ECSP23034049A - Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 - Google Patents
Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2Info
- Publication number
- ECSP23034049A ECSP23034049A ECSENADI202334049A ECDI202334049A ECSP23034049A EC SP23034049 A ECSP23034049 A EC SP23034049A EC SENADI202334049 A ECSENADI202334049 A EC SENADI202334049A EC DI202334049 A ECDI202334049 A EC DI202334049A EC SP23034049 A ECSP23034049 A EC SP23034049A
- Authority
- EC
- Ecuador
- Prior art keywords
- formula
- compounds
- inhibitors
- acyltransferase
- preparation
- Prior art date
Links
Classifications
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- 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
- 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
- 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
- C07D417/02—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 two hetero rings
- C07D417/12—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 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se inventan compuestos de fórmula I [IMAGEN ADJUNTA] y sales farmacéuticamente aceptables, ésteres y profármacos de los mismos, que son inhibidores de DGAT2. También se proporcionan métodos de preparación de compuestos de Fórmula I, composiciones farmacéuticas que comprenden compuestos de Fórmula I y métodos de uso de estos compuestos para tratar la esteatosis hepática, esteatohepatitis no alcohólica (EHNA), fibrosis, diabetes mellitus de tipo 2, obesidad, hiperlipidemia, hipercolesterolemia, ateroesclerosis, declive cognitivo, demencia, enfermedades cardiorrenales tales como enfermedades renales crónicas e insuficiencia cardíaca y enfermedades y afecciones relacionadas, que comprenden administrar un compuesto de Fórmula I a un paciente que lo necesita.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063089063P | 2020-10-08 | 2020-10-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP23034049A true ECSP23034049A (es) | 2023-06-30 |
Family
ID=78709520
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI202334049A ECSP23034049A (es) | 2020-10-08 | 2023-05-08 | Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US12410159B2 (es) |
| EP (1) | EP4225735A1 (es) |
| JP (1) | JP7482324B2 (es) |
| KR (1) | KR20230079427A (es) |
| CN (1) | CN116457346A (es) |
| AR (1) | AR123701A1 (es) |
| AU (1) | AU2021358946A1 (es) |
| CA (1) | CA3195032A1 (es) |
| CL (1) | CL2023000978A1 (es) |
| CO (1) | CO2023004366A2 (es) |
| CR (1) | CR20230160A (es) |
| DO (1) | DOP2023000068A (es) |
| EC (1) | ECSP23034049A (es) |
| IL (1) | IL301799A (es) |
| MX (1) | MX2023003844A (es) |
| PE (1) | PE20240217A1 (es) |
| TW (1) | TW202229232A (es) |
| WO (1) | WO2022076496A1 (es) |
| ZA (1) | ZA202304150B (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2023279857A1 (en) * | 2022-06-03 | 2024-11-14 | Domain Therapeutics | Novel par-2 inhibitors |
| AR131250A1 (es) | 2022-12-02 | 2025-02-26 | Merck Sharp & Dohme Llc | Preparación de derivados condensados de azol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6691498A (en) | 1997-03-07 | 1998-09-22 | Metabasis Therapeutics, Inc. | Novel benzimidazole inhibitors of fructose-1,6-bisphosphatase |
| WO1998039342A1 (en) | 1997-03-07 | 1998-09-11 | Metabasis Therapeutics, Inc. | Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase |
| US6284748B1 (en) | 1997-03-07 | 2001-09-04 | Metabasis Therapeutics, Inc. | Purine inhibitors of fructose 1,6-bisphosphatase |
| US6489476B1 (en) | 1998-09-09 | 2002-12-03 | Metabasis Therapeutics, Inc. | Heteroaromatic compounds containing a phosphonate group that are inhibitors of fructose-1,6-bisphosphatase |
| AU2001277056B2 (en) | 2000-07-25 | 2005-09-29 | Merck & Co., Inc. | N-substituted indoles useful in the treatment of diabetes |
| EP1357908A4 (en) | 2001-01-30 | 2009-07-15 | Merck & Co Inc | "ACYLSULFAMIDES FOR THE TREATMENT OF FATIBILITY, DIABETES AND LIPID DISORDERS" |
| WO2003053363A2 (en) | 2001-12-19 | 2003-07-03 | Millennium Pharmaceuticals, Inc. | Human diacylglycerol acyltransferase 2 (dgat2) family members and uses therefor |
| AR040241A1 (es) | 2002-06-10 | 2005-03-23 | Merck & Co Inc | Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia |
| US7393960B2 (en) | 2002-08-29 | 2008-07-01 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| CN100457730C (zh) | 2002-08-29 | 2009-02-04 | 默克公司 | 具有抗糖尿病活性的吲哚化合物 |
| US7319170B2 (en) | 2003-01-17 | 2008-01-15 | Merck & Co., Inc. | N-cyclohexylaminocarbonyl benzensulfonmide derivatives |
| US20080287479A1 (en) | 2006-12-20 | 2008-11-20 | Pfizer Inc | Inhibitors of serine palmitoyltransferase |
| CA2691010A1 (en) | 2007-06-28 | 2008-12-31 | Merck Frosst Canada Ltd. | Substituted fused pyrimidines as antagonists of gpr105 activity |
| WO2009001836A1 (en) | 2007-06-28 | 2008-12-31 | Semiconductor Energy Laboratory Co., Ltd. | Manufacturing method of semiconductor device |
| US20110301079A1 (en) | 2007-09-21 | 2011-12-08 | Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. | Neuromedin u receptor agonists and uses thereof |
| US8124766B2 (en) * | 2008-12-03 | 2012-02-28 | Madrigal Pharmaceuticals, Inc. | Inhibitors of diacylglycerol acyltransferase |
| WO2010077839A1 (en) * | 2008-12-15 | 2010-07-08 | Wyeth Llc (Formerly Known As Wyeth) | Substituted oxindol cb2 agonists for pain treatment |
| TW201201815A (en) | 2010-05-28 | 2012-01-16 | Gilead Sciences Inc | 1'-substituted-carba-nucleoside prodrugs for antiviral treatment |
| AU2013245353A1 (en) | 2012-04-06 | 2014-09-25 | Pfizer Inc. | Diacylglycerol acyltransferase 2 inhibitors |
| AR098394A1 (es) | 2013-11-25 | 2016-05-26 | Lilly Co Eli | Inhibidores de dgat2 (diacilglicerol o-aciltransferasa 2) |
| BR112016012011B8 (pt) | 2013-11-26 | 2021-12-14 | Hewlett Packard Development Co | Cabeçote de impressão de ejeção de fluido, aparelho de ejeção de fluido e método |
| CR20160405A (es) | 2014-03-17 | 2016-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| WO2016036636A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016036633A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016036638A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| AU2016294347B2 (en) | 2015-07-10 | 2022-07-28 | Ionis Pharmaceuticals, Inc. | Modulators of diacyglycerol acyltransferase 2 (DGAT2) |
| AR109179A1 (es) | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| CA3043206A1 (en) * | 2016-11-18 | 2018-05-24 | Merck Sharp & Dohme Corp. | Indole derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| MA46856A (fr) * | 2016-11-18 | 2019-09-25 | Merck Sharp & Dohme | Dérivés d'indazole utiles en tant qu'inhibiteurs de la diacylglycéride o-acyltransférase 2 |
| TWI771766B (zh) | 2019-10-04 | 2022-07-21 | 美商輝瑞股份有限公司 | 二醯基甘油醯基轉移酶２ 抑制劑 |
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| MX2023003842A (es) | 2020-10-08 | 2023-04-14 | Merck Sharp & Dohme Llc | Preparacion de derivados de benzoimidazolona como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2. |
| US11541039B2 (en) | 2020-10-08 | 2023-01-03 | Endogena Therapeutics, Inc. | Compounds and their use as therapeutically active substances in the treatment and/or reducing signs or symptoms of diseases involving the retinal pigment epithelium |
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-
2021
- 2021-10-06 JP JP2023521377A patent/JP7482324B2/ja active Active
- 2021-10-06 US US17/494,896 patent/US12410159B2/en active Active
- 2021-10-06 CN CN202180076390.9A patent/CN116457346A/zh active Pending
- 2021-10-06 MX MX2023003844A patent/MX2023003844A/es unknown
- 2021-10-06 KR KR1020237014915A patent/KR20230079427A/ko active Pending
- 2021-10-06 IL IL301799A patent/IL301799A/en unknown
- 2021-10-06 CA CA3195032A patent/CA3195032A1/en active Pending
- 2021-10-06 CR CR20230160A patent/CR20230160A/es unknown
- 2021-10-06 TW TW110137151A patent/TW202229232A/zh unknown
- 2021-10-06 EP EP21811162.3A patent/EP4225735A1/en active Pending
- 2021-10-06 AR ARP210102767A patent/AR123701A1/es unknown
- 2021-10-06 WO PCT/US2021/053681 patent/WO2022076496A1/en not_active Ceased
- 2021-10-06 PE PE2023001362A patent/PE20240217A1/es unknown
- 2021-10-06 AU AU2021358946A patent/AU2021358946A1/en active Pending
-
2023
- 2023-04-04 CL CL2023000978A patent/CL2023000978A1/es unknown
- 2023-04-04 ZA ZA2023/04150A patent/ZA202304150B/en unknown
- 2023-04-05 CO CONC2023/0004366A patent/CO2023004366A2/es unknown
- 2023-04-05 DO DO2023000068A patent/DOP2023000068A/es unknown
- 2023-05-08 EC ECSENADI202334049A patent/ECSP23034049A/es unknown
-
2024
- 2024-05-23 US US18/672,808 patent/US12428411B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| KR20230079427A (ko) | 2023-06-07 |
| US12410159B2 (en) | 2025-09-09 |
| CA3195032A1 (en) | 2022-04-14 |
| AU2021358946A1 (en) | 2023-06-08 |
| JP2023541714A (ja) | 2023-10-03 |
| PE20240217A1 (es) | 2024-02-16 |
| CL2023000978A1 (es) | 2023-09-29 |
| MX2023003844A (es) | 2023-04-14 |
| AR123701A1 (es) | 2023-01-04 |
| DOP2023000068A (es) | 2023-05-31 |
| AU2021358946A9 (en) | 2024-02-08 |
| US20220112181A1 (en) | 2022-04-14 |
| CO2023004366A2 (es) | 2023-04-27 |
| WO2022076496A1 (en) | 2022-04-14 |
| TW202229232A (zh) | 2022-08-01 |
| CN116457346A (zh) | 2023-07-18 |
| US20240327391A1 (en) | 2024-10-03 |
| US12428411B2 (en) | 2025-09-30 |
| ZA202304150B (en) | 2024-12-18 |
| JP7482324B2 (ja) | 2024-05-13 |
| CR20230160A (es) | 2023-06-02 |
| EP4225735A1 (en) | 2023-08-16 |
| IL301799A (en) | 2023-05-01 |
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