PE20120617A1 - Procesos para preparar cobicistat y sus productos intermedios - Google Patents
Procesos para preparar cobicistat y sus productos intermediosInfo
- Publication number
- PE20120617A1 PE20120617A1 PE2011001737A PE2011001737A PE20120617A1 PE 20120617 A1 PE20120617 A1 PE 20120617A1 PE 2011001737 A PE2011001737 A PE 2011001737A PE 2011001737 A PE2011001737 A PE 2011001737A PE 20120617 A1 PE20120617 A1 PE 20120617A1
- Authority
- PE
- Peru
- Prior art keywords
- compound
- formula
- prepare
- cobicistat
- processes
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
- C07C209/62—Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
- C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
- C07C209/70—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton by reduction of unsaturated amines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
- C07C303/34—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfuric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C307/02—Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
- C07C307/04—Diamides of sulfuric acids
- C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D277/28—Radicals substituted by nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Abstract
REFERIDA A UN METODO PARA PREPARAR UN COMPUESTO DE FORMULA (I) QUE COMPRENDE a) DIMERIZAR UN COMPUESTO DE FORMULA (II) PARA PROPORCIONAR UN COMPUESTO DE FORMULA (V), b) DESPROTEGER EL COMPUESTO (V) PROPORCIONANDO UN COMPUESTO (VI), c) REDUCIR EL COMPUESTO (VI) A UN COMPUESTO (VII), d) CONVERTIR EL COMPUESTO (VII) A LA SAL CORRESPONDIENTE MEDIANTE TRATAMIENTO CON UN ACIDO Y UN SOLVENTE ORGANICO, e) CONVERTIR LA SAL DE d) EN UN COMPUESTO DE FORMULA (IX) Y f) ACOPLAR EL COMPUESTO (IX) CON UN ACIDO DE FORMULA (Xa) PROPORCIONANDO EL COMPUESTO DE FORMULA (I), DONDE R1 ES -S(=O)2NRaRb; Ra Y Rb SON ALQUILO C1-C8 O JUNTOS Ra Y Rb FORMAN CON EL NITROGENO AL CUAL ESTAN UNIDOS UN ANILLO SATURADO DE 3 O 4 MIEMBROS O UN ANILLO SATURADO O PARCIALMENTE INSATURADO DE 5, 6 O 7 MIEMBROS QUE COMPRENDE 1 O 2 HETEROATOMOS
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US16649809P | 2009-04-03 | 2009-04-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20120617A1 true PE20120617A1 (es) | 2012-05-26 |
Family
ID=42634770
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2011001737A PE20120617A1 (es) | 2009-04-03 | 2010-04-01 | Procesos para preparar cobicistat y sus productos intermedios |
Country Status (27)
Country | Link |
---|---|
US (4) | US8497396B2 (es) |
EP (2) | EP3009434A1 (es) |
JP (8) | JP5612662B2 (es) |
KR (3) | KR20180077324A (es) |
CN (4) | CN107382997B (es) |
AP (1) | AP2887A (es) |
AR (1) | AR076027A1 (es) |
AU (1) | AU2010232559B2 (es) |
BR (1) | BRPI1012638B8 (es) |
CA (4) | CA3083433C (es) |
CL (1) | CL2011002370A1 (es) |
CO (1) | CO6400216A2 (es) |
EA (2) | EA022739B1 (es) |
EC (1) | ECSP11011391A (es) |
ES (1) | ES2548252T3 (es) |
HK (4) | HK1166976A1 (es) |
IL (4) | IL215399A (es) |
MX (2) | MX2011010397A (es) |
NZ (4) | NZ617773A (es) |
PE (1) | PE20120617A1 (es) |
PT (1) | PT2414325E (es) |
SG (2) | SG174585A1 (es) |
TW (2) | TWI464165B (es) |
UA (1) | UA108738C2 (es) |
UY (1) | UY32535A (es) |
WO (1) | WO2010115000A2 (es) |
ZA (1) | ZA201107430B (es) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA108738C2 (uk) * | 2009-04-03 | 2015-06-10 | Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки | |
JP2012140390A (ja) * | 2011-01-06 | 2012-07-26 | Sumitomo Chemical Co Ltd | α−アミノ−γ−ブチロラクトンの製造方法 |
US20140187771A1 (en) * | 2011-05-02 | 2014-07-03 | Gilead Sciences, Inc. | Amorphous solid salts |
SG11201404527QA (en) | 2012-02-03 | 2014-08-28 | Gilead Sciences Inc | Methods and intermediates for preparing pharmaceutical agents |
CN103694196A (zh) * | 2012-09-27 | 2014-04-02 | 上海迪赛诺化学制药有限公司 | 细胞色素p450单加氧酶抑制剂中间体及其制法和用途 |
WO2014047849A1 (zh) * | 2012-09-27 | 2014-04-03 | 上海迪赛诺化学制药有限公司 | 细胞色素p450单加氧酶抑制剂中间体及其制法和用途 |
WO2014057498A2 (en) | 2012-10-08 | 2014-04-17 | Mylan Laboratories Ltd. | Process for the preparation of cobicistat intermediates |
US20160200716A1 (en) * | 2012-12-26 | 2016-07-14 | Assia Chemical Industries Ltd. | Cobicistat dichlohydrate salt |
CN104370777A (zh) * | 2013-08-13 | 2015-02-25 | 上海迪赛诺化学制药有限公司 | 合成(2r,5r)-1,6-二苯基己烷-2,5-二胺及其盐的中间体及所述中间体的制备方法和应用 |
WO2015079415A1 (en) * | 2013-11-29 | 2015-06-04 | Mylan Laboratories Ltd. | Amorphous cobicistat solid dispersion |
EP3077373B1 (en) | 2013-12-03 | 2018-09-12 | Mylan Laboratories Ltd. | Preparation of cobicistat intermediates |
CN104193643B (zh) * | 2014-09-12 | 2016-02-10 | 宁波九胜创新医药科技有限公司 | 用于合成抗艾滋病药物增强剂cobicistat的中间体 |
CN104447472A (zh) * | 2014-11-06 | 2015-03-25 | 江苏森萱医药化工股份有限公司 | D)-2-苄基-n,n-二甲基氮杂环丙烷基-1-磺酰胺合成方法 |
CN104557565B (zh) * | 2015-01-08 | 2016-07-06 | 浙江工业大学 | 抗艾滋病药物增强剂Cobicistat关键中间体盐酸盐的制备方法 |
WO2016128885A1 (en) * | 2015-02-09 | 2016-08-18 | Laurus Labs Private Limited | A process for preparation of cobicistat |
US10351556B2 (en) | 2015-02-18 | 2019-07-16 | Msn Laboratories Private Limited | Process for the preparation of 1,3-thiazol-5-ylmethyl [(2R,5R)-5-{[(2s)-2-[(methyl{[2-(propan-2-yl)-1,3-thiazol-4YL] methyl} carbamoyl) amino]-4-(morpholin-4-yl)butanoyl]amino)-1,6-diphenylhexan-2-yl]carbamate |
CN107674039A (zh) * | 2016-08-01 | 2018-02-09 | 上海朴颐化学科技有限公司 | 一种可比西他中间体的制备方法 |
EP3518935A1 (en) | 2016-09-27 | 2019-08-07 | Gilead Sciences, Inc. | Therapeutic compositions for treatment of human immunodeficiency virus |
CN109912530A (zh) * | 2017-12-13 | 2019-06-21 | 上海奥博生物医药技术有限公司 | 一种可比司他原料杂质的制备方法 |
CN109232301B (zh) * | 2018-10-15 | 2021-01-01 | 天津希恩思生化科技有限公司 | 一种四异丙基肼的制备方法 |
CN110642721B (zh) * | 2018-12-21 | 2022-09-30 | 安徽贝克生物制药有限公司 | 盐酸司来吉兰的制备方法 |
CN110878071A (zh) * | 2019-11-21 | 2020-03-13 | 华南农业大学 | 一种α-氨基-γ-丁内酯及其盐的制备方法 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI1183026T1 (sl) * | 1999-06-04 | 2006-10-31 | Abbott Lab | Izboljsane farmacevtske spojine, vsebujoce ritonavir |
US20030153771A1 (en) | 2001-09-27 | 2003-08-14 | Kolb Hartmuth C. | Large scale synthesis of optically pure aziridines |
WO2003106445A1 (en) * | 2002-06-12 | 2003-12-24 | Qsi Pharma A/S | Compounds and methods for controlling bacterial virulence |
CA2573692A1 (en) * | 2004-07-23 | 2006-02-23 | The Procter & Gamble Company | Liquid detergent composition for improved low temperature grease cleaning and starch soil cleaning |
US7786153B2 (en) * | 2005-03-02 | 2010-08-31 | Abbott Laboratories Inc. | Compounds that are useful for improving pharmacokinetics |
CN103275033B (zh) * | 2006-07-07 | 2015-04-29 | 吉里德科学公司 | 治疗剂的药代动力学特性调节剂 |
US9891239B2 (en) * | 2007-02-23 | 2018-02-13 | Gilead Sciences, Inc. | Modulators of pharmacokinetic properties of therapeutics |
CN101796040A (zh) * | 2007-07-06 | 2010-08-04 | 吉里德科学公司 | 治疗剂的药代动力学特性调节剂 |
AU2008346823B2 (en) * | 2008-01-04 | 2015-03-12 | Gilead Sciences, Inc. | Inhibitors of cytochrome P450 |
US10039718B2 (en) | 2008-05-02 | 2018-08-07 | Gilead Sciences, Inc. | Use of solid carrier particles to improve the processability of a pharmaceutical agent |
UA108738C2 (uk) | 2009-04-03 | 2015-06-10 | Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки |
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2010
- 2010-01-04 UA UAA201111540A patent/UA108738C2/ru unknown
- 2010-03-31 TW TW99109929A patent/TWI464165B/zh active
- 2010-03-31 AR ARP100101077 patent/AR076027A1/es unknown
- 2010-03-31 TW TW103133537A patent/TW201518283A/zh unknown
- 2010-04-01 ES ES10713075.9T patent/ES2548252T3/es active Active
- 2010-04-01 BR BRPI1012638A patent/BRPI1012638B8/pt active IP Right Grant
- 2010-04-01 KR KR1020187018487A patent/KR20180077324A/ko not_active Application Discontinuation
- 2010-04-01 CN CN201710518109.8A patent/CN107382997B/zh active Active
- 2010-04-01 US US12/752,639 patent/US8497396B2/en active Active
- 2010-04-01 CA CA3083433A patent/CA3083433C/en active Active
- 2010-04-01 PT PT107130759T patent/PT2414325E/pt unknown
- 2010-04-01 MX MX2011010397A patent/MX2011010397A/es active IP Right Grant
- 2010-04-01 WO PCT/US2010/029633 patent/WO2010115000A2/en active Application Filing
- 2010-04-01 NZ NZ617773A patent/NZ617773A/en unknown
- 2010-04-01 AU AU2010232559A patent/AU2010232559B2/en active Active
- 2010-04-01 CN CN202010112624.8A patent/CN111217808A/zh active Pending
- 2010-04-01 SG SG2011069937A patent/SG174585A1/en unknown
- 2010-04-01 SG SG10201404926UA patent/SG10201404926UA/en unknown
- 2010-04-01 CA CA2925137A patent/CA2925137C/en active Active
- 2010-04-01 EA EA201190179A patent/EA022739B1/ru unknown
- 2010-04-01 EP EP15171216.3A patent/EP3009434A1/en not_active Withdrawn
- 2010-04-01 JP JP2012503704A patent/JP5612662B2/ja active Active
- 2010-04-01 PE PE2011001737A patent/PE20120617A1/es active IP Right Grant
- 2010-04-01 EP EP10713075.9A patent/EP2414325B1/en active Active
- 2010-04-01 NZ NZ708978A patent/NZ708978A/en unknown
- 2010-04-01 NZ NZ59486410A patent/NZ594864A/en unknown
- 2010-04-01 CN CN201080014307.7A patent/CN102438982B/zh active Active
- 2010-04-01 CA CA2754698A patent/CA2754698C/en active Active
- 2010-04-01 NZ NZ726536A patent/NZ726536A/en unknown
- 2010-04-01 MX MX2013003678A patent/MX338731B/es unknown
- 2010-04-01 KR KR1020177009970A patent/KR101874557B1/ko active IP Right Grant
- 2010-04-01 CN CN201510160505.9A patent/CN104876888B/zh active Active
- 2010-04-01 AP AP2011005864A patent/AP2887A/xx active
- 2010-04-01 CA CA3008903A patent/CA3008903C/en active Active
- 2010-04-01 EA EA201590979A patent/EA201590979A1/ru unknown
- 2010-04-01 KR KR1020117026120A patent/KR101728375B1/ko active IP Right Grant
- 2010-04-05 UY UY32535A patent/UY32535A/es not_active Application Discontinuation
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2011
- 2011-09-06 CO CO11114749A patent/CO6400216A2/es not_active Application Discontinuation
- 2011-09-26 CL CL2011002370A patent/CL2011002370A1/es unknown
- 2011-09-27 IL IL215399A patent/IL215399A/en active IP Right Grant
- 2011-10-11 ZA ZA2011/07430A patent/ZA201107430B/en unknown
- 2011-10-12 EC ECSP11011391 patent/ECSP11011391A/es unknown
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2012
- 2012-08-06 HK HK12107693.1A patent/HK1166976A1/zh unknown
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2013
- 2013-06-24 US US13/925,302 patent/US8853210B2/en active Active
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2014
- 2014-05-20 JP JP2014104007A patent/JP5986599B2/ja active Active
- 2014-09-03 US US14/476,622 patent/US9115100B2/en active Active
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2015
- 2015-03-10 IL IL237642A patent/IL237642A/en active IP Right Grant
- 2015-03-10 IL IL237643A patent/IL237643A/en active IP Right Grant
- 2015-07-14 US US14/799,090 patent/US9428473B2/en active Active
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2016
- 2016-01-28 JP JP2016014135A patent/JP6180561B2/ja active Active
- 2016-03-02 HK HK16102438.8A patent/HK1214265A1/zh unknown
- 2016-09-09 HK HK16110713.7A patent/HK1223912A1/zh unknown
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2017
- 2017-01-11 IL IL250068A patent/IL250068A0/en unknown
- 2017-02-27 JP JP2017034914A patent/JP6336161B2/ja active Active
- 2017-07-28 JP JP2017146329A patent/JP6491706B2/ja active Active
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2018
- 2018-04-23 HK HK18105259.5A patent/HK1245785A1/zh unknown
- 2018-06-18 JP JP2018115527A patent/JP2018162274A/ja not_active Withdrawn
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2020
- 2020-08-07 JP JP2020134426A patent/JP2020189861A/ja not_active Withdrawn
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2022
- 2022-10-19 JP JP2022167506A patent/JP2023002679A/ja not_active Withdrawn
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