JP7134177B2 - 大環状広域抗生物質 - Google Patents

大環状広域抗生物質 Download PDF

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JP7134177B2
JP7134177B2 JP2019542369A JP2019542369A JP7134177B2 JP 7134177 B2 JP7134177 B2 JP 7134177B2 JP 2019542369 A JP2019542369 A JP 2019542369A JP 2019542369 A JP2019542369 A JP 2019542369A JP 7134177 B2 JP7134177 B2 JP 7134177B2
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alkyl
compounds
formula
another embodiment
optionally substituted
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JP2020507564A5 (enExample
JP2020507564A (ja
Inventor
スミス，ピーター，アンドリュー
ロバーツ，タッカー，カラン
ヒグチ，ロバート，アイ．
パラセッリ，プラスナ
ケーラー，マイケル，エフ．，ティー．
シュワルツ，ジェイコブ，ブラッドリー
クロフォード，ジェイムス，ジョン
キュー． リー，クオン
ハナン，エミリー，ジェイ．
フー，フイヨン
チェン，ヨンシェン
ユ，ジヨン
コリン マイケル ウィンシップ ポール
マクレオド カラム
ブレンチ トビー
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アールキューエックス ファーマシューティカルズ，インク．
ジェネンテック， インク．
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • 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
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
    • C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2019542369A 2017-02-15 2018-02-22 大環状広域抗生物質 Active JP7134177B2 (ja)

Priority Applications (1)

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JP2022137159A JP7461425B2 (ja) 2017-02-15 2022-08-30 大環状広域抗生物質

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2017/073575 2017-02-15
CNPCT/CN2017/073575 2017-02-15
CNPCT/CN2017/085075 2017-05-19
CNPCT/CN2017/085075 2017-05-19
PCT/CN2018/076957 WO2018149419A1 (en) 2017-02-15 2018-02-22 Macrocyclic broad spectrum antibiotics

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JP2020507564A5 JP2020507564A5 (enExample) 2021-08-26
JP7134177B2 true JP7134177B2 (ja) 2022-09-09

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US (2) US20210198316A9 (enExample)
EP (2) EP4371982A3 (enExample)
JP (2) JP7134177B2 (enExample)
KR (1) KR102671585B1 (enExample)
CN (1) CN110520413B (enExample)
AU (2) AU2018222093B2 (enExample)
BR (1) BR112019017003A2 (enExample)
CL (1) CL2019002305A1 (enExample)
CO (1) CO2019010001A2 (enExample)
CR (2) CR20210144A (enExample)
ES (1) ES2979245T3 (enExample)
IL (1) IL268483B2 (enExample)
MA (1) MA47514A (enExample)
MX (2) MX2019009752A (enExample)
MY (1) MY199461A (enExample)
PE (2) PE20191618A1 (enExample)
PH (1) PH12019501904A1 (enExample)
SG (2) SG11201907448RA (enExample)
UA (1) UA126027C2 (enExample)
WO (1) WO2018149419A1 (enExample)
ZA (1) ZA201905371B (enExample)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
KR20180109858A (ko) 2015-11-20 2018-10-08 알큐엑스 파마슈티컬스, 인크. 마크로시클릭 광범위 항생제
IL265389B1 (en) 2016-09-16 2026-07-01 Quince Therapeutics Inc Ketone compounds lysine inhibitors gingerapine, preparations containing them and uses thereof
IL288294B (en) 2019-05-28 2022-09-01 Hoffmann La Roche A broad-spectrum macrocyclic antibiotic
CN112480007B (zh) * 2020-12-08 2022-11-18 宿迁市科莱博生物化学有限公司 一种1，3-二甲基-1h-吡唑-4-羧酸的合成方法
EP4284804A1 (en) 2021-01-26 2023-12-06 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
CN116284026B (zh) * 2023-03-16 2024-05-14 天津师范大学 一种水溶性阳离子分子笼及其合成方法与应用

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WO2015179441A2 (en) 2014-05-20 2015-11-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
JP2016501864A (ja) 2012-11-21 2016-01-21 アールキューエックス ファーマシューティカルズ，インク． 大環状広域抗生物質
WO2017084629A1 (en) 2015-11-20 2017-05-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2017084630A1 (en) 2015-11-20 2017-05-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2018183198A1 (en) 2017-03-27 2018-10-04 Genentech, Inc. Process for making arylomyin ring analogs

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CN102939095A (zh) * 2010-03-09 2013-02-20 默沙东公司 增强β-内酰胺抗菌药物的活性的桥联脂糖肽类
MX2013003035A (es) * 2010-09-15 2013-12-16 Scripps Research Inst Analogos de arilomicina como antibióticos de amplio espectro.
WO2012166665A2 (en) * 2011-05-27 2012-12-06 Rqx Pharmaceuticals, Inc. Broad spectrum antibiotics
KR20140140580A (ko) * 2012-03-14 2014-12-09 더 스크립스 리서치 인스티튜트 광범위 항생제 아릴로마이신 유사체
CN104620391B (zh) * 2012-10-23 2017-09-19 富士电机株式会社 半导体装置及其制造方法
CN103788176A (zh) * 2012-10-31 2014-05-14 上海来益生物药物研究开发中心有限责任公司 一种arylomycin类化合物及其制备方法和应用
US20190067498A1 (en) * 2017-08-28 2019-02-28 Meng Tao Light-induced aluminum plating on silicon for solar cell metallization

Patent Citations (5)

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JP2016501864A (ja) 2012-11-21 2016-01-21 アールキューエックス ファーマシューティカルズ，インク． 大環状広域抗生物質
WO2015179441A2 (en) 2014-05-20 2015-11-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2017084629A1 (en) 2015-11-20 2017-05-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2017084630A1 (en) 2015-11-20 2017-05-26 Rqx Pharmaceuticals, Inc. Macrocyclic broad spectrum antibiotics
WO2018183198A1 (en) 2017-03-27 2018-10-04 Genentech, Inc. Process for making arylomyin ring analogs

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MX2019009752A (es) 2019-11-11
US20230133667A1 (en) 2023-05-04
CO2019010001A2 (es) 2020-04-01
US20200024309A1 (en) 2020-01-23
EP3583096A4 (en) 2021-01-06
SG10202108876TA (en) 2021-09-29
MY199461A (en) 2023-10-30
WO2018149419A1 (en) 2018-08-23
IL268483B1 (en) 2023-10-01
CN110520413B (zh) 2023-02-17
RU2019126728A3 (enExample) 2021-09-15
EP3583096B1 (en) 2024-03-27
PE20242298A1 (es) 2024-12-11
ES2979245T3 (es) 2024-09-25
JP2022180390A (ja) 2022-12-06
KR102671585B1 (ko) 2024-06-04
NZ779474A (en) 2025-12-19
ZA201905371B (en) 2025-01-29
EP3583096C0 (en) 2024-03-27
CN110520413A (zh) 2019-11-29
AU2018222093B2 (en) 2022-03-31
IL268483B2 (en) 2024-02-01
BR112019017003A2 (pt) 2020-04-14
SG11201907448RA (en) 2019-09-27
EP3583096A1 (en) 2019-12-25
CR20190428A (es) 2020-02-13
US20210198316A9 (en) 2021-07-01
JP2020507564A (ja) 2020-03-12
AU2022201724B9 (en) 2024-03-21
CL2019002305A1 (es) 2020-04-13
CR20210144A (es) 2021-05-13
KR20190127720A (ko) 2019-11-13
UA126027C2 (uk) 2022-08-03
IL268483A (en) 2019-09-26
MA47514A (fr) 2019-12-25
RU2019126728A (ru) 2021-03-16
EP4371982A2 (en) 2024-05-22
EP4371982A3 (en) 2024-08-21
PH12019501904A1 (en) 2019-10-21
AU2022201724B2 (en) 2024-02-29
PE20191618A1 (es) 2019-11-05
AU2022201724A1 (en) 2022-04-07
JP7461425B2 (ja) 2024-04-03
NZ756220A (en) 2021-09-24
AU2018222093A1 (en) 2019-08-29
MX2022014485A (es) 2022-12-13
CA3053205A1 (en) 2018-08-23

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