AR112348A1 - Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak - Google Patents
Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jakInfo
- Publication number
- AR112348A1 AR112348A1 ARP180102151A AR112348A1 AR 112348 A1 AR112348 A1 AR 112348A1 AR P180102151 A ARP180102151 A AR P180102151A AR 112348 A1 AR112348 A1 AR 112348A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- alkyl
- independently selected
- optionally
- alkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 229910052757 nitrogen Inorganic materials 0.000 abstract 7
- 229910052717 sulfur Inorganic materials 0.000 abstract 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000002911 monocyclic heterocycle group Chemical group 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000006555 (C3-C5) cycloalkyl group Chemical group 0.000 abstract 1
- -1 C-NH-CH3 Chemical group 0.000 abstract 1
- 125000006519 CCH3 Chemical group 0.000 abstract 1
- 125000006414 CCl Chemical group ClC* 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
- A61K31/535—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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: X¹ y X² se seleccionan, cada uno independientemente, entre N y CH; X³ se selecciona entre el grupo que consiste en N, CH, C-CH₃, C-CF₃, C-CHF₂, C-CH₂-O-CH₃, C-SMe, C-NMe₂, C-NH-CH₃, C-Cl, C-CN, y C-OMe; el resto de fórmula (2) se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (3); Rᵃ, Rᵇ, Rᶜ, y Rᶠ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃; Rᵈ, Rᵉ, Rᵍ, Rʰ, Rⁱ, Rʲ, Rˡ, Rᵐ, Rⁿ y Rᵒ se seleccionan, cada uno independientemente, entre el grupo que consiste en H y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con 1 a 3 halógenos; opcionalmente, Rᵈ y Rᵉ pueden unirse para formar un anillo de ciclopropilo; A se selecciona entre el grupo que consiste en: (a) un grupo heterocíclico monocíclico de 4 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, S(O)₂ y O, y (b) un grupo heterocíclico multicíclico de 6 a 10 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde L está ligado a un átomo de carbono en A, y A está opcionalmente sustituido con 1 a 3 grupos Rᵏ; cada Rᵏ se selecciona independientemente entre el grupo que consiste en F, CN, alcoxi C₁₋₃, ciclopropilo, y alquilo C₁₋₃, en donde el grupo alquilo C₁₋₃ puede estar opcionalmente sustituido con OH, OMe o 1 a 3 halógenos; R¹ se selecciona entre el grupo que consiste en los compuestos del grupo de fórmulas (4), en donde Rᵖ y Rq se seleccionan, cada uno independientemente, entre el grupo que consiste en H, cicloalquilo C₃₋₅ y alquilo C₁₋₆, en donde el grupo alquilo C₁₋₆ puede estar opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alcoxi C₁₋₃ y -S-alquilo C₁₋₃, o Rᵖ y Rq forman un grupo heterocíclico monocíclico de 4 a 6 miembros que contiene un átomo de nitrógeno y que opcionalmente contiene un heteroátomo adicional seleccionado entre N, S, y O, en donde el grupo heterocíclico monocíclico de 4 a 6 miembros está opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre el grupo que consiste en alquilo C₁₋₆, alcoxi C₁₋₃, -S-alquilo C₁₋₃ y alquilo C₁₋₃-alcoxi C₁₋₃; R² se selecciona entre el grupo que consiste en H, Cl, OMe, Me y F; R³ se selecciona entre el grupo que consiste en H y F; R⁴ se selecciona entre el grupo que consiste en H y F; y R⁵ se selecciona entre el grupo que consiste en H, Me y F.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762539642P | 2017-08-01 | 2017-08-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR112348A1 true AR112348A1 (es) | 2019-10-16 |
Family
ID=63209687
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP180102151 AR112348A1 (es) | 2017-08-01 | 2018-07-31 | Compuestos bicíclicos de pirazolo y triazolo como inhibidores de quinasas jak |
Country Status (23)
| Country | Link |
|---|---|
| US (4) | US10392368B2 (es) |
| EP (1) | EP3652169A1 (es) |
| JP (2) | JP7098716B2 (es) |
| KR (1) | KR20200036004A (es) |
| CN (1) | CN111032646B (es) |
| AR (1) | AR112348A1 (es) |
| AU (1) | AU2018312349A1 (es) |
| BR (1) | BR112020002265A2 (es) |
| CA (1) | CA3069990A1 (es) |
| CL (1) | CL2020000283A1 (es) |
| CO (1) | CO2020001469A2 (es) |
| EA (1) | EA038912B1 (es) |
| IL (1) | IL272031A (es) |
| MA (1) | MA49570A (es) |
| MX (1) | MX2020001170A (es) |
| MY (1) | MY200629A (es) |
| PE (1) | PE20201028A1 (es) |
| PH (1) | PH12020500201A1 (es) |
| SG (1) | SG11202000602YA (es) |
| TW (1) | TW201920150A (es) |
| UA (1) | UA125318C2 (es) |
| WO (1) | WO2019027960A1 (es) |
| ZA (1) | ZA202000561B (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202000602YA (en) | 2017-08-01 | 2020-02-27 | Theravance Biopharma R&D Ip Llc | Pyrazolo and triazolo bicyclic compounds as jak kinase inhibitors |
| CA3125039A1 (en) * | 2019-01-23 | 2020-07-30 | Theravance Biopharma R&D Ip, Llc | Imidazo[1,5-a]pyridine, 1,2,4-triazolo[4,3-a]pyridine and imidazo[1,5-a]pyrazine as jak inhibitors |
| US20220257596A1 (en) * | 2019-07-15 | 2022-08-18 | Novartis Ag | Methods for treating meibomian gland dysfunction with liver x receptor agonists |
| AU2021252213A1 (en) * | 2020-04-08 | 2022-11-03 | Pfizer Inc. | Crystalline forms of 3-cyano-1-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo(1,5-a)pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutaneacetonitrile, and use thereof |
| TW202207918A (zh) | 2020-05-14 | 2022-03-01 | 美商施萬生物製藥研發Ｉｐ有限責任公司 | 腸道選擇性ｊａｋ３抑制劑的投與 |
| CN114075220A (zh) * | 2020-08-13 | 2022-02-22 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| WO2022033544A1 (zh) * | 2020-08-13 | 2022-02-17 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| CN116157388A (zh) * | 2020-09-10 | 2023-05-23 | 四川海思科制药有限公司 | 一种碳环酰胺衍生物及其在医药上的应用 |
| WO2022199599A1 (zh) * | 2021-03-23 | 2022-09-29 | 凯复(苏州)生物医药有限公司 | 丙烯酰基取代的化合物、包含其的药物组合物及其用途 |
| KR20230163469A (ko) * | 2021-03-29 | 2023-11-30 | 브리스톨-마이어스 스큅 컴퍼니 | 6-(시클로프로판카르복스아미도)-4-((2-메톡시-3-(1-메틸-1h-1,2,4-트리아졸-3-일)페닐)아미노)-n-(메틸-d3)피리다진-3-카르복스아미드의 결정 형태 |
| CN113061137B (zh) * | 2021-04-02 | 2022-08-02 | 广西医科大学 | 含氮杂环衍生物或其药学上可接受的盐和用途 |
| AU2022270072A1 (en) * | 2021-05-03 | 2023-11-02 | Incyte Corporation | Jak1 pathway inhibitors for the treatment of prurigo nodularis |
| US20250051360A1 (en) * | 2021-12-23 | 2025-02-13 | Sunshine Lake Pharma Co., Ltd. | Substituted heteroaryl compound, and composition and use thereof |
| WO2023165562A1 (zh) * | 2022-03-02 | 2023-09-07 | 南京明德新药研发有限公司 | 含氮杂环类化合物及其应用 |
| GB202213163D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
| GB202213164D0 (en) | 2022-09-08 | 2022-10-26 | Cambridge Entpr Ltd | Novel compounds, compositions and therapeutic uses thereof |
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| US8765743B2 (en) | 2008-06-05 | 2014-07-01 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
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2018
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- 2018-07-31 UA UAA202001352A patent/UA125318C2/uk unknown
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- 2018-07-31 MY MYPI2020000251A patent/MY200629A/en unknown
- 2018-07-31 US US16/050,227 patent/US10392368B2/en active Active
- 2018-07-31 EP EP18755621.2A patent/EP3652169A1/en not_active Withdrawn
- 2018-07-31 TW TW107126579A patent/TW201920150A/zh unknown
- 2018-07-31 EA EA202090413A patent/EA038912B1/ru unknown
- 2018-07-31 KR KR1020207005956A patent/KR20200036004A/ko not_active Withdrawn
- 2018-07-31 MA MA049570A patent/MA49570A/fr unknown
- 2018-07-31 CA CA3069990A patent/CA3069990A1/en not_active Abandoned
- 2018-07-31 CN CN201880050675.3A patent/CN111032646B/zh active Active
- 2018-07-31 MX MX2020001170A patent/MX2020001170A/es unknown
- 2018-07-31 WO PCT/US2018/044508 patent/WO2019027960A1/en active Application Filing
- 2018-07-31 BR BR112020002265-9A patent/BR112020002265A2/pt not_active Application Discontinuation
- 2018-07-31 AR ARP180102151 patent/AR112348A1/es unknown
- 2018-07-31 AU AU2018312349A patent/AU2018312349A1/en not_active Abandoned
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2021
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| CN111032646B (zh) | 2023-01-03 |
| JP7098716B2 (ja) | 2022-07-11 |
| US20190040043A1 (en) | 2019-02-07 |
| JP2020529987A (ja) | 2020-10-15 |
| KR20200036004A (ko) | 2020-04-06 |
| PE20201028A1 (es) | 2020-10-05 |
| EA038912B1 (ru) | 2021-11-09 |
| CN111032646A (zh) | 2020-04-17 |
| US20200216423A1 (en) | 2020-07-09 |
| US20190315724A1 (en) | 2019-10-17 |
| US10392368B2 (en) | 2019-08-27 |
| IL272031A (en) | 2020-03-31 |
| AU2018312349A1 (en) | 2020-02-06 |
| MX2020001170A (es) | 2020-03-12 |
| MY200629A (en) | 2024-01-06 |
| JP2021098751A (ja) | 2021-07-01 |
| ZA202000561B (en) | 2022-04-28 |
| BR112020002265A2 (pt) | 2020-07-28 |
| US10968205B2 (en) | 2021-04-06 |
| CA3069990A1 (en) | 2019-02-07 |
| US10538513B2 (en) | 2020-01-21 |
| CO2020001469A2 (es) | 2020-05-29 |
| EA202090413A1 (ru) | 2020-06-24 |
| PH12020500201A1 (en) | 2020-10-12 |
| US20220119369A1 (en) | 2022-04-21 |
| EP3652169A1 (en) | 2020-05-20 |
| CL2020000283A1 (es) | 2020-06-12 |
| MA49570A (fr) | 2020-05-20 |
| TW201920150A (zh) | 2019-06-01 |
| UA125318C2 (uk) | 2022-02-16 |
| WO2019027960A1 (en) | 2019-02-07 |
| SG11202000602YA (en) | 2020-02-27 |
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