JP7754623B2 - mPGES-1阻害剤としての化合物 - Google Patents

mPGES-1阻害剤としての化合物

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Publication number
JP7754623B2
JP7754623B2 JP2020526121A JP2020526121A JP7754623B2 JP 7754623 B2 JP7754623 B2 JP 7754623B2 JP 2020526121 A JP2020526121 A JP 2020526121A JP 2020526121 A JP2020526121 A JP 2020526121A JP 7754623 B2 JP7754623 B2 JP 7754623B2
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Prior art keywords
compound
mpges
configuration
linker
compounds
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JP2020526121A
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English (en)
Japanese (ja)
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JP2021504307A (ja
Inventor
ヨハネス アルベルトゥス マリア スメイティンク,
ジュリアン デーヴィッド ベイラス,
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Khondrion IP BV
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Khondrion IP BV
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Priority to JP2023147032A priority Critical patent/JP2024009799A/ja
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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
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/66Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 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 in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A61K31/355Tocopherols, e.g. vitamin E
    • 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/4462Non condensed piperidines, e.g. piperocaine only substituted in position 3
    • 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
    • A61K31/4468Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • 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
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/56Nitrogen atoms
    • 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
    • C07D405/02Heterocyclic 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 two hetero rings
    • C07D405/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2020526121A 2017-11-22 2018-11-22 mPGES-1阻害剤としての化合物 Active JP7754623B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023147032A JP2024009799A (ja) 2017-11-22 2023-09-11 mPGES-1阻害剤としての化合物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP17203033.0 2017-11-22
EP17203033 2017-11-22
PCT/EP2018/082146 WO2019101826A1 (en) 2017-11-22 2018-11-22 Compounds as mpges-1 inhibitors

Related Child Applications (1)

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JP2023147032A Division JP2024009799A (ja) 2017-11-22 2023-09-11 mPGES-1阻害剤としての化合物

Publications (2)

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JP2021504307A JP2021504307A (ja) 2021-02-15
JP7754623B2 true JP7754623B2 (ja) 2025-10-15

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JP2020526121A Active JP7754623B2 (ja) 2017-11-22 2018-11-22 mPGES-1阻害剤としての化合物
JP2023147032A Pending JP2024009799A (ja) 2017-11-22 2023-09-11 mPGES-1阻害剤としての化合物

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Country Status (16)

Country Link
US (1) US11672787B2 (enExample)
EP (1) EP3713564B1 (enExample)
JP (2) JP7754623B2 (enExample)
KR (2) KR20250109241A (enExample)
CN (1) CN111417393A (enExample)
AU (1) AU2018371153B2 (enExample)
BR (1) BR112020010089A2 (enExample)
CA (1) CA3079483A1 (enExample)
ES (1) ES2963906T3 (enExample)
IL (1) IL274821A (enExample)
MX (1) MX2020005238A (enExample)
MY (1) MY207603A (enExample)
PL (1) PL3713564T3 (enExample)
SG (1) SG11202003743SA (enExample)
WO (1) WO2019101826A1 (enExample)
ZA (1) ZA202002103B (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3058033A1 (en) * 2017-04-05 2018-10-11 Khondrion Ip B.V. Treatment of mitochondrial diseases
NL2024431B1 (en) * 2019-12-11 2021-09-07 Sulfateq Bv Compounds for treatment of alzheimer’s disease
NL2025730B1 (en) * 2020-06-02 2022-01-20 Sulfateq Bv Compounds for treatment of sepsis
WO2025242849A1 (en) * 2024-05-24 2025-11-27 Khondrion Ip B.V. Chromanyl derivatives for use in the treatment of bone disorders

Citations (5)

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Publication number Priority date Publication date Assignee Title
JP2011503005A (ja) 2007-11-06 2011-01-27 エジソン ファーマシューティカルズ, インコーポレイテッド ミトコンドリア病を治療するための4−(p−キノリル)−2−ヒドロキシブタンアミド誘導体
JP2015522067A (ja) 2012-07-12 2015-08-03 コンドリオン アイピー ビー.ブイ.Khondrion Ip B.V. ミトコンドリア病を治療するためのクロマニル誘導体
JP2016511743A (ja) 2012-12-19 2016-04-21 スルファテック・ベスローテン・フェンノートシャップSulfateq B.V. 細胞保護のための化合物
WO2017060432A1 (en) 2015-10-08 2017-04-13 Khondrion Ip B.V. Novel compounds for treating mitochondrial disease
JP2017524674A (ja) 2014-06-17 2017-08-31 スルファテック・ベスローテン・フェンノートシャップSulfateq B.V. 慢性閉塞性気道疾患の治療のための6−ヒドロキシ−2,5,7,8−テトラメチルクロマン−化合物

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WO2006063466A1 (en) 2004-12-17 2006-06-22 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1h-phenantrho[9,10-d]imidazoles as mpges-1 inhibitors
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
DE102006053475A1 (de) 2006-11-14 2008-06-19 Eberhard-Karls-Universität Tübingen Zubereitungen zur Hemmung der Prostaglandin E2 Synthese
DE102006058450A1 (de) 2006-12-12 2008-06-19 Eberhard-Karls-Universität Tübingen Zubereitungen zur Hemmung der Prostaglandin E2 Synthese
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UY32138A (es) 2008-09-25 2010-04-30 Boehringer Ingelheim Int Amidas sustituidas del ácido 2-(2,6-dicloro-fenilamino)-6-fluoro-1-metil-1h-bencimidazol-5-carboxílico y sus sales farmacéuticamente aceptables
UY32470A (es) 2009-03-05 2010-10-29 Boehringer Ingelheim Int Derivados de 2-{2-cloro-5-[(sustituido) metil]fenilamino} -1-metil]fenilamino}-1-metilbencimidazol-5-carboxamidas-n-(sustituidas) y sus sales fisiológicamente aceptables, composiciones conteniéndolos y aplicaciones
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WO2012110860A1 (en) 2011-02-17 2012-08-23 Glenmark Pharmaceuticals S.A. TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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WO2013072825A1 (en) 2011-11-16 2013-05-23 Glenmark Pharmaceuticals S.A. Phtalazinone derivatives as mpegs -1 inhibitors
AR089939A1 (es) 2012-02-09 2014-10-01 Glenmark Pharmaceuticals Sa COMPUESTOS BICICLICOS COMO INHIBIDORES DE mPGES-1
WO2013153535A1 (en) 2012-04-13 2013-10-17 Glenmark Pharmaceuticals S.A. TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
US9388156B2 (en) * 2012-07-12 2016-07-12 Khondiron IP B.V. Chromanyl derivatives for treating mitochondrial disease
ES2838625T3 (es) 2014-04-14 2021-07-02 Shanghai hengrui pharmaceutical co ltd Derivados de amida y sales farmacéuticamente aceptables de los mismos, su método de preparación y aplicación médica de los mismos
AU2016268975B2 (en) * 2015-05-22 2021-08-12 Sulfateq B.V. Compound for the prophylaxis or treatment of organ damage
CA3058033A1 (en) * 2017-04-05 2018-10-11 Khondrion Ip B.V. Treatment of mitochondrial diseases
AU2018371152B2 (en) * 2017-11-22 2024-02-08 Khondrion Ip B.V. Novel compounds for use in treating depression and migraine

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011503005A (ja) 2007-11-06 2011-01-27 エジソン ファーマシューティカルズ, インコーポレイテッド ミトコンドリア病を治療するための4−(p−キノリル)−2−ヒドロキシブタンアミド誘導体
JP2015522067A (ja) 2012-07-12 2015-08-03 コンドリオン アイピー ビー.ブイ.Khondrion Ip B.V. ミトコンドリア病を治療するためのクロマニル誘導体
JP2016511743A (ja) 2012-12-19 2016-04-21 スルファテック・ベスローテン・フェンノートシャップSulfateq B.V. 細胞保護のための化合物
JP2017524674A (ja) 2014-06-17 2017-08-31 スルファテック・ベスローテン・フェンノートシャップSulfateq B.V. 慢性閉塞性気道疾患の治療のための6−ヒドロキシ−2,5,7,8−テトラメチルクロマン−化合物
WO2017060432A1 (en) 2015-10-08 2017-04-13 Khondrion Ip B.V. Novel compounds for treating mitochondrial disease

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BR112020010089A2 (pt) 2020-11-03
SG11202003743SA (en) 2020-06-29
EP3713564C0 (en) 2023-11-15
KR20200090818A (ko) 2020-07-29
ES2963906T3 (es) 2024-04-03
PL3713564T3 (pl) 2024-04-08
RU2020120235A (ru) 2021-12-22
MY207603A (en) 2025-03-06
AU2018371153B2 (en) 2023-07-13
MX2020005238A (es) 2020-08-24
CA3079483A1 (en) 2019-05-31
AU2018371153A1 (en) 2020-06-04
EP3713564B1 (en) 2023-11-15
CN111417393A (zh) 2020-07-14
ZA202002103B (en) 2023-12-20
KR20250109241A (ko) 2025-07-16
US20200345706A1 (en) 2020-11-05
WO2019101826A1 (en) 2019-05-31
JP2024009799A (ja) 2024-01-23
US11672787B2 (en) 2023-06-13
IL274821A (en) 2020-07-30
EP3713564A1 (en) 2020-09-30
JP2021504307A (ja) 2021-02-15

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