IL250909B - N-Alkylaryl-5-oxyaryl-octahydro-cyclopent[c]pyrrole negative allosteric modulators of nr2b - Google Patents
N-Alkylaryl-5-oxyaryl-octahydro-cyclopent[c]pyrrole negative allosteric modulators of nr2bInfo
- Publication number
- IL250909B IL250909B IL250909A IL25090917A IL250909B IL 250909 B IL250909 B IL 250909B IL 250909 A IL250909 A IL 250909A IL 25090917 A IL25090917 A IL 25090917A IL 250909 B IL250909 B IL 250909B
- Authority
- IL
- Israel
- Prior art keywords
- oxyaryl
- nr2b
- octahydro
- cyclopenta
- alkylaryl
- Prior art date
Links
- 229940126662 negative allosteric modulator Drugs 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
-
- 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
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
-
- 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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D403/06—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 carbon chain containing only aliphatic carbon 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
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyrrole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462056284P | 2014-09-26 | 2014-09-26 | |
| PCT/US2015/051694 WO2016049165A1 (en) | 2014-09-26 | 2015-09-23 | N-alkylaryl-5-oxyaryl-octahydro-cyclopenta[c]pyrrole negative allosteric modulators of nr2b |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL250909A0 IL250909A0 (en) | 2017-04-30 |
| IL250909B true IL250909B (en) | 2019-06-30 |
Family
ID=55581945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL250909A IL250909B (en) | 2014-09-26 | 2017-03-02 | N-Alkylaryl-5-oxyaryl-octahydro-cyclopent[c]pyrrole negative allosteric modulators of nr2b |
Country Status (40)
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3579B1 (ar) | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
| WO2019079783A1 (en) | 2017-10-20 | 2019-04-25 | Vanderbilt University | ANTAGONISTS OF THE MUSCARINIC RECEPTOR OF ACETYLCHOLINE M4 |
| JP2021503443A (ja) | 2017-10-31 | 2021-02-12 | ヴァンダービルト ユニバーシティー | ムスカリン性アセチルコリン受容体ｍ４のアンタゴニスト |
| WO2019152809A1 (en) | 2018-02-02 | 2019-08-08 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor m4 |
| PE20210452A1 (es) | 2018-03-05 | 2021-03-08 | Arcus Biosciences Inc | Inhibidores de la arginasa |
| JP7318015B2 (ja) * | 2019-06-04 | 2023-07-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 特に抑うつ病性障害の処置のための、ｎｒ２ｂネガティブ調節剤としてのプリン誘導体および医薬としてのその使用 |
| EP3980420B1 (en) | 2019-06-04 | 2023-04-19 | Boehringer Ingelheim International GmbH | Imidazopyrazine derivatives and the use thereof as medicament |
| CN111481543A (zh) * | 2020-05-21 | 2020-08-04 | 苏州健雄职业技术学院 | Nr2b负变构调节剂联合gaba受体调节剂在制备治疗阿尔兹海默症的药物中的用途 |
| CN116744922A (zh) * | 2020-12-04 | 2023-09-12 | 诺华股份有限公司 | Nr2b-nmda受体nam在治疗抑郁症中的剂量方案 |
| IL303357A (en) * | 2020-12-04 | 2023-08-01 | Novartis Ag | Dosage regimen for a nr2b-nmda receptor nam for the treatment of depression |
| JP2021058765A (ja) * | 2021-01-19 | 2021-04-15 | 株式会社藤商事 | 遊技機 |
| EP4313041A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTAL[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
| CN117120053A (zh) * | 2021-03-26 | 2023-11-24 | 诺华股份有限公司 | 新的环戊二烯并[c]吡咯NR2B负变构调节剂 |
| EP4531851A1 (en) | 2022-06-02 | 2025-04-09 | Novartis AG | Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders |
| IL322082A (en) | 2023-01-12 | 2025-09-01 | Novartis Ag | Engineered ketoreductase polypeptides |
| TW202539663A (zh) | 2023-12-06 | 2025-10-16 | 瑞士商諾華公司 | 用於治療抑鬱障礙之組成物和方法 |
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| US5532243A (en) | 1992-02-14 | 1996-07-02 | The Dupont Merck Pharmaceutical Company | Antipsychotic nitrogen-containing bicyclic compounds |
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| DE4341403A1 (de) | 1993-12-04 | 1995-06-08 | Basf Ag | N-substituierte 3-Azabicycloalkan-Derivate, ihre Herstellung und Verwendung |
| US5726172A (en) * | 1996-01-16 | 1998-03-10 | Merck & Co., Inc. | Tocolytic oxytocin receptor antagonists |
| US6369076B1 (en) * | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
| AU2005219438B2 (en) | 2004-03-03 | 2011-02-17 | Chemocentryx, Inc. | Bicyclic and bridged nitrogen heterocycles |
| US7696241B2 (en) | 2004-03-04 | 2010-04-13 | Bristol-Myers Squibb Company | Bicyclic compounds as modulators of androgen receptor function and method |
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| JP2008507543A (ja) | 2004-07-22 | 2008-03-13 | グラクソ グループ リミテッド | 抗細菌剤 |
| HUP0401523A3 (en) | 2004-07-29 | 2007-05-02 | Richter Gedeon Vegyeszet | Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them |
| AU2006236625A1 (en) | 2005-04-19 | 2006-10-26 | Merck & Co., Inc. | N-alkyl-azacycloalkyl NMDA/NR2B antagonists |
| EP1849772A1 (en) | 2006-04-28 | 2007-10-31 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
| US8299113B2 (en) | 2006-04-28 | 2012-10-30 | Laboratorios Del Dr. Esteve, S.A. | Bicyclic tetrahydropyrrole compounds |
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| JP2011500727A (ja) | 2007-10-22 | 2011-01-06 | シェーリング コーポレイション | Ｇｐｒ１１９の活性のモジュレーターとしての二環式ヘテロ環誘導体およびその使用 |
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| WO2010068851A1 (en) | 2008-12-12 | 2010-06-17 | Vanderbilt Universtiy | 3.3.0 bicyclic glyt1 inhibitors and methods of making and using same |
| FR2945533B1 (fr) | 2009-05-12 | 2011-05-27 | Sanofi Aventis | Derives de cyclopenta°c!pyrrolyl-alkylcarbamates d'heterocycles a 5 chainons, leur preparation et leur application en therapeutique |
| FR2945534B1 (fr) * | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
| BR112012016733A2 (pt) | 2010-01-07 | 2015-09-01 | Du Pont | "composto, composição fungicida e método" |
| WO2011149993A2 (en) | 2010-05-25 | 2011-12-01 | Abbott Laboratories | SUBSTITUTED OCTAHYDROCYCLOPENTA[c]PYRROLES AS CALCIUM CHANNEL MODULATORS |
| CN102432598A (zh) * | 2010-09-29 | 2012-05-02 | 江苏恒瑞医药股份有限公司 | 三环化合物、其制备方法及其在医药上的应用 |
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| JO3611B1 (ar) * | 2011-08-10 | 2020-08-27 | Janssen Sciences Ireland Uc | سايكلو بنتا (سي (بيرول 4,3 ثاني هيدرو 1 hمستبدله [8,1] نافثيريدينونات مضادة للجراثيم |
| DK2796460T3 (en) | 2011-12-21 | 2018-08-27 | Jiangsu Hengrui Medicine Co | SEXUAL PYRROL HETEROARYL RING DERIVATIVES, METHOD OF PREPARATION AND MEDICAL APPLICATIONS THEREOF |
| HRP20191937T1 (hr) * | 2012-09-25 | 2020-01-10 | F. Hoffmann - La Roche Ag | Derivati heksahidropirolo [3,4-c]pirola i srodni spojevi kao inhibitori autotaksina (atx) i kao inhibitori proizvodnje lizofosfatidne kiseline (lpa) za liječenje npr. bubrežnih bolesti |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| US9418332B2 (en) | 2013-08-16 | 2016-08-16 | Qualcomm Incorporated | Post ghost plasticity |
| EP3036221B1 (en) * | 2013-09-26 | 2018-11-07 | Cadent Therapeutics, Inc. | Selective octahydro-cyclopenta[c]pyrrole negative modulators of nr2b |
| UA118582C2 (uk) | 2014-03-26 | 2019-02-11 | Ф. Хоффманн-Ля Рош Аг | Біциклічні сполуки як інгібітори продукції аутотаксину (atx) і лізофосфатидилової кислоти (lpa) |
| JO3579B1 (ar) | 2014-09-26 | 2020-07-05 | Luc Therapeutics Inc | مُعدِلات تفاغرية سالبة لمستقبل nr2b من المركب n-ألكيل أريل-5-أوكسي أريل-ثامن هيدرو-خماسي الحلقة [c] بيرول |
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2015
- 2015-09-22 JO JOP/2015/0237A patent/JO3579B1/ar active
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active Active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 EP EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 MX MX2017003940A patent/MX374657B/es active IP Right Grant
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en not_active Ceased
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en not_active IP Right Cessation
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
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2017
- 2017-02-13 ZA ZA2017/01061A patent/ZA201701061B/en unknown
- 2017-02-28 CL CL2017000474A patent/CL2017000474A1/es unknown
- 2017-03-02 IL IL250909A patent/IL250909B/en active IP Right Grant
- 2017-03-15 CO CONC2017/0002494A patent/CO2017002494A2/es unknown
- 2017-03-17 PH PH12017500513A patent/PH12017500513A1/en unknown
- 2017-03-24 GT GT201700062A patent/GT201700062A/es unknown
- 2017-04-24 EC ECIEPI201725302A patent/ECSP17025302A/es unknown
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2019
- 2019-01-23 JP JP2019008873A patent/JP6772307B2/ja active Active
- 2019-01-23 US US16/255,500 patent/US10781174B2/en active Active
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2020
- 2020-06-15 CY CY20201100542T patent/CY1123533T1/el unknown
- 2020-08-12 US US16/991,684 patent/US20200369610A1/en not_active Abandoned
- 2020-09-30 JP JP2020166129A patent/JP7216060B2/ja active Active
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2022
- 2022-05-03 US US17/735,386 patent/US12145909B2/en active Active
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2023
- 2023-01-19 JP JP2023006525A patent/JP7612722B2/ja active Active
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2024
- 2024-12-25 JP JP2024228390A patent/JP2025060835A/ja active Pending
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