JP7491900B2 - Tlr7/8アンタゴニストおよびそれらの使用 - Google Patents
Tlr7/8アンタゴニストおよびそれらの使用 Download PDFInfo
- Publication number
- JP7491900B2 JP7491900B2 JP2021505638A JP2021505638A JP7491900B2 JP 7491900 B2 JP7491900 B2 JP 7491900B2 JP 2021505638 A JP2021505638 A JP 2021505638A JP 2021505638 A JP2021505638 A JP 2021505638A JP 7491900 B2 JP7491900 B2 JP 7491900B2
- Authority
- JP
- Japan
- Prior art keywords
- methyl
- piperidin
- mmol
- trifluoromethyl
- compound
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
- 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
- C07D495/10—Spiro-condensed systems
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/14—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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024080418A JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Tlr7/8アンタゴニストおよびそれらの使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862712439P | 2018-07-31 | 2018-07-31 | |
| US62/712,439 | 2018-07-31 | ||
| PCT/EP2019/070312 WO2020025517A1 (en) | 2018-07-31 | 2019-07-29 | Tlr7/8 antagonists and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024080418A Division JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Tlr7/8アンタゴニストおよびそれらの使用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021533125A JP2021533125A (ja) | 2021-12-02 |
| JP2021533125A5 JP2021533125A5 (https=) | 2022-08-08 |
| JPWO2020025517A5 JPWO2020025517A5 (https=) | 2022-08-08 |
| JP7491900B2 true JP7491900B2 (ja) | 2024-05-28 |
Family
ID=67660056
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021505638A Active JP7491900B2 (ja) | 2018-07-31 | 2019-07-29 | Tlr7/8アンタゴニストおよびそれらの使用 |
| JP2024080418A Pending JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Tlr7/8アンタゴニストおよびそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024080418A Pending JP2024105611A (ja) | 2018-07-31 | 2024-05-16 | Tlr7/8アンタゴニストおよびそれらの使用 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20210300940A1 (https=) |
| EP (1) | EP3830080A1 (https=) |
| JP (2) | JP7491900B2 (https=) |
| KR (2) | KR20260047300A (https=) |
| CN (1) | CN112513024A (https=) |
| AU (2) | AU2019313441B2 (https=) |
| BR (2) | BR122023023308A2 (https=) |
| CA (1) | CA3108099A1 (https=) |
| IL (1) | IL280479A (https=) |
| MX (2) | MX2021000093A (https=) |
| SG (1) | SG11202100818RA (https=) |
| TW (3) | TWI827641B (https=) |
| WO (1) | WO2020025517A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3005766A1 (en) | 2015-12-17 | 2017-06-22 | Merck Patent Gmbh | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders |
| JP7125385B2 (ja) | 2016-08-08 | 2022-08-24 | 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 | Tlr7/8アンタゴニストおよびそれらの使用 |
| SG11202005547YA (en) * | 2017-12-19 | 2020-07-29 | Merck Patent Gmbh | Tlr7/8 antagonists and uses thereof |
| JPWO2020203609A1 (https=) * | 2019-03-29 | 2020-10-08 | ||
| JP2022081710A (ja) * | 2019-03-29 | 2022-06-01 | ユーティアイ リミテッド パートナーシップ | 関節リウマチを治療するためのt型カルシウムチャネル阻害剤の使用 |
| EP4031539A1 (en) * | 2019-09-16 | 2022-07-27 | F. Hoffmann-La Roche AG | Piperidinyl amine compounds for the treatment of autoimmune disease |
| KR20220122637A (ko) | 2019-11-28 | 2022-09-02 | 바이엘 악티엔게젤샤프트 | 면역 활성화를 위한 dgk알파 억제제로서의 치환된 아미노퀴놀론 |
| JP7832124B2 (ja) * | 2020-05-14 | 2026-03-17 | メルク ヘルスケア コマンディトゲゼルシャフト アウフ アクティーン | コロナウイルス感染症治療のためのtlr7/8拮抗薬 |
| CN116745291A (zh) | 2020-12-17 | 2023-09-12 | 阿斯利康(瑞典)有限公司 | N-(2-(4-氰基噻唑烷-3-基)-2-氧代乙基)-喹啉-4-甲酰胺 |
| CR20230478A (es) | 2021-04-16 | 2023-11-30 | Gilead Sciences Inc | Compuestos de tienopirrol. |
| KR20240056747A (ko) | 2021-09-10 | 2024-04-30 | 길리애드 사이언시즈, 인코포레이티드 | 티에노피롤 화합물 |
| WO2024153063A1 (zh) * | 2023-01-18 | 2024-07-25 | 苏州科睿思制药有限公司 | Enpatoran的晶型及其制备方法和用途 |
Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104557913A (zh) | 2013-10-28 | 2015-04-29 | 上海汇伦生命科技有限公司 | 吡啶并嘧啶类化合物,其制备方法和用途 |
| JP2016536320A (ja) | 2013-11-12 | 2016-11-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 神経変性疾患の処置用の神経新生薬としてのピリド[4,3−b]ピラジン−2−カルボキサミド |
| JP2016539079A (ja) | 2013-10-14 | 2016-12-15 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 選択的に置換されたキノリン化合物 |
| WO2017004405A1 (en) | 2015-07-01 | 2017-01-05 | Northwestern University | Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity |
| WO2017031427A1 (en) | 2015-08-19 | 2017-02-23 | 3-V Biosciences, Inc. | COMPOUNDS AND METHODS FOR INHIBITING mTOR |
| CN106632089A (zh) | 2016-11-04 | 2017-05-10 | 中山大学 | 一类喹唑啉类化合物及其制备方法与应用 |
| WO2017106607A1 (en) | 2015-12-17 | 2017-06-22 | Merck Patent Gmbh | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders |
| JP2020527577A (ja) | 2017-07-18 | 2020-09-10 | 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Merck Patent Gesellschaft mit beschraenkter Haftung | Tlr7/8アンタゴニストおよびそれらの使用 |
| JP2021506862A (ja) | 2017-12-19 | 2021-02-22 | 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Merck Patent Gesellschaft mit beschraenkter Haftung | Tlr7/8アンタゴニストおよびそれらの使用 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI529171B (zh) * | 2013-07-29 | 2016-04-11 | 赫孚孟拉羅股份公司 | 1,7-萘啶衍生物 |
| CN111801015B (zh) * | 2017-12-12 | 2022-03-18 | 先正达参股股份有限公司 | 植物生长调节 |
-
2019
- 2019-07-29 SG SG11202100818RA patent/SG11202100818RA/en unknown
- 2019-07-29 AU AU2019313441A patent/AU2019313441B2/en active Active
- 2019-07-29 MX MX2021000093A patent/MX2021000093A/es unknown
- 2019-07-29 BR BR122023023308-5A patent/BR122023023308A2/pt unknown
- 2019-07-29 JP JP2021505638A patent/JP7491900B2/ja active Active
- 2019-07-29 CA CA3108099A patent/CA3108099A1/en active Pending
- 2019-07-29 KR KR1020267009849A patent/KR20260047300A/ko active Pending
- 2019-07-29 CN CN201980051004.3A patent/CN112513024A/zh active Pending
- 2019-07-29 BR BR112021001618-0A patent/BR112021001618A2/pt unknown
- 2019-07-29 KR KR1020217005440A patent/KR102947440B1/ko active Active
- 2019-07-29 WO PCT/EP2019/070312 patent/WO2020025517A1/en not_active Ceased
- 2019-07-29 US US17/250,489 patent/US20210300940A1/en active Pending
- 2019-07-29 EP EP19755290.4A patent/EP3830080A1/en active Pending
- 2019-07-30 TW TW108126963A patent/TWI827641B/zh active
- 2019-07-30 TW TW114108280A patent/TW202542153A/zh unknown
- 2019-07-30 TW TW112144948A patent/TWI880472B/zh active
-
2021
- 2021-01-06 MX MX2024013464A patent/MX2024013464A/es unknown
- 2021-01-28 IL IL280479A patent/IL280479A/en unknown
-
2024
- 2024-05-16 JP JP2024080418A patent/JP2024105611A/ja active Pending
- 2024-05-30 AU AU2024203629A patent/AU2024203629A1/en active Pending
Patent Citations (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2016539079A (ja) | 2013-10-14 | 2016-12-15 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 選択的に置換されたキノリン化合物 |
| CN104557913A (zh) | 2013-10-28 | 2015-04-29 | 上海汇伦生命科技有限公司 | 吡啶并嘧啶类化合物,其制备方法和用途 |
| JP2016536320A (ja) | 2013-11-12 | 2016-11-24 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | 神経変性疾患の処置用の神経新生薬としてのピリド[4,3−b]ピラジン−2−カルボキサミド |
| WO2017004405A1 (en) | 2015-07-01 | 2017-01-05 | Northwestern University | Substituted quinazoline compounds and uses thereof for modulating glucocerebrosidase activity |
| WO2017031427A1 (en) | 2015-08-19 | 2017-02-23 | 3-V Biosciences, Inc. | COMPOUNDS AND METHODS FOR INHIBITING mTOR |
| WO2017106607A1 (en) | 2015-12-17 | 2017-06-22 | Merck Patent Gmbh | Polycyclic tlr7/8 antagonists and use thereof in the treatment of immune disorders |
| CN106632089A (zh) | 2016-11-04 | 2017-05-10 | 中山大学 | 一类喹唑啉类化合物及其制备方法与应用 |
| JP2020527577A (ja) | 2017-07-18 | 2020-09-10 | 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Merck Patent Gesellschaft mit beschraenkter Haftung | Tlr7/8アンタゴニストおよびそれらの使用 |
| JP2021506862A (ja) | 2017-12-19 | 2021-02-22 | 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Merck Patent Gesellschaft mit beschraenkter Haftung | Tlr7/8アンタゴニストおよびそれらの使用 |
Also Published As
| Publication number | Publication date |
|---|---|
| MX2024013464A (es) | 2024-12-06 |
| KR20210040085A (ko) | 2021-04-12 |
| WO2020025517A1 (en) | 2020-02-06 |
| KR102947440B1 (ko) | 2026-04-03 |
| JP2024105611A (ja) | 2024-08-06 |
| TW202542153A (zh) | 2025-11-01 |
| CN112513024A (zh) | 2021-03-16 |
| AU2019313441B2 (en) | 2024-05-23 |
| KR20260047300A (ko) | 2026-04-07 |
| IL280479A (en) | 2021-03-01 |
| BR112021001618A2 (pt) | 2021-04-27 |
| TW202019899A (zh) | 2020-06-01 |
| US20210300940A1 (en) | 2021-09-30 |
| TW202423913A (zh) | 2024-06-16 |
| EP3830080A1 (en) | 2021-06-09 |
| AU2019313441A1 (en) | 2021-03-18 |
| CA3108099A1 (en) | 2020-02-06 |
| SG11202100818RA (en) | 2021-02-25 |
| JP2021533125A (ja) | 2021-12-02 |
| BR122023023308A2 (pt) | 2024-02-20 |
| TWI827641B (zh) | 2024-01-01 |
| AU2024203629A1 (en) | 2024-06-20 |
| TWI880472B (zh) | 2025-04-11 |
| MX2021000093A (es) | 2021-03-25 |
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