CN106998685A - 14‑元酮内酯及其制备和使用方法 - Google Patents
14‑元酮内酯及其制备和使用方法 Download PDFInfo
- Publication number
- CN106998685A CN106998685A CN201580066344.5A CN201580066344A CN106998685A CN 106998685 A CN106998685 A CN 106998685A CN 201580066344 A CN201580066344 A CN 201580066344A CN 106998685 A CN106998685 A CN 106998685A
- Authority
- CN
- China
- Prior art keywords
- optionally substituted
- alkyl
- compound
- hydrogen
- group
- 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.)
- Pending
Links
- 0 CC(C[C@@](*)C(C[C@@](C(COC([C@@](C)C([C@@]1C)=O)=O)=*2)N(CCCC[n]3nnc(-c4cc(N)ccc4)c3)C2=*)=O)[C@@]1OC1OC(CI)CC([*+]2*C2)C1O Chemical compound CC(C[C@@](*)C(C[C@@](C(COC([C@@](C)C([C@@]1C)=O)=O)=*2)N(CCCC[n]3nnc(-c4cc(N)ccc4)c3)C2=*)=O)[C@@]1OC1OC(CI)CC([*+]2*C2)C1O 0.000 description 22
- BMLOTRRICALRKN-XGEHTFHBSA-N C[C@H](C[C@@H]1N(C)C)O[C@@H](C)[C@@H]1O Chemical compound C[C@H](C[C@@H]1N(C)C)O[C@@H](C)[C@@H]1O BMLOTRRICALRKN-XGEHTFHBSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
- C07H17/08—Hetero rings containing eight or more ring members, e.g. erythromycins
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P31/04—Antibacterial agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Tropical Medicine & Parasitology (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462061571P | 2014-10-08 | 2014-10-08 | |
| US62/061,571 | 2014-10-08 | ||
| PCT/US2015/054700 WO2016057798A1 (en) | 2014-10-08 | 2015-10-08 | 14-membered ketolides and methods of their preparation and use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106998685A true CN106998685A (zh) | 2017-08-01 |
Family
ID=55653777
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201580066344.5A Pending CN106998685A (zh) | 2014-10-08 | 2015-10-08 | 14‑元酮内酯及其制备和使用方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10633407B2 (enExample) |
| EP (1) | EP3211997A4 (enExample) |
| JP (1) | JP2017531663A (enExample) |
| CN (1) | CN106998685A (enExample) |
| CA (1) | CA2963815A1 (enExample) |
| HK (1) | HK1242920A1 (enExample) |
| WO (1) | WO2016057798A1 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113646319A (zh) * | 2018-11-19 | 2021-11-12 | 齐卡尼治疗股份有限公司 | C11-环取代的13元大环内酯及其用途 |
| WO2025228440A1 (zh) * | 2024-04-30 | 2025-11-06 | 苏州信诺维医药科技股份有限公司 | 大环内酯类化合物、其制备方法及其用途 |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2014248014B2 (en) | 2013-04-04 | 2018-11-08 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
| EP3211997A4 (en) | 2014-10-08 | 2018-10-24 | President and Fellows of Harvard College | 14-membered ketolides and methods of their preparation and use |
| EP3273969A4 (en) | 2015-03-25 | 2018-11-21 | President and Fellows of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
| US11673910B2 (en) | 2017-04-28 | 2023-06-13 | Zikani Therapeutics, Inc. | Macrolides with modified desosamine sugars and uses thereof |
| SG11202105227QA (en) | 2018-11-19 | 2021-06-29 | Zikani Therapeutics Inc | C10-alkylene substituted 13-membered macrolides and uses thereof |
| IL303173A (en) * | 2023-05-23 | 2024-12-01 | Yeda Res & Dev | Active macrolide antibiotic compounds against pathogens |
Citations (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002032918A2 (en) * | 2000-10-18 | 2002-04-25 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| CN1351608A (zh) * | 1999-05-24 | 2002-05-29 | 辉瑞产品公司 | 13-甲基红霉素衍生物 |
| CN1373767A (zh) * | 1999-04-16 | 2002-10-09 | 奥索-麦克尼尔药品公司 | 酮式大环内酯抗菌剂 |
| WO2003050132A1 (en) * | 2001-12-05 | 2003-06-19 | Ortho-Mcneil Pharmaceutical, Inc. | 6-o-acyl ketolide derivatives of erythromycine useful as antibacterials |
| WO2004080391A2 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| US20050090461A1 (en) * | 1998-06-29 | 2005-04-28 | Leadlay Peter F. | Polyketides and their synthesis |
| US6939861B2 (en) * | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
| CN101103039A (zh) * | 2005-01-12 | 2008-01-09 | 阿尔法马股份公司 | 作为抗菌剂的红霉素衍生物 |
| US20080287376A1 (en) * | 2004-07-28 | 2008-11-20 | Mohammad Salman | Ketolide Derivatives as Antibacterial Agents |
| US20090170790A1 (en) * | 2004-10-25 | 2009-07-02 | Biswajit Das | Ketolide derivatives as antibacterial agents |
| CN101631795A (zh) * | 2007-03-13 | 2010-01-20 | 辉瑞产品公司 | 基于红霉素的大环内酯 |
| WO2011018510A1 (en) * | 2009-08-13 | 2011-02-17 | Basilea Pharmaceutica Ag | New macrolides and their use |
| US20110201566A1 (en) * | 2008-10-24 | 2011-08-18 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
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| ZA859575B (en) | 1984-12-21 | 1986-08-27 | Hoffmann La Roche | Oxetanones |
| FR2718450B1 (fr) * | 1994-04-08 | 1997-01-10 | Roussel Uclaf | Nouveaux dérivés de l'érythromycine, leur procédé de préparation et leur application comme médicaments. |
| JP3652394B2 (ja) | 1995-01-27 | 2005-05-25 | 高砂香料工業株式会社 | N−置換−7−アミノ−5−ヒドロキシ−3−オキソヘプタン酸誘導体およびその製造法 |
| HN1998000074A (es) | 1997-06-11 | 1999-01-08 | Pfizer Prod Inc | Derivados de macrolidos c-4 sustituidos |
| AU7986098A (en) | 1997-06-27 | 1999-01-19 | Merck & Co., Inc. | 9a-aza-3-ketolides, compositions containing such compounds and methods of treatment |
| HN1998000159A (es) | 1997-10-29 | 1999-02-09 | Monsanto Co | Derivados de 9- amino - 3 ceto eritromicina |
| FR2785612A1 (fr) | 1998-11-10 | 2000-05-12 | Hoechst Marion Roussel Inc | Nouveaux derives de l'erythromycine, leur procede de preparation et leur application comme medicaments |
| US6262030B1 (en) | 1998-11-03 | 2001-07-17 | Pfizer Inc. | Erythromycin derivatives |
| HRP990116B1 (en) | 1999-04-20 | 2007-10-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | NOVEL 8a AND 9a- 15-MEMBERED LACTAMES |
| AU6316400A (en) * | 1999-08-06 | 2001-03-05 | Taisho Pharmaceutical Co., Ltd. | Erythromycin a derivatives |
| AU6748500A (en) | 1999-08-24 | 2001-03-19 | Abbott Laboratories | 9a-azalides with antibacterial activity |
| NZ518665A (en) | 2000-01-27 | 2005-02-25 | Pfizer Prod Inc | Azalide antibiotic compositions |
| JP4596591B2 (ja) | 2000-03-09 | 2010-12-08 | 塩野義製薬株式会社 | 8a−オキサホモエリスロマイシン誘導体、製造方法、合成中間体および医薬組成物 |
| US6440942B1 (en) * | 2000-12-22 | 2002-08-27 | Enanta Pharmaceuticals, Inc. | 14-membered macrolides derived from leucomycins |
| RU2330069C2 (ru) * | 2002-11-29 | 2008-07-27 | Мершан Корпорейшн | Способ получения макролидного соединения и штаммы streptomyces sp., mortierella sp. и micromonosporaceae |
| JPWO2004065346A1 (ja) | 2003-01-21 | 2006-05-18 | 住友化学株式会社 | (−)−テトラヒドロリプスタチンおよびその中間体の製造方法 |
| HRP20030381B1 (en) | 2003-05-14 | 2007-05-31 | GlaxoSmithKline istra�iva�ki centar Zagreb d.o.o. | 3-DECLADINOZYL 9a-N-CARBAMOYL AND 9a-N-THIOCARBAMOYL DERIVATIVES 9-DEOXO-9-DIHYDRO-9a-AZA-9a-HOMOERYTHROMICYNE A |
| US7276487B2 (en) | 2003-09-23 | 2007-10-02 | Enanta Pharmaceuticals, Inc. | 9a, 11-3C-bicyclic 9a-azalide derivatives |
| US7767797B1 (en) | 2004-09-30 | 2010-08-03 | Synovo Gmbh | Macrocyclic compounds and methods of use thereof |
| US20060096158A1 (en) | 2004-11-08 | 2006-05-11 | Robinson J M | Lactones as new oxygenate fuel additives, fuels based thereon and methods for using same |
| EP1841775A2 (en) * | 2005-01-12 | 2007-10-10 | Alpharma APS | Erythromycin derivatives as antibacterial agents |
| CN101142225B (zh) | 2005-01-13 | 2011-09-07 | 葛兰素集团有限公司 | 具有抗炎活性的大环内酯 |
| EP1879903A1 (en) | 2005-05-10 | 2008-01-23 | GlaxoSmithKline istrazivacki centar Zagreb d.o.o. | Ether linked macrolides useful for the treatment of microbial infections |
| CN101228171A (zh) | 2005-07-26 | 2008-07-23 | 默克勒有限公司 | 作为5-脂氧化酶和环加氧酶抑制剂的吡咯里嗪和中氮茚化合物的大环内酯偶联物 |
| EP1935893A4 (en) | 2005-10-13 | 2009-07-22 | Eisai R&D Man Co Ltd | TOTAL SYNTHESIS OF PLADIENOLIDE B AND PLADIENOLIDE D |
| JP5015016B2 (ja) | 2006-02-07 | 2012-08-29 | 大正製薬株式会社 | 10a−アザライド化合物 |
| WO2008023248A2 (en) * | 2006-08-24 | 2008-02-28 | Wockhardt Research Centre | Novel macrolides and ketolides having antimicrobial activity |
| CA2703475A1 (en) | 2007-10-25 | 2009-04-30 | Cempra Pharmaceuticals, Inc. | Process for the preparation of macrolide antibacterial agents |
| US20090209547A1 (en) | 2008-02-15 | 2009-08-20 | In Jong Kim | C-8 halogenated macrolides |
| KR100980379B1 (ko) | 2008-04-02 | 2010-09-06 | 주식회사 파마코스텍 | 광학활성을 갖는 5-히드록시-3-옥소헵타노에이트 유도체의제조방법 |
| WO2010015703A2 (en) | 2008-08-07 | 2010-02-11 | Glaxosmithkline Istrazivacki Centar Zagreb D.O.O. | Novel 6-o-substituted 15-membered 8a- and 9a-lactams |
| ES2608285T3 (es) | 2009-09-10 | 2017-04-07 | Cempra Pharmaceuticals, Inc. | Procedimientos para el tratamiento de paludismo, tuberculosis y enfermedades por MAC |
| JP5890785B2 (ja) | 2010-03-10 | 2016-03-22 | センプラ ファーマシューティカルズ,インコーポレイテッド | マクロライド抗生物質の非経口製剤 |
| MX361413B (es) | 2010-03-22 | 2018-12-05 | Cempra Pharmaceuticals Inc Star | Formas cristalinas de un macrólido y usos para las mismas. |
| WO2011131749A1 (en) | 2010-04-23 | 2011-10-27 | Glaxo Group Limited | New 14 and 15 membered macrolides for the treatment of neutrophil dominated inflammatory diseases |
| KR101945324B1 (ko) * | 2010-05-20 | 2019-02-07 | 셈프라 파마슈티컬스, 인크. | 매크로라이드들 및 케톨라이드들과 이의 중간체들을 제조하는 공정들 |
| WO2012001089A1 (en) | 2010-07-01 | 2012-01-05 | Novartis Ag | Antibiotic compositions |
| US8975232B2 (en) | 2010-07-29 | 2015-03-10 | President And Fellows Of Harvard College | Macrocyclic kinase inhibitors and uses thereof |
| US8796474B1 (en) * | 2010-08-23 | 2014-08-05 | Rutgers, The State University Of New Jersey | Macrolide compounds and methods and intermediates useful for their preparation |
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| WO2012051126A2 (en) | 2010-10-10 | 2012-04-19 | Synovo Gmbh | Anti-inflammatory macrolides |
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| WO2012127351A1 (en) * | 2011-03-22 | 2012-09-27 | Wockhardt Limited | Process for preparation of ketolide compounds |
| JP6023192B2 (ja) | 2011-07-01 | 2016-11-09 | プレジデント アンド フェローズ オブ ハーバード カレッジ | 大環状インスリン分解酵素(ide)阻害剤およびその使用 |
| KR20140139083A (ko) | 2012-03-27 | 2014-12-04 | 셈프라 파마슈티컬스, 인크. | 마크롤라이드계 항생제를 투여하기 위한 비경구 제제 |
| RU2015138796A (ru) | 2013-03-14 | 2017-04-19 | Семпра Фармасьютикалс, Инк. | Способы и составы для лечения респираторных заболеваний |
| JP6675973B2 (ja) | 2013-03-15 | 2020-04-08 | センプラ ファーマシューティカルズ,インコーポレイテッド | マクロライド抗菌薬を調製するための集束的な方法 |
| AU2014248014B2 (en) | 2013-04-04 | 2018-11-08 | President And Fellows Of Harvard College | Macrolides and methods of their preparation and use |
| EP3211997A4 (en) | 2014-10-08 | 2018-10-24 | President and Fellows of Harvard College | 14-membered ketolides and methods of their preparation and use |
| CA2978670A1 (en) | 2015-03-25 | 2016-09-29 | President And Fellows Of Harvard College | Synthesis of desosamines |
| EP3273969A4 (en) | 2015-03-25 | 2018-11-21 | President and Fellows of Harvard College | Macrolides with modified desosamine sugars and uses thereof |
-
2015
- 2015-10-08 EP EP15848340.4A patent/EP3211997A4/en active Pending
- 2015-10-08 CN CN201580066344.5A patent/CN106998685A/zh active Pending
- 2015-10-08 CA CA2963815A patent/CA2963815A1/en not_active Abandoned
- 2015-10-08 US US15/517,843 patent/US10633407B2/en active Active
- 2015-10-08 JP JP2017519264A patent/JP2017531663A/ja active Pending
- 2015-10-08 HK HK18102636.6A patent/HK1242920A1/zh unknown
- 2015-10-08 WO PCT/US2015/054700 patent/WO2016057798A1/en not_active Ceased
-
2020
- 2020-04-08 US US16/843,259 patent/US11466046B2/en active Active
-
2022
- 2022-07-25 US US17/872,769 patent/US20230109357A1/en not_active Abandoned
Patent Citations (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050090461A1 (en) * | 1998-06-29 | 2005-04-28 | Leadlay Peter F. | Polyketides and their synthesis |
| CN1373767A (zh) * | 1999-04-16 | 2002-10-09 | 奥索-麦克尼尔药品公司 | 酮式大环内酯抗菌剂 |
| US6939861B2 (en) * | 1999-04-16 | 2005-09-06 | Kosan Biosciences, Inc. | Amido macrolides |
| CN1351608A (zh) * | 1999-05-24 | 2002-05-29 | 辉瑞产品公司 | 13-甲基红霉素衍生物 |
| WO2002032918A2 (en) * | 2000-10-18 | 2002-04-25 | Ortho-Mcneil Pharmaceutical, Inc. | Ketolide antibacterials |
| WO2003050132A1 (en) * | 2001-12-05 | 2003-06-19 | Ortho-Mcneil Pharmaceutical, Inc. | 6-o-acyl ketolide derivatives of erythromycine useful as antibacterials |
| US8063021B2 (en) * | 2002-01-17 | 2011-11-22 | Kosan Biosciences Incorporated | Ketolide anti-infective compounds |
| WO2004080391A2 (en) * | 2003-03-10 | 2004-09-23 | Optimer Pharmaceuticals, Inc. | Novel antibacterial agents |
| US20080287376A1 (en) * | 2004-07-28 | 2008-11-20 | Mohammad Salman | Ketolide Derivatives as Antibacterial Agents |
| US20090170790A1 (en) * | 2004-10-25 | 2009-07-02 | Biswajit Das | Ketolide derivatives as antibacterial agents |
| CN101103039A (zh) * | 2005-01-12 | 2008-01-09 | 阿尔法马股份公司 | 作为抗菌剂的红霉素衍生物 |
| CN101631795A (zh) * | 2007-03-13 | 2010-01-20 | 辉瑞产品公司 | 基于红霉素的大环内酯 |
| US20110201566A1 (en) * | 2008-10-24 | 2011-08-18 | Cempra Pharmaceuticals, Inc. | Methods for treating resistant diseases using triazole containing macrolides |
| CN102245022A (zh) * | 2008-10-24 | 2011-11-16 | 森普拉制药公司 | 治疗胃肠病的方法 |
| WO2011018510A1 (en) * | 2009-08-13 | 2011-02-17 | Basilea Pharmaceutica Ag | New macrolides and their use |
Non-Patent Citations (1)
| Title |
|---|
| MASATAKA HIKOTA ET AL: "Stereoselective Synthesis of Erythronolide A via an Extremely Efficient Macrolactonization by the Modified Yamaguchi Method", 《J.ORG.CHEM.》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113646319A (zh) * | 2018-11-19 | 2021-11-12 | 齐卡尼治疗股份有限公司 | C11-环取代的13元大环内酯及其用途 |
| WO2025228440A1 (zh) * | 2024-04-30 | 2025-11-06 | 苏州信诺维医药科技股份有限公司 | 大环内酯类化合物、其制备方法及其用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2963815A1 (en) | 2016-04-14 |
| US20170305953A1 (en) | 2017-10-26 |
| WO2016057798A1 (en) | 2016-04-14 |
| US10633407B2 (en) | 2020-04-28 |
| EP3211997A4 (en) | 2018-10-24 |
| JP2017531663A (ja) | 2017-10-26 |
| EP3211997A1 (en) | 2017-09-06 |
| US20200361980A1 (en) | 2020-11-19 |
| US20230109357A1 (en) | 2023-04-06 |
| HK1242920A1 (zh) | 2018-07-06 |
| US11466046B2 (en) | 2022-10-11 |
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Application publication date: 20170801 |