MX2019010221A - Formas cristalinas del derivado de 4-pirimidinsulfamida aprocitentan. - Google Patents
Formas cristalinas del derivado de 4-pirimidinsulfamida aprocitentan.Info
- Publication number
- MX2019010221A MX2019010221A MX2019010221A MX2019010221A MX2019010221A MX 2019010221 A MX2019010221 A MX 2019010221A MX 2019010221 A MX2019010221 A MX 2019010221A MX 2019010221 A MX2019010221 A MX 2019010221A MX 2019010221 A MX2019010221 A MX 2019010221A
- Authority
- MX
- Mexico
- Prior art keywords
- crystalline forms
- bromo
- aprocitentan
- rimidin
- sulfamide
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/4035—Isoindoles, e.g. phthalimide
-
- 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
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
- A61K31/54—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
- A61K31/549—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 having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
Abstract
La presente invención se refiere a formas cristalinas novedosas de {5-(4-bromo-fenil)-6-[2-(5-bromo-pirimidin-2-iloxi)-etoxi]-piri midin-4-il}-sulfamida, procedimientos para la preparación de las mismas, composiciones farmacéuticas que comprenden dichas formas cristalinas, composiciones farmacéuticas preparadas a partir de tales formas cristalinas y su uso como antagonistas del receptor de endotelina. También se refiere a usos nuevos de la {5-(4-bromo-fenil)-6-[2-(5-bromo-pirimidin-2-iloxi)-etoxi]-pirimi din-4-il}-sulfamida, ya sea sola o en combinación con otros ingredientes activos o agentes terapéuticos.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP2017054489 | 2017-02-27 | ||
| EP2017061487 | 2017-05-12 | ||
| PCT/EP2018/054627 WO2018154101A1 (en) | 2017-02-27 | 2018-02-26 | Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2019010221A true MX2019010221A (es) | 2019-10-21 |
Family
ID=60268369
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019010222A MX2019010222A (es) | 2017-02-27 | 2017-11-06 | Combinaciones de un derivado de 4-pirimidinsulfamida con ingredientes activos para el tratamiento de enfermedades relacionadas con endotelina. |
| MX2019010221A MX2019010221A (es) | 2017-02-27 | 2018-02-26 | Formas cristalinas del derivado de 4-pirimidinsulfamida aprocitentan. |
| MX2021007184A MX2021007184A (es) | 2017-02-27 | 2019-08-27 | Formas cristalinas del derivado de 4-pirimidinsulfamida aprocitentan. |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019010222A MX2019010222A (es) | 2017-02-27 | 2017-11-06 | Combinaciones de un derivado de 4-pirimidinsulfamida con ingredientes activos para el tratamiento de enfermedades relacionadas con endotelina. |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2021007184A MX2021007184A (es) | 2017-02-27 | 2019-08-27 | Formas cristalinas del derivado de 4-pirimidinsulfamida aprocitentan. |
Country Status (17)
| Country | Link |
|---|---|
| US (5) | US11174247B2 (es) |
| EP (3) | EP3658140A1 (es) |
| JP (3) | JP7223701B2 (es) |
| KR (3) | KR102568472B1 (es) |
| CN (3) | CN110325186A (es) |
| AU (2) | AU2017400276B2 (es) |
| BR (2) | BR112019017658A2 (es) |
| CA (2) | CA3053991A1 (es) |
| CL (3) | CL2019002470A1 (es) |
| IL (3) | IL297993A (es) |
| MA (2) | MA49664A (es) |
| MX (3) | MX2019010222A (es) |
| PH (2) | PH12019501937A1 (es) |
| SG (3) | SG11201907435PA (es) |
| TW (2) | TWI786089B (es) |
| UA (1) | UA126122C2 (es) |
| WO (2) | WO2018153513A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MA49664A (fr) | 2017-02-27 | 2020-06-03 | Idorsia Pharmaceuticals Ltd | Combinaisons d'un dérivé de 4-pyrimidinesulfamide avec des principes actifs pour le traitement de maladies liées à l'endothéline |
| BR112020010831A2 (pt) * | 2017-11-30 | 2020-11-10 | Idorsia Pharmaceuticals Ltd | composição farmacêutica, aprocitentan, e, método |
| AU2019410727A1 (en) | 2018-12-21 | 2021-08-12 | Actelion Pharmaceuticals Ltd | Pharmaceutical composition for the treatment of pulmonary arterial hypertension |
| TW202042818A (zh) | 2019-01-25 | 2020-12-01 | 瑞士商艾克泰聯製藥有限公司 | 用於治療慢性血栓性肺高血壓之醫藥組成物 |
| CN112569357B (zh) * | 2019-09-30 | 2023-03-28 | 深圳奥萨制药有限公司 | 双重内皮素受体拮抗剂与利尿剂的组合物 |
| CN112679441A (zh) * | 2019-10-18 | 2021-04-20 | 普济生物科技（台州）有限公司 | 阿普昔腾坦的晶型、制备方法及其用途 |
| WO2021088645A1 (zh) * | 2019-11-07 | 2021-05-14 | 苏州科睿思制药有限公司 | 一种Aprocitentan晶型及其制备方法和用途 |
| WO2021237004A1 (en) | 2020-05-21 | 2021-11-25 | Teva Pharmaceuticals International Gmbh | Solid state forms of aprocitentan and process for preparation thereof |
| KR20230038234A (ko) | 2020-07-10 | 2023-03-17 | 아스트라제네카 아베 | 만성 신장 질환 치료를 위한 지보텐탄 및 다파글리플로진의 조합 |
| WO2023111797A1 (en) * | 2021-12-17 | 2023-06-22 | Janssen Biotech, Inc. | Pyrimidine sulfamide derivatives and process for manufacturing them |
| WO2023227490A1 (en) | 2022-05-22 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | Aprocitentan for the treatment of hypertension |
| WO2023227721A1 (en) | 2022-05-25 | 2023-11-30 | Idorsia Pharmaceuticals Ltd | Crystalline forms of sodium (5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)(sulfamoyl)amide |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0634175B1 (de) * | 1993-07-15 | 2001-01-10 | F. Hoffmann-La Roche Ag | Pharmazeutische Kombination, die einen Hemmer des Renin-Angiotensin-Systems und einen Endothelin-Antagonisten enthält |
| JP4245130B2 (ja) | 2000-12-18 | 2009-03-25 | アクテリオン ファーマシューティカルズ リミテッド | 新規なスルファミド類 |
| EG24716A (en) * | 2002-05-17 | 2010-06-07 | Novartis Ag | Combination of organic compounds |
| US20070196510A1 (en) | 2006-02-17 | 2007-08-23 | Gerber Michael J | Method for treating resistant hypertension |
| WO2007146900A2 (en) | 2006-06-15 | 2007-12-21 | Gilead Colorado, Inc. | Antihypertensive therapy method |
| PE20080991A1 (es) | 2006-06-27 | 2008-09-05 | Novartis Ag | Formas de dosificacion solidas de valsartan, amlodipina e hidroclorotiazida y metodo para elaborarlas |
| MX2010001837A (es) * | 2007-08-17 | 2010-03-10 | Actelion Pharmaceuticals Ltd | Derivados de 4-pirimidinasulfamida. |
| EP2190433A2 (en) * | 2007-08-22 | 2010-06-02 | Gilead Colorado, Inc. | Therapy for complications of diabetes |
| CN102614189B (zh) * | 2012-04-17 | 2014-10-22 | 北京哈三联科技股份有限公司 | 含缬沙坦、氨氯地平和氢氯噻嗪的微丸药物组合 |
| EP2907811A1 (en) | 2014-02-14 | 2015-08-19 | Actelion Pharmaceuticals Ltd. | Process for manufacturing pyrimidine sulfamide derivatives |
| AU2015342929A1 (en) | 2014-11-07 | 2017-05-25 | Abbvie Inc. | Methods of treating CKD using predictors of fluid retention |
| WO2017185142A1 (en) | 2016-04-29 | 2017-11-02 | Adelaide Research & Innovation Pty Ltd | Method for preventing and/or treating atrial fibrillation |
| MA49664A (fr) | 2017-02-27 | 2020-06-03 | Idorsia Pharmaceuticals Ltd | Combinaisons d'un dérivé de 4-pyrimidinesulfamide avec des principes actifs pour le traitement de maladies liées à l'endothéline |
| BR112020010831A2 (pt) | 2017-11-30 | 2020-11-10 | Idorsia Pharmaceuticals Ltd | composição farmacêutica, aprocitentan, e, método |
| AU2019410727A1 (en) * | 2018-12-21 | 2021-08-12 | Actelion Pharmaceuticals Ltd | Pharmaceutical composition for the treatment of pulmonary arterial hypertension |
-
2017
- 2017-11-06 MA MA049664A patent/MA49664A/fr unknown
- 2017-11-06 BR BR112019017658-6A patent/BR112019017658A2/pt unknown
- 2017-11-06 US US16/489,227 patent/US11174247B2/en active Active
- 2017-11-06 SG SG11201907435PA patent/SG11201907435PA/en unknown
- 2017-11-06 WO PCT/EP2017/078371 patent/WO2018153513A1/en active Application Filing
- 2017-11-06 CA CA3053991A patent/CA3053991A1/en active Pending
- 2017-11-06 KR KR1020197028199A patent/KR102568472B1/ko active IP Right Grant
- 2017-11-06 JP JP2019546291A patent/JP7223701B2/ja active Active
- 2017-11-06 KR KR1020237016438A patent/KR20230074610A/ko active IP Right Grant
- 2017-11-06 CN CN201780087445.XA patent/CN110325186A/zh active Pending
- 2017-11-06 MX MX2019010222A patent/MX2019010222A/es unknown
- 2017-11-06 AU AU2017400276A patent/AU2017400276B2/en active Active
- 2017-11-06 EP EP17794712.4A patent/EP3658140A1/en active Pending
- 2017-11-06 UA UAA201909965A patent/UA126122C2/uk unknown
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2018
- 2018-02-26 WO PCT/EP2018/054627 patent/WO2018154101A1/en active Application Filing
- 2018-02-26 SG SG11201907604UA patent/SG11201907604UA/en unknown
- 2018-02-26 TW TW107106403A patent/TWI786089B/zh active
- 2018-02-26 IL IL297993A patent/IL297993A/en unknown
- 2018-02-26 SG SG10202111695RA patent/SG10202111695RA/en unknown
- 2018-02-26 CN CN202311718027.XA patent/CN117946011A/zh active Pending
- 2018-02-26 CA CA3053994A patent/CA3053994A1/en active Pending
- 2018-02-26 AU AU2018225309A patent/AU2018225309B2/en active Active
- 2018-02-26 MX MX2019010221A patent/MX2019010221A/es unknown
- 2018-02-26 EP EP18708945.3A patent/EP3585391A1/en not_active Withdrawn
- 2018-02-26 BR BR112019017644-6A patent/BR112019017644A2/pt unknown
- 2018-02-26 KR KR1020197028200A patent/KR102577375B1/ko active IP Right Grant
- 2018-02-26 MA MA047596A patent/MA47596A/fr unknown
- 2018-02-26 JP JP2019546286A patent/JP2020508338A/ja active Pending
- 2018-02-26 US US16/489,194 patent/US10919881B2/en active Active
- 2018-02-26 EP EP21202979.7A patent/EP4014976A1/en active Pending
- 2018-02-26 TW TW111142832A patent/TW202330502A/zh unknown
- 2018-02-26 CN CN201880014146.8A patent/CN110381948A/zh active Pending
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2019
- 2019-08-22 IL IL26885019A patent/IL268850A/en unknown
- 2019-08-22 IL IL26885219A patent/IL268852A/en unknown
- 2019-08-22 PH PH12019501937A patent/PH12019501937A1/en unknown
- 2019-08-22 PH PH12019501938A patent/PH12019501938A1/en unknown
- 2019-08-27 CL CL2019002470A patent/CL2019002470A1/es unknown
- 2019-08-27 MX MX2021007184A patent/MX2021007184A/es unknown
- 2019-08-27 CL CL2019002464A patent/CL2019002464A1/es unknown
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2020
- 2020-06-30 CL CL2020001762A patent/CL2020001762A1/es unknown
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2021
- 2021-01-12 US US17/146,801 patent/US11680058B2/en active Active
- 2021-09-10 US US17/472,349 patent/US11787782B2/en active Active
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2022
- 2022-12-16 JP JP2022201112A patent/JP2023027305A/ja active Pending
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2023
- 2023-05-17 US US18/319,402 patent/US20230391757A1/en active Pending
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