RU2761344C2 - Введение дейтерированных усилителей cftr - Google Patents

Введение дейтерированных усилителей cftr Download PDF

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RU2761344C2
RU2761344C2 RU2018114447A RU2018114447A RU2761344C2 RU 2761344 C2 RU2761344 C2 RU 2761344C2 RU 2018114447 A RU2018114447 A RU 2018114447A RU 2018114447 A RU2018114447 A RU 2018114447A RU 2761344 C2 RU2761344 C2 RU 2761344C2
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compound
pharmaceutically acceptable
ivacaftor
ctp
acceptable salt
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RU2018114447A
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English (en)
Russian (ru)
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RU2018114447A3 (enExample
RU2018114447A (ru
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Вирджиния БРАМАН
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Вертекс Фармасьютикалз (Юроп) Лимитед
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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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/12—Mucolytics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Pulmonology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
RU2018114447A 2015-09-21 2016-09-21 Введение дейтерированных усилителей cftr RU2761344C2 (ru)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201562221531P 2015-09-21 2015-09-21
US62/221,531 2015-09-21
US201562238511P 2015-10-07 2015-10-07
US62/238,511 2015-10-07
US201662348855P 2016-06-10 2016-06-10
US62/348,855 2016-06-10
PCT/US2016/052922 WO2017053455A1 (en) 2015-09-21 2016-09-21 Administration of deuterated cftr potentiators

Publications (3)

Publication Number Publication Date
RU2018114447A RU2018114447A (ru) 2019-10-23
RU2018114447A3 RU2018114447A3 (enExample) 2020-02-21
RU2761344C2 true RU2761344C2 (ru) 2021-12-07

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RU2018114447A RU2761344C2 (ru) 2015-09-21 2016-09-21 Введение дейтерированных усилителей cftr

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US (2) US20180353500A1 (enExample)
EP (2) EP4292588A3 (enExample)
JP (2) JP6849686B2 (enExample)
KR (1) KR102828163B1 (enExample)
CN (1) CN108367002A (enExample)
AU (2) AU2016326441B2 (enExample)
BR (1) BR112018005454A2 (enExample)
CA (1) CA2998911C (enExample)
HK (1) HK1258472A1 (enExample)
IL (2) IL257993A (enExample)
MA (1) MA42950A (enExample)
MX (1) MX388470B (enExample)
RU (1) RU2761344C2 (enExample)
SG (1) SG10201913588YA (enExample)
UA (1) UA124619C2 (enExample)
WO (1) WO2017053455A1 (enExample)

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* Cited by examiner, † Cited by third party
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US12458635B2 (en) 2008-08-13 2025-11-04 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
HUE047354T2 (hu) 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
EP2819670B1 (en) 2012-02-27 2026-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical Composition and Their Administration
TW202140422A (zh) 2014-10-06 2021-11-01 美商維泰克斯製藥公司 囊腫纖維化症跨膜傳導調節蛋白之調節劑
US10196384B2 (en) 2015-03-31 2019-02-05 Vertex Pharmaceuticals (Europe) Limited Deuterated CFTR modulators
HK1258472A1 (zh) 2015-09-21 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂的施用
HK1258473A1 (zh) 2015-09-25 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂
ES2946970T3 (es) 2016-03-31 2023-07-28 Vertex Pharma Regulador de conductancia transmembrana de moduladores de fibrosis quística
GEP20217329B (en) 2016-09-30 2021-12-10 Vertex Pharma Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
EA202192783A1 (ru) 2016-12-09 2022-02-24 Вертекс Фармасьютикалз Инкорпорейтед Модулятор регулятора трансмембранной проводимости при муковисцидозе, фармацевтические композиции, способы лечения и способ получения указанного модулятора
MA54105A (fr) 2017-06-08 2021-09-15 Vertex Pharma Méthodes de traitement de la fibrose kystique
IL272032B2 (en) 2017-07-17 2026-04-01 Vertex Pharma Combination therapy for the treatment of cystic fibrosis including N-(1,3-DIMETHYLPYRAZOL-4-YL)SULFONYL-6-[3-(3,3,3-TRIFLUORO-2,2- DIMETHYL-PROPOXY)PYRAZOL-1-YL]-2-[(4S)-2,2,4- TRIMETHYLPYRROLIDIN-1-YL]PYRIDINE-3-CARBOXAMIDE and
CA3069225A1 (en) * 2017-07-17 2019-01-24 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
MA49752A (fr) 2017-08-02 2021-04-21 Vertex Pharma Procédés de préparation de composés de pyrrolidine
CA3078893A1 (en) 2017-10-19 2019-04-25 Vertex Pharmaceuticals Incorporated Crystalline forms and compositions of cftr modulators
WO2019109021A1 (en) 2017-12-01 2019-06-06 Vertex Pharmaceuticals Incorporated Processes for making modulators of cystic fibrosis transmembrane conductance regulator
KR102716244B1 (ko) 2017-12-08 2024-10-14 버텍스 파마슈티칼스 인코포레이티드 낭포성 섬유증 막횡단 전도 조절자의 조정제의 제조 방법
TWI810243B (zh) 2018-02-05 2023-08-01 美商維泰克斯製藥公司 用於治療囊腫纖化症之醫藥組合物
RS64018B1 (sr) 2018-02-15 2023-03-31 Vertex Pharma Makrocikli kao modulatori transmembranskog regulatora provodnosti cistične fibroze, njihove farmaceutske kompozicije, njihova upotreba u lečenju cistične fibroze i proces njihove izrade
WO2019200246A1 (en) 2018-04-13 2019-10-17 Alexander Russell Abela Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
MA54227B1 (fr) 2018-11-14 2023-03-31 Vertex Pharma Méthodes de traitement de la fibrose kystique
TWI848092B (zh) 2019-04-03 2024-07-11 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白調節劑
WO2020214921A1 (en) 2019-04-17 2020-10-22 Vertex Pharmaceuticals Incorporated Solid forms of modulators of cftr
FR3096890B1 (fr) 2019-06-07 2021-05-14 H4 Orphan Pharma Utilisation d’une molécule opioïde pour traiter l’œil sec et l’œil allergique.
TWI867024B (zh) 2019-08-14 2024-12-21 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
WO2021030556A1 (en) 2019-08-14 2021-02-18 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
TWI899097B (zh) 2019-08-14 2025-10-01 美商維泰克斯製藥公司 製備cftr調節劑之方法
US11873300B2 (en) 2019-08-14 2024-01-16 Vertex Pharmaceuticals Incorporated Crystalline forms of CFTR modulators
FR3109524B1 (fr) 2020-04-22 2022-04-08 H4 Orphan Pharma Utilisation d’un ligand multifonctionnel pour traiter l’œil sec et les dysfonctionnements des glandes de Meibomius et des glandes lacrymales.
FR3111071B1 (fr) 2020-06-04 2023-01-13 H4 Orphan Pharma Utilisation de ligands multifonctionnels pour traiter les syndromes de détresse respiratoire et le choc cytokinique liés aux infections virales à coronavirus.
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
WO2022036060A1 (en) 2020-08-13 2022-02-17 Vertex Pharmaceuticals Incorporated Crystalline forms of cftr modulators
TW202233635A (zh) 2020-10-07 2022-09-01 美商維泰克斯製藥公司 囊腫纖維化跨膜傳導調節蛋白之調節劑
WO2022076627A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
BR112023006470A2 (pt) 2020-10-07 2023-09-26 Vertex Pharma Moduladores de regulador de condutância transmembrana de fibrose cística
WO2022076628A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US20230382924A1 (en) 2020-10-07 2023-11-30 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023004072A (es) 2020-10-07 2023-07-05 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica.
US20230373974A1 (en) 2020-10-07 2023-11-23 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
WO2022076626A1 (en) 2020-10-07 2022-04-14 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US12612416B2 (en) 2020-10-07 2026-04-28 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator
MX2023006770A (es) 2020-12-10 2023-08-14 Vertex Pharma Metodos de tratamiento para fibrosis quistica.
CN119095597A (zh) 2022-02-03 2024-12-06 弗特克斯药品有限公司 治疗囊性纤维化的方法
CA3251045A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated MODULATORS OF THE TRANSMEMBRANE CONDUCTANCE REGULATOR IN CYSTIC FIBROSIS
PE20250606A1 (es) 2022-04-06 2025-02-26 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica
AU2023273614A1 (en) 2022-05-16 2024-11-07 Vertex Pharmaceuticals Incorporated Methods of treatment for cystic fibrosis
IL327468A (en) 2023-10-04 2026-05-01 Vertex Pharma Solid forms of cystic fibrosis transmembrane conductance regulator
CN122374316A (zh) 2023-10-04 2026-07-10 弗特克斯药品有限公司 囊性纤维化跨膜传导调控因子的调节剂
WO2025166342A1 (en) 2024-02-04 2025-08-07 Vertex Pharmaceuticals Incorporated Combination of vanzacaftor, tezacaftor, deutivacaftor for use in treating cystic fibrosis
ES3069804T3 (en) 2024-02-07 2026-06-10 Vertex Pharma Compositions for the treatment of cftr-mediated diseases

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HUE047354T2 (hu) * 2011-05-18 2020-04-28 Vertex Pharmaceuticals Europe Ltd Ivacaftor deuterizált származékai
EP2819670B1 (en) 2012-02-27 2026-05-20 Vertex Pharmaceuticals Incorporated Pharmaceutical Composition and Their Administration
CN109364075B (zh) * 2012-11-21 2021-10-29 顶点制药（欧洲）有限公司 氘化cftr增效剂
US20140221424A1 (en) * 2013-01-30 2014-08-07 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions for use in the treatment of cystic fibrosis
HK1258472A1 (zh) 2015-09-21 2019-11-15 Vertex Pharmaceuticals (Europe) Limited 氘代cftr增效剂的施用

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201391615A1 (ru) * 2011-05-18 2014-03-31 Консерт Фармасъютиклс, Инк. Дейтерированные потенциаторы cftr
WO2014078842A1 (en) * 2012-11-19 2014-05-22 Concert Pharmaceuticals, Inc. Deuterated cftr potentiators

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IL257993A (en) 2018-05-31
EP3352757A1 (en) 2018-08-01
MX2018003331A (es) 2018-08-16
KR20180058745A (ko) 2018-06-01
US20200375973A1 (en) 2020-12-03
AU2016326441B2 (en) 2021-11-25
JP7196217B2 (ja) 2022-12-26
CA2998911A1 (en) 2017-03-30
JP2018534348A (ja) 2018-11-22
CA2998911C (en) 2023-05-23
CN108367002A (zh) 2018-08-03
EP4292588A2 (en) 2023-12-20
MX388470B (es) 2025-03-20
WO2017053455A1 (en) 2017-03-30
AU2022201135A1 (en) 2022-03-17
EP3352757C0 (en) 2023-08-16
HK1258472A1 (zh) 2019-11-15
EP3352757A4 (en) 2018-08-01
BR112018005454A2 (pt) 2018-10-09
NZ741069A (en) 2024-12-20
MA42950A (fr) 2018-08-01
AU2016326441A1 (en) 2018-04-19
AU2022201135B2 (en) 2024-03-28
JP6849686B2 (ja) 2021-03-24
SG10201913588YA (en) 2020-02-27
KR102828163B1 (ko) 2025-07-02
RU2018114447A3 (enExample) 2020-02-21
RU2018114447A (ru) 2019-10-23
US20180353500A1 (en) 2018-12-13
UA124619C2 (uk) 2021-10-20
EP4292588A3 (en) 2024-02-28
EP3352757B1 (en) 2023-08-16
IL291517A (en) 2022-05-01
JP2021091723A (ja) 2021-06-17

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