EA032203B1 - Производные тубулизина - Google Patents

Производные тубулизина Download PDF

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Publication number
EA032203B1
EA032203B1 EA201691963A EA201691963A EA032203B1 EA 032203 B1 EA032203 B1 EA 032203B1 EA 201691963 A EA201691963 A EA 201691963A EA 201691963 A EA201691963 A EA 201691963A EA 032203 B1 EA032203 B1 EA 032203B1
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EA
Eurasian Patent Office
Prior art keywords
cancer
mmol
resin
antibody
mixture
Prior art date
Application number
EA201691963A
Other languages
English (en)
Russian (ru)
Other versions
EA201691963A1 (ru
Inventor
Лакшмаях Гинджипалли
Дорин Тоадер
Фэнцзян Ван
Original Assignee
МЕДИММЬЮН ЭлЭлСи
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.)
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Publication date
Application filed by МЕДИММЬЮН ЭлЭлСи filed Critical МЕДИММЬЮН ЭлЭлСи
Publication of EA201691963A1 publication Critical patent/EA201691963A1/ru
Publication of EA032203B1 publication Critical patent/EA032203B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • A61K47/6829Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/30Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0212Peptides 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal 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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
EA201691963A 2014-04-11 2015-04-10 Производные тубулизина EA032203B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461978460P 2014-04-11 2014-04-11
PCT/US2015/025235 WO2015157594A1 (en) 2014-04-11 2015-04-10 Tubulysin derivatives

Publications (2)

Publication Number Publication Date
EA201691963A1 EA201691963A1 (ru) 2017-06-30
EA032203B1 true EA032203B1 (ru) 2019-04-30

Family

ID=54264545

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201691963A EA032203B1 (ru) 2014-04-11 2015-04-10 Производные тубулизина

Country Status (19)

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

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW201542594A (zh) 2014-04-11 2015-11-16 Medimmune Llc 雙特異性her2抗體
SG11201608203RA (en) 2014-04-11 2016-10-28 Medimmune Llc Tubulysin derivatives
SG11201706820RA (en) * 2015-02-25 2017-09-28 Univ Rice William M Desacetoxytubulysin h and analogs thereof
CA3003468C (en) 2015-11-10 2024-06-18 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
WO2017180813A1 (en) 2016-04-15 2017-10-19 Macrogenics, Inc. Novel b7-h3 binding molecules, antibody drug conjugates thereof and methods of use thereof
US20200023072A1 (en) 2016-10-11 2020-01-23 Medimmune Limited Antibody-drug conjugates with immune-mediated therapy agents
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
US11998584B2 (en) * 2017-12-31 2024-06-04 Hangzhou Dac Biotech Co., Ltd. Conjugate of a tubulysin analog with branched linkers
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
KR20210106467A (ko) 2018-12-21 2021-08-30 리제너론 파마슈티칼스 인코포레이티드 튜불리신 및 단백질-튜불리신 접합체
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
BR112021026142A2 (pt) * 2019-06-24 2022-02-08 Hangzhou Dac Biotech Co Ltd Composto conjugado ligado à cadeia lateral da fórmula, célula de tumor, composição farmacêutica, agente quimioterapêutico, e, agentes sinergísticos
CA3185601A1 (en) * 2020-06-24 2021-12-30 Regeneron Pharmaceuticals, Inc. Tubulysins and protein-tubulysin conjugates
AR123480A1 (es) 2020-09-11 2022-12-07 Medimmune Ltd Moléculas de unión terapéuticas
JP2024544520A (ja) 2021-11-10 2024-12-03 アストラゼネカ・アクチエボラーグ 抗体分子及び複合体
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
IL317733A (en) 2022-06-27 2025-02-01 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for cancer treatment
WO2025078841A2 (en) 2023-10-11 2025-04-17 Antikor Biopharma Limited Antibodies, conjugates, and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060148014A1 (en) * 2004-12-09 2006-07-06 Sergei Agoulnik Tubulin isotype screening in cancer therapy using hemiasterlin analogs
US20080108820A1 (en) * 2002-03-22 2008-05-08 Campagna Silvio A Hemiasterlin Derivatives and Uses Thereof
US20130129753A1 (en) * 2011-11-17 2013-05-23 Pfizer Inc. Cytotoxic peptides and antibody drug conjugates thereof
US20130197259A1 (en) * 2009-08-03 2013-08-01 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1394860B1 (it) * 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
IN2014CN04961A (enExample) * 2011-12-05 2015-09-18 Igenica Biotherapeutics Inc
ES2628156T3 (es) * 2013-02-14 2017-08-01 Bristol-Myers Squibb Company Compuestos de tubulisina, métodos para su fabricación y su uso
SG11201608203RA (en) * 2014-04-11 2016-10-28 Medimmune Llc Tubulysin derivatives
WO2015155345A1 (en) * 2014-04-11 2015-10-15 Medimmune Limited Antibodies and antibody-drug conjugates
TW201542594A (zh) * 2014-04-11 2015-11-16 Medimmune Llc 雙特異性her2抗體

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080108820A1 (en) * 2002-03-22 2008-05-08 Campagna Silvio A Hemiasterlin Derivatives and Uses Thereof
US20060148014A1 (en) * 2004-12-09 2006-07-06 Sergei Agoulnik Tubulin isotype screening in cancer therapy using hemiasterlin analogs
US20130197259A1 (en) * 2009-08-03 2013-08-01 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
US20130129753A1 (en) * 2011-11-17 2013-05-23 Pfizer Inc. Cytotoxic peptides and antibody drug conjugates thereof

Also Published As

Publication number Publication date
KR20160142392A (ko) 2016-12-12
JP2017510661A (ja) 2017-04-13
CN106458942A (zh) 2017-02-22
TW201625662A (zh) 2016-07-16
US9427479B2 (en) 2016-08-30
EA201691963A1 (ru) 2017-06-30
IL247822A0 (en) 2016-11-30
AR100006A1 (es) 2016-08-31
US20150291657A1 (en) 2015-10-15
EP3129362A4 (en) 2017-08-23
AU2015243379A1 (en) 2016-11-03
UY36075A (es) 2015-10-30
MA39862A (fr) 2017-02-15
SG11201608203RA (en) 2016-10-28
PH12016501995A1 (en) 2017-01-09
US20160339114A1 (en) 2016-11-24
MX2016013373A (es) 2017-05-02
WO2015157594A1 (en) 2015-10-15
US10159745B2 (en) 2018-12-25
AU2015243379B2 (en) 2018-02-01
NZ725131A (en) 2018-03-23
CL2016002548A1 (es) 2017-02-24
CA2945318A1 (en) 2015-10-15
EP3129362A1 (en) 2017-02-15

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