HUE029582T2 - Double-substituted benzothienylpyrrolotriazines and their use as FGFR inhibitors - Google Patents
Double-substituted benzothienylpyrrolotriazines and their use as FGFR inhibitors Download PDFInfo
- Publication number
- HUE029582T2 HUE029582T2 HUE12798738A HUE12798738A HUE029582T2 HU E029582 T2 HUE029582 T2 HU E029582T2 HU E12798738 A HUE12798738 A HU E12798738A HU E12798738 A HUE12798738 A HU E12798738A HU E029582 T2 HUE029582 T2 HU E029582T2
- Authority
- HU
- Hungary
- Prior art keywords
- mmol
- solution
- formula
- methyl
- hydrogen
- Prior art date
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Treatment Of Liquids With Adsorbents In General (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11193841 | 2011-12-15 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HUE029582T2 true HUE029582T2 (en) | 2017-03-28 |
Family
ID=47326168
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HUE12798738A HUE029582T2 (en) | 2011-12-15 | 2012-12-10 | Double-substituted benzothienylpyrrolotriazines and their use as FGFR inhibitors |
Country Status (42)
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10388493B2 (en) | 2011-09-16 | 2019-08-20 | Lam Research Corporation | Component of a substrate support assembly producing localized magnetic fields |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
| US10124003B2 (en) | 2013-07-18 | 2018-11-13 | Taiho Pharmaceutical Co., Ltd. | Therapeutic agent for FGFR inhibitor-resistant cancer |
| PT3023100T (pt) | 2013-07-18 | 2019-05-29 | Taiho Pharmaceutical Co Ltd | Fármaco antitumoral para administração intermitente de inibidor de fgfr |
| KR102228034B1 (ko) * | 2013-10-21 | 2021-03-16 | 제노스코 | 치환된 피리미딘 화합물 및 syk 억제제로서의 이의 용도 |
| JP2017538708A (ja) * | 2014-12-11 | 2017-12-28 | バイエル・ファルマ・アクティエンゲゼルシャフト | ｐａｎ ＦＧＦＲ阻害剤の使用およびｐａｎ ＦＧＦＲ阻害剤を用いる治療に適格な癌を有する患者を同定する方法 |
| MX2017011635A (es) * | 2015-03-09 | 2018-02-09 | Bayer Pharma AG | Combinaciones que contienen 2,3-dihidroimidazo[1,2-c]quinazolina sustituida. |
| EP3394056B1 (en) | 2015-12-22 | 2021-04-14 | Shy Therapeutics LLC | Compounds for the treatment of cancer and inflammatory disease |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| KR20220110859A (ko) | 2016-03-04 | 2022-08-09 | 다이호야쿠힌고교 가부시키가이샤 | 악성 종양 치료용 제제 및 조성물 |
| AU2017241524B2 (en) | 2016-03-28 | 2021-07-08 | Incyte Corporation | Pyrrolotriazine compounds as TAM inhibitors |
| CN107513068A (zh) * | 2016-06-16 | 2017-12-26 | 中国科学院上海药物研究所 | 一种具有fgfr抑制活性的新型化合物及其制备和应用 |
| AU2017378324B2 (en) * | 2016-12-16 | 2021-09-02 | Cystic Fibrosis Foundation | Bycyclic heteroaryl derivatives as CFTR potentiators |
| CA3066939A1 (en) | 2017-06-21 | 2018-12-27 | SHY Therapeutics LLC | Compounds that interact with the ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| WO2019034075A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr和egfr抑制剂 |
| WO2019034076A1 (zh) * | 2017-08-15 | 2019-02-21 | 南京明德新药研发股份有限公司 | Fgfr抑制剂及其医药用途 |
| TWI821200B (zh) | 2017-09-27 | 2023-11-11 | 美商英塞特公司 | Tam抑制劑之鹽 |
| MX2020004285A (es) | 2017-10-25 | 2020-07-29 | Bayer Pharma AG | Proceso para preparar el benzotiofen-2-il boronato. |
| WO2019105734A1 (en) | 2017-11-28 | 2019-06-06 | Bayer Consumer Care Ag | Combinations of copanlisib |
| MX2020009762A (es) | 2018-03-19 | 2021-01-08 | Taiho Pharmaceutical Co Ltd | Composicion farmaceutica que incluye alquil sulfato de sodio. |
| WO2019180141A1 (en) | 2018-03-23 | 2019-09-26 | Bayer Aktiengesellschaft | Combinations of rogaratinib |
| US11241438B2 (en) | 2018-06-29 | 2022-02-08 | Incyte Corporation | Formulations of an AXL/MER inhibitor |
| US12391705B2 (en) | 2018-12-19 | 2025-08-19 | Shy Therapeutics, Llc | Compounds that interact with the Ras superfamily for the treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| CA3128073A1 (en) * | 2019-01-31 | 2020-08-06 | Bayer Aktiengesellschaft | The monohydrate of rogaratinib hydrochloride and solid states thereof |
| JP7355834B2 (ja) * | 2019-02-15 | 2023-10-03 | 石薬集団中奇制薬技術（石家庄）有限公司 | 固体形態のｆｇｆｒ阻害剤化合物およびその製造方法 |
| WO2020170355A1 (ja) * | 2019-02-20 | 2020-08-27 | 大鵬薬品工業株式会社 | Ｆｇｆｒ１変異腫瘍の治療方法 |
| CN109928976A (zh) * | 2019-02-26 | 2019-06-25 | 泰州亿腾景昂药业有限公司 | 一种工业化生产eoc317的方法 |
| SI3953357T1 (sl) | 2019-04-12 | 2024-08-30 | Blueprint Medicines Corporation | Pirolotriazinski derivati za zdravljenje bolezni, posredovanih s KIT in PDGFRA |
| WO2020231990A1 (en) * | 2019-05-13 | 2020-11-19 | Relay Therapeutics, Inc. | Fgfr inhibitors and methods of use thereof |
| CN114641293B (zh) * | 2019-11-08 | 2024-05-31 | 石药集团中奇制药技术（石家庄）有限公司 | 一种fgfr抑制剂的用途 |
| CN111004234A (zh) * | 2019-11-28 | 2020-04-14 | 湖南农业大学 | 一种2-苯基咪唑并[1,2-α]吡啶类化合物的C3位卤化方法 |
| EP4114401A1 (en) | 2020-03-06 | 2023-01-11 | Incyte Corporation | Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors |
| CN117402161A (zh) * | 2022-07-06 | 2024-01-16 | 上海科恩泰生物医药科技有限公司 | 一种具有fgfr抑制作用的亚砜亚胺类化合物、包含其的药物组合物及其用途 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202530228A (zh) | 2023-10-12 | 2025-08-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2258459T3 (es) | 1999-05-21 | 2006-09-01 | Bristol-Myers Squibb Company | Pirrolotriazinas inhibidoras de quinasas. |
| ES2299434T3 (es) | 1999-09-17 | 2008-06-01 | ABBOTT GMBH & CO. KG | Inhibidores de kinasa utilizados como agentes terapeuticos. |
| JPWO2004096806A1 (ja) * | 2003-04-30 | 2006-07-13 | 大日本住友製薬株式会社 | 縮合イミダゾール誘導体 |
| DE10327439A1 (de) * | 2003-06-18 | 2005-01-05 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Imidazopyridazinon- und Imidazopyridonderivate, deren Herstellung und deren Verwendung als Arzneimittel |
| DE602005014964D1 (de) | 2004-04-02 | 2009-07-30 | Osi Pharm Inc | Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren |
| UY28931A1 (es) | 2004-06-03 | 2005-12-30 | Bayer Pharmaceuticals Corp | Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis |
| TW200635927A (en) * | 2004-12-22 | 2006-10-16 | Bristol Myers Squibb Co | Synthetic process |
| JP5116687B2 (ja) | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ［２，１−ｆ］［１，２，４］トリアジン−４−イルアミンＩＧＦ−１Ｒキナーゼ阻害剤 |
| AU2006316605B2 (en) * | 2005-11-17 | 2012-04-26 | Osi Pharmaceuticals, Inc. | Fused bicyclic mTOR inhibitors |
| US7514435B2 (en) | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| KR101461680B1 (ko) | 2005-12-02 | 2014-11-19 | 바이엘 헬스케어 엘엘씨 | 과다-증식성 장애 및 맥관형성과 관련된 질환의 치료에유용한 치환된 4-아미노-피롤로트리아진 유도체 |
| PE20070855A1 (es) * | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
| JP5193876B2 (ja) | 2005-12-02 | 2013-05-08 | バイエル・ヘルスケア・エルエルシー | オーロラキナーゼの阻害により癌を処置するために有用なピロロトリアジン誘導体 |
| WO2007079164A2 (en) | 2005-12-29 | 2007-07-12 | Abbott Laboratories | Protein kinase inhibitors |
| US8124759B2 (en) | 2007-05-09 | 2012-02-28 | Abbott Laboratories | Inhibitors of protein kinases |
| US8476431B2 (en) | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
| JP5656976B2 (ja) | 2009-04-29 | 2015-01-21 | ローカス ファーマシューティカルズ インコーポレイテッド | ピロロトリアジン化合物 |
| UY34484A (es) * | 2011-12-15 | 2013-07-31 | Bayer Ip Gmbh | Benzotienilo-pirrolotriazinas disustituidas y sus usos |
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2012
- 2012-12-03 UY UY0001034484A patent/UY34484A/es unknown
- 2012-12-10 IN IN4310CHN2014 patent/IN2014CN04310A/en unknown
- 2012-12-10 US US14/365,424 patent/US20140336173A1/en not_active Abandoned
- 2012-12-10 PE PE2014000926A patent/PE20141855A1/es active IP Right Grant
- 2012-12-10 SI SI201230702A patent/SI2791140T1/sl unknown
- 2012-12-10 RS RS20160733A patent/RS55144B1/sr unknown
- 2012-12-10 UA UAA201407930A patent/UA116768C2/uk unknown
- 2012-12-10 EA EA201400707A patent/EA029556B1/ru not_active IP Right Cessation
- 2012-12-10 BR BR112014014531-8A patent/BR112014014531B1/pt not_active IP Right Cessation
- 2012-12-10 ES ES12798738.6T patent/ES2591203T3/es active Active
- 2012-12-10 CA CA2859133A patent/CA2859133C/en active Active
- 2012-12-10 CU CU2016000039A patent/CU24426B1/es unknown
- 2012-12-10 JP JP2014546445A patent/JP6050829B2/ja not_active Expired - Fee Related
- 2012-12-10 ME MEP-2016-181A patent/ME02517B/me unknown
- 2012-12-10 PT PT127987386T patent/PT2791140T/pt unknown
- 2012-12-10 HU HUE12798738A patent/HUE029582T2/en unknown
- 2012-12-10 EP EP12798738.6A patent/EP2791140B1/en active Active
- 2012-12-10 DK DK12798738.6T patent/DK2791140T3/en active
- 2012-12-10 AU AU2012350750A patent/AU2012350750B2/en not_active Ceased
- 2012-12-10 PL PL12798738T patent/PL2791140T3/pl unknown
- 2012-12-10 WO PCT/EP2012/074977 patent/WO2013087578A1/en not_active Ceased
- 2012-12-10 LT LTEP12798738.6T patent/LT2791140T/lt unknown
- 2012-12-10 CN CN201280069882.6A patent/CN104245700B/zh not_active Expired - Fee Related
- 2012-12-10 MX MX2014006905A patent/MX367158B/es active IP Right Grant
- 2012-12-10 MY MYPI2014701550A patent/MY178660A/en unknown
- 2012-12-10 KR KR1020147019406A patent/KR102057444B1/ko not_active Expired - Fee Related
- 2012-12-10 SG SG11201402325QA patent/SG11201402325QA/en unknown
- 2012-12-10 HR HRP20161130TT patent/HRP20161130T1/hr unknown
- 2012-12-12 AR ARP120104679A patent/AR089207A1/es unknown
- 2012-12-12 JO JOP/2012/0377A patent/JO3295B1/ar active
- 2012-12-14 TW TW101147336A patent/TWI567076B/zh not_active IP Right Cessation
- 2012-12-14 US US13/715,553 patent/US9206184B2/en active Active
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2014
- 2014-05-14 IL IL232611A patent/IL232611A/en active IP Right Grant
- 2014-06-09 CO CO14123802A patent/CO7030961A2/es unknown
- 2014-06-09 CU CUP2014000065A patent/CU20140065A7/es unknown
- 2014-06-10 DO DO2014000127A patent/DOP2014000127A/es unknown
- 2014-06-11 TN TNP2014000255A patent/TN2014000255A1/en unknown
- 2014-06-12 EC ECIEPI20144722A patent/ECSP14004722A/es unknown
- 2014-06-12 CL CL2014001547A patent/CL2014001547A1/es unknown
- 2014-06-13 PH PH12014501355A patent/PH12014501355A1/en unknown
- 2014-06-13 GT GT201400113A patent/GT201400113A/es unknown
- 2014-06-17 CR CR20140288A patent/CR20140288A/es unknown
- 2014-07-14 ZA ZA2014/05140A patent/ZA201405140B/en unknown
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2016
- 2016-08-31 CY CY20161100853T patent/CY1118112T1/el unknown
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2017
- 2017-07-17 AU AU2017206140A patent/AU2017206140A1/en not_active Abandoned
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2018
- 2018-02-20 US US15/900,725 patent/US20190016724A1/en not_active Abandoned
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2019
- 2019-06-18 AU AU2019204255A patent/AU2019204255A1/en not_active Abandoned
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2021
- 2021-11-01 US US17/516,542 patent/US20220153745A1/en not_active Abandoned
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