MA39862A - Dérivés de tubulysine - Google Patents

Dérivés de tubulysine

Info

Publication number
MA39862A
MA39862A MA039862A MA39862A MA39862A MA 39862 A MA39862 A MA 39862A MA 039862 A MA039862 A MA 039862A MA 39862 A MA39862 A MA 39862A MA 39862 A MA39862 A MA 39862A
Authority
MA
Morocco
Prior art keywords
tubulysin
derivatives
tubulysin derivatives
conjugates
cancers
Prior art date
Application number
MA039862A
Other languages
English (en)
Inventor
Lakshmaiah Gingipalli
Dorin Toader
Fengjiang Wang
Original Assignee
Lakshmaiah Gingipalli
Medimmune Llc
Dorin Toader
Fengjiang Wang
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
Application filed by Lakshmaiah Gingipalli, Medimmune Llc, Dorin Toader, Fengjiang Wang filed Critical Lakshmaiah Gingipalli
Publication of MA39862A publication Critical patent/MA39862A/fr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K38/05—Dipeptides
    • 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
    • A61K38/07—Tetrapeptides
    • 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
    • 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
    • A61K47/6801—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
    • A61K47/6817—Toxins
    • A61K47/6829—Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0212—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -N-C-N-C(=0)-, e.g. retro-inverso peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cell Biology (AREA)
  • Toxicology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention concerne de nouveaux dérivés de tubulysine qui peuvent être utiles en tant qu'agents cytotoxiques pour conférer des avantages thérapeutiques dans le traitement de divers types de cancers, seuls ou sous forme de conjugués de médicaments avec des anticorps. Les dérivés de tubulysine sont constitués d'un échafaudage tétrapeptidique comprenant des pipéridines substituées par des groupes méthyle et éthyle. Les conjugués de tubulysine comprennent en outre des anticorps monoclonaux liés par l'intermédiaire de lieurs succinimide.
MA039862A 2014-04-11 2015-04-10 Dérivés de tubulysine MA39862A (fr)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461978460P 2014-04-11 2014-04-11

Publications (1)

Publication Number Publication Date
MA39862A true MA39862A (fr) 2017-02-15

Family

ID=54264545

Family Applications (1)

Application Number Title Priority Date Filing Date
MA039862A MA39862A (fr) 2014-04-11 2015-04-10 Dérivés de tubulysine

Country Status (19)

Country Link
US (2) US9427479B2 (fr)
EP (1) EP3129362A4 (fr)
JP (1) JP2017510661A (fr)
KR (1) KR20160142392A (fr)
CN (1) CN106458942A (fr)
AR (1) AR100006A1 (fr)
AU (1) AU2015243379B2 (fr)
CA (1) CA2945318A1 (fr)
CL (1) CL2016002548A1 (fr)
EA (1) EA032203B1 (fr)
IL (1) IL247822A0 (fr)
MA (1) MA39862A (fr)
MX (1) MX2016013373A (fr)
NZ (1) NZ725131A (fr)
PH (1) PH12016501995A1 (fr)
SG (1) SG11201608203RA (fr)
TW (1) TW201625662A (fr)
UY (1) UY36075A (fr)
WO (1) WO2015157594A1 (fr)

Families Citing this family (21)

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Publication number Priority date Publication date Assignee Title
KR20160142392A (ko) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 튜부리신 유도체
ES2819863T3 (es) 2014-04-11 2021-04-19 Medimmune Llc Anticuerpos contra HER2 biespecíficos
KR20170137725A (ko) 2015-02-25 2017-12-13 윌리엄 마쉬 라이스 유니버시티 데스아세톡시투불리신 h 및 이의 유사체
SG10202103712VA (en) 2015-11-10 2021-05-28 Medimmune Llc Binding molecules specific for asct2 and uses thereof
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
US10723727B2 (en) * 2016-02-01 2020-07-28 Pfizer Inc. Tubulysin analogs and methods for their preparation
TWI781098B (zh) 2016-04-15 2022-10-21 美商宏觀基因股份有限公司 新穎的ｂ７-ｈ３-結合分子、其抗體藥物綴合物及其使用方法
JP2019534882A (ja) 2016-10-11 2019-12-05 メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ 免疫介在性療法薬を有する抗体−薬物コンジュゲート
JP7150820B2 (ja) 2017-08-01 2022-10-11 メディミューン，エルエルシー Ｂｃｍａモノクローナル抗体薬剤コンジュゲート
MX2020006192A (es) * 2017-12-31 2020-08-20 Hangzhou Dac Biotech Co Ltd Un conjugado de un analogo de tubulisina con enlazadores ramificados.
CN109456212A (zh) * 2018-12-03 2019-03-12 康化（上海）新药研发有限公司 一种沙库比曲中间体的合成方法
MY208067A (en) 2018-12-21 2025-04-11 Regeneron Pharma Tubulysins and protein-tubulysin conjugates
TWI753252B (zh) * 2019-05-03 2022-01-21 中國大陸商杭州多禧生物科技有限公司 含支鏈連接體的Ｔｕｂｕｌｙｓｉｎ同系物偶聯物
MX2021015887A (es) * 2019-06-24 2022-03-22 Hangzhou Dac Biotech Co Ltd Un conjugado de un agente citotóxico y una molécula de unión a células con enlazadores ramificados.
CN115867563B (zh) * 2020-06-24 2025-06-27 里珍纳龙药品有限公司 微管溶素及蛋白质-微管溶素偶联物
US11795225B2 (en) 2020-09-11 2023-10-24 Medimmune Limited Therapeutic binding molecules
EP4429765A1 (fr) 2021-11-10 2024-09-18 Astrazeneca AB Molécules d'anticorps et conjugués
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
MA71241A (fr) 2022-06-27 2025-04-30 Astrazeneca Ab Combinaisons impliquant des inhibiteurs de tyrosine kinase du récepteur du facteur de croissance épidermique pour traiter le cancer
WO2025078841A2 (fr) 2023-10-11 2025-04-17 Antikor Biopharma Limited Anticorps, conjugués et leurs utilisations

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Publication number Priority date Publication date Assignee Title
US7064211B2 (en) * 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
WO2006063135A2 (fr) * 2004-12-09 2006-06-15 Eisai R & D Management Co., Ltd. Criblage d'isotype de tubuline en therapie du cancer, au moyen d'analogues d'hemiasterline
IT1394860B1 (it) * 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) * 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
CN104185477B (zh) * 2011-11-17 2017-05-24 辉瑞公司 细胞毒性肽及其抗体‑药物缀合物
MX2014006739A (es) * 2011-12-05 2015-06-05 Igenica Biotherapeutics Inc Conjugados de anticuerpo-farmaco y compuestos relacionados, composiciones , y metodos.
SI2956173T1 (sl) * 2013-02-14 2017-06-30 Bristol-Myers Squibb Company Spojine tubulizina, postopki pridobivanja in uporaba
WO2015155345A1 (fr) * 2014-04-11 2015-10-15 Medimmune Limited Anticorps et conjugués anticorps-médicament
ES2819863T3 (es) * 2014-04-11 2021-04-19 Medimmune Llc Anticuerpos contra HER2 biespecíficos
KR20160142392A (ko) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 튜부리신 유도체

Also Published As

Publication number Publication date
US9427479B2 (en) 2016-08-30
JP2017510661A (ja) 2017-04-13
AR100006A1 (es) 2016-08-31
CL2016002548A1 (es) 2017-02-24
PH12016501995A1 (en) 2017-01-09
EP3129362A1 (fr) 2017-02-15
UY36075A (es) 2015-10-30
CA2945318A1 (fr) 2015-10-15
US20150291657A1 (en) 2015-10-15
TW201625662A (zh) 2016-07-16
WO2015157594A1 (fr) 2015-10-15
US20160339114A1 (en) 2016-11-24
SG11201608203RA (en) 2016-10-28
CN106458942A (zh) 2017-02-22
EA032203B1 (ru) 2019-04-30
AU2015243379A1 (en) 2016-11-03
IL247822A0 (en) 2016-11-30
EP3129362A4 (fr) 2017-08-23
KR20160142392A (ko) 2016-12-12
MX2016013373A (es) 2017-05-02
US10159745B2 (en) 2018-12-25
EA201691963A1 (ru) 2017-06-30
NZ725131A (en) 2018-03-23
AU2015243379B2 (en) 2018-02-01

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