
cysteine
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
Application number
AU2013279099A
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English (en)
Inventor
George Badescu
John Burt
Antony Godwin
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Abzena UK Ltd
Original Assignee
Polytherics Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Priority claimed from GBGB1210838.7A external-priority patent/GB201210838D0/en
Priority claimed from GB201306706A external-priority patent/GB201306706D0/en
Application filed by Polytherics Ltd filed Critical Polytherics Ltd
Publication of AU2013279099A1 publication Critical patent/AU2013279099A1/en
Abandoned legal-status Critical Current

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Classifications

    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6871—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting an enzyme
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/50—Immunoglobulins specific features characterized by immunoglobulin fragments
    • C07K2317/52—Constant or Fc region; Isotype
    • C07K2317/53—Hinge

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Immunology (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Oncology (AREA)
  • Cell Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2013279099A 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates Abandoned AU2013279099A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GBGB1210838.7A GB201210838D0 (en) 2012-06-19 2012-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates
GB1210838.7 2012-06-19
GB1306706.1 2013-04-12
GB201306706A GB201306706D0 (en) 2013-04-12 2013-04-12 Novel process for preparation of antibody conjugates and novel antibody conjugates
PCT/GB2013/051593 WO2013190292A2 (en) 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates

Publications (1)

Publication Number Publication Date
AU2013279099A1 true AU2013279099A1 (en) 2014-12-18

Family

ID=48699187

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2013279099A Abandoned AU2013279099A1 (en) 2012-06-19 2013-06-19 Novel process for preparation of antibody conjugates and novel antibody conjugates

Country Status (16)

Country Link
US (1) US20150125473A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
EP (1) EP2861261A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
JP (1) JP2015521615A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
KR (1) KR20150023027A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CN (1) CN104379178A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
AU (1) AU2013279099A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
BR (1) BR112014031613A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
CA (1) CA2876365A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
HK (1) HK1204924A1 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IL (1) IL235646A0 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
IN (1) IN2014DN10428A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
MX (1) MX2014015682A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
RU (1) RU2015101333A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
SG (1) SG11201407600UA (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
WO (1) WO2013190292A2 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)
ZA (1) ZA201408916B (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html)

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NO2789793T3 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) * 2012-10-24 2018-01-27
CA2902872A1 (en) 2013-03-15 2014-09-18 Regeneron Pharmaceuticals, Inc. Biologically active molecules, conjugates thereof, and therapeutic uses
AU2014311361B2 (en) 2013-08-26 2018-11-29 Regeneron Pharmaceuticals, Inc. Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
CN106536560B (zh) * 2014-05-23 2021-03-09 诺华股份有限公司 从含二硫化物的蛋白质制备缀合物的方法
JP6800021B2 (ja) 2014-06-02 2020-12-16 レゲネロン ファーマシューティカルス，インコーポレーテッド 抗体−薬物コンジュゲート、それらの製造、及びそれらの治療用途
MY198629A (en) * 2014-07-24 2023-09-11 Genentech Inc Methods of conjugating an agent to a thiol moiety in a protein that contains at least one trisulfide bond
US10835616B2 (en) 2014-10-14 2020-11-17 Polytherics Limited Process for the conjugation of a peptide or protein with a reagent comprising a leaving group including a portion of PEG
MX2017005199A (es) * 2014-10-24 2017-07-26 Polytherics Ltd Conjugados y reactivos de conjugacion.
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
US20170281796A1 (en) * 2014-12-08 2017-10-05 Sorrento Therapeutics, Inc. c-Met Antibody Drug Conjugate
EA201791461A1 (ru) 2015-01-14 2017-11-30 Бристол-Майерс Сквибб Компани Бензодиазепиновые димеры с мостиковым гетероариленом, их конъюгаты, способы получения и применение
JP6894375B2 (ja) * 2015-02-05 2021-06-30 アブリンクス エン．ヴェー． Ｃ末端で操作されたシステインを介して連結されたＮａｎｏｂｏｄｙダイマー
CN107995912A (zh) 2015-03-27 2018-05-04 里珍纳龙药品有限公司 美登素类衍生物、其偶联物和使用方法
WO2017025458A1 (en) 2015-08-07 2017-02-16 Gamamabs Pharma Antibodies, antibody drug conjugates and methods of use
TWI618697B (zh) 2015-11-03 2018-03-21 財團法人工業技術研究院 化合物、連接子－藥物、及配體－藥物耦合體
KR20180099892A (ko) 2016-01-25 2018-09-05 리제너론 파아마슈티컬스, 인크. 메이탄시노이드 유도체, 그의 접합체, 및 사용 방법
CN109152845B (zh) * 2016-04-14 2022-07-12 宝力泰锐克斯有限公司 含有在环内包含至少两个(-ch2-ch2-o-)单元的接头的缀合物和缀合试剂
GB201614162D0 (en) * 2016-08-18 2016-10-05 Polytherics Ltd Antibodies, uses thereof and conjugates thereof
EP3534949A4 (en) * 2016-11-07 2020-07-22 Seattle Genetics, Inc. DISTRIBUTION OF GENETICALLY MODIFIED CYSTEINE HAIRDRESSES
US11376317B2 (en) 2017-08-30 2022-07-05 University Of Maryland, College Park FcRn-targeted mucosal vaccination against RSV
AU2019235634A1 (en) 2018-03-13 2020-10-22 Zymeworks Bc Inc. Anti-HER2 biparatopic antibody-drug conjugates and methods of use
US11591371B2 (en) 2018-04-02 2023-02-28 University Of Maryland, College Park FcRn-targeted mucosal vaccination against influenza infections
GB201820864D0 (en) * 2018-12-20 2019-02-06 J A Kemp Antibody-drug conjugates
US12109273B2 (en) 2019-02-15 2024-10-08 Wuxi Xdc Singapore Private Limited Process for preparing antibody-drug conjugates with improved homogeneity
CN113423730B (zh) 2019-02-15 2024-01-05 上海药明合联生物技术有限公司 用于制备具有改善的同质性的抗体-药物缀合物的方法
CN115066263A (zh) * 2019-11-18 2022-09-16 克莱奥药品有限公司 定向缀合技术
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GB0316294D0 (en) * 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
US20080305044A1 (en) * 2004-11-29 2008-12-11 Seattle Genetics, Inc. Engineered Antibodies and Immunoconjugates
US20110077383A1 (en) * 2007-07-03 2011-03-31 Medimmune, Llc Hinge domain engineering
TWI640535B (zh) * 2008-01-31 2018-11-11 建南德克公司 抗-ｃｄ７９ｂ抗體及免疫共軛物及使用方法
RU2496521C2 (ru) * 2008-04-24 2013-10-27 Кантаб Байофармасьютикалз Патентс Лимитед Конъюгаты фактора ix с увеличенным временем полужизни
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Also Published As

Publication number Publication date
WO2013190292A3 (en) 2014-03-20
RU2015101333A (ru) 2016-08-10
US20150125473A1 (en) 2015-05-07
HK1204924A1 (en) 2015-12-11
WO2013190292A2 (en) 2013-12-27
IL235646A0 (en) 2015-01-29
IN2014DN10428A (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) 2015-08-21
CA2876365A1 (en) 2013-12-27
MX2014015682A (es) 2015-07-23
CN104379178A (zh) 2015-02-25
EP2861261A2 (en) 2015-04-22
BR112014031613A2 (pt) 2017-07-25
KR20150023027A (ko) 2015-03-04
ZA201408916B (en) 2015-11-25
SG11201407600UA (en) 2014-12-30
JP2015521615A (ja) 2015-07-30

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