PE20191005A1 - 1,2,4-triazolonas 2,4,5-trisustituidas - Google Patents
1,2,4-triazolonas 2,4,5-trisustituidasInfo
- Publication number
- PE20191005A1 PE20191005A1 PE2019000896A PE2019000896A PE20191005A1 PE 20191005 A1 PE20191005 A1 PE 20191005A1 PE 2019000896 A PE2019000896 A PE 2019000896A PE 2019000896 A PE2019000896 A PE 2019000896A PE 20191005 A1 PE20191005 A1 PE 20191005A1
- Authority
- PE
- Peru
- Prior art keywords
- compounds
- alkyl
- cycloalkyl
- haloalkyl
- halogen
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
- C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D249/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
- C07D413/02—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
-
- 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
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- 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
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Referido a un compuesto de formula (I), caracterizado porque R1 es alquiloC5-C8, haloalquiloC2-C8, cicloalquilo C4-C8, entre otros; R2 H, o halogeno; R3 es alquilo C1-C6; cicloalquiloC3-C8, haloalquilo C1-C6, entre otros; R4 alquilo C1-C6 opcionalmente sustituido, cicloalquilo C3-C8 o fenilo; R5 es halogeno, alquilo C1-C6, ente otros. Son compuestos 1,2,4-TRIAZOLONAS 2,4,5-trisustituidas que inhiben la dihidroorotato deshidrogenasa (DHODH); un compuesto seleccionado es 5-fluoro-4-[3-metil-5-oxo-4-(propan-2-il)-4,5-dihidro-1H-1,2,4-triazol-1-il]-N-(2-metilfenil)-2-{[(2S)-1,1,1-trifluoropropan-2-il]oxi}benzamida. Tambien se refiere a metodos de preparacion de dichos compuestos, compuestos intermedios utiles para preparar dichos compuestos, composiciones farmaceuticas y combinaciones que comprenden dichos compuestos y el uso de dichos compuestos para preparar composiciones farmaceuticas como un unico agente o en combinacion con otros ingredientes activos, para el tratamiento o la profilaxis de enfermedades, en particular de trastornos hiperproliferativos como el cancer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CNPCT/CN2016/103643 | 2016-10-27 | ||
US201762569296P | 2017-10-06 | 2017-10-06 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20191005A1 true PE20191005A1 (es) | 2019-07-15 |
Family
ID=60164720
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2019000896A PE20191005A1 (es) | 2016-10-27 | 2017-10-25 | 1,2,4-triazolonas 2,4,5-trisustituidas |
Country Status (26)
Country | Link |
---|---|
US (4) | US10815215B2 (es) |
EP (1) | EP3532468B1 (es) |
JP (1) | JP7084389B2 (es) |
KR (1) | KR20190084954A (es) |
CN (2) | CN115557907A (es) |
AU (1) | AU2017351688B2 (es) |
BR (1) | BR112019008458A2 (es) |
CA (1) | CA3041643A1 (es) |
CL (1) | CL2019001160A1 (es) |
CO (1) | CO2019004137A2 (es) |
CR (1) | CR20190212A (es) |
CU (1) | CU24572B1 (es) |
DO (1) | DOP2019000110A (es) |
EC (1) | ECSP19030002A (es) |
GE (1) | GEP20217248B (es) |
IL (1) | IL266214B (es) |
JO (1) | JOP20190094A1 (es) |
MX (1) | MX2019005009A (es) |
NI (1) | NI201900041A (es) |
PE (1) | PE20191005A1 (es) |
PH (1) | PH12019500932A1 (es) |
TN (1) | TN2019000136A1 (es) |
TW (1) | TW201827414A (es) |
UA (1) | UA123688C2 (es) |
UY (1) | UY37461A (es) |
WO (1) | WO2018077923A1 (es) |
Families Citing this family (29)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10968216B2 (en) * | 2016-10-27 | 2021-04-06 | Bayer Aktiengesellschaft | 4,5-annulated 1,2,4-triazolones |
JOP20190094A1 (ar) | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
EP3553052A1 (en) * | 2018-04-10 | 2019-10-16 | Bayer AG | 5-oxo-4,5-dihydro-1h-1,2,4-triazol derivatives for the treatment of cancer |
TW201945346A (zh) | 2018-04-10 | 2019-12-01 | 德商拜耳廠股份有限公司 | 2,4,5-三取代的1,2,4-三唑酮之製備方法 |
WO2019197269A1 (en) * | 2018-04-11 | 2019-10-17 | Bayer Aktiengesellschaft | Combinations of copanlisib with triazolone derivatives and their use in the treatment of cancer |
JP7126556B2 (ja) | 2018-09-28 | 2022-08-26 | 富士フイルム株式会社 | シタラビンを含む抗腫瘍剤、シタラビンと併用される抗腫瘍効果増強剤、抗腫瘍用キット、およびシタラビンと併用される抗腫瘍剤 |
TW202043208A (zh) * | 2019-01-11 | 2020-12-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
WO2020161663A1 (en) * | 2019-02-07 | 2020-08-13 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
TW202104207A (zh) * | 2019-04-17 | 2021-02-01 | 美商健生生物科技公司 | 二氫乳清酸脫氫酶抑制劑 |
EP3750892A1 (en) | 2019-06-14 | 2020-12-16 | Yerevan State University | Novel 5-cyclopropyl-furo[3,4-c]pyridine-3,4(1h,5h)-dione 1,1' substituted derivatives and their uses |
AU2020338985A1 (en) * | 2019-08-29 | 2022-04-14 | Janssen Biotech, Inc. | Substituted urea dihydroorotate dehydrogenase inhibitors |
EP4041714B1 (en) * | 2019-10-10 | 2023-12-13 | Janssen Biotech, Inc. | Bi-aryl dihydroorotate dehydrogenase inhibitors |
CN114222732B (zh) * | 2019-10-28 | 2023-04-04 | 南京明德新药研发有限公司 | 一种尿酸促排剂及其合成方法和其在医药上的应用 |
EP4100124A1 (en) * | 2020-02-04 | 2022-12-14 | Janssen Biotech, Inc. | Heterocyclic compounds as dihydroorotate dehydrogenase inhibitors |
EP3912627B1 (en) | 2020-05-20 | 2022-09-07 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment of coronavirus infections |
WO2021240429A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Benzofuran and benzopyran dihydroorotate dehydrogenase inhibitors |
WO2021240423A1 (en) * | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
JP2023527213A (ja) * | 2020-05-29 | 2023-06-27 | メッドシャイン ディスカバリー インコーポレイテッド | トリアゾロン系化合物 |
WO2021240424A1 (en) | 2020-05-29 | 2021-12-02 | Janssen Biotech, Inc. | Indazole and benzoisoxazole dihydroorotate dehydrogenase inhibitors |
CN116804004A (zh) * | 2020-07-14 | 2023-09-26 | 南京征祥医药有限公司 | 作为dhodh抑制剂的化合物 |
CN111773214B (zh) * | 2020-07-17 | 2021-04-20 | 中国人民解放军军事科学院军事医学研究院 | 2,4,5-三取代的1,2,4-三唑酮在制备抗病毒药物中的用途 |
EP3960170A1 (en) | 2020-08-25 | 2022-03-02 | Bayer AG | Dosing schedule for a method of treatment with dhodh inhibitors |
GB2598624A (en) * | 2020-09-07 | 2022-03-09 | Lorico Aurelio | Use of triazole analogues for inhibition of a tripartite VOR protein complex in multicellular organisms |
WO2022063299A1 (zh) * | 2020-09-28 | 2022-03-31 | 微境生物医药科技(上海)有限公司 | 用作dhodh抑制剂的1,2,4-三唑酮衍生物 |
WO2022070071A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
WO2022070069A1 (en) * | 2020-09-30 | 2022-04-07 | Janssen Biotech, Inc. | Dihydroorotate dehydrogenase inhibitors |
WO2022167402A1 (en) | 2021-02-02 | 2022-08-11 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of therapy comprising administering a therapeutically effective combination comprising a dhodh inhibitor and an idh inhibitor |
CN117616026A (zh) * | 2021-07-05 | 2024-02-27 | 微境生物医药科技(上海)有限公司 | 用作dhodh抑制剂的1,2,4-三唑酮衍生物及其制备方法和用途 |
WO2023093812A1 (zh) * | 2021-11-26 | 2023-06-01 | 南京明德新药研发有限公司 | 三氮唑酮类化合物的晶型及其应用 |
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US4098896A (en) | 1975-09-29 | 1978-07-04 | Chevron Research Company | 1-Halohydrocarbylthio-3-hydrocarbylthio-4-substituted-1,2,4-delta2 -triazolidin-5-ones |
DE3936622A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Halogenierte sulfonylaminocarbonyltriazolinone |
DE3934081A1 (de) | 1989-10-12 | 1991-04-18 | Bayer Ag | Sulfonylaminocarbonyltriazolinone |
DE3709574A1 (de) | 1987-03-24 | 1988-10-06 | Bayer Ag | Substituierte triazolinone |
DE3936623A1 (de) | 1989-11-03 | 1991-05-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber schwefel gebundenen substituenten |
DE4110795A1 (de) | 1991-04-04 | 1992-10-08 | Bayer Ag | Sulfonylaminocarbonyltriazolinone mit ueber sauerstoff gebundenen substituenten |
DE3916208A1 (de) | 1989-05-18 | 1990-11-22 | Bayer Ag | Substituierte triazolone |
DE4342190A1 (de) | 1993-12-10 | 1995-06-14 | Bayer Ag | Verfahren und neue Zwischenprodukte zur Herstellung von Triazolinonen |
DE4433968A1 (de) | 1994-09-23 | 1996-03-28 | Bayer Ag | Verfahren zur Herstellung von Alkoxytriazolinonen |
DE19627901A1 (de) | 1996-07-11 | 1998-01-15 | Bayer Ag | Substituierte aromatische Carbonylverbindungen und ihre Derivate |
US6444613B1 (en) | 1999-03-12 | 2002-09-03 | Hoechst Schering Agrevo Gmbh | Defoliant |
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ES2503815T3 (es) | 2010-09-01 | 2014-10-07 | Bayer Intellectual Property Gmbh | Amidas de ácidos N-(tetrazol-5-il)- y N-(triazol-5-il)arilcarboxílicos y su uso como herbicidas |
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CN103006645A (zh) * | 2011-09-27 | 2013-04-03 | 华东理工大学 | 2-氨基苯并噻唑衍生物作为dhodh抑制剂的应用 |
TWI568722B (zh) * | 2012-06-15 | 2017-02-01 | 葛蘭馬克製藥公司 | 作爲mPGES-1抑制劑之三唑酮化合物 |
US20160251341A1 (en) | 2015-02-27 | 2016-09-01 | Verseon Corporation | Substituted triazole compounds as serine protease inhibitors |
CN106543139B (zh) | 2015-09-17 | 2020-03-17 | 沈阳中化农药化工研发有限公司 | 一种三唑酮类化合物及其用途 |
JOP20190094A1 (ar) * | 2016-10-27 | 2019-04-25 | Broad Inst Inc | مركبات 1، 2، 4-تريازولون تحمل ثلاثة بدائل عند المواقع 2، 4، 5 مفيدة كمثبطات لديهيدروجيناز ثنائي هيدرو أوروتات (dhodh) |
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2017
- 2017-06-16 JO JOP/2019/0094A patent/JOP20190094A1/ar unknown
- 2017-10-25 CA CA3041643A patent/CA3041643A1/en active Pending
- 2017-10-25 EP EP17788234.7A patent/EP3532468B1/en active Active
- 2017-10-25 PE PE2019000896A patent/PE20191005A1/es unknown
- 2017-10-25 TN TNP/2019/000136A patent/TN2019000136A1/en unknown
- 2017-10-25 WO PCT/EP2017/077252 patent/WO2018077923A1/en unknown
- 2017-10-25 US US16/345,168 patent/US10815215B2/en active Active
- 2017-10-25 GE GEAP201715096A patent/GEP20217248B/en unknown
- 2017-10-25 UA UAA201905676A patent/UA123688C2/uk unknown
- 2017-10-25 CN CN202210811374.6A patent/CN115557907A/zh active Pending
- 2017-10-25 AU AU2017351688A patent/AU2017351688B2/en not_active Expired - Fee Related
- 2017-10-25 BR BR112019008458A patent/BR112019008458A2/pt not_active IP Right Cessation
- 2017-10-25 CR CR20190212A patent/CR20190212A/es unknown
- 2017-10-25 MX MX2019005009A patent/MX2019005009A/es unknown
- 2017-10-25 KR KR1020197011905A patent/KR20190084954A/ko not_active Application Discontinuation
- 2017-10-25 CN CN201780066589.7A patent/CN110023302B/zh active Active
- 2017-10-25 CU CU2019000045A patent/CU24572B1/es unknown
- 2017-10-25 JP JP2019522859A patent/JP7084389B2/ja active Active
- 2017-10-27 TW TW106137255A patent/TW201827414A/zh unknown
- 2017-10-27 UY UY0001037461A patent/UY37461A/es not_active Application Discontinuation
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2019
- 2019-04-23 IL IL266214A patent/IL266214B/en unknown
- 2019-04-25 PH PH12019500932A patent/PH12019500932A1/en unknown
- 2019-04-26 DO DO2019000110A patent/DOP2019000110A/es unknown
- 2019-04-26 NI NI201900041A patent/NI201900041A/es unknown
- 2019-04-26 EC ECSENADI201930002A patent/ECSP19030002A/es unknown
- 2019-04-26 CL CL2019001160A patent/CL2019001160A1/es unknown
- 2019-04-26 CO CONC2019/0004137A patent/CO2019004137A2/es unknown
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2020
- 2020-08-18 US US16/996,721 patent/US11130745B2/en active Active
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2021
- 2021-08-20 US US17/407,951 patent/US11713304B2/en active Active
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2023
- 2023-04-20 US US18/137,281 patent/US20230365524A1/en active Pending
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