ES2964946T3 - Métodos para tratar esclerosis múltiple usando compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton - Google Patents

Métodos para tratar esclerosis múltiple usando compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton Download PDF

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ES2964946T3
ES2964946T3 ES16805251T ES16805251T ES2964946T3 ES 2964946 T3 ES2964946 T3 ES 2964946T3 ES 16805251 T ES16805251 T ES 16805251T ES 16805251 T ES16805251 T ES 16805251T ES 2964946 T3 ES2964946 T3 ES 2964946T3
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compound
multiple sclerosis
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formula
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Tammy Dellovade
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Merck Patent GmbH
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Merck Patent GmbH
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ES16805251T 2015-11-17 2016-11-16 Métodos para tratar esclerosis múltiple usando compuestos de pirimidina con actividad inhibidora de tirosina cinasa de bruton Active ES2964946T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562256199P 2015-11-17 2015-11-17
PCT/US2016/062154 WO2017087445A1 (en) 2015-11-17 2016-11-16 Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity

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ES2964946T3 true ES2964946T3 (es) 2024-04-10

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US (2) US10716788B2 (enExample)
EP (2) EP4295910A3 (enExample)
JP (1) JP6891173B2 (enExample)
KR (1) KR102780243B1 (enExample)
CN (1) CN108884076B (enExample)
AU (1) AU2016357735B2 (enExample)
BR (1) BR112018007517B1 (enExample)
CL (1) CL2018001252A1 (enExample)
DK (1) DK3377484T3 (enExample)
ES (1) ES2964946T3 (enExample)
FI (1) FI3377484T3 (enExample)
HR (1) HRP20231547T1 (enExample)
HU (1) HUE064244T2 (enExample)
IL (1) IL258978B (enExample)
LT (1) LT3377484T (enExample)
MX (1) MX386146B (enExample)
MY (1) MY199473A (enExample)
NZ (1) NZ741294A (enExample)
PH (1) PH12018500736A1 (enExample)
PL (1) PL3377484T3 (enExample)
PT (1) PT3377484T (enExample)
RS (1) RS64908B1 (enExample)
SI (1) SI3377484T1 (enExample)
UA (1) UA123159C2 (enExample)
WO (1) WO2017087445A1 (enExample)
ZA (1) ZA201802348B (enExample)

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TW202510883A (zh) * 2015-11-04 2025-03-16 德商默克專利有限公司 使用具有ｂｔｋ抑制活性之嘧啶及吡啶化合物治療癌症之方法
KR102780243B1 (ko) * 2015-11-17 2025-03-14 메르크 파텐트 게엠베하 Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물을 사용하여 다발성 경화증을 치료하는 방법
EP3810590A1 (en) * 2018-06-19 2021-04-28 Merck Patent GmbH Novel crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain
MX2021000094A (es) * 2018-07-20 2021-03-25 Merck Patent Gmbh Compuesto de amino-pirimidina sustituido para usarse en un metodo para tratamiento y prevencion de esclerosis multiple.
CA3168146A1 (en) 2020-01-20 2021-07-29 Genzyme Corporation Therapeutic tyrosine kinase inhibitors for relapsing multiple sclerosis (rms)
CN112250666B (zh) * 2020-10-09 2022-01-14 广东东阳光药业有限公司 取代的嘧啶类化合物及其用途
JP2023551679A (ja) * 2020-12-02 2023-12-12 テリオス ファーマ， インコーポレイテッド 眼科疾患を治療するための方法及び組成物
CA3201936A1 (en) 2020-12-10 2022-06-16 Minhua Chen Crystal form of tolebrutinib and preparation method thereof
IL303834A (en) 2020-12-23 2023-08-01 Genzyme Corp 4-amino-3-(4-phenoxyphenyl)-1,3-dihydro-2H-imidazo[4,5-C]pyridin-2-one derivatives and their salts
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
US20260000669A1 (en) 2022-06-24 2026-01-01 Merck Patent Gmbh Treatment regimen for autoimmune diseases and inflammatory diseases
WO2024099241A1 (zh) * 2022-11-07 2024-05-16 天津征程医药科技有限公司 氘代的嘧啶衍生物以及包含该化合物的药物组合物
WO2025096900A1 (en) * 2023-11-03 2025-05-08 Board Of Regents, The University Of Texas System Synthetic network materials and methods of making and use thereof
US12414950B1 (en) * 2024-05-21 2025-09-16 Telios Pharma Inc. Methods of treating indolent systemic mastocytosis

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GB0512844D0 (en) * 2005-06-23 2005-08-03 Novartis Ag Organic compounds
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JP2011500823A (ja) * 2007-10-22 2011-01-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Ｐｉ３キナーゼ阻害物質としてのピリドスルホンアミド誘導体
MX2012002641A (es) 2009-09-10 2012-03-14 Hoffmann La Roche Inhibidores de cinasa janus (jak).
KR101301533B1 (ko) 2010-02-09 2013-09-04 한미사이언스 주식회사 암세포 성장 억제 효과를 갖는 신규 피리미딘 유도체
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JP6612751B2 (ja) * 2013-07-31 2019-11-27 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂｔｋの阻害剤としてのピリジン、ピリミジン及びピラジンならびにその使用
KR20160060100A (ko) * 2013-09-22 2016-05-27 칼리토르 사이언시즈, 엘엘씨 치환된 아미노피리미딘 화합물 및 이용 방법
TW202510883A (zh) * 2015-11-04 2025-03-16 德商默克專利有限公司 使用具有ｂｔｋ抑制活性之嘧啶及吡啶化合物治療癌症之方法
KR102780243B1 (ko) * 2015-11-17 2025-03-14 메르크 파텐트 게엠베하 Btk 억제 활성을 갖는 피리미딘 및 피리딘 화합물을 사용하여 다발성 경화증을 치료하는 방법

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MX386146B (es) 2025-03-18
FI3377484T3 (fi) 2023-11-30
HUE064244T2 (hu) 2024-02-28
EP4295910A3 (en) 2024-03-20
PH12018500736A1 (en) 2018-10-01
ZA201802348B (en) 2020-08-26
MY199473A (en) 2023-10-31
EP3377484B1 (en) 2023-09-06
DK3377484T3 (da) 2023-11-27
US10716788B2 (en) 2020-07-21
JP2018538264A (ja) 2018-12-27
BR112018007517A2 (pt) 2018-10-23
IL258978A (en) 2018-07-31
BR112018007517B1 (pt) 2023-09-26
AU2016357735B2 (en) 2021-01-14
US20170136018A1 (en) 2017-05-18
MX2018005463A (es) 2018-08-01
CN108884076B (zh) 2021-07-30
PL3377484T3 (pl) 2024-04-08
RS64908B1 (sr) 2023-12-29
WO2017087445A1 (en) 2017-05-26
IL258978B (en) 2021-04-29
NZ741294A (en) 2023-07-28
CA3002224A1 (en) 2017-05-26
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CN108884076A (zh) 2018-11-23
UA123159C2 (uk) 2021-02-24
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AU2016357735A1 (en) 2018-04-26
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US20200316068A1 (en) 2020-10-08
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PT3377484T (pt) 2023-12-14
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CL2018001252A1 (es) 2018-08-17

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