SA518392325B1 - حمض (2s،4r)-5-(5'-كلورو -2'-فلورو-[1،1'-باي فينيل ]-4-يل )-2-(إيثوكسي ميثيل )-4-(3-هيدروكسي أيزوكسازول -5-كربوكساميدو )-2-ميثيل بنتانويك بلوري واستخداماته - Google Patents
حمض (2s،4r)-5-(5'-كلورو -2'-فلورو-[1،1'-باي فينيل ]-4-يل )-2-(إيثوكسي ميثيل )-4-(3-هيدروكسي أيزوكسازول -5-كربوكساميدو )-2-ميثيل بنتانويك بلوري واستخداماتهInfo
- Publication number
- SA518392325B1 SA518392325B1 SA518392325A SA518392325A SA518392325B1 SA 518392325 B1 SA518392325 B1 SA 518392325B1 SA 518392325 A SA518392325 A SA 518392325A SA 518392325 A SA518392325 A SA 518392325A SA 518392325 B1 SA518392325 B1 SA 518392325B1
- Authority
- SA
- Saudi Arabia
- Prior art keywords
- crystalline
- hydroxyisoxazole
- carboxamido
- ethoxymethyl
- biphenyl
- Prior art date
Links
- IFWBKJFCPSEDNJ-CJAUYULYSA-N (2s,4r)-5-[4-(5-chloro-2-fluorophenyl)phenyl]-2-(ethoxymethyl)-2-methyl-4-[(3-oxo-1,2-oxazole-5-carbonyl)amino]pentanoic acid Chemical compound C([C@H](C[C@@](C)(COCC)C(O)=O)NC(=O)C=1ONC(=O)C=1)C(C=C1)=CC=C1C1=CC(Cl)=CC=C1F IFWBKJFCPSEDNJ-CJAUYULYSA-N 0.000 title 1
- 102000003729 Neprilysin Human genes 0.000 abstract 1
- 108090000028 Neprilysin Proteins 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
- C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
- C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
- C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members 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
- C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
-
- 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
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/42—Oxazoles
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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)
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662305393P | 2016-03-08 | 2016-03-08 | |
| US201662346336P | 2016-06-06 | 2016-06-06 | |
| PCT/US2017/021172 WO2017156009A1 (en) | 2016-03-08 | 2017-03-07 | Crystalline(2s,4r)-5-(5'-chloro-2'-fluoro-[1,1'-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SA518392325B1 true SA518392325B1 (ar) | 2022-08-03 |
Family
ID=58387911
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SA518392325A SA518392325B1 (ar) | 2016-03-08 | 2018-09-02 | حمض (2s،4r)-5-(5'-كلورو -2'-فلورو-[1،1'-باي فينيل ]-4-يل )-2-(إيثوكسي ميثيل )-4-(3-هيدروكسي أيزوكسازول -5-كربوكساميدو )-2-ميثيل بنتانويك بلوري واستخداماته |
Country Status (30)
| Country | Link |
|---|---|
| US (6) | US10100021B2 (enExample) |
| EP (1) | EP3408260B1 (enExample) |
| JP (2) | JP7306828B2 (enExample) |
| KR (2) | KR20220035991A (enExample) |
| CN (1) | CN108779084A (enExample) |
| AU (1) | AU2017229466C1 (enExample) |
| CA (1) | CA3015505C (enExample) |
| CL (1) | CL2018002539A1 (enExample) |
| CO (1) | CO2018010568A2 (enExample) |
| CY (1) | CY1124397T1 (enExample) |
| DK (1) | DK3408260T3 (enExample) |
| ES (1) | ES2880123T3 (enExample) |
| HR (1) | HRP20211169T1 (enExample) |
| HU (1) | HUE055546T2 (enExample) |
| IL (1) | IL261244B (enExample) |
| LT (1) | LT3408260T (enExample) |
| MX (1) | MX377177B (enExample) |
| MY (1) | MY198185A (enExample) |
| PH (1) | PH12018501876A1 (enExample) |
| PL (1) | PL3408260T3 (enExample) |
| PT (1) | PT3408260T (enExample) |
| RS (1) | RS62172B1 (enExample) |
| RU (1) | RU2756223C2 (enExample) |
| SA (1) | SA518392325B1 (enExample) |
| SG (1) | SG11201807591VA (enExample) |
| SI (1) | SI3408260T1 (enExample) |
| SM (1) | SMT202100434T1 (enExample) |
| TW (1) | TWI731943B (enExample) |
| WO (1) | WO2017156009A1 (enExample) |
| ZA (1) | ZA201805840B (enExample) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE055546T2 (hu) | 2016-03-08 | 2021-12-28 | Theravance Biopharma R&D Ip Llc | Kristályos (2S,4R)-5-(5'-klór-2-fluor-[1,1'-bifenil]-4-il)-2-(etoximetil)-4-(3-hidroxi izoxazol-5-karboxamido)-2-metilpentánsav és alkalmazásaik |
| CN115487175B (zh) * | 2019-09-20 | 2024-05-14 | 深圳信立泰药业股份有限公司 | 血管紧张素ii受体拮抗剂代谢产物与nep抑制剂的复合物治疗心衰的用途 |
| KR102485499B1 (ko) * | 2022-07-15 | 2023-01-09 | 오가노이드사이언스 주식회사 | 신장 질환의 치료 또는 예방용 조성물 |
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| US4189604A (en) | 1975-07-22 | 1980-02-19 | Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai | Bestatin |
| US4206232A (en) | 1976-05-10 | 1980-06-03 | E. R. Squibb & Sons, Inc. | Relieving hypertension with carboxyalkylacylamino acids |
| IL58849A (en) | 1978-12-11 | 1983-03-31 | Merck & Co Inc | Carboxyalkyl dipeptides and derivatives thereof,their preparation and pharmaceutical compositions containing them |
| FR2480747A1 (fr) | 1980-04-17 | 1981-10-23 | Roques Bernard | Derives d'acides amines et leur application therapeutique |
| US4906615A (en) | 1980-12-18 | 1990-03-06 | Schering Corporation | Substituted dipeptides as inhibitors of enkephalinases |
| US4722810A (en) | 1984-08-16 | 1988-02-02 | E. R. Squibb & Sons, Inc. | Enkephalinase inhibitors |
| US4939261A (en) | 1984-06-08 | 1990-07-03 | Ciba-Geigy Corporation | N-substituted butyramide derivatives useful for treatment of conditions responsive to inhibition of enkephalinase |
| EP0225292A3 (en) | 1985-12-06 | 1988-11-30 | Ciba-Geigy Ag | Certain n-substituted butyramide derivatives |
| US4929641B1 (en) | 1988-05-11 | 1994-08-30 | Schering Corp | Mercapto-acylamino acid antihypertensives |
| KR880007441A (ko) | 1986-12-11 | 1988-08-27 | 알렌 제이.스피겔 | 스피로-치환된 글루타르아미드 이뇨제 |
| FR2623498B1 (fr) | 1987-11-24 | 1990-04-06 | Bioprojet Soc Civ | Nouveaux composes enantiomeres derives d'amino-acides, leur procede de preparation et leurs applications therapeutiques |
| GB8820844D0 (en) | 1988-09-05 | 1988-10-05 | Pfizer Ltd | Therapeutic agents |
| US5599951A (en) | 1989-09-15 | 1997-02-04 | Societe Civile Bioprojet | Amino acid derivatives, the process for their preparation and their applications to therapy |
| US5294632A (en) | 1991-05-01 | 1994-03-15 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipetide derivatives |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| US5217996A (en) | 1992-01-22 | 1993-06-08 | Ciba-Geigy Corporation | Biaryl substituted 4-amino-butyric acid amides |
| US5508272A (en) | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| DE19510566A1 (de) | 1995-03-23 | 1996-09-26 | Kali Chemie Pharma Gmbh | Benzazepin-, Benzoxazepin- und Benzothiazepin-N-essigsäurederivate sowie Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel |
| EP0821670A1 (en) | 1995-04-21 | 1998-02-04 | Novartis AG | N-aroylamino acid amides as endothelin inhibitors |
| US6660756B2 (en) | 2001-03-28 | 2003-12-09 | Pfizer Inc. | N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase |
| GB0119305D0 (en) | 2001-04-12 | 2001-10-03 | Aventis Pharma Gmbh | Mercaptoacetylamide derivatives,a process for their preparation and their use |
| WO2006027680A1 (en) | 2004-09-10 | 2006-03-16 | Pfizer Limited | 3-(1-carbamoylcyclohexyl) propionic acid derivatives as inhibitors of neutral endopeptidase enzyme |
| AR057882A1 (es) | 2005-11-09 | 2007-12-26 | Novartis Ag | Compuestos de accion doble de bloqueadores del receptor de angiotensina e inhibidores de endopeptidasa neutra |
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| WO2007106708A2 (en) | 2006-03-10 | 2007-09-20 | Novartis Ag | Combinations of the angiotensin ii antagonist valsartan and the nep inhibitor daglutril |
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| AR070176A1 (es) | 2008-01-17 | 2010-03-17 | Novartis Ag | Procesos de sintesis de inhibidores de nep, compuestos intermediarios y uso de los mismos en la sintesis |
| CN102448928B (zh) | 2009-05-28 | 2014-10-01 | 诺华股份有限公司 | 作为中性溶酶(neprilysin)抑制剂的取代的氨基丁酸衍生物 |
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| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| WO2011088797A1 (en) | 2010-01-22 | 2011-07-28 | Novartis Ag | Intermediates of neutral endopeptidase inhibitors and preparation method thereof |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| US8993631B2 (en) | 2010-11-16 | 2015-03-31 | Novartis Ag | Method of treating contrast-induced nephropathy |
| CA2819153A1 (en) | 2010-12-15 | 2012-06-21 | Theravance, Inc. | Neprilysin inhibitors |
| HRP20151115T1 (en) | 2010-12-15 | 2015-11-20 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| KR101854874B1 (ko) * | 2011-02-17 | 2018-05-04 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제로서 치환된 아미노부티릭 유도체 |
| US8449890B2 (en) | 2011-02-17 | 2013-05-28 | Theravance, Inc. | Neprilysin inhibitors |
| CN103596928B (zh) | 2011-05-31 | 2017-02-15 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| WO2012166389A1 (en) | 2011-05-31 | 2012-12-06 | Theravance, Inc. | Neprilysin inhibitors |
| EP2714660B1 (en) | 2011-05-31 | 2018-09-26 | Theravance Biopharma R&D IP, LLC | Neprilysin inhibitors |
| TWI560172B (en) | 2011-11-02 | 2016-12-01 | Theravance Biopharma R&D Ip Llc | Neprilysin inhibitors |
| ES2609810T3 (es) | 2012-05-31 | 2017-04-24 | Theravance Biopharma R&D Ip, Llc | Inhibidores de neprilisina donadores de óxido nítrico |
| PT2864292T (pt) | 2012-06-08 | 2017-07-10 | Theravance Biopharma R&D Ip Llc | Inibidores de neprisilina |
| CN104470521B (zh) | 2012-06-08 | 2017-04-12 | 施万生物制药研发Ip有限责任公司 | 脑啡肽酶抑制剂 |
| KR102104954B1 (ko) * | 2012-08-08 | 2020-04-27 | 세라밴스 바이오파마 알앤디 아이피, 엘엘씨 | 네프릴리신 억제제 |
| JP6130061B2 (ja) * | 2013-06-19 | 2017-05-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | インドリン−２−オン又はピロロ−ピリジン／ピリミジン−２−オン誘導体 |
| AU2015210983B2 (en) * | 2014-01-30 | 2018-10-04 | Theravance Biopharma R&D Ip, Llc | Neprilysin inhibitors |
| HUE055546T2 (hu) | 2016-03-08 | 2021-12-28 | Theravance Biopharma R&D Ip Llc | Kristályos (2S,4R)-5-(5'-klór-2-fluor-[1,1'-bifenil]-4-il)-2-(etoximetil)-4-(3-hidroxi izoxazol-5-karboxamido)-2-metilpentánsav és alkalmazásaik |
-
2017
- 2017-03-07 HU HUE17712605A patent/HUE055546T2/hu unknown
- 2017-03-07 MX MX2018010727A patent/MX377177B/es active IP Right Grant
- 2017-03-07 MY MYPI2018702868A patent/MY198185A/en unknown
- 2017-03-07 RU RU2018135072A patent/RU2756223C2/ru active
- 2017-03-07 EP EP17712605.9A patent/EP3408260B1/en active Active
- 2017-03-07 SI SI201730845T patent/SI3408260T1/sl unknown
- 2017-03-07 US US15/452,333 patent/US10100021B2/en active Active
- 2017-03-07 JP JP2018546864A patent/JP7306828B2/ja active Active
- 2017-03-07 PT PT177126059T patent/PT3408260T/pt unknown
- 2017-03-07 AU AU2017229466A patent/AU2017229466C1/en active Active
- 2017-03-07 DK DK17712605.9T patent/DK3408260T3/da active
- 2017-03-07 KR KR1020227008251A patent/KR20220035991A/ko not_active Ceased
- 2017-03-07 ES ES17712605T patent/ES2880123T3/es active Active
- 2017-03-07 CN CN201780016076.5A patent/CN108779084A/zh active Pending
- 2017-03-07 HR HRP20211169TT patent/HRP20211169T1/hr unknown
- 2017-03-07 CA CA3015505A patent/CA3015505C/en active Active
- 2017-03-07 LT LTEP17712605.9T patent/LT3408260T/lt unknown
- 2017-03-07 SG SG11201807591VA patent/SG11201807591VA/en unknown
- 2017-03-07 SM SM20210434T patent/SMT202100434T1/it unknown
- 2017-03-07 KR KR1020187028757A patent/KR20180114225A/ko not_active Ceased
- 2017-03-07 WO PCT/US2017/021172 patent/WO2017156009A1/en not_active Ceased
- 2017-03-07 RS RS20210963A patent/RS62172B1/sr unknown
- 2017-03-07 PL PL17712605T patent/PL3408260T3/pl unknown
- 2017-03-07 TW TW106107450A patent/TWI731943B/zh active
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2018
- 2018-08-20 IL IL261244A patent/IL261244B/en unknown
- 2018-08-30 ZA ZA2018/05840A patent/ZA201805840B/en unknown
- 2018-09-02 SA SA518392325A patent/SA518392325B1/ar unknown
- 2018-09-03 PH PH12018501876A patent/PH12018501876A1/en unknown
- 2018-09-05 CL CL2018002539A patent/CL2018002539A1/es unknown
- 2018-09-10 US US16/125,991 patent/US10472335B2/en active Active
- 2018-10-02 CO CONC2018/0010568A patent/CO2018010568A2/es unknown
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2019
- 2019-09-25 US US16/582,051 patent/US10752599B2/en active Active
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2020
- 2020-07-14 US US16/928,206 patent/US11230536B2/en active Active
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2021
- 2021-07-30 CY CY20211100685T patent/CY1124397T1/el unknown
- 2021-10-29 JP JP2021177448A patent/JP2022017433A/ja active Pending
- 2021-12-14 US US17/550,564 patent/US11718591B2/en active Active
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2024
- 2024-02-15 US US18/442,885 patent/US12351561B2/en active Active
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