AR117229A1 - Compuestos heteroaromáticos como inhibidores de vanina - Google Patents
Compuestos heteroaromáticos como inhibidores de vaninaInfo
- Publication number
- AR117229A1 AR117229A1 ARP190103518A ARP190103518A AR117229A1 AR 117229 A1 AR117229 A1 AR 117229A1 AR P190103518 A ARP190103518 A AR P190103518A AR P190103518 A ARP190103518 A AR P190103518A AR 117229 A1 AR117229 A1 AR 117229A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- membered
- optionally substituted
- cycloalkyl
- Prior art date
Links
- 150000002390 heteroarenes Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
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
- C07D401/14—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
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
- C07D209/44—Iso-indoles; Hydrogenated iso-indoles
- C07D209/48—Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D211/78—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
- C07D413/02—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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/056—Triazole or tetrazole radicals
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Biotechnology (AREA)
- Genetics & Genomics (AREA)
- Molecular Biology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Los compuestos de la fórmula (1), que son adecuados para el tratamiento de enfermedades relacionadas con vanina, y los procesos para fabricar estos compuestos, las preparaciones farmacéuticas que contienen estos compuestos y sus métodos de uso. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde n indica 1 ó 2; R¹, R² y R³ se seleccionan, independientemente entre sí, del grupo que consiste en C₁₋₄-alquilo opcionalmente sustituido con hidroxi, CH₃-O-, CH₃-SO₂-, fenil-CH₂- opcionalmente sustituido con 1 a 3 átomos de halógeno y heteroaril-C₁₋₂- alquil- de 5 - 6 miembros, o R² y R³ juntos forman un carbociclo de 3 - 6 miembros o un heterociclilo de 4 - 6 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N y O; o R¹, R² y R³ juntos pueden formar un carbociclo bicíclico de 5 - 8 miembros o un heterociclilo bicíclico de 6 - 8 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N y O; en donde, en la definición de R¹, R² y R³ mencionada, alquilo, cicloalquilo, heteroarilo y heterociclilo se sustituyen opcionalmente con 1 a 3 átomos de halógeno; R⁴ indica R⁴.¹R⁴.²N-, heteroarilo de 5 - 6 miembros, NC- o heterociclilo de 5 - 6 miembros; o R⁴ indica un grupo de la fórmula R⁴.ᵃ o R⁴.ᵇ en donde X indica CH₂, -NRX u O; en donde RX indica H o C₁₋₃-alquilo; R⁴.ᵃ y R⁴.ᵇ, independientemente entre sí, se sustituyen opcionalmente con metilo; R⁴.¹ se selecciona del grupo que consiste en C₁₋₄-alquil-CO- opcionalmente sustituido con 1 - 3 átomos de F, C₃₋₄-cicloalquilo o C₁₋₂-alcoxi, C₃₋₅-cicloalquil-CO- sustituido con R⁴.¹.¹ y R⁴.¹.², heterociclil-CO- de 4 - 6 miembros sustituido con R⁴.¹.³ y R⁴.¹.⁴, heterociclil-CH₂-CO- de 4 - 6 miembros, heteroaril-CO- de 5 - 6 miembros opcionalmente sustituido con 1 átomo de halógeno, H₃C-O- o 1 a 2 metilo, fenil-CO- sustituido con R⁴.¹.⁵ y R⁴.¹.⁶, (C₁₋₃-alquil)(C₁₋₃alquil)N-CO- y heteroarilo de 5 - 6 miembros; en donde R⁴.¹.¹, R⁴.¹.² se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.¹.³, R⁴.¹.⁴ se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.¹.⁵, R⁴.¹.⁶ se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.² se selecciona del grupo que consiste en H, C₁₋₄-alquilo, C₃₋₄-cicloalquilo, C₃₋₄-cicloalquil-C₁₋₂-alquil- y fenil-C₁₋₂-alquil-; en donde, en la definición de R⁴.² mencionada, alquilo, cicloalquilo y fenilo se sustituyen opcionalmente con 1 - 3 átomos de F o un C₁₋₂-alquil-O; R⁵ indica H o C₁₋₂-alquilo; o R⁴ y R⁵ juntos forman un heterociclilo de 4 - 6 miembros que contiene 1 heteroátomo seleccionado del grupo que consiste en N y O; o una sal de aquel aceptable desde el punto de vista farmacéutico.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18209721 | 2018-12-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR117229A1 true AR117229A1 (es) | 2021-07-21 |
Family
ID=64572152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190103518A AR117229A1 (es) | 2018-12-03 | 2019-12-02 | Compuestos heteroaromáticos como inhibidores de vanina |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US11078182B2 (es) |
| EP (1) | EP3891139A1 (es) |
| JP (2) | JP7130873B2 (es) |
| KR (1) | KR20210100150A (es) |
| CN (2) | CN113166104A (es) |
| AR (1) | AR117229A1 (es) |
| AU (1) | AU2019391279B2 (es) |
| BR (1) | BR112021007915A2 (es) |
| CA (1) | CA3116830A1 (es) |
| CL (2) | CL2021001198A1 (es) |
| CO (1) | CO2021007173A2 (es) |
| CR (1) | CR20210294A (es) |
| DO (1) | DOP2021000071A (es) |
| EA (1) | EA202191476A1 (es) |
| EC (1) | ECSP21040278A (es) |
| IL (1) | IL283397B2 (es) |
| JO (2) | JOP20210127A1 (es) |
| MA (1) | MA54378A (es) |
| MX (1) | MX2021006520A (es) |
| PE (1) | PE20211769A1 (es) |
| PH (1) | PH12021551280A1 (es) |
| SA (1) | SA521422152B1 (es) |
| SG (1) | SG11202104437XA (es) |
| TW (1) | TWI838430B (es) |
| UA (1) | UA128374C2 (es) |
| WO (1) | WO2020114943A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112021000650A2 (pt) | 2018-08-28 | 2021-04-13 | Boehringer Ingelheim International Gmbh | Compostos heteroaromáticos como inibidores de vanina |
| KR20210113184A (ko) | 2018-11-30 | 2021-09-15 | 코멧 테라퓨틱스, 인코포레이티드 | 사이클릭 판테테인 유도체 및 이들의 용도 |
| US12240828B2 (en) * | 2018-12-03 | 2025-03-04 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as vanin inhibitors |
| TWI838430B (zh) * | 2018-12-03 | 2024-04-11 | 德商百靈佳殷格翰國際股份有限公司 | 作為vanin抑制劑之雜芳族化合物 |
| AU2019393953B2 (en) | 2018-12-03 | 2024-12-05 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as Vanin inhibitors |
| US20230107927A1 (en) | 2020-02-28 | 2023-04-06 | First Wave Bio, Inc. | Methods of treating iatrogenic autoimmune colitis |
| US20250197414A1 (en) * | 2022-03-18 | 2025-06-19 | Shanghai Meiyue Biotech Development Co., Ltd. | Salt form and crystal form of vanin enzyme inhibitor, method for preparing same, and use thereof |
| KR20250161024A (ko) * | 2023-03-21 | 2025-11-14 | 아토스 테라퓨틱스, 인크. | 바닌-1 억제제 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20030195192A1 (en) * | 2002-04-05 | 2003-10-16 | Fortuna Haviv | Nicotinamides having antiangiogenic activity |
| WO2005035524A1 (en) | 2003-10-09 | 2005-04-21 | Abbott Laboratories | Pyrrolidinyl urea derivatives as angiogensis inhibitors |
| WO2014048547A1 (en) | 2012-09-25 | 2014-04-03 | Merck Patent Gmbh | Alpha hydroxy amides |
| WO2016193844A1 (en) * | 2015-05-29 | 2016-12-08 | Pfizer Inc. | Novel heterocyclic compounds as inhibitors of vanin-1 enzyme |
| CA3030381A1 (en) * | 2016-07-14 | 2018-01-18 | Pfizer Inc. | Pyrimidine carboxamides as inhibitors of vanin-1 enzyme |
| EP3638680B1 (en) | 2017-06-12 | 2022-08-10 | Boehringer Ingelheim International GmbH | Heteroaromatic compounds as vanin inhibitors |
| BR112021000650A2 (pt) | 2018-08-28 | 2021-04-13 | Boehringer Ingelheim International Gmbh | Compostos heteroaromáticos como inibidores de vanina |
| US12240828B2 (en) * | 2018-12-03 | 2025-03-04 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as vanin inhibitors |
| TWI838430B (zh) * | 2018-12-03 | 2024-04-11 | 德商百靈佳殷格翰國際股份有限公司 | 作為vanin抑制劑之雜芳族化合物 |
| AU2019393953B2 (en) * | 2018-12-03 | 2024-12-05 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as Vanin inhibitors |
-
2019
- 2019-12-02 TW TW108143868A patent/TWI838430B/zh active
- 2019-12-02 CA CA3116830A patent/CA3116830A1/en active Pending
- 2019-12-02 JO JOP/2021/0127A patent/JOP20210127A1/ar unknown
- 2019-12-02 AR ARP190103518A patent/AR117229A1/es not_active Application Discontinuation
- 2019-12-02 UA UAA202103638A patent/UA128374C2/uk unknown
- 2019-12-02 CN CN201980078414.7A patent/CN113166104A/zh active Pending
- 2019-12-02 CR CR20210294A patent/CR20210294A/es unknown
- 2019-12-02 US US16/699,799 patent/US11078182B2/en active Active
- 2019-12-02 EA EA202191476A patent/EA202191476A1/ru unknown
- 2019-12-02 CN CN202210061725.6A patent/CN114478485B/zh active Active
- 2019-12-02 KR KR1020217020910A patent/KR20210100150A/ko active Pending
- 2019-12-02 PE PE2021000809A patent/PE20211769A1/es unknown
- 2019-12-02 JO JOP/2021/0128A patent/JOP20210128A1/ar unknown
- 2019-12-02 MX MX2021006520A patent/MX2021006520A/es unknown
- 2019-12-02 WO PCT/EP2019/083252 patent/WO2020114943A1/en not_active Ceased
- 2019-12-02 JP JP2021531556A patent/JP7130873B2/ja active Active
- 2019-12-02 SG SG11202104437XA patent/SG11202104437XA/en unknown
- 2019-12-02 AU AU2019391279A patent/AU2019391279B2/en active Active
- 2019-12-02 MA MA054378A patent/MA54378A/fr unknown
- 2019-12-02 BR BR112021007915-7A patent/BR112021007915A2/pt unknown
- 2019-12-02 IL IL283397A patent/IL283397B2/en unknown
- 2019-12-02 EP EP19817182.9A patent/EP3891139A1/en active Pending
-
2021
- 2021-04-16 DO DO2021000071A patent/DOP2021000071A/es unknown
- 2021-05-06 CL CL2021001198A patent/CL2021001198A1/es unknown
- 2021-05-31 CO CONC2021/0007173A patent/CO2021007173A2/es unknown
- 2021-06-01 PH PH12021551280A patent/PH12021551280A1/en unknown
- 2021-06-01 SA SA521422152A patent/SA521422152B1/ar unknown
- 2021-06-03 EC ECSENADI202140278A patent/ECSP21040278A/es unknown
- 2021-06-25 US US17/358,111 patent/US20220048885A1/en not_active Abandoned
- 2021-12-30 CL CL2021003568A patent/CL2021003568A1/es unknown
-
2022
- 2022-08-24 JP JP2022133354A patent/JP2022188014A/ja not_active Withdrawn
- 2022-11-02 US US18/051,953 patent/US20230295112A1/en not_active Abandoned
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