AR083694A1 - USO DE COMPUESTOS FARMACEUTICOS ACTIVOS PARA EL TRATAMIENTO DE ESTADOS PATOLOGICOS DEL SISTEMA NERVIOSO CENTRAL, COMPOSICION FARMACEUTICA, MODULADOR ALOSTERICO NEGATIVO DEL GABA A a5, METODO - Google Patents
USO DE COMPUESTOS FARMACEUTICOS ACTIVOS PARA EL TRATAMIENTO DE ESTADOS PATOLOGICOS DEL SISTEMA NERVIOSO CENTRAL, COMPOSICION FARMACEUTICA, MODULADOR ALOSTERICO NEGATIVO DEL GABA A a5, METODOInfo
- Publication number
- AR083694A1 AR083694A1 ARP110104078A ARP110104078A AR083694A1 AR 083694 A1 AR083694 A1 AR 083694A1 AR P110104078 A ARP110104078 A AR P110104078A AR P110104078 A ARP110104078 A AR P110104078A AR 083694 A1 AR083694 A1 AR 083694A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- gaba
- haloalkyl
- hydrogen
- negative allosteric
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- A61K31/54—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
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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- 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
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- 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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- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Uso farmacéutico de moduladores alostéricos negativos selectivos del GABA A a5 para el tratamiento, prevención y/o retardo de la progresión de estados patológicos del sistema nervioso central (SNC) relacionados con la inhibición GABAérgica excesiva en el cerebro.Reivindicación 8: Uso según una cualquiera de las reivindicaciones de 1 a 7, en el que el modulador alostérico negativo del GABA A a5 se elige entre compuestos de la fórmula (1) ó compuestos de la fórmula (2), en las que: R1 es hidrógeno, halógeno, alquilo, haloalquilo o ciano; R2 es hidrógeno, halógeno, alquilo, haloalquilo o ciano; R3 es hidrógeno, alquilo o heterocicloalquilalquilo, dicho heterocicloalquilalquilo está opcionalmente sustituido por uno o más hidroxi, oxo, alquilo, alcoxi, haloalquilo, hidroxialquilo, halógeno o ciano; R4 es arilo o heteroarilo, cada uno está opcionalmente sustituido por uno, dos o tres halógenos; R5 es hidrógeno, alquilo, haloalquilo o hidroxialquilo; R6 es -C(O)-NR7R8; R7 es hidrógeno; R8 es alquilo; o R7 y R8 junto con el átomo de nitrógeno al que están unidos forman un heterocicloalquilo o un heteroarilo, cada uno está opcionalmente sustituido por uno o más hidroxi, oxo, alquilo, alcoxi, haloalquilo, hidroxialquilo, halógeno o ciano; o una sal farmacéuticamente aceptable de los mismos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10190267A EP2457569A1 (en) | 2010-11-05 | 2010-11-05 | Use of active pharmaceutical compounds for the treatment of central nervous system conditions |
| EP10191396 | 2010-11-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR083694A1 true AR083694A1 (es) | 2013-03-13 |
Family
ID=44897774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110104078A AR083694A1 (es) | 2010-11-05 | 2011-11-03 | USO DE COMPUESTOS FARMACEUTICOS ACTIVOS PARA EL TRATAMIENTO DE ESTADOS PATOLOGICOS DEL SISTEMA NERVIOSO CENTRAL, COMPOSICION FARMACEUTICA, MODULADOR ALOSTERICO NEGATIVO DEL GABA A a5, METODO |
Country Status (20)
| Country | Link |
|---|---|
| US (5) | US8835425B2 (es) |
| EP (1) | EP2635277B1 (es) |
| JP (6) | JP2013544808A (es) |
| KR (2) | KR20150123967A (es) |
| CN (1) | CN103189062B (es) |
| AR (1) | AR083694A1 (es) |
| AU (1) | AU2011325190B2 (es) |
| BR (1) | BR112013010895A2 (es) |
| CA (1) | CA2812664C (es) |
| ES (1) | ES2711973T3 (es) |
| HK (1) | HK1182015A1 (es) |
| IL (1) | IL225438A (es) |
| MX (1) | MX341471B (es) |
| MY (1) | MY164595A (es) |
| NZ (1) | NZ608592A (es) |
| PL (1) | PL2635277T3 (es) |
| RU (1) | RU2563167C2 (es) |
| SG (2) | SG10201509163VA (es) |
| TW (1) | TW201240665A (es) |
| WO (1) | WO2012059482A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9206160B2 (en) | 2012-06-26 | 2015-12-08 | Saniona Aps | Phenyl triazole derivative and its use for modulating the GABAA receptor complex |
| AU2014368961B2 (en) * | 2013-12-20 | 2019-10-17 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| AU2016279052A1 (en) * | 2015-06-19 | 2018-02-15 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| LT3551627T (lt) * | 2016-12-08 | 2022-04-25 | F. Hoffmann-La Roche Ag | Nauji izoksazolilo eterio dariniai kaip gaba a alfa5 teigiami alosteriniai moduliatoriai (pam) |
| US11505555B2 (en) | 2016-12-19 | 2022-11-22 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| US20180170941A1 (en) * | 2016-12-19 | 2018-06-21 | Agenebio, Inc. | Benzodiazepine derivatives, compositions, and methods for treating cognitive impairment |
| EA202190076A1 (ru) | 2018-06-19 | 2021-09-22 | Эйджинбайо, Инк. | Производные бензодиазепина, композиции и способы лечения когнитивных нарушений |
| BR102019014802A2 (pt) | 2018-07-20 | 2020-02-04 | Boehringer Ingelheim Int | difluorometil-fenil triazóis |
| HU231223B1 (hu) | 2018-09-28 | 2022-01-28 | Richter Gedeon Nyrt. | GABAA A5 receptor modulátor hatású biciklusos vegyületek |
| US11572344B2 (en) | 2018-11-20 | 2023-02-07 | Nflection Therapeutics, Inc. | Cyanoaryl-aniline compounds for treatment of dermal disorders |
| WO2021191837A1 (en) | 2020-03-26 | 2021-09-30 | Richter Gedeon Nyrt. | 1,3-dihydro-2h-pyrrolo[3,4-c]pyridine derivatives as gabaa α5 receptor modulators |
| IL301496A (en) * | 2020-09-24 | 2023-05-01 | Nflection Therapeutics Inc | Treatment of impaired cognitive function with pyrrolpyridine-anil compounds |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0028583D0 (en) | 2000-11-23 | 2001-01-10 | Merck Sharp & Dohme | Therapeutic compounds |
| PT1540335E (pt) * | 2002-08-19 | 2010-06-23 | Helicon Therapeutics Inc | Métodos de identificação de estimuladores cognitivos |
| GB0311859D0 (en) * | 2003-05-22 | 2003-06-25 | Merck Sharp & Dohme | Therapeutic agents |
| WO2006045429A1 (en) | 2004-10-20 | 2006-05-04 | F. Hoffmann-La Roche Ag | Halogen substituted benzodiazepine derivatives |
| CA2584259C (en) * | 2004-10-20 | 2013-04-02 | F. Hoffmann-La Roche Ag | Imidazo-benzodiazepine derivatives |
| JP4885967B2 (ja) * | 2005-10-11 | 2012-02-29 | エフ．ホフマン−ラ ロシュ アーゲー | イミダゾベンゾジアゼピン誘導体 |
| ES2550994T3 (es) | 2007-12-04 | 2015-11-13 | F. Hoffmann-La Roche Ag | Derivados de isoxazol-piridina |
| WO2010053127A1 (ja) | 2008-11-05 | 2010-05-14 | 協和発酵キリン株式会社 | α1GABAA受容体またはα5GABAA受容体の調整剤 |
| US8222246B2 (en) * | 2009-04-02 | 2012-07-17 | Hoffmann-La Roche Inc. | Substituted isoxazoles |
| US8227461B2 (en) * | 2009-04-30 | 2012-07-24 | Hoffmann-La Roche Inc. | Isoxazoles |
| JP5466292B2 (ja) | 2009-05-05 | 2014-04-09 | エフ．ホフマン−ラ ロシュ アーゲー | イソオキサゾール−ピリジン誘導体 |
| AU2010244555A1 (en) * | 2009-05-07 | 2011-11-03 | F. Hoffmann-La Roche Ag | Isoxazole-pyridine derivatives as GABA modulators |
| EP2298296A1 (en) * | 2009-08-25 | 2011-03-23 | CNRS Centre National De La Recherche Scientifique | Composition and method for treating cognitive impairments in down syndrome subjects |
| EP2575455A4 (en) * | 2010-06-03 | 2014-01-15 | Univ California | METHODS AND COMPOSITIONS FOR TREATING A SUBJECT FOR INJURY OF THE CENTRAL NERVOUS SYSTEM (CNS) |
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2011
- 2011-11-01 AU AU2011325190A patent/AU2011325190B2/en active Active
- 2011-11-01 BR BR112013010895A patent/BR112013010895A2/pt not_active Application Discontinuation
- 2011-11-01 NZ NZ608592A patent/NZ608592A/en not_active IP Right Cessation
- 2011-11-01 KR KR1020157030443A patent/KR20150123967A/ko not_active Application Discontinuation
- 2011-11-01 WO PCT/EP2011/069178 patent/WO2012059482A1/en active Application Filing
- 2011-11-01 PL PL11776453T patent/PL2635277T3/pl unknown
- 2011-11-01 MX MX2013004900A patent/MX341471B/es active IP Right Grant
- 2011-11-01 KR KR1020137014355A patent/KR20130083927A/ko active Application Filing
- 2011-11-01 EP EP11776453.0A patent/EP2635277B1/en active Active
- 2011-11-01 RU RU2013124992/15A patent/RU2563167C2/ru not_active IP Right Cessation
- 2011-11-01 SG SG10201509163VA patent/SG10201509163VA/en unknown
- 2011-11-01 SG SG2013024831A patent/SG189248A1/en unknown
- 2011-11-01 ES ES11776453T patent/ES2711973T3/es active Active
- 2011-11-01 US US13/286,240 patent/US8835425B2/en active Active
- 2011-11-01 CN CN201180053164.5A patent/CN103189062B/zh active Active
- 2011-11-01 MY MYPI2013001520A patent/MY164595A/en unknown
- 2011-11-01 CA CA2812664A patent/CA2812664C/en active Active
- 2011-11-01 JP JP2013537115A patent/JP2013544808A/ja active Pending
- 2011-11-03 AR ARP110104078A patent/AR083694A1/es unknown
- 2011-11-03 TW TW100140197A patent/TW201240665A/zh unknown
-
2013
- 2013-03-21 IL IL225438A patent/IL225438A/en active IP Right Grant
- 2013-08-12 HK HK13109401.9A patent/HK1182015A1/zh unknown
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2014
- 2014-08-05 US US14/451,938 patent/US20140343046A1/en not_active Abandoned
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2016
- 2016-07-08 JP JP2016135853A patent/JP2016216484A/ja active Pending
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2018
- 2018-03-20 JP JP2018052303A patent/JP2018115183A/ja active Pending
-
2019
- 2019-03-27 US US16/366,526 patent/US20190270734A1/en not_active Abandoned
- 2019-08-05 JP JP2019143620A patent/JP2019206574A/ja active Pending
-
2020
- 2020-11-10 US US17/094,172 patent/US20210053959A1/en not_active Abandoned
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2021
- 2021-06-23 JP JP2021104284A patent/JP2021152067A/ja active Pending
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2023
- 2023-02-09 US US18/107,741 patent/US20230183225A1/en active Pending
- 2023-07-27 JP JP2023122478A patent/JP2023139241A/ja active Pending
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