JP6196551B2 - ビロキサジン塩を製造する方法及びその新規な多形 - Google Patents
ビロキサジン塩を製造する方法及びその新規な多形 Download PDFInfo
- Publication number
- JP6196551B2 JP6196551B2 JP2013505028A JP2013505028A JP6196551B2 JP 6196551 B2 JP6196551 B2 JP 6196551B2 JP 2013505028 A JP2013505028 A JP 2013505028A JP 2013505028 A JP2013505028 A JP 2013505028A JP 6196551 B2 JP6196551 B2 JP 6196551B2
- Authority
- JP
- Japan
- Prior art keywords
- viloxazine
- group
- base
- reaction
- epichlorohydrin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Links
- 0 C=*N(CCO)CC(COc1ccccc1)O Chemical compound C=*N(CCO)CC(COc1ccccc1)O 0.000 description 1
- YWPHCCPCQOJSGZ-NSHDSACASA-N CCOc(cccc1)c1OC[C@H]1OCCNC1 Chemical compound CCOc(cccc1)c1OC[C@H]1OCCNC1 YWPHCCPCQOJSGZ-NSHDSACASA-N 0.000 description 1
- YWPHCCPCQOJSGZ-LLVKDONJSA-N CCOc1ccccc1OC[C@@H]1OCCNC1 Chemical compound CCOc1ccccc1OC[C@@H]1OCCNC1 YWPHCCPCQOJSGZ-LLVKDONJSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/32—Alcohol-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/28—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
- C07C217/30—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring
- C07C217/32—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
- C07C217/34—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines having the oxygen atom of at least one of the etherified hydroxy groups further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
- C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32315110P | 2010-04-12 | 2010-04-12 | |
| US61/323,151 | 2010-04-12 | ||
| PCT/US2011/032013 WO2011130194A2 (en) | 2010-04-12 | 2011-04-12 | Methods for producing viloxazine salts and novel polymorphs thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015141683A Division JP2016006062A (ja) | 2010-04-12 | 2015-07-15 | ビロキサジン塩を製造する方法及びその新規な多形 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013530129A JP2013530129A (ja) | 2013-07-25 |
| JP6196551B2 true JP6196551B2 (ja) | 2017-09-13 |
Family
ID=44065289
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013505028A Active JP6196551B2 (ja) | 2010-04-12 | 2011-04-12 | ビロキサジン塩を製造する方法及びその新規な多形 |
| JP2015141683A Pending JP2016006062A (ja) | 2010-04-12 | 2015-07-15 | ビロキサジン塩を製造する方法及びその新規な多形 |
| JP2016199937A Pending JP2017039754A (ja) | 2010-04-12 | 2016-10-11 | ビロキサジン塩を製造する方法及びその新規な多形 |
| JP2017227668A Active JP6663413B2 (ja) | 2010-04-12 | 2017-11-28 | ビロキサジン又はその薬学的に許容される塩を製造する方法 |
| JP2019103598A Pending JP2019194191A (ja) | 2010-04-12 | 2019-06-03 | ビロキサジン塩を製造する方法及びその新規な多形 |
Family Applications After (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015141683A Pending JP2016006062A (ja) | 2010-04-12 | 2015-07-15 | ビロキサジン塩を製造する方法及びその新規な多形 |
| JP2016199937A Pending JP2017039754A (ja) | 2010-04-12 | 2016-10-11 | ビロキサジン塩を製造する方法及びその新規な多形 |
| JP2017227668A Active JP6663413B2 (ja) | 2010-04-12 | 2017-11-28 | ビロキサジン又はその薬学的に許容される塩を製造する方法 |
| JP2019103598A Pending JP2019194191A (ja) | 2010-04-12 | 2019-06-03 | ビロキサジン塩を製造する方法及びその新規な多形 |
Country Status (8)
| Country | Link |
|---|---|
| US (7) | US9403783B2 (https=) |
| EP (1) | EP2558437B1 (https=) |
| JP (5) | JP6196551B2 (https=) |
| AU (1) | AU2011240773C1 (https=) |
| CA (4) | CA3215310A1 (https=) |
| ES (1) | ES2552166T3 (https=) |
| MX (5) | MX347218B (https=) |
| WO (1) | WO2011130194A2 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX347218B (es) * | 2010-04-12 | 2017-04-20 | Supernus Pharmaceuticals Inc | Metodos para producir sales de viloxazina y polimorfos novedosos de las mismas. |
| CN110799191B (zh) | 2017-06-16 | 2023-05-26 | 贝塔制药有限公司 | N-(2-(2-(二甲氨基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)氨基)苯基)丙烯酰胺及其盐的药物制剂 |
| CN108760719A (zh) * | 2018-08-17 | 2018-11-06 | 北京理工大学 | 一种利用拉曼光谱分析cl-20的晶型纯度的方法 |
| KR20260023103A (ko) | 2021-03-18 | 2026-02-20 | 슈퍼너스 파마슈티컬스, 인크. | 치환된 몰폴린의 유도체 및 이의 용도 |
| KR20250134715A (ko) * | 2022-03-18 | 2025-09-11 | 슈퍼너스 파마슈티컬스, 인크. | 치환된 몰폴린의 유도체의 제조 방법 |
| WO2023248154A1 (en) * | 2022-06-22 | 2023-12-28 | Glenmark Life Sciences Limited | Process for the preparation of viloxazine hydrochloride |
| EP4317141A1 (en) | 2022-08-04 | 2024-02-07 | Curia Spain S.A.U. | Process and intermediates for the preparation of viloxazine and other 2-substituted morpholine derivatives |
| CN119707868A (zh) * | 2023-09-27 | 2025-03-28 | 西安远大科创医药科技有限公司 | 一种盐酸维洛沙嗪产品杂质及其合成方法与应用 |
| CN119707851A (zh) * | 2023-09-27 | 2025-03-28 | 西安远大科创医药科技有限公司 | 一种盐酸维洛沙嗪产品杂质及其合成方法与应用 |
| KR20250094621A (ko) * | 2023-12-18 | 2025-06-25 | 주식회사 아스트로젠 | (s)-빌록사진 또는 이의 염의 개선된 제조 방법 |
| WO2025219523A1 (en) | 2024-04-19 | 2025-10-23 | Cambrex Profarmaco Milano S.R.L. | "intermediates and processes for the preparation of viloxazine" |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
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| GB1138405A (en) | 1966-12-28 | 1969-01-01 | Ici Ltd | Morpholine derivatives |
| US3712890A (en) * | 1969-06-20 | 1973-01-23 | Ici Ltd | Process for making 2-aryloxymethyl morpholines |
| US3857839A (en) * | 1969-06-20 | 1974-12-31 | Ici Ltd | For cyclising 1-aryloxy-3 beta-substituted ethylamino-2-propanols |
| ES411826A1 (es) * | 1973-02-20 | 1976-01-01 | Liade Sa Lab | Procedimiento de obtencion de 1-ariloxi - 2 - propanolami- nas farmacologicamente activos. |
| JPS5188972A (en) | 1975-01-29 | 1976-08-04 | 22*77 indeniruokishimechiru **4 chikanmoruhorinjudotainoseiho | |
| JPS5283677A (en) | 1976-01-01 | 1977-07-12 | Yamanouchi Pharmaceut Co Ltd | Derivative of 2-(7-indenyloxymethyl)-4-substituted morpholine |
| US4711887A (en) * | 1982-04-23 | 1987-12-08 | Imperial Chemical Industries Plc | Hydrazinopyridazine compounds |
| JPH06306025A (ja) * | 1992-11-30 | 1994-11-01 | Sankyo Co Ltd | ジアリールアルカン誘導体 |
| US5760069A (en) * | 1995-02-08 | 1998-06-02 | Boehringer Mannheim Pharmaceuticals Corporation-Smithkline Beecham Corporation Limited Partnership #1 | Method of treatment for decreasing mortality resulting from congestive heart failure |
| CA2214034A1 (en) * | 1995-03-10 | 1996-09-19 | University Of Iowa Research Foundation | Preparation of n-arylmethyl aziridine derivatives, 1,4,7,10-tetraazacyclododecane derivatives obtained therefrom and n-arylmethyl-ethanol-amine sulphonate esters as intermediates |
| AUPO565997A0 (en) * | 1997-03-17 | 1997-04-10 | Fujisawa Pharmaceutical Co., Ltd. | Propanolamine derivatives |
| US6953855B2 (en) * | 1998-12-11 | 2005-10-11 | Targacept, Inc. | 3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof |
| DE19919153A1 (de) * | 1999-04-27 | 2000-11-02 | Consortium Elektrochem Ind | Herstellung von acrylierten flüssigkristallinen Verbindungen |
| FR2796069B3 (fr) * | 1999-07-09 | 2001-08-24 | Sanofi Synthelabo | Nouveaux procedes de preparation de derives de 2-(2- arylmorpholin-2-yl)ethanol substitues, enantiomeriquement purs, et composes intermediaires utiles dans ces procedes |
| PT1257277E (pt) * | 2000-02-24 | 2005-09-30 | Pharmacia & Upjohn Co Llc | Novas combinacoes de farmacos |
| US20030040436A1 (en) * | 2000-10-23 | 2003-02-27 | Emerson Ralph W. | Use of benzyl ester compositions for controlling non-arthropod pest populations |
| TWI329105B (en) * | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| US7326790B2 (en) * | 2003-05-02 | 2008-02-05 | Rigel Pharmaceuticals, Inc. | Diphenylisoxazole compounds and hydro isomers thereof |
| JP4210573B2 (ja) * | 2003-10-10 | 2009-01-21 | 花王株式会社 | 置換フェノキシプロパノールアミン類 |
| CA2567935C (en) * | 2004-05-27 | 2009-10-27 | Pfizer Limited | Aminopyridine derivatives as selective dopamine d3 agonists |
| US20060118002A1 (en) * | 2004-12-03 | 2006-06-08 | Sud-Chemie Inc. | Organoclay composition containing quat mixtures |
| KR20080045266A (ko) * | 2005-09-06 | 2008-05-22 | 스미스클라인 비참 코포레이션 | 벤즈이미다졸 티오펜을 제조하기 위한 위치선택적인 방법 |
| PE20070855A1 (es) * | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
| CN100415709C (zh) * | 2006-05-15 | 2008-09-03 | 西北大学 | β-(3,4-二羟基苯基)-α-羟基丙酸冰片酯、其合成方法和用途 |
| WO2008047388A2 (en) | 2006-10-20 | 2008-04-24 | Ind-Swift Laboratories Limited | Improved process for the preparation of ranolazine |
| ES2539947T3 (es) * | 2008-06-02 | 2015-07-07 | Cipla Limited | Procedimiento para la síntesis de arformoterol |
| EP2341912B1 (en) * | 2008-09-05 | 2014-01-22 | Supernus Pharmaceuticals, Inc. | Method of treatment of attention deficit/hyperactivity disorder (adhd) |
| US9296940B2 (en) * | 2009-12-21 | 2016-03-29 | Baker Hughes Incorporated | Dithiazine derivatives |
| MX347218B (es) * | 2010-04-12 | 2017-04-20 | Supernus Pharmaceuticals Inc | Metodos para producir sales de viloxazina y polimorfos novedosos de las mismas. |
| TWI596088B (zh) * | 2011-01-25 | 2017-08-21 | 陶氏農業科學公司 | 4-胺基-6-(經取代的苯基)吡啶甲酸酯及6-胺基-2-(經取代的苯基)-4-嘧啶羧酸酯之芳烷酯以及其等作為除草劑之用途 |
| EP2922849B1 (en) * | 2012-11-21 | 2017-07-12 | RaQualia Pharma Inc. | Polymorphs of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2h-pyran-4-carboxylic acid as 5-hydroxytryptamine-4 (5-ht4) receptor agonists for the treatment of gastrointestinal diseases |
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2011
- 2011-04-12 MX MX2014010356A patent/MX347218B/es unknown
- 2011-04-12 MX MX2014010369A patent/MX357614B/es unknown
- 2011-04-12 AU AU2011240773A patent/AU2011240773C1/en active Active
- 2011-04-12 WO PCT/US2011/032013 patent/WO2011130194A2/en not_active Ceased
- 2011-04-12 CA CA3215310A patent/CA3215310A1/en active Pending
- 2011-04-12 MX MX2014010358A patent/MX357613B/es unknown
- 2011-04-12 JP JP2013505028A patent/JP6196551B2/ja active Active
- 2011-04-12 CA CA3126096A patent/CA3126096C/en active Active
- 2011-04-12 EP EP11718804.5A patent/EP2558437B1/en active Active
- 2011-04-12 CA CA2795408A patent/CA2795408C/en active Active
- 2011-04-12 US US13/084,612 patent/US9403783B2/en active Active
- 2011-04-12 MX MX2012011821A patent/MX2012011821A/es active IP Right Grant
- 2011-04-12 MX MX2014010368A patent/MX355697B/es unknown
- 2011-04-12 CA CA2992219A patent/CA2992219A1/en not_active Abandoned
- 2011-04-12 ES ES11718804.5T patent/ES2552166T3/es active Active
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2014
- 2014-12-19 US US14/577,380 patent/US9434703B2/en active Active
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2015
- 2015-07-15 JP JP2015141683A patent/JP2016006062A/ja active Pending
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2016
- 2016-06-24 US US15/192,098 patent/US10005743B2/en active Active
- 2016-10-11 JP JP2016199937A patent/JP2017039754A/ja active Pending
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2017
- 2017-11-28 JP JP2017227668A patent/JP6663413B2/ja active Active
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2018
- 2018-05-24 US US15/988,190 patent/US10160733B2/en active Active
- 2018-11-13 US US16/189,299 patent/US20190300492A1/en not_active Abandoned
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2019
- 2019-06-03 JP JP2019103598A patent/JP2019194191A/ja active Pending
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2021
- 2021-08-04 US US17/393,834 patent/US20220024885A1/en active Pending
-
2025
- 2025-09-15 US US19/328,907 patent/US20260008759A1/en active Pending
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