AR109487A1 - Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas bet - Google Patents
Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas betInfo
- Publication number
- AR109487A1 AR109487A1 ARP170102425A ARP170102425A AR109487A1 AR 109487 A1 AR109487 A1 AR 109487A1 AR P170102425 A ARP170102425 A AR P170102425A AR P170102425 A ARP170102425 A AR P170102425A AR 109487 A1 AR109487 A1 AR 109487A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- hydrogen
- alkoxy
- halogen
- heterocycloalkyl
- Prior art date
Links
- 102000004169 proteins and genes Human genes 0.000 title abstract 2
- 108090000623 proteins and genes Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 19
- 229910052739 hydrogen Inorganic materials 0.000 abstract 12
- 239000001257 hydrogen Substances 0.000 abstract 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 12
- 229910052736 halogen Inorganic materials 0.000 abstract 7
- 150000002367 halogens Chemical group 0.000 abstract 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 7
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- -1 - (CH2) dOR11 Chemical group 0.000 abstract 5
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- 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
- A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se ha descubierto que éstos compuestos y sales de los mismos inhiben la unión de la familia BET de proteínas que contienen bromodominios a, por ejemplo, residuos de lisina acetilados y, por tanto, pueden tener uso en terapia, por ejemplo, en el tratamiento de enfermedades autoinmunitarias e inflamatorias, tales como artritis reumatoide; y cánceres. Reivindicación 1: Un compuesto de fórmula (1), o una sal del mismo, en la que R¹ representa un compuesto de fórmula (2) ó (3); R² es hidrógeno, alquilo C₁₋₆, alcoxi C₁₋₆, cicloalquilo C₃₋₇, heterocicloalquilo o -CHR⁵(CH₂)ᶜR⁶; cada R³ está independientemente seleccionado del grupo que consiste en halógeno, -CN, alquilo C₁₋₃, alcoxi C₁₋₃, -NO₂, -CONR⁷R⁸, -NR⁷COR⁸, -OCOR⁸, -CO₂R⁸, -SO₂NR⁷R⁸, -NR⁷SO₂R⁸, -SO₂R⁸, -R⁸, -NR⁷R⁸ y -OR⁸, con la condición de que cuando a es 2, un R³ está seleccionado del grupo que consiste en halógeno, -CN, alquilo C₁₋₃ y alcoxi C₁₋₃; R⁴ᵃ es hidrógeno, alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CN, -OH, -NR⁹R¹⁰; R⁴ᵇ es hidrógeno o alquilo C₁₋₃; cada R⁴ᶜ está independientemente seleccionado del grupo que consiste en alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CN, -OH y -NR⁹R¹⁰; R⁵ es hidrógeno, alquilo C₁₋₃ o -(CH₂)ᵈOR¹¹; R⁶ es hidrógeno, alquilo C₁₋₃, -(CH₂)ᵈOR¹¹, cicloalquilo C₃₋₇ o heterocicloalquilo, en donde los grupos alquilo C₁₋₃, -(CH₂)ᵈOR¹¹, cicloalquilo C₃₋₇, heterocicloalquilo pueden estar opcionalmente sustituidos con uno o dos sustituyentes independientemente seleccionados del grupo que consiste en alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -CH₂OH, -COOH y -COCH₃; R⁷ es hidrógeno o alquilo C₁₋₃ y R⁸ es -Y-Z, o cuando R³ es -CONR⁷R⁸, R⁷ y R⁸ junto con el nitrógeno al que están unidos pueden formar un heterocicloalquilo, en donde el grupo heterocicloalquilo puede estar opcionalmente sustituido con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃, halógeno, -NH₂, -CH₂NH₂, -CO₂H, -OH, -CN y -CH₂OH; Y es un enlace o alquileno C₁₋₃, en donde el grupo alquileno C₁₋₃ puede estar opcionalmente sustituido con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃; Z es hidrógeno, alquilo C₁₋₃, cicloalquilo C₃₋₇, heterocicloalquilo, arilo, heteroarilo, -SO₂NR¹²R¹³, -NR¹²SO₂R¹³, -SO₂R¹² o -NR¹²R¹³; en donde alquilo C₁₋₃, cicloalquilo C₃₋₇, heterocicloalquilo, arilo o heteroarilo pueden estar opcionalmente sustituidos con uno o dos grupos independientemente seleccionados de alquilo C₁₋₃, alcoxi C₁₋₃, halógeno, -NH₂, -CH₂NH₂, -CO₂H, -OH, -CN y -CH₂OH; R⁹ es hidrógeno o CH₃; R¹⁰ es hidrógeno o alquilo C₁₋₃; R¹¹ es hidrógeno o alquilo C₁₋₃; R¹² es hidrógeno o alquilo C₁₋₃; R¹³ es hidrógeno o alquilo C₁₋₃; a representa 0, 1 ó 2; b representa 0, 1 ó 2; cada c y d independientemente representan 0 ó 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1614934.6A GB201614934D0 (en) | 2016-09-02 | 2016-09-02 | Chemical compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR109487A1 true AR109487A1 (es) | 2018-12-12 |
Family
ID=57140084
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP170102425A AR109487A1 (es) | 2016-09-02 | 2017-08-31 | Derivados de imidazo-2-il-piridin-2-ona como inhibidores de la unión de las proteínas bet |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US20190175571A1 (es) |
| EP (1) | EP3507283A1 (es) |
| JP (1) | JP2019526577A (es) |
| KR (1) | KR20190042701A (es) |
| CN (1) | CN109790147A (es) |
| AR (1) | AR109487A1 (es) |
| AU (1) | AU2017317724A1 (es) |
| BR (1) | BR112019004241A2 (es) |
| CA (1) | CA3035312A1 (es) |
| CL (1) | CL2019000538A1 (es) |
| CO (1) | CO2019001871A2 (es) |
| CR (1) | CR20190106A (es) |
| DO (1) | DOP2019000047A (es) |
| EA (1) | EA201990410A1 (es) |
| GB (1) | GB201614934D0 (es) |
| JO (1) | JOP20190029A1 (es) |
| MA (1) | MA46085A (es) |
| MX (1) | MX2019002491A (es) |
| PE (1) | PE20190478A1 (es) |
| PH (1) | PH12019500460A1 (es) |
| SG (1) | SG11201901673SA (es) |
| TW (1) | TW201817724A (es) |
| UY (1) | UY37393A (es) |
| WO (1) | WO2018041947A1 (es) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MY199759A (en) | 2016-09-02 | 2023-11-21 | Tisento Therapeutics Inc | Fused bicyclic sgc stimulators |
| GB201905721D0 (en) | 2019-04-24 | 2019-06-05 | Univ Dundee | Compounds |
| CN111588721B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物zl0580用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111588725B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物arv-825用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111686107B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物plx51107用于制备预防或治疗非洲猪瘟药物的新用途 |
| CN111686114B (zh) * | 2020-07-16 | 2021-06-08 | 中国农业科学院兰州兽医研究所 | 化合物i-bet-762用于制备预防或治疗非洲猪瘟药物的新用途 |
| WO2024018423A1 (en) * | 2022-07-21 | 2024-01-25 | Tay Therapeutics Limited | Pyrroles and imidazoles as bet protein inhibitors |
| CN117257964B (zh) * | 2023-10-25 | 2024-04-02 | 苏州大学 | 基于碳酸氢铵的微波诱导吲哚美辛原位无定形化增溶技术 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3406329A1 (de) * | 1984-02-22 | 1985-08-22 | Merck Patent Gmbh, 6100 Darmstadt | Pyridone |
| GB9004781D0 (en) | 1990-03-02 | 1990-04-25 | Glaxo Group Ltd | Device |
| DE4034060A1 (de) * | 1990-10-26 | 1992-04-30 | Basf Ag | Biskationische azofarbstoffe |
| DE19809994B4 (de) * | 1997-03-19 | 2006-02-09 | Basf Ag | Clathrate von Bis-[6-hydroxy-4-methyl-5-(3-methylimidazolium-1-yl)-3-(phen-4-ylazo)-pyridin-2-on]ethylen |
| GB0201677D0 (en) | 2002-01-25 | 2002-03-13 | Glaxo Group Ltd | Medicament dispenser |
| PE20060285A1 (es) * | 2004-03-30 | 2006-05-08 | Aventis Pharma Inc | Piridonas sustituidas como inhibidores de pol(adp-ribosa)-polimerasa (parp) |
| GB0515584D0 (en) | 2005-07-28 | 2005-09-07 | Glaxo Group Ltd | Medicament dispenser |
| AR058289A1 (es) | 2005-12-12 | 2008-01-30 | Glaxo Group Ltd | Colector para ser usado en dispensador de medicamento |
| AU2007292155B2 (en) * | 2006-09-05 | 2012-11-01 | Kyowa Kirin Co., Ltd. | Imidazole derivative |
| MX2010010317A (es) * | 2008-03-21 | 2010-10-04 | Novartis Ag | Compuestos heterociclicos novedosos y usos de los mismos. |
| ES2567283T3 (es) * | 2008-06-03 | 2016-04-21 | Intermune, Inc. | Compuestos y métodos para tratar trastornos inflamatorios y fibróticos |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US9309199B2 (en) * | 2010-03-04 | 2016-04-12 | Merck Sharp & Dohme Corp. | Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders |
| AR092742A1 (es) * | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| WO2014096965A2 (en) * | 2012-12-21 | 2014-06-26 | Rvx Therapeutics Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| CN104788423B (zh) * | 2015-03-13 | 2016-10-26 | 成都理工大学 | 一种新的囊性纤维化跨膜传导调节因子抑制剂 |
| GB201504689D0 (en) * | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
-
2016
- 2016-09-02 GB GBGB1614934.6A patent/GB201614934D0/en not_active Ceased
-
2017
- 2017-06-16 JO JOP/2019/0029A patent/JOP20190029A1/ar unknown
- 2017-08-31 CA CA3035312A patent/CA3035312A1/en not_active Abandoned
- 2017-08-31 PE PE2019000455A patent/PE20190478A1/es unknown
- 2017-08-31 KR KR1020197009266A patent/KR20190042701A/ko not_active Ceased
- 2017-08-31 UY UY0001037393A patent/UY37393A/es not_active Application Discontinuation
- 2017-08-31 EA EA201990410A patent/EA201990410A1/ru unknown
- 2017-08-31 EP EP17758878.7A patent/EP3507283A1/en not_active Withdrawn
- 2017-08-31 AU AU2017317724A patent/AU2017317724A1/en not_active Abandoned
- 2017-08-31 MX MX2019002491A patent/MX2019002491A/es unknown
- 2017-08-31 CN CN201780059730.0A patent/CN109790147A/zh active Pending
- 2017-08-31 WO PCT/EP2017/071868 patent/WO2018041947A1/en not_active Ceased
- 2017-08-31 BR BR112019004241A patent/BR112019004241A2/pt not_active Application Discontinuation
- 2017-08-31 TW TW106129714A patent/TW201817724A/zh unknown
- 2017-08-31 MA MA046085A patent/MA46085A/fr unknown
- 2017-08-31 CR CR20190106A patent/CR20190106A/es unknown
- 2017-08-31 US US16/326,991 patent/US20190175571A1/en not_active Abandoned
- 2017-08-31 SG SG11201901673SA patent/SG11201901673SA/en unknown
- 2017-08-31 AR ARP170102425A patent/AR109487A1/es unknown
- 2017-08-31 JP JP2019511919A patent/JP2019526577A/ja active Pending
-
2019
- 2019-02-27 CO CONC2019/0001871A patent/CO2019001871A2/es unknown
- 2019-02-28 CL CL2019000538A patent/CL2019000538A1/es unknown
- 2019-02-28 DO DO2019000047A patent/DOP2019000047A/es unknown
- 2019-03-01 PH PH12019500460A patent/PH12019500460A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| SG11201901673SA (en) | 2019-03-28 |
| BR112019004241A2 (pt) | 2019-06-04 |
| JOP20190029A1 (ar) | 2019-02-25 |
| CA3035312A1 (en) | 2018-03-08 |
| CL2019000538A1 (es) | 2019-05-17 |
| CO2019001871A2 (es) | 2019-03-08 |
| DOP2019000047A (es) | 2019-03-15 |
| GB201614934D0 (en) | 2016-10-19 |
| MX2019002491A (es) | 2019-07-08 |
| UY37393A (es) | 2018-03-23 |
| TW201817724A (zh) | 2018-05-16 |
| JP2019526577A (ja) | 2019-09-19 |
| EP3507283A1 (en) | 2019-07-10 |
| KR20190042701A (ko) | 2019-04-24 |
| CN109790147A (zh) | 2019-05-21 |
| EA201990410A1 (ru) | 2019-09-30 |
| US20190175571A1 (en) | 2019-06-13 |
| PE20190478A1 (es) | 2019-04-04 |
| CR20190106A (es) | 2019-05-02 |
| PH12019500460A1 (en) | 2019-12-16 |
| WO2018041947A1 (en) | 2018-03-08 |
| MA46085A (fr) | 2019-07-10 |
| AU2017317724A1 (en) | 2019-03-21 |
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