CL2015000578A1 - Compuesto n-(2-(6-fluoro-1-h-indol-3-il)etil)-3-(2,2,3,3-tetrafluoropropoxi)bencilamina o su sal, antagonista del receptor 5-ht6; composicion farmaceutica; uso en el tratamiento de la enfermedad de alzheimer. - Google Patents
Compuesto n-(2-(6-fluoro-1-h-indol-3-il)etil)-3-(2,2,3,3-tetrafluoropropoxi)bencilamina o su sal, antagonista del receptor 5-ht6; composicion farmaceutica; uso en el tratamiento de la enfermedad de alzheimer.Info
- Publication number
- CL2015000578A1 CL2015000578A1 CL2015000578A CL2015000578A CL2015000578A1 CL 2015000578 A1 CL2015000578 A1 CL 2015000578A1 CL 2015000578 A CL2015000578 A CL 2015000578A CL 2015000578 A CL2015000578 A CL 2015000578A CL 2015000578 A1 CL2015000578 A1 CL 2015000578A1
- Authority
- CL
- Chile
- Prior art keywords
- tetrafluoropropoxy
- benzylamine
- indol
- alzheimer
- fluoro
- Prior art date
Links
- YBAWYTYNMZWMMJ-UHFFFAOYSA-N 2-(6-fluoro-1h-indol-3-yl)-n-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine Chemical compound FC(F)C(F)(F)COC1=CC=CC(CNCCC=2C3=CC=C(F)C=C3NC=2)=C1 YBAWYTYNMZWMMJ-UHFFFAOYSA-N 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 239000003751 serotonin 6 antagonist Substances 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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698664P | 2012-09-09 | 2012-09-09 | |
| US201361782084P | 2013-03-14 | 2013-03-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CL2015000578A1 true CL2015000578A1 (es) | 2015-05-15 |
Family
ID=49118521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CL2015000578A CL2015000578A1 (es) | 2012-09-09 | 2015-03-06 | Compuesto n-(2-(6-fluoro-1-h-indol-3-il)etil)-3-(2,2,3,3-tetrafluoropropoxi)bencilamina o su sal, antagonista del receptor 5-ht6; composicion farmaceutica; uso en el tratamiento de la enfermedad de alzheimer. |
Country Status (33)
| Country | Link |
|---|---|
| US (4) | US9375418B2 (OSRAM) |
| EP (1) | EP2892563B1 (OSRAM) |
| JP (2) | JP6693744B2 (OSRAM) |
| KR (2) | KR102342127B1 (OSRAM) |
| CN (1) | CN104619344A (OSRAM) |
| AP (1) | AP2015008306A0 (OSRAM) |
| AU (1) | AU2013311573B2 (OSRAM) |
| BR (1) | BR112015005117B1 (OSRAM) |
| CA (1) | CA2883751C (OSRAM) |
| CL (1) | CL2015000578A1 (OSRAM) |
| CY (1) | CY1121062T1 (OSRAM) |
| DK (1) | DK2892563T3 (OSRAM) |
| EA (1) | EA030448B1 (OSRAM) |
| ES (1) | ES2703630T3 (OSRAM) |
| GE (1) | GEP201706776B (OSRAM) |
| HR (1) | HRP20182069T1 (OSRAM) |
| IL (1) | IL237369B (OSRAM) |
| JO (1) | JO3459B1 (OSRAM) |
| LT (1) | LT2892563T (OSRAM) |
| MX (1) | MX368305B (OSRAM) |
| MY (1) | MY182539A (OSRAM) |
| NI (1) | NI201500031A (OSRAM) |
| NZ (1) | NZ630589A (OSRAM) |
| PL (1) | PL2892563T3 (OSRAM) |
| PT (1) | PT2892563T (OSRAM) |
| RS (1) | RS58104B1 (OSRAM) |
| RU (1) | RU2675786C2 (OSRAM) |
| SG (1) | SG11201501774QA (OSRAM) |
| SI (1) | SI2892563T1 (OSRAM) |
| SM (1) | SMT201800678T1 (OSRAM) |
| TN (1) | TN2015000076A1 (OSRAM) |
| TW (1) | TWI632909B (OSRAM) |
| WO (1) | WO2014037532A1 (OSRAM) |
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| BRPI0412263B1 (pt) | 2003-07-22 | 2019-10-15 | Arena Pharmaceuticals, Inc. | Derivados de diaril e aril heteroaril uréia, uso e composição farmacêutica contendo os mesmos, bem como processo para preparação da dita composição |
| WO2009074607A1 (en) | 2007-12-12 | 2009-06-18 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| WO2009123714A2 (en) | 2008-04-02 | 2009-10-08 | 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 |
| EP3112366B1 (en) | 2013-03-14 | 2018-02-28 | Janssen Pharmaceutica NV | P2x7 modulators |
| JO3773B1 (ar) | 2013-03-14 | 2021-01-31 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調控劑 |
| ES2689526T3 (es) | 2013-03-14 | 2018-11-14 | Janssen Pharmaceutica Nv | Moduladores de P2X7 |
| AU2014230814B2 (en) | 2013-03-14 | 2017-12-21 | Boehringer Ingelheim International Gmbh | Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin 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 |
| EA201790600A1 (ru) | 2014-09-12 | 2017-07-31 | Янссен Фармацевтика Нв | Модулирующие p2x7 n-ацил-триазолопиразины |
| WO2016039977A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulators |
| KR102510588B1 (ko) | 2014-09-12 | 2023-03-17 | 베링거 인겔하임 인터내셔날 게엠베하 | 카텝신 c의 스피로사이클릭 억제제 |
| 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 |
| MX2017014192A (es) * | 2015-05-07 | 2018-08-01 | Axovant Sciences Gmbh | Composiciones y metodos de tratamiento de una enfermedad neurodegenerativa. |
| EP4119141A1 (en) | 2015-06-12 | 2023-01-18 | Axovant Sciences GmbH | Nelotanserin for the prophylaxis and treatment of rem sleep behavior disorder |
| EP3322415A4 (en) | 2015-07-15 | 2019-03-13 | Axovant Sciences GmbH | DIARYL AND ARYLHETEROARYL UREA DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR FOR PROPHYLAXIS AND TREATMENT OF HALLUCINATIONS RELATED TO A NEUROGENERATIVE DISEASE |
| CN118806909A (zh) * | 2016-04-26 | 2024-10-22 | H.隆德贝克有限公司 | 乙酰胆碱酯酶抑制剂和艾达鲁吡啶用于减少帕金森氏病患者跌倒的用途 |
| 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 |
| MX381768B (es) | 2016-05-18 | 2025-03-13 | Suven Life Sciences Ltd | Combinación de antagonistas puros del receptor 5-ht6 con inhibidores de la acetilcolinesterasa. |
| 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 |
| SMT202100240T1 (it) * | 2017-05-24 | 2021-05-07 | H Lundbeck As | Combinazione di un antagonista del recettore di 5-ht6 e un inibitore della acetilcolinesterasi per l'uso nel trattamento della malattia di alzheimer in una sottopopolazione di pazienti portatori di alleli apoe4 |
| MA53722A (fr) | 2018-09-28 | 2022-03-30 | Janssen Pharmaceutica Nv | Modulateurs de la monoacylglycérol lipase |
| WO2020065613A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CN114555596B (zh) | 2019-09-30 | 2025-02-25 | 詹森药业有限公司 | 放射性标记的mgl pet配体 |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
| US11891387B2 (en) | 2020-03-26 | 2024-02-06 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| 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 |
| CN121013715A (zh) * | 2024-03-22 | 2025-11-25 | 艾瑞克·奎因 | 镁和利多卡因组合物 |
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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 |
| US5202336A (en) | 1986-09-24 | 1993-04-13 | Bayer Aktiengesellschaft | Antiflammatory quinolin methoxy phenylsulphonamides |
| DE3632329A1 (de) | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| SE9103745D0 (sv) | 1991-12-18 | 1991-12-18 | Wikstroem Haakan | Aryl-triflates and related compounds |
| CA2147991A1 (en) | 1993-09-01 | 1995-03-09 | Richard A. Glennon | Tryptamine analogs with 5-ht1d selectivity |
| US5504101A (en) | 1994-05-06 | 1996-04-02 | Allelix Biopharmaceuticals, Inc. | 5-HT-1D receptor ligands |
| WO1999016746A1 (en) | 1997-09-29 | 1999-04-08 | Aventis Pharmaceuticals Inc. | Aminoalkylphenol derivatives and related compounds |
| GB9820113D0 (en) | 1998-09-15 | 1998-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| DK1149078T3 (da) | 1998-12-11 | 2006-07-10 | Univ Virginia Commonwealth | Selektive 5-HT6-receptorligander |
| MXPA01007033A (es) | 1999-01-13 | 2003-07-21 | Millennium Pharm Inc | Heterociclos funcionalizados como moduladores de receptores de quimiocinas. |
| US6750348B1 (en) | 1999-03-24 | 2004-06-15 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds |
| KR100894189B1 (ko) * | 2001-03-29 | 2009-04-22 | 일라이 릴리 앤드 캄파니 | 5-ｈｔ6 수용체의 길항제로서의 ｎ-(2-아릴에틸)벤질아민 |
| 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 |
| PT2040755E (pt) | 2006-06-23 | 2011-07-08 | Esteve Labor Dr | Combinação de um inibidor de colinesterase e um composto com afinidade para o receptor 5-ht6 |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| AU2010275431A1 (en) * | 2009-07-23 | 2012-02-23 | 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 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 BR BR112015005117-0A patent/BR112015005117B1/pt active IP Right Grant
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en not_active Ceased
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt unknown
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active Active
- 2013-09-06 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 EA EA201590353A patent/EA030448B1/ru not_active IP Right Cessation
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 SM SM20180678T patent/SMT201800678T1/it unknown
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active Ceased
- 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 CL CL2015000578A patent/CL2015000578A1/es unknown
- 2015-03-06 NI NI201500031A patent/NI201500031A/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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