ES2651165T3 - 2-aminopirimidin-6-onas y análogos que presentan actividades anti-cáncer y antiproliferativa - Google Patents

2-aminopirimidin-6-onas y análogos que presentan actividades anti-cáncer y antiproliferativa Download PDF

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Publication number
ES2651165T3
ES2651165T3 ES14764032.0T ES14764032T ES2651165T3 ES 2651165 T3 ES2651165 T3 ES 2651165T3 ES 14764032 T ES14764032 T ES 14764032T ES 2651165 T3 ES2651165 T3 ES 2651165T3
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alkyl
formula
optionally substituted
partially
hydrogen
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Spanish (es)
Inventor
Michael D. Kaufman
Daniel L Flynn
Yu Mi Ahn
Lakshminarayana Vogeti
Timothy Malcolm CALDWELL
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Deciphera Pharmaceuticals LLC
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Deciphera Pharmaceuticals LLC
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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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
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    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Otolaryngology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
ES14764032.0T 2013-03-15 2014-03-14 2-aminopirimidin-6-onas y análogos que presentan actividades anti-cáncer y antiproliferativa Active ES2651165T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361792812P 2013-03-15 2013-03-15
US201361792812P 2013-03-15
PCT/US2014/029661 WO2014145025A2 (en) 2013-03-15 2014-03-14 2-aminopyrimidin-6-ones and analogs exhibiting anti-cancer and anti-proliferative activities

Publications (1)

Publication Number Publication Date
ES2651165T3 true ES2651165T3 (es) 2018-01-24

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ES14764032.0T Active ES2651165T3 (es) 2013-03-15 2014-03-14 2-aminopirimidin-6-onas y análogos que presentan actividades anti-cáncer y antiproliferativa

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Country Link
US (1) US9181223B2 (https=)
EP (1) EP2968286B1 (https=)
JP (6) JP6165314B2 (https=)
KR (5) KR20260042557A (https=)
CN (2) CN105120864B (https=)
AU (5) AU2014233411B2 (https=)
BR (1) BR112015022288B1 (https=)
CA (1) CA2903285C (https=)
DK (1) DK2968286T3 (https=)
ES (1) ES2651165T3 (https=)
FR (1) FR26C1012I1 (https=)
IL (4) IL241000B (https=)
MX (1) MX365574B (https=)
NL (1) NL301373I2 (https=)
PH (1) PH12015502114B1 (https=)
PT (1) PT2968286T (https=)
RU (1) RU2015143717A (https=)
SG (1) SG11201507660TA (https=)
WO (1) WO2014145025A2 (https=)

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AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
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JP7131837B2 (ja) * 2017-06-19 2022-09-06 アビスコ セラピューティクス カンパニー リミテッド Csf-1r阻害活性を有するアザアリール誘導体、その製造方法および応用
CN118416236A (zh) 2018-01-31 2024-08-02 德西费拉制药有限责任公司 治疗胃肠道间质瘤的组合疗法
IL276398B2 (en) 2018-01-31 2026-03-01 Deciphera Pharmaceuticals Llc Combination therapy for mastocytosis
CN110845476B (zh) * 2018-08-21 2022-11-18 上海和誉生物医药科技有限公司 一种高选择性csf1r抑制剂、其制备方法和在药学上的应用
BR112021012812A2 (pt) 2018-12-28 2021-12-07 Deciphera Pharmaceuticals Llc Csf1r inhibitors para uso e tratamento de câncer
WO2020185812A1 (en) 2019-03-11 2020-09-17 Teva Pharmaceuticals International Gmbh Solid state forms of ripretinib
US11518758B2 (en) 2019-05-10 2022-12-06 Deciphera Pharmaceuticals, Llc Heteroarylaminopyrimidine amide autophagy inhibitors and methods of use thereof
PE20220597A1 (es) 2019-05-10 2022-04-22 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de fenilaminopirimidina amida y metodos de uso de estos
PE20221083A1 (es) 2019-06-17 2022-07-05 Deciphera Pharmaceuticals Llc Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso
TWI878335B (zh) 2019-08-12 2025-04-01 美商迪賽孚爾製藥有限公司 治療胃腸道基質瘤方法
EP4013412B1 (en) 2019-08-12 2026-01-28 Deciphera Pharmaceuticals, LLC Ripretinib for treating gastrointestinal stromal tumors
MX2022008103A (es) 2019-12-30 2022-09-19 Deciphera Pharmaceuticals Llc Formulaciones de inhibidores de la cinasa amorfa y metodos de estas.
EP4084779B1 (en) 2019-12-30 2024-10-09 Deciphera Pharmaceuticals, LLC Compositions of 1-(4-bromo-5-(1-ethyl-7-(methylamino)-2-oxo-1,2-dihydro-1,6-naphthyridin-3-yl)-2-fluorophenyl)-3-phenylurea
IL302807A (en) 2020-11-18 2023-07-01 Deciphera Pharmaceuticals Llc Gcn2 and perk kinase inhibitors and methods of use thereof
CN115385896B (zh) * 2021-05-24 2024-11-15 上海和誉生物医药科技有限公司 一种csf-1r抑制剂中间体或其酸式盐的制备方法
CN113880812A (zh) * 2021-11-17 2022-01-04 上海皓元生物医药科技有限公司 一种csf-ir抑制剂的制备方法
PE20250609A1 (es) 2021-12-03 2025-02-26 Deciphera Pharmaceuticals Llc Inhibidores de gcn2 y perk quinasa y metodos de uso de los mismos
CA3240263A1 (en) 2021-12-09 2023-06-15 Daniel L. Flynn Raf kinase inhibitors and methods of use thereof
WO2023125812A1 (zh) * 2021-12-31 2023-07-06 上海海雁医药科技有限公司 取代的嘧啶酮衍生物、其药物组合物及医药上的用途
US11779572B1 (en) 2022-09-02 2023-10-10 Deciphera Pharmaceuticals, Llc Methods of treating gastrointestinal stromal tumors
CN117624132B (zh) * 2023-11-28 2026-04-21 上海相辉医药科技有限公司 一种CSF-1R激酶抑制剂Vimseltinib(DCC-3014)的制备方法
WO2025122952A1 (en) * 2023-12-08 2025-06-12 Deciphera Pharmaceuticals, Llc Formulations of vimseltinib
US20250206720A1 (en) * 2023-12-08 2025-06-26 Deciphera Pharmaceuticals, Llc Solid forms of an ulk inhibitor
WO2025231106A1 (en) * 2024-05-01 2025-11-06 Deciphera Pharmaceuticals, Llc Csf-1r inhibitors and methods of use thereof

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WO2008046216A1 (en) * 2006-10-18 2008-04-24 Methylgene, Inc. Kinase inhibitors and uses thereof
AU2007338792B2 (en) * 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
JP5444365B2 (ja) * 2008-10-29 2014-03-19 デシフェラ ファーマシューティカルズ,エルエルシー 抗癌活性および抗増殖活性を示すシクロプロパンアミドおよび類似物質
WO2014145023A1 (en) * 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc 1,2,4-triazol-5-ones and analogs exhibiting anti-cancer and anti-proliferative activities
DK2968286T3 (en) * 2013-03-15 2018-01-02 Deciphera Pharmaceuticals Llc 2-AMINOPYRIMIDIN-6-ONES AND ANALOGS THAT HAVE ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
WO2014145015A2 (en) * 2013-03-15 2014-09-18 Deciphera Pharmaceuticals, Llc Imidazolidinones and analogs exhibiting anti-cancer and anti-proliferative activities

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JP2019094350A (ja) 2019-06-20
AU2014233411B2 (en) 2018-09-13
IL241000B (en) 2018-07-31
BR112015022288A2 (pt) 2017-12-19
KR102293086B1 (ko) 2021-08-25
CN107311981A (zh) 2017-11-03
AU2022204166C1 (en) 2024-06-20
WO2014145025A3 (en) 2015-01-08
EP2968286B1 (en) 2017-09-13
EP2968286A2 (en) 2016-01-20
FR26C1012I1 (fr) 2026-04-24
AU2018271293A1 (en) 2018-12-20
JP7169412B2 (ja) 2022-11-10
AU2022204166A1 (en) 2022-06-30
IL275422A (en) 2020-08-31
IL241000A0 (en) 2015-11-30
JP6165314B2 (ja) 2017-07-19
JP6936823B2 (ja) 2021-09-22
IL289629A (en) 2022-03-01
PH12015502114A1 (en) 2016-01-25
KR20260042557A (ko) 2026-03-31
JP2017193567A (ja) 2017-10-26
KR102399891B1 (ko) 2022-05-20
US9181223B2 (en) 2015-11-10
AU2022204166B2 (en) 2024-02-15
CA2903285A1 (en) 2014-09-18
AU2020205294B2 (en) 2022-03-17
IL289629B1 (en) 2023-04-01
NL301373I2 (nl) 2026-03-30
HK1220398A1 (en) 2017-05-05
JP2024105360A (ja) 2024-08-06
KR20240013846A (ko) 2024-01-30
BR112015022288B1 (pt) 2022-06-21
RU2015143717A3 (https=) 2018-03-28
KR20210107143A (ko) 2021-08-31
AU2020205294A1 (en) 2020-08-06
AU2014233411A1 (en) 2015-09-17
MX365574B (es) 2019-06-06
IL260502B (en) 2020-07-30
PH12015502114B1 (en) 2018-06-29
MX2015012736A (es) 2016-05-31
EP2968286A4 (en) 2016-09-14
KR102628583B1 (ko) 2024-01-25
JP7536064B2 (ja) 2024-08-19
AU2024202088A1 (en) 2024-05-02
JP2016521255A (ja) 2016-07-21
JP2023010738A (ja) 2023-01-20
CA2903285C (en) 2021-05-11
AU2018271293B2 (en) 2020-04-16
CN105120864A (zh) 2015-12-02
CN107311981B (zh) 2020-05-29
KR20220070054A (ko) 2022-05-27
JP2021191770A (ja) 2021-12-16
US20140275085A1 (en) 2014-09-18
CN105120864B (zh) 2017-05-17
IL289629B2 (en) 2023-08-01
PT2968286T (pt) 2017-12-12
SG11201507660TA (en) 2015-10-29
KR20150128996A (ko) 2015-11-18
DK2968286T3 (en) 2018-01-02
WO2014145025A2 (en) 2014-09-18
RU2015143717A (ru) 2017-04-28
IL275422B (en) 2022-02-01

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