IL237369B - N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease - Google Patents
N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's diseaseInfo
- Publication number
- IL237369B IL237369B IL237369A IL23736915A IL237369B IL 237369 B IL237369 B IL 237369B IL 237369 A IL237369 A IL 237369A IL 23736915 A IL23736915 A IL 23736915A IL 237369 B IL237369 B IL 237369B
- Authority
- IL
- Israel
- Prior art keywords
- tetrafluoropropoxy
- benzylamine
- indol
- fluoro
- disease
- Prior art date
Links
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 title 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 239000000544 cholinesterase inhibitor Substances 0.000 title 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 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
- A61K31/40—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
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
- A61P25/28—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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698664P | 2012-09-09 | 2012-09-09 | |
| US201361782084P | 2013-03-14 | 2013-03-14 | |
| PCT/EP2013/068516 WO2014037532A1 (en) | 2012-09-09 | 2013-09-06 | Methods of treating alzheimer's disease and pharmaceutical compositions thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL237369A0 IL237369A0 (en) | 2015-04-30 |
| IL237369B true IL237369B (en) | 2018-11-29 |
Family
ID=49118521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL237369A IL237369B (en) | 2012-09-09 | 2015-02-23 | N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease |
Country Status (33)
| Country | Link |
|---|---|
| US (4) | US9375418B2 (2) |
| EP (1) | EP2892563B1 (2) |
| JP (2) | JP6693744B2 (2) |
| KR (2) | KR102342127B1 (2) |
| CN (1) | CN104619344A (2) |
| AP (1) | AP2015008306A0 (2) |
| AU (1) | AU2013311573B2 (2) |
| BR (1) | BR112015005117B1 (2) |
| CA (1) | CA2883751C (2) |
| CL (1) | CL2015000578A1 (2) |
| CY (1) | CY1121062T1 (2) |
| DK (1) | DK2892563T3 (2) |
| EA (1) | EA030448B1 (2) |
| ES (1) | ES2703630T3 (2) |
| GE (1) | GEP201706776B (2) |
| HR (1) | HRP20182069T1 (2) |
| IL (1) | IL237369B (2) |
| JO (1) | JO3459B1 (2) |
| LT (1) | LT2892563T (2) |
| MX (1) | MX368305B (2) |
| MY (1) | MY182539A (2) |
| NI (1) | NI201500031A (2) |
| NZ (1) | NZ630589A (2) |
| PL (1) | PL2892563T3 (2) |
| PT (1) | PT2892563T (2) |
| RS (1) | RS58104B1 (2) |
| RU (1) | RU2675786C2 (2) |
| SG (1) | SG11201501774QA (2) |
| SI (1) | SI2892563T1 (2) |
| SM (1) | SMT201800678T1 (2) |
| TN (1) | TN2015000076A1 (2) |
| TW (1) | TWI632909B (2) |
| WO (1) | WO2014037532A1 (2) |
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| DE602004000260T2 (de) | 2003-07-22 | 2006-08-24 | Arena Pharmaceuticals, Inc., San Diego | Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen |
| EP2508177A1 (en) | 2007-12-12 | 2012-10-10 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| US9126946B2 (en) | 2008-10-28 | 2015-09-08 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
| JO3459B1 (ar) | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
| US9604982B2 (en) | 2013-03-14 | 2017-03-28 | Janssen Pharmaceutica Nv | P2X7 modulators |
| TWI644671B (zh) | 2013-03-14 | 2018-12-21 | 比利時商健生藥品公司 | P2x7調節劑 |
| US9040534B2 (en) | 2013-03-14 | 2015-05-26 | Janssen Pharmaceutica Nv | [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators |
| JO3509B1 (ar) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| ES2845473T3 (es) | 2013-03-14 | 2021-07-26 | Boehringer Ingelheim Int | (Bencil-ciano-metil)-amidas sustituidas de ácido 2-aza-biciclo[2.2.1]heptano-3-carboxílico inhibidores de la catepsina- C |
| JO3639B1 (ar) | 2014-07-04 | 2020-08-27 | H Lundbeck As | صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد |
| EP3511331A1 (en) | 2014-09-12 | 2019-07-17 | Boehringer Ingelheim International GmbH | Spirocyclic inhibitors of cathepsin c |
| WO2016039977A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulators |
| AU2015315693B2 (en) | 2014-09-12 | 2020-01-16 | Janssen Pharmaceutica Nv | P2X7 modulating n-acyl-triazolopyrazines |
| CN105175307A (zh) * | 2014-11-18 | 2015-12-23 | 苏州晶云药物科技有限公司 | Lu AE58054的盐酸盐晶型A及其制备方法和用途 |
| JP2018515607A (ja) * | 2015-05-07 | 2018-06-14 | アクソファント サイエンシーズ ゲーエムベーハーAxovant Sciences Gmbh | 神経変性疾患を処置する組成物および方法 |
| US10022355B2 (en) | 2015-06-12 | 2018-07-17 | Axovant Sciences Gmbh | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of REM sleep behavior disorder |
| BR112018000728A2 (pt) | 2015-07-15 | 2018-09-04 | Axovant Sciences Gmbh | resumo método para a profilaxia e/ou tratamento de alucinações visuais em um sujeito com necessidade do mesmo |
| US10383849B2 (en) * | 2016-04-26 | 2019-08-20 | H. Lundbeck A/S | Use of an acetylcholinesterase inhibitor and idalopirdine for reducing falls in Parkinson's disease patients |
| US10864191B2 (en) | 2016-05-11 | 2020-12-15 | H. Lundbeck A/S | 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity |
| EA036347B1 (ru) | 2016-05-18 | 2020-10-29 | Сувен Лайф Сайенсиз Лимитед | Комбинация чистых антагонистов 5-ht6 рецепторов с ингибиторами ацетилхолинэстеразы |
| CN106309436A (zh) * | 2016-07-25 | 2017-01-11 | 宁波大学 | 可用作乙酰胆碱酯酶抑制剂的色胺衍生物及其用途 |
| CN107118146B (zh) * | 2017-04-13 | 2019-09-03 | 宁波大学 | 一种6-溴色胺衍生物及其制备方法和用途 |
| BR112019001145A2 (pt) * | 2017-05-24 | 2019-04-30 | H. Lundbeck A/S | combinação de um antagonista do receptor 5-ht6 e de um inibidor de acetilcolinesterase para uso no tratamento da doença de alzheimer em uma subpopulação de pacientes portadores de alelos de apoe4 |
| MY205440A (en) | 2018-09-28 | 2024-10-21 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| KR20210069079A (ko) | 2018-09-28 | 2021-06-10 | 얀센 파마슈티카 엔.브이. | 모노아실글리세롤 리파아제 조절제 |
| JP7697934B2 (ja) | 2019-09-30 | 2025-06-24 | ヤンセン ファーマシューティカ エヌ.ベー. | 放射線標識されたmgl petリガンド |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
| BR112022019077A2 (pt) | 2020-03-26 | 2022-12-27 | Janssen Pharmaceutica Nv | Moduladores da monoacilglicerol lipase |
| EP3960174B1 (en) | 2020-08-28 | 2024-10-30 | Westfälische Wilhelms-Universität Münster | Parasympathetic active phenyl-glycosid-substituted hydroxy-methyl-piperidine and -pyrrolidine alkaloids for medicinal use |
| WO2025198622A1 (en) * | 2024-03-22 | 2025-09-25 | Queen Aaric | Magnesium and lidocaine composition |
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| US3597149A (en) | 1969-04-29 | 1971-08-03 | Showa Denko Kk | Inhibition of gas-fume fading of dyed cellulose acetate material |
| FR2181559A1 (en) | 1972-04-28 | 1973-12-07 | Aec Chimie Organique Bio | N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity |
| JPS5764632A (en) | 1980-10-09 | 1982-04-19 | Mitsui Toatsu Chem Inc | Novel 2-arylethyl ether derivative and thioether derivative, their production and insecticide and acaricide |
| DE3632329A1 (de) | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| US5202336A (en) | 1986-09-24 | 1993-04-13 | Bayer Aktiengesellschaft | Antiflammatory quinolin methoxy phenylsulphonamides |
| SE9103745D0 (sv) | 1991-12-18 | 1991-12-18 | Wikstroem Haakan | Aryl-triflates and related compounds |
| DE69411143T2 (de) | 1993-09-01 | 1998-10-22 | Allelix Biopharma | Tryptamin analoge mit 5-ht1d selektivität |
| US5504101A (en) | 1994-05-06 | 1996-04-02 | Allelix Biopharmaceuticals, Inc. | 5-HT-1D receptor ligands |
| AU752008B2 (en) | 1997-09-29 | 2002-09-05 | Aventis Pharmaceuticals Inc. | Aminoalkylphenol derivatives and related compounds |
| GB9820113D0 (en) | 1998-09-15 | 1998-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| CA2353962C (en) | 1998-12-11 | 2009-09-29 | Virginia Commonwealth University | Selective 5-ht6 receptor ligands |
| CZ20012502A3 (cs) | 1999-01-13 | 2002-03-13 | Millennium Pharmaceuticals, Inc. | Funkcionalizované heterocykly jako modulátory chemokinových receptorů |
| US6750348B1 (en) | 1999-03-24 | 2004-06-15 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds |
| DK1859798T3 (en) | 2001-03-29 | 2016-03-21 | Lilly Co Eli | N- (2-arylethyl) -BENZYLAMINER as antagonists of 5-HT6 receptor |
| RU2252936C2 (ru) | 2002-12-05 | 2005-05-27 | Институт физиологически активных веществ РАН | S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты) |
| PE20071143A1 (es) * | 2006-01-13 | 2008-01-20 | Wyeth Corp | Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6 |
| JP2009541423A (ja) | 2006-06-23 | 2009-11-26 | ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ | コリンエステラーゼ阻害剤と5‐ht6レセプター親和性の化合物との組合せ |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| US20120184532A1 (en) * | 2009-07-23 | 2012-07-19 | Shire Llc | Galantamine amino acid and peptide prodrugs and uses thereof |
| TW201139370A (en) | 2009-12-23 | 2011-11-16 | Lundbeck & Co As H | Processes for the manufacture of a pharmaceutically active agent |
| JO3459B1 (ar) | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
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2013
- 2013-08-21 JO JOP/2013/0248A patent/JO3459B1/ar active
- 2013-09-06 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active Active
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 2013-09-06 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 SM SM20180678T patent/SMT201800678T1/it unknown
- 2013-09-06 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 BR BR112015005117-0A patent/BR112015005117B1/pt active IP Right Grant
- 2013-09-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active Ceased
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt unknown
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en not_active Ceased
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 EA EA201590353A patent/EA030448B1/ru not_active IP Right Cessation
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-09 US US14/021,033 patent/US9375418B2/en active Active
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2015
- 2015-02-23 IL IL237369A patent/IL237369B/en active IP Right Grant
- 2015-03-02 TN TNP2015000076A patent/TN2015000076A1/fr unknown
- 2015-03-06 NI NI201500031A patent/NI201500031A/es unknown
- 2015-03-06 CL CL2015000578A patent/CL2015000578A1/es unknown
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2016
- 2016-03-30 US US15/084,712 patent/US9687473B2/en active Active
- 2016-06-28 US US15/194,947 patent/US9789085B2/en active Active
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2017
- 2017-09-06 US US15/696,880 patent/US10660878B2/en active Active
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2018
- 2018-12-06 JP JP2018228631A patent/JP2019059760A/ja active Pending
- 2018-12-21 CY CY181101390T patent/CY1121062T1/el unknown
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