ECSP19043120A - Pirrolopirimidinas como potenciadores de cftr - Google Patents
Pirrolopirimidinas como potenciadores de cftrInfo
- Publication number
- ECSP19043120A ECSP19043120A ECSENADI201943120A ECDI201943120A ECSP19043120A EC SP19043120 A ECSP19043120 A EC SP19043120A EC SENADI201943120 A ECSENADI201943120 A EC SENADI201943120A EC DI201943120 A ECDI201943120 A EC DI201943120A EC SP19043120 A ECSP19043120 A EC SP19043120A
- Authority
- EC
- Ecuador
- Prior art keywords
- cftr
- compounds
- cystic fibrosis
- pyrrolopyrimidines
- potentials
- Prior art date
Links
- 150000004944 pyrrolopyrimidines Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 abstract 4
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 abstract 4
- 201000003883 Cystic fibrosis Diseases 0.000 abstract 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 206010010774 Constipation Diseases 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010033645 Pancreatitis Diseases 0.000 abstract 1
- 208000021386 Sjogren Syndrome Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 201000009267 bronchiectasis Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 239000003623 enhancer Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 201000009890 sinusitis Diseases 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
- 208000005494 xerophthalmia Diseases 0.000 abstract 1
Classifications
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/08—Bronchodilators
-
- 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
- A61P11/12—Mucolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
- 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
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Saccharide Compounds (AREA)
Abstract
La presente invención se refiere a compuestos de la Fórmula I, I en donde R1a, R1b, R2, R3, R4, W, Y y Z son como se describen en este documento, y a sales farmacéuticamente aceptable de los mismos. Los compuestos son potenciadores del regulador de conductancia transmembranal de la fibrosis quística (CFTR). La invención también da a conocer composiciones farmacéuticas que comprenden el compuesto opcionalmente en combinación con agentes terapéuticos adicionales, y métodos de potenciación, en mamíferos incluyendo humanos, de CFTR por la administración de los compuestos. Estos compuestos son útiles para el tratamiento de fibrosis quística (CF), asma, bronquiectasia, enfermedad pulmonar obstructiva crónica (COPD), constipación, diabetes mellitus, xeroftalmia, pancreatitis, rinosinusitis, síndrome de Sjögren y otros trastornos asociados con CFTR.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662423919P | 2016-11-18 | 2016-11-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP19043120A true ECSP19043120A (es) | 2019-08-30 |
Family
ID=62144793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI201943120A ECSP19043120A (es) | 2016-11-18 | 2019-06-17 | Pirrolopirimidinas como potenciadores de cftr |
Country Status (21)
| Country | Link |
|---|---|
| US (5) | US10301315B2 (es) |
| EP (1) | EP3541390B1 (es) |
| JP (3) | JP6978507B2 (es) |
| KR (2) | KR102585398B1 (es) |
| CN (2) | CN115850268A (es) |
| AU (2) | AU2017362350B2 (es) |
| BR (1) | BR112019010167A2 (es) |
| CA (1) | CA3044050A1 (es) |
| CL (1) | CL2019001334A1 (es) |
| CO (1) | CO2019005993A2 (es) |
| CR (1) | CR20190292A (es) |
| DO (1) | DOP2019000126A (es) |
| EC (1) | ECSP19043120A (es) |
| IL (2) | IL296279A (es) |
| MX (2) | MX2021012639A (es) |
| PE (1) | PE20200739A1 (es) |
| PH (1) | PH12019501098A1 (es) |
| RU (2) | RU2021129721A (es) |
| SG (1) | SG10202106949XA (es) |
| UA (1) | UA125400C2 (es) |
| WO (1) | WO2018094137A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2800565T1 (sl) | 2012-01-06 | 2020-10-30 | Lundbeck La Jolla Research Center, Inc. | Karbamatne spojine in metode izdelave in uporabe le-teh |
| MA54649A (fr) | 2014-10-06 | 2022-04-27 | Vertex Pharma | Modulateurs de régulateur de conductance transmembranaire de la fibrose kystique |
| US20180369209A1 (en) * | 2015-12-22 | 2018-12-27 | Proteostasis Therapeutics, Inc. | Methods of treating pulmonary diseases and disorders |
| WO2018064632A1 (en) | 2016-09-30 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| JP6978507B2 (ja) * | 2016-11-18 | 2021-12-08 | システィック・ファイブロシス・ファンデーション | Ｃｆｔｒ増強物質としてのピロロピリミジン |
| LT3551622T (lt) | 2016-12-09 | 2021-02-25 | Vertex Pharmaceuticals Incorporated | Cistinės fibrozės transmembraninio laidumo reguliatoriaus moduliatorius, farmacinė kompozicija, gydymo būdai, ir moduliatoriaus gamybos būdas |
| SG10201911076QA (en) * | 2016-12-16 | 2020-01-30 | Cystic Fibrosis Found | Bycyclic heteroaryl derivatives as cftr potentiators |
| US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| CA3069226A1 (en) | 2017-07-17 | 2019-01-24 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| KR102606188B1 (ko) | 2017-08-02 | 2023-11-23 | 버텍스 파마슈티칼스 인코포레이티드 | 피롤리딘 화합물을 제조하기 위한 공정 |
| WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
| MA51039A (fr) | 2017-12-08 | 2020-10-14 | Vertex Pharma | Procédés pour préparer des modulateurs du régulateur de la conductance transmembranaire de la mucoviscidose |
| TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
| SG11202006614VA (en) | 2018-02-15 | 2020-08-28 | Vertex Pharma | Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cycstic fibrosis, and process for making them |
| US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
| WO2020250116A1 (en) * | 2019-06-10 | 2020-12-17 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of cf, copd, and bronchiectasis |
| AU2020313422A1 (en) | 2019-07-15 | 2022-01-27 | Novartis Ag | Formulations of (S)-3-amino-6-methoxy-N-(3,3,3-trifluoro-2-hydroxy-2-methylpropyl)-5-(trifluoromethyl)picolinamide |
| TW202115092A (zh) | 2019-08-14 | 2021-04-16 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| TW202120517A (zh) | 2019-08-14 | 2021-06-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| JP2022544383A (ja) | 2019-08-14 | 2022-10-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ｃｆｔｒモジュレータの結晶形態 |
| CN111138439B (zh) * | 2020-01-17 | 2021-06-25 | 厦门大学 | 氟代吡咯并嘧啶类化合物及其制备方法和应用 |
| US20230192700A1 (en) | 2020-03-06 | 2023-06-22 | Bayer Aktiengesellschaft | Pyrazolopyrazines acting on cancers via inhibition of cdk12 |
| CA3188234A1 (en) | 2020-08-20 | 2022-02-24 | Jeffrey Axelrod | Methods for treating respiratory diseases characterized by mucus hypersecretion |
| WO2024096629A1 (ko) * | 2022-11-02 | 2024-05-10 | 일동제약 주식회사 | Cftr 조절제 화합물을 포함하는 점안용 조성물 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL176526B1 (pl) * | 1992-12-17 | 1999-06-30 | Pfizer | Pirolopirymidyny jako związki o działaniu antagonistów czynnika uwalniającego kortykotropinę |
| IL149462A0 (en) | 2001-05-09 | 2002-11-10 | Warner Lambert Co | Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor |
| US20030208067A1 (en) | 2001-05-30 | 2003-11-06 | Cao Sheldon Xiaodong | Inhibitors of protein kinase for the treatment of disease |
| WO2004100868A2 (en) * | 2003-04-23 | 2004-11-25 | Abbott Laboratories | Method of treating transplant rejection |
| CA2553724A1 (en) * | 2004-02-03 | 2005-08-18 | Abbott Laboratories | Aminobenzoxazoles as therapeutic agents |
| CA2635231C (en) * | 2005-12-29 | 2014-07-15 | Abbott Laboratories | Protein kinase inhibitors |
| BRPI0708779A2 (pt) * | 2006-03-11 | 2011-06-14 | Vernalis R & D | derivados de pirrolopirimidina utilizados como inibidores de hsp90 |
| NZ571182A (en) * | 2006-04-04 | 2010-09-30 | Univ California | Pyrazolo[3,4-d]pyrimidines |
| EA201070572A1 (ru) * | 2007-11-07 | 2010-12-30 | Фолдркс Фармасьютикалз, Инк. | Модуляция транспорта белков |
| MX2011007326A (es) | 2009-01-08 | 2011-10-19 | Curis Inc | Inhibidores de fosfoinositida 3-quinasa con una porcion de enlace de cinc. |
| US20130123281A1 (en) | 2011-11-11 | 2013-05-16 | Beta Cat Pharmaceuticals, Llc | Compositions and Methods for Inhibition of TBL-1 Binding to Disease-Associated Molecules |
| US8828998B2 (en) * | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| WO2014060431A1 (en) * | 2012-10-16 | 2014-04-24 | Almirall, S.A. | Pyrrolotriazinone derivatives as pi3k inhibitors |
| WO2015091532A1 (en) | 2013-12-19 | 2015-06-25 | Almirall, S.A. | Pyrrolopyrimidine derivatives as pi3k inhibitors |
| JP6978507B2 (ja) | 2016-11-18 | 2021-12-08 | システィック・ファイブロシス・ファンデーション | Ｃｆｔｒ増強物質としてのピロロピリミジン |
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2017
- 2017-11-17 JP JP2019547579A patent/JP6978507B2/ja active Active
- 2017-11-17 MX MX2021012639A patent/MX2021012639A/es unknown
- 2017-11-17 CA CA3044050A patent/CA3044050A1/en active Pending
- 2017-11-17 IL IL296279A patent/IL296279A/en unknown
- 2017-11-17 PE PE2019001045A patent/PE20200739A1/es unknown
- 2017-11-17 WO PCT/US2017/062148 patent/WO2018094137A1/en active Application Filing
- 2017-11-17 CN CN202211239693.0A patent/CN115850268A/zh active Pending
- 2017-11-17 EP EP17872726.9A patent/EP3541390B1/en active Active
- 2017-11-17 AU AU2017362350A patent/AU2017362350B2/en active Active
- 2017-11-17 KR KR1020197017510A patent/KR102585398B1/ko active IP Right Grant
- 2017-11-17 BR BR112019010167A patent/BR112019010167A2/pt active IP Right Grant
- 2017-11-17 UA UAA201906838A patent/UA125400C2/uk unknown
- 2017-11-17 RU RU2021129721A patent/RU2021129721A/ru unknown
- 2017-11-17 SG SG10202106949XA patent/SG10202106949XA/en unknown
- 2017-11-17 KR KR1020237033420A patent/KR20230146104A/ko active Application Filing
- 2017-11-17 CN CN201780083801.0A patent/CN110337294B/zh active Active
- 2017-11-17 MX MX2019005822A patent/MX2019005822A/es unknown
- 2017-11-17 RU RU2019118623A patent/RU2757457C2/ru active
- 2017-11-17 US US15/815,809 patent/US10301315B2/en active Active
- 2017-11-17 CR CR20190292A patent/CR20190292A/es unknown
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2019
- 2019-04-05 US US16/377,005 patent/US10494374B2/en active Active
- 2019-05-15 IL IL266668A patent/IL266668B2/en unknown
- 2019-05-16 CL CL2019001334A patent/CL2019001334A1/es unknown
- 2019-05-16 PH PH12019501098A patent/PH12019501098A1/en unknown
- 2019-05-17 DO DO2019000126A patent/DOP2019000126A/es unknown
- 2019-06-07 CO CONC2019/0005993A patent/CO2019005993A2/es unknown
- 2019-06-17 EC ECSENADI201943120A patent/ECSP19043120A/es unknown
- 2019-09-20 US US16/578,277 patent/US20200017512A1/en not_active Abandoned
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2021
- 2021-02-18 US US17/179,062 patent/US20210171534A1/en not_active Abandoned
- 2021-11-10 JP JP2021183048A patent/JP7360434B2/ja active Active
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2022
- 2022-03-16 AU AU2022201816A patent/AU2022201816B2/en active Active
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2023
- 2023-04-13 US US18/134,455 patent/US20230250100A1/en active Pending
- 2023-09-29 JP JP2023169299A patent/JP2023182694A/ja active Pending
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