ECSP17025302A - N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostéricos negativos de nr2b - Google Patents
N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostéricos negativos de nr2bInfo
- Publication number
- ECSP17025302A ECSP17025302A ECIEPI201725302A ECPI201725302A ECSP17025302A EC SP17025302 A ECSP17025302 A EC SP17025302A EC IEPI201725302 A ECIEPI201725302 A EC IEPI201725302A EC PI201725302 A ECPI201725302 A EC PI201725302A EC SP17025302 A ECSP17025302 A EC SP17025302A
- Authority
- EC
- Ecuador
- Prior art keywords
- alkylaril
- pirrol
- oxyaryl
- negative allosteric
- allosteric modulators
- Prior art date
Links
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title abstract 3
- 102000034527 Retinoid X Receptors Human genes 0.000 title abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 title abstract 2
- 229940126662 negative allosteric modulator Drugs 0.000 title abstract 2
- 208000012902 Nervous system disease Diseases 0.000 abstract 1
- 208000025966 Neurological disease Diseases 0.000 abstract 1
Classifications
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- 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
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- 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
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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
- C07D401/06—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
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- 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)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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)
- Pyrrole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (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)
Abstract
La presente invención se refiere a un modulador alostérico negativo de N-alquiarilo-5-oxiarilo-octadihidrociclopentano[c]pirrol para receptores NR2B, los cuales son importantes en el tratamiento de enfermedades neurológicas y tienen la siguiente formula: (I) Dónde R1, R2, L1, L2, X, Y y Y están descritos en la presente.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462056284P | 2014-09-26 | 2014-09-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
ECSP17025302A true ECSP17025302A (es) | 2018-11-30 |
Family
ID=55581945
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ECIEPI201725302A ECSP17025302A (es) | 2014-09-26 | 2017-04-24 | N-alquilaril-5-oxiaril-octahidro ciclopenta[c]pirrol moduladores alostéricos negativos de nr2b |
Country Status (40)
Country | Link |
---|---|
US (4) | US10239835B2 (es) |
EP (4) | EP4282412A3 (es) |
JP (5) | JP6473227B2 (es) |
KR (1) | KR102479356B1 (es) |
CN (1) | CN106795111B (es) |
AP (1) | AP2017009832A0 (es) |
AR (1) | AR103199A1 (es) |
AU (1) | AU2015320721B2 (es) |
BR (1) | BR112017006093B1 (es) |
CA (1) | CA2962569C (es) |
CL (1) | CL2017000474A1 (es) |
CO (1) | CO2017002494A2 (es) |
CR (1) | CR20170114A (es) |
CU (1) | CU24482B1 (es) |
CY (1) | CY1123533T1 (es) |
DK (1) | DK3197868T3 (es) |
EA (1) | EA034937B1 (es) |
EC (1) | ECSP17025302A (es) |
ES (3) | ES2911004T3 (es) |
GT (1) | GT201700062A (es) |
HR (1) | HRP20200959T1 (es) |
HU (1) | HUE049698T2 (es) |
IL (1) | IL250909B (es) |
JO (1) | JO3579B1 (es) |
LT (1) | LT3197868T (es) |
MX (1) | MX374657B (es) |
MY (1) | MY182342A (es) |
NZ (1) | NZ729569A (es) |
PE (1) | PE20170893A1 (es) |
PH (1) | PH12017500513A1 (es) |
PL (1) | PL3197868T3 (es) |
PT (1) | PT3197868T (es) |
RS (1) | RS60497B1 (es) |
SG (1) | SG11201702023QA (es) |
SI (1) | SI3197868T1 (es) |
TN (1) | TN2017000076A1 (es) |
TW (1) | TWI687407B (es) |
UY (1) | UY36326A (es) |
WO (1) | WO2016049165A1 (es) |
ZA (1) | ZA201701061B (es) |
Families Citing this family (14)
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 |
KR102776114B1 (ko) | 2017-10-20 | 2025-03-07 | 반더빌트유니버시티 | 무스카린성 아세틸콜린 수용체 m4의 길항제 |
US11352344B2 (en) | 2017-10-31 | 2022-06-07 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
AU2019216492A1 (en) | 2018-02-02 | 2020-08-20 | Vanderbilt University | Antagonists of the muscarinic acetylcholine receptor M4 |
CN111818928A (zh) | 2018-03-05 | 2020-10-23 | 艾库斯生物科学有限公司 | 精氨酸酶抑制剂 |
CN113950478B (zh) * | 2019-06-04 | 2024-02-02 | 勃林格殷格翰国际有限公司 | 作为nr2b负向调节剂的嘌呤衍生物及其作为药物的用途,特别是用于治疗抑郁病症 |
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 |
WO2022118264A1 (en) | 2020-12-04 | 2022-06-09 | 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 |
PE20250399A1 (es) | 2021-03-26 | 2025-02-11 | Novartis Ag | Nuevos moduladores alostericos negativos ciclopenta[c]pirrol de nr2b |
EP4313042A4 (en) * | 2021-03-26 | 2025-01-15 | Novartis AG | NEW CYCLOPENTA[C PYRROL NEGATIVE ALLOSTERIC MODULATORS OF NR2B |
AU2023278502A1 (en) | 2022-06-02 | 2025-01-02 | Novartis Ag | Subcutaneous administration of onfasprodil and dosing methods for use in the treatment of depression disorders |
WO2024150146A1 (en) | 2023-01-12 | 2024-07-18 | Novartis Ag | Engineered ketoreductase polypeptides |
WO2025120013A1 (en) | 2023-12-06 | 2025-06-12 | Novartis Ag | Compositions and methods for treating depression disorders |
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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 |
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EP1720545B1 (en) | 2004-03-03 | 2014-10-29 | 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 |
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EP2378885A4 (en) | 2008-12-12 | 2013-01-02 | Univ Vanderbilt | 3.3.0 BICYCLIC GLYT1 INHIBITORS AND METHOD FOR THE PRODUCTION AND USE THEREOF |
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FR2945534B1 (fr) * | 2009-05-12 | 2012-11-16 | Sanofi Aventis | DERIVES DE CYCLOPENTAL[c]PYRROLE-2-CARBOXYLATES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE |
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PE20150758A1 (es) * | 2012-09-25 | 2015-05-15 | Hoffmann La Roche | Nuevos derivados biciclicos |
AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
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ES2707739T3 (es) * | 2013-09-26 | 2019-04-04 | Cadent Therapeutics Inc | Moduladores negativos de octahidro-ciclopenta[c]pirrol selectivo de NR2B |
ES2753549T3 (es) | 2014-03-26 | 2020-04-13 | Hoffmann La Roche | Compuestos bicíclicos como inhibidores de la producción de autotaxina (ATX) y ácido lisofosfatídico (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 EP23185898.6A patent/EP4282412A3/en active Pending
- 2015-09-23 EA EA201790713A patent/EA034937B1/ru not_active IP Right Cessation
- 2015-09-23 CA CA2962569A patent/CA2962569C/en active Active
- 2015-09-23 SG SG11201702023QA patent/SG11201702023QA/en unknown
- 2015-09-23 RS RS20200721A patent/RS60497B1/sr unknown
- 2015-09-23 BR BR112017006093-0A patent/BR112017006093B1/pt active IP Right Grant
- 2015-09-23 CR CR20170114A patent/CR20170114A/es unknown
- 2015-09-23 PL PL15844057T patent/PL3197868T3/pl unknown
- 2015-09-23 NZ NZ729569A patent/NZ729569A/en not_active IP Right Cessation
- 2015-09-23 TN TN2017000076A patent/TN2017000076A1/en unknown
- 2015-09-23 KR KR1020177007813A patent/KR102479356B1/ko active Active
- 2015-09-23 AP AP2017009832A patent/AP2017009832A0/en unknown
- 2015-09-23 EP EP20159713.5A patent/EP3683207B1/en active Active
- 2015-09-23 US US15/506,592 patent/US10239835B2/en active Active
- 2015-09-23 EP EP21202255.2A patent/EP3974420B1/en active Active
- 2015-09-23 CN CN201580051671.3A patent/CN106795111B/zh active Active
- 2015-09-23 DK DK15844057.8T patent/DK3197868T3/da active
- 2015-09-23 MX MX2017003940A patent/MX374657B/es active IP Right Grant
- 2015-09-23 WO PCT/US2015/051694 patent/WO2016049165A1/en not_active Application Discontinuation
- 2015-09-23 ES ES20159713T patent/ES2911004T3/es active Active
- 2015-09-23 ES ES15844057T patent/ES2791327T3/es active Active
- 2015-09-23 PE PE2017000506A patent/PE20170893A1/es unknown
- 2015-09-23 MY MYPI2017700652A patent/MY182342A/en unknown
- 2015-09-23 AU AU2015320721A patent/AU2015320721B2/en active Active
- 2015-09-23 PT PT158440578T patent/PT3197868T/pt unknown
- 2015-09-23 EP EP15844057.8A patent/EP3197868B1/en active Active
- 2015-09-23 HR HRP20200959TT patent/HRP20200959T1/hr unknown
- 2015-09-23 LT LTEP15844057.8T patent/LT3197868T/lt unknown
- 2015-09-23 ES ES21202255T patent/ES2956546T3/es active Active
- 2015-09-23 CU CU2017000037A patent/CU24482B1/es unknown
- 2015-09-23 JP JP2017516358A patent/JP6473227B2/ja active Active
- 2015-09-23 SI SI201531255T patent/SI3197868T1/sl unknown
- 2015-09-23 HU HUE15844057A patent/HUE049698T2/hu unknown
- 2015-09-25 AR ARP150103084A patent/AR103199A1/es active IP Right Grant
- 2015-09-25 UY UY0001036326A patent/UY36326A/es active IP Right Grant
- 2015-09-25 TW TW104131936A patent/TWI687407B/zh active
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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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