EA201690408A1 - Производные этинила - Google Patents
Производные этинилаInfo
- Publication number
- EA201690408A1 EA201690408A1 EA201690408A EA201690408A EA201690408A1 EA 201690408 A1 EA201690408 A1 EA 201690408A1 EA 201690408 A EA201690408 A EA 201690408A EA 201690408 A EA201690408 A EA 201690408A EA 201690408 A1 EA201690408 A1 EA 201690408A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- group
- halogen
- lower alkyl
- hydrogen
- pyridinyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
- C07D239/96—Two oxygen atoms
-
- 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
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
-
- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- 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
- C07D401/02—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
- C07D401/10—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 aromatic 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
- C07D405/02—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
- C07D405/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
- C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
-
- 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
- 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
- C07D487/06—Peri-condensed systems
-
- 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
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Abstract
Данное соединение относится к соединениям формулы Iгде Y представляет собой N или C-R; G представляет собой 5- или 6-членное ароматическое или гетероароматическое кольцо, содержащее 0, 1, 2 или 3 гетероатома, выбранное из группы, включающей фенил, пиридинил с различными N-позициями, имидазолил, пиразинил, пиримидинил, тиофенил, тиазолил, пиразолил или тиадиазолил, которое, возможно, замещено 1, 2 или 3 заместителями, выбранными из группы, включающей галоген, низший алкил, низший алкокси, низший алкокси, замещенный галогеном или NRR'; R и R' независимо друг от друга представляют собой водород или низший алкил или могут образовывать вместе с атомом N, к которому они присоединены, пяти- или шестичленную насыщенную гетероциклическую группу, которая может содержать дополнительный кислород, NH или N-низшую алкильную группу; Rпредставляет собой водород, галоген или низший алкил, замещенный галогеном; Rпредставляет собой водород, галоген или низший алкил, замещенный галогеном; Rпредставляет собой водород, низший алкил, низший алкоксиалкил, циклоалкил или гетероциклоалкил; или Rвместе с ближайшим атомом углерода в группе G может образовывать группупри этом А представляет собой -СН-, -СНСНили -С(СН)-, Rпредставляет собой фенил или пиридинил, где атом N в пиридинилгруппе может находиться в различных позициях; или к их фармацевтически приемлемой соли или соли присоединения кислоты, к рацемической смеси или их соответствующему энантиомеру и/или оптическому изомеру и/или стереоизомеру. Неожиданно было обнаружено, что соединения общей формулы I являются положительными аллостерическими модуляторами (РАМ) метаботропного рецептора глутамата 4 (mGluR4), могут быть использованы для лечения болезни
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13185856 | 2013-09-25 | ||
| PCT/EP2014/070100 WO2015044075A1 (en) | 2013-09-25 | 2014-09-22 | Ethynyl derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201690408A1 true EA201690408A1 (ru) | 2016-07-29 |
| EA029352B1 EA029352B1 (ru) | 2018-03-30 |
Family
ID=49230629
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201690408A EA029352B1 (ru) | 2013-09-25 | 2014-09-22 | Производные этинила |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US20160207890A1 (ru) |
| EP (1) | EP3049409B1 (ru) |
| JP (1) | JP6134441B2 (ru) |
| KR (1) | KR101757603B1 (ru) |
| CN (1) | CN105579447B (ru) |
| AR (1) | AR097721A1 (ru) |
| AU (1) | AU2014327504B2 (ru) |
| BR (1) | BR112016005994A2 (ru) |
| CA (1) | CA2924376A1 (ru) |
| CL (1) | CL2016000677A1 (ru) |
| CR (1) | CR20160075A (ru) |
| DK (1) | DK3049409T3 (ru) |
| EA (1) | EA029352B1 (ru) |
| ES (1) | ES2630319T3 (ru) |
| HK (1) | HK1220200A1 (ru) |
| HU (1) | HUE034849T2 (ru) |
| IL (1) | IL244039B (ru) |
| MA (1) | MA38885B1 (ru) |
| MX (1) | MX370341B (ru) |
| MY (1) | MY183953A (ru) |
| PE (1) | PE20160666A1 (ru) |
| PH (1) | PH12016500427A1 (ru) |
| PL (1) | PL3049409T3 (ru) |
| SG (1) | SG11201602029VA (ru) |
| SI (1) | SI3049409T1 (ru) |
| TW (1) | TWI527801B (ru) |
| UA (1) | UA116277C2 (ru) |
| WO (1) | WO2015044075A1 (ru) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2721776C2 (ru) * | 2015-07-15 | 2020-05-22 | Ф. Хоффманн-Ля Рош Аг | Производные этинила как модуляторы метаботропного рецептора глутамата |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6286577B2 (ja) * | 2014-02-25 | 2018-02-28 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | エチニル誘導体 |
| WO2016146600A1 (en) * | 2015-03-19 | 2016-09-22 | F. Hoffmann-La Roche Ag | 3-(4-ethynylphenyl)hexahydropyrimidin-2,4-dione derivatives as modulators of mglur4 |
| AR105556A1 (es) * | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| US10308656B2 (en) | 2015-08-18 | 2019-06-04 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of Ku70/80 and uses thereof |
| SI3484889T1 (sl) * | 2016-07-18 | 2020-11-30 | F. Hoffmann-La Roche Ag | Derivati etinila |
| MX2021000841A (es) | 2018-07-26 | 2021-03-26 | Domain Therapeutics | Derivados de quinazolinona sustituidos y su uso como moduladores alostericos positivos de mglur4. |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH10330359A (ja) * | 1997-03-31 | 1998-12-15 | Nippon Bayeragrochem Kk | フエニルアセチレン誘導体及び除草剤 |
| GB0503646D0 (en) * | 2005-02-22 | 2005-03-30 | Novartis Ag | Organic compounds |
| MX2009013169A (es) * | 2007-06-03 | 2010-04-30 | Univ Vanderbilt | Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos. |
| CN102740699A (zh) * | 2009-09-04 | 2012-10-17 | 范德比尔特大学 | 用于治疗神经学上的功能失调的mglur4变构增效剂、组合物和方法 |
| MX2012009377A (es) * | 2010-02-11 | 2012-09-12 | Univ Vanderbilt | Benzotiazoles y azabenzotiazoles como potenciadores alostericos mglur4, composiciones y metodos para tratar la disfuncion neurologica. |
| US8420661B2 (en) * | 2010-04-13 | 2013-04-16 | Hoffmann-La Roche Inc. | Arylethynyl derivatives |
| MX2012013031A (es) * | 2010-05-12 | 2012-12-17 | Univ Vanderbilt | Potenciadores alostericos mglur4 de sulfona heterociclica, composiciones y metodos para tratar disfuncion neurologica. |
| UA110862C2 (uk) * | 2011-10-07 | 2016-02-25 | Ф. Хоффманн-Ля Рош Аг | Похідні етинілу як алостеричні модулятори метаботропного рецептора глутамату mglur 5 |
| CN102503888A (zh) * | 2011-10-08 | 2012-06-20 | 西安交通大学 | 2-芳基-1,3-异喹啉二酮类抗肿瘤化合物及其合成方法和用途 |
-
2014
- 2014-09-22 AU AU2014327504A patent/AU2014327504B2/en not_active Ceased
- 2014-09-22 WO PCT/EP2014/070100 patent/WO2015044075A1/en active Application Filing
- 2014-09-22 CN CN201480052343.0A patent/CN105579447B/zh active Active
- 2014-09-22 PL PL14781474T patent/PL3049409T3/pl unknown
- 2014-09-22 EA EA201690408A patent/EA029352B1/ru not_active IP Right Cessation
- 2014-09-22 EP EP14781474.3A patent/EP3049409B1/en active Active
- 2014-09-22 PE PE2016000237A patent/PE20160666A1/es active IP Right Grant
- 2014-09-22 MX MX2016002717A patent/MX370341B/es active IP Right Grant
- 2014-09-22 SI SI201430272T patent/SI3049409T1/sl unknown
- 2014-09-22 ES ES14781474.3T patent/ES2630319T3/es active Active
- 2014-09-22 BR BR112016005994A patent/BR112016005994A2/pt not_active Application Discontinuation
- 2014-09-22 JP JP2016517337A patent/JP6134441B2/ja active Active
- 2014-09-22 DK DK14781474.3T patent/DK3049409T3/en active
- 2014-09-22 SG SG11201602029VA patent/SG11201602029VA/en unknown
- 2014-09-22 UA UAA201604513A patent/UA116277C2/uk unknown
- 2014-09-22 CA CA2924376A patent/CA2924376A1/en not_active Abandoned
- 2014-09-22 MY MYPI2016000532A patent/MY183953A/en unknown
- 2014-09-22 HU HUE14781474A patent/HUE034849T2/en unknown
- 2014-09-22 MA MA38885A patent/MA38885B1/fr unknown
- 2014-09-22 KR KR1020167007447A patent/KR101757603B1/ko active IP Right Grant
- 2014-09-22 AR ARP140103499A patent/AR097721A1/es unknown
- 2014-09-23 TW TW103132854A patent/TWI527801B/zh not_active IP Right Cessation
-
2016
- 2016-02-09 IL IL244039A patent/IL244039B/en not_active IP Right Cessation
- 2016-02-16 CR CR20160075A patent/CR20160075A/es unknown
- 2016-03-04 PH PH12016500427A patent/PH12016500427A1/en unknown
- 2016-03-23 CL CL2016000677A patent/CL2016000677A1/es unknown
- 2016-03-25 US US15/081,573 patent/US20160207890A1/en not_active Abandoned
- 2016-07-15 HK HK16108345.7A patent/HK1220200A1/zh unknown
- 2016-09-30 US US15/283,010 patent/US9676732B2/en active Active
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2721776C2 (ru) * | 2015-07-15 | 2020-05-22 | Ф. Хоффманн-Ля Рош Аг | Производные этинила как модуляторы метаботропного рецептора глутамата |
| RU2721776C9 (ru) * | 2015-07-15 | 2020-10-22 | Ф. Хоффманн-Ля Рош Аг | Производные этинила как модуляторы метаботропного рецептора глутамата |
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